World Academy of Science, Engineering and Technology

Authors: Harshada Vaidya-Kannur, Dattatraya Naik

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Propolis, one of the beehive products also referred as bee-glue is sticky dark coloured complex mixture of compounds. The volatile oil can be isolated from the propolis by hydrodistillation. The mark that is left behind after the removal of volatile oil is referred as the de-oiled propolis. Antioxidant as well as anti-inflammatory properties of total ethanolic extract of de-oiled propolis (TEEDP) was investigated. Another lot of deoiled propolis was successively exacted with hexane, ethyl acetate and ethanol. Activities of these fractions were also determined. Antioxidant activity was determined by studying ABTS, DPPH and NO radical scavenging. Determination of anti-inflammatory activity was carried out by topical TPA induced mouse ear oedema model. It is noteworthy that ethyl acetate fraction of deoiled propolis (EAFDP) exhibited 49.45 % TEAC activity at the concentration 0.2 mg/ml which is equivalent to the activity of trolox at the concentration 0.2 mg/ml. Its DPPH scavenging activity (72.56%) was closely comparable to that of trolox (75%). However its NO scavenging activity was comparatively low. From IC50 values it could be concluded that the efficiency of scavenging ABTS radicals by the de-oiled propolis was more pronounced as compared to scavenging of other radicals. Studies by TPA induced mouse ear inflammation model indicated that the de-oiled propolis of Indian origin had significant topical anti-inflammatory activity. The EAFDP was found to be the most active fraction for this activity also. The purification of EAFP yielded six pure crystalline compounds. These compounds were identified by their physical data and spectral data.

Keywords: anti-inflammatory activity, anti-oxidant activity, column chromatography, de-oiled propolis

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Authors: Abdallah Habbab, Khaled Sekkoum, Nasser Belboukhari

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Objective: This study is designed to examine the chemical composition, antioxidant and antibacterial activities of the essential oil extracted from leaves of Vitex agnus-castus. Methods: The essential oils of dry leaves of Vitex agnus-castus L. were obtained by hydro-distillation, afforded oil in the yield of 5.5% and their volatile constituents were identified by GC/MS. Antioxidant activity of the sample was determined by test system DPPH. Antifungal activity was tested against three fungal strains (Aspergillus flavus, Penicillium escpansum and Aspergillus ochraceus) by direct contact method. Results: Forty-three compounds were identified, representing 98.02% of the oil. Major components of the oil were 1,8-cineole (18.27 %), caryophyllene (8.60 %), N-(M-fluorophenyl)-maleimide (6.30 %), (+)-epi-bicyclosesquiphellandrene (6.00 %), terpinen-4-ol (5.57 %), pyrrolo (3,2,1-jk) carbazole (5.43 %), caryophyllene oxide (4.79 %), and phenol (4.09 %). Conclusion: The chemical constituents in the essential oil from the locally grown Vitex agnus-castus were identified. Therefore, the essential oil of Vitex agnus-castus is an active candidate which would be used as antioxidant, or antifungal agent in new drugs preparation for therapy of diseases.

Keywords: Vitex agnus-castus, essential oil, GC/MS, DPPH, 1, 8-cineole

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Authors: B. Sathyanarayana

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As per the report of World Health Organization, more than 80% of world population uses medicines made from herbal and natural materials. They have stood the test of time for their safety, efficacy, cultural acceptability and lesser side effects. Quality assurance and control measures, such as national quality specification and standards for herbal materials, good manufacturing practices (GMP) for herbal medicines, labelling, and licensing schemes for manufacturing, imports and marketing, should be in place in every country where herbal medicines are regulated. These measures are vital for ensuring the safety and efficacy of herbal medicines. In the case of herbal products challenge begins at the stage of designing itself except the classical products. Selection of herbal ingredients, officinal parts to be used, proportions are vital. Once the formulation is designed one should take utmost care to produce the standardized product of assured quality and safety. Quality control measures should cover the validation of quality and identity of raw materials, in process control (as per SOP and GMP norms) and at the level of final product. Quality testing, safety and efficacy studies of the final product are required to ensure the safe and effective use of the herbal products in human beings. Medicinal plants being the materials of natural resource are subjected to great variation making it really difficult to fix quality standards especially in the case of polyherbal preparations. Manufacturing also needs modification according to the type of ingredients present. Hence, it becomes essential to develop Standard operative Procedure for a specific herbal product. Present paper throws a light on the challenges that are encountered during the design and development of herbal products.

Keywords: herbal product, challenges, quality, safety, efficacy

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Authors: Malvina Hoxha, Valerie Capra, Carola Buccellati, Angelo Sala, Clara Cena, Roberta Fruttero, Massimo Bertinaria, G. Enrico Rovati

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Today COXIBs are used in the treatment of arthritis and many other painful conditions in selected patients with high gastrointestinal risk and low CV risk. Previously we found a new mechanism of action of a traditional NSAID (diclofenac) and a COXIB (lumiracoxib) that possess weak competitive antagonism at the TP receptor. We hypothesize that modifying the structure of a known specific inhibitor of cyclooxygenase-2 (COXIB), so that it becomes also a more potent thromboxane antagonist will preserve the anti-inflammatory and gastrointestinal safety typical of COXIBs and prevent the cardiovascular risk associated with long term therapy.

Keywords: cyclooxygenase, inflammation, lumiracoxib, thromboxane A2

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Authors: Mebruka Mohammed, Daniel Bisrat, Asfaw Debella, Tarekegn Birhanu

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Lack of quality control standards for medicinal plants and their preparations is considered major barrier to their integration in to effective primary health care in Ethiopia. Poor quality herbal preparations led to countless adverse reactions extending to death. Denial of penetration for the Ethiopian medicinal plants in to the world’s booming herbal market is also another significant loss resulting from absence of herbal quality control system. Thus, in the present study, Gnidia stenophylla Gilg (popular antimalarial plant of south eastern Ethiopia), is standardized and a full monograph is produced that can serve as a guideline in quality control of the crude drug. Morphologically, the roots are found to be cylindrical and tapering towards the end. It has a hard, corky and friable touch with saddle brown color externally and it is relatively smooth and pale brown internally. It has got characteristic pungent odor and very bitter taste. Microscopically it has showed lignified xylem vessels, wider medullary rays with some calcium oxalate crystals, reddish brown secondary metabolite contents and slender shaped long fibres. Physicochemical standards quantified and resulted: foreign matter (5.25%), moisture content (6.69%), total ash (40.80%), acid insoluble ash (8.00%), water soluble ash (2.30%), alcohol soluble extractive (15.27%), water soluble extractive (10.98%), foaming index (100.01 ml/g), swelling index (7.60 ml/g). Phytochemically: Phenols, flavonoids, steroids, tannins and saponins were detected in the root extract; TLC and HPLC fingerprints were produced and an analytical marker was also tentatively characterized as 3-(3,4-dihydro-3,5-dihydroxy-2-(4-hydroxy-5-methylhex-1-en-2-yl)-7-methoxy-4-oxo-2H-chromen-8-yl)-5-hydroxy-2-(4-hydroxyphenyl)-7-methoxy-4H-chromen-4-one. Residue wise pesticides (i.e. DDT, DDE, g-BHC) and radiochemical levels fall below the WHO limit while Heavy metals (i.e. Co, Ni, Cr, Pb, and Cu), total aerobic count and fungal load lie way above the WHO limit. In conclusion, the result can be taken as signal that employing non standardized medicinal plants could cause many health risks of the Ethiopian people and Africans’ at large (as 80% of inhabitants in the continent depends on it for primary health care). Therefore, following a more universal approach to herbal quality by adopting the WHO guidelines and developing monographs using the various quality parameters is inevitable to minimize quality breach and promote effective herbal drug usage.

Keywords: Gnidia stenophylla Gilg, standardization/monograph, pharmacognostic, residue/impurity, quality

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Authors: Hassan Sher

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Agriculture has a pivotal role in Pakistan’s economy, accounting for about one-fourth of the GDP and employing almost half the population. However, the competitiveness, productivity, growth, employment potential, export opportunity, and contribution to GDP of the sector is significantly hampered by agriculture marketing laws/regulations at the provincial level that reward rent seeking behavior, promote monopoly power, artificially reduce farmer incomes while inflating prices to consumers, and act as disincentives to investment. Although of more recent vintage than some other provincial agricultural marketing laws, the NWFP Agricultural and Livestock Produce Markets Act, 2007 is a throwback to a colonial paradigm, where restrictions on agricultural produce marketing and Government control of distribution channels is the norm. The Swat Valley (in which we include its tributary valleys) is an area of Pakistan in which there is poverty is both extreme and pervasive. For many, a significant portion of the family’s income comes from selling plants that are used as herbs, medicines, and perfumes. Earlier studies have shown that the benefit they derive from this work is less than they might because of: Lack of knowledge concerning which plants and which plant parts are valuable, Lack of knowledge concerning optimal preservation and storage of material, illiteracy. Another concern that much of the plant material sold from the valley is collected in the wild, without an appreciation of the negative impact continued collecting has on wild populations. We propose: Creating colored cards to help inhabitants recognize the 25 most valuable plants in their area; Developing and sharing protocols for growing the 25 most valuable plants in a home garden; Developing and sharing efficient mechanisms for drying plants so they do not lose value; Encouraging increased literacy by incorporating numbers and a few words in the handouts.

Keywords: food security, medicinal plants, industrial plants, economic development

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Authors: N. Boussoualim, H. Trabsa, I. Krache, S. Aouachria, S. Boumerfeg, L. Arrar, A. Baghiani

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The aim of this study consisted in evaluating the antioxidant in vivo properties, anti-hemolytic and XOR inhibitory effect of Globularia alypum L. (GA) extracts. GA was submitted to extraction and fractionation to give crude (CrE), chloroformique (ChE), ethyle acetate (EAE) and aqueos (AqE) extracts. Total polyphenols contents of GA extracts were determined; EAE is the most rich in polyphenols (157,74±5,27 mg GAE/mg of extract). GA Extracts inhibited XO in a concentration-dependent manner, the EAE showed the highest inhibitory properties on the XOR activity (IC50=0,083±0,001 mg/ml), followed by CrE and ChE. The antioxidant activities of the CrE, EAE, and AqE were tested by an in vivo assay in mice, the plasma ability to inhibit DPPH radical was measured, The CrE was found to exhibit the greatest scavenger activity with 48.41±2.763%, followed by AqE and EAE (40.54±7.51% and 41.79±1.654%, respectively). Total antioxidant capacity of red blood cells was measured, from the kinetics of hemolysis obtained. The calculated HT50 reveal an extension of time for half hemolysis in all treated groups compared with the control group. CrE increase significantly HT50 (112,8±2,427). The hemolysis is lagged, indicating that endogenous antioxidants in the erythrocytes can trap radicals to protect them against free-radical-induced hemolysis. Antimicrobial activities of the extracts were determined by the disc diffusion method. Test microorganisms were; 4 Gram positive, 7 gram negative bacteria, most active extracts were EAE and CrE. We deduce a great relationship between the effect on the extracts antibacterial effect and their contents in flavonoid.

Keywords: Globularia alypum, Xanthine oxidoreductase, in vivo-antioxidant activity, hemolysis, polyphenol

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Authors: Lotfollah Rezagholizadeh

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Background and Aim: Diabetes mellitus is related to high mortality and morbidity caused by the early development of atherosclerosis correlated to diabetic macroangiopathy. The endothelium-derived vasodilator, nitric oxide (NO) has been implicated in the development of vascular complications via the regulation of blood flow, and various antiatherosclerotic actions. Patients with type 2 diabetes (T2D) have a decreased level of endothelial nitric oxide release. In this study we aimed to examine the effect of aquatic seed extract of Cichorium intybus L. (chicory) and metformin (a known prescription drug for diabetes) on NO levels in T2D rats. Methods: Five groups of adult male Wistar rats were used (n=6): Non-diabetic controls without extract treatment (Control), Non-diabetic controls with extract treatment (Chicory-control), T2D rats without extract treatment (NIA/STZ), T2D rats treated with the extract (Chicory-NIA/STZ), and T2D groups that received metformin (100 mg/kg) but no extract (Metformin-NIA/STZ). T2D was induced with intraperitoneal (i.p) injection of niacinamide (NIA, 200 mg/kg), 15 min after an i.p administration of streptozotocin (STZ, 55 mg/kg). Lyophilized chicory extract (125 mg/kg) was dissolved in 0.2 ml normal saline and administered one dose a day. The experiments lasted for 3 weeks after the diabetes induction. NO analysis was performed by assay based on the Griess reaction. Data were reported as the mean ± SD and statistical analysis was performed by ANOVA. Results: Serum nitric oxide levels decreased significantly in NIA/STZ group compared with Control and Chicory-control. Treatment with chicory extract caused a significant increase in serum levels of NO in Chicory-NIA/STZ group compare to NIA/STZ group (p<05). Metformin-NIA/STZ group did not show considerable difference when compared with NIA/STZ, with respect to NO levels. In a group of rats made diabetic by STZ alone (type 1 diabetic rats, T1D), chicory did not have a significant ameliorating effect. Conclusion: In this study, we clearly showed a relationship between low serum nitric oxide levels and diabetes mellitus in rats. The increase in serum nitric oxide by chicory extract is an indication of antiatherogenic effect of this plant. Chicory seed extract was more efficient than metformin in improving the NO levels in NO-deficient T2D diabetic rats.

Keywords: type 2 diabetes mellitus, nitric oxide, chicory, metformin

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Authors: Amr A. Fouad, Waleed H. Albuali, Iyad Jresat

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The protective effect of thymoquinone (TQ) was investigated in rats exposed to testicular injury induced by sodium arsenite (10mg/kg/day, orally, for two days). TQ treatment (10mg/kg/day, intraperitoneal injection) was applied for five days, starting three day before arsenic administration. TQ significantly attenuated the arsenic-induced decreases of serum testosterone, and testicular reduced glutathione level, and significantly decreased the elevations of testicular malondialdehyde and nitric oxide levels resulted from arsenic administration. Also, TQ ameliorated the arsenic-induced testicular tissue injury observed by histopathological examination. In addition, TQ decreased the arsenic-induced expression of inducible nitric oxide synthase and caspase-3 in testicular tissue. It was concluded that TQ may represent a potential candidate to protect against arsenic-induced testicular injury.

Keywords: thymoquinone, arsenic, testes, rats

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Authors: Mustafa Ali Abugila, Basma Nuri Kajruba, Hanan Elhadi, Rehab Ramadan Wali

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Iron deficiency anemia is characterized by a decrease of Hb (hemoglobin), serum iron, ferritin, and RBC (red blood cells) (shape and size). Also, it is characterized by an increase in total iron binding capacity (TIBC). Red blood cells become microctytic and hypochromic due to a decrease in iron content. This study was conducted in the north west of Libya and included 210 women in childbearing age (18-45 years) who were visiting women clinic. After filling the questionnaire, blood samples were taken and analyzed for hematological and biochemical profiles. Biochemical tests included measurement of serum iron, ferritin, and total iron binding capacity (TIBC). Among the total sample (210 women), there were 87 (41.42%) pregnant and 123 (58.57%) non-pregnant women (includes married and single). Pregnant women (87) were classified according to the gestational age into first, second, and third trimesters. The means of biochemical and hematological parameters in the studied samples were: Hb = 10.37± 2.02 g/dl, RBC = 3.78± 1.037 m/m3, serum iron 61.86± 40.28 µg/dl, and TIBC = 386.01 ± 94.91 µg/dl. In this study, we considered that any women have hemoglobin below 11.5 g/dl is anemic. 89.1%, 69.5%, and 47.8% of pregnant women who belong to third trimester had low (below normal value) Hb, serum iron, and ferritin, i.e. iron deficiency anemia was more common in third trimester among the first and the second trimesters. Third trimester pregnant women also had high TIBC more than first and second trimesters.

Keywords: red blood cells, hemoglobin, total iron binding capacity, ferritin

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Authors: B.S. Roopa

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Objectives: To investigate the prevalence of concomitant use of GPDs in patients treated with NSAIDs and GPDs in recommended dose and frequency as prophylaxis. And also to know the association between risk factors and prescription of GPDs in patients treated with NSAIDs. Methods: Study was a prospective, observational, cross-sectional survey. Data from patients with prescription of NSAIDs at the out-patient departments of secondary care Hospital, Nilgiris, India were collected in a specially designed proforma for a period of 45 days. Analysis using χ2 tests for discrete variables. Factors that might be associated with prescription of GPD with NSIADs were assessed in multiple logistic regression models. Results: Three hundred and three patients were included in this study, and the rate of GPD prescription was 89.1%. Most of the patients received H2-receptor antagonist, and, to a lesser degree, antacid and proton pump inhibitor. Patients with history of GI ulcer/bleeding were much more likely to be co-prescribed GPD than those who had no history of GI disorders .Compared with patients who were managed in general outpatient clinic, those managed in Secondary care hospital in Nilgrisis, India were more likely to receive GPD. Conclusions: The prescription rate of GPD with NSAIDs is high. Patients were prescribed with H2RA with dose of 150mg twice daily, which are not effective in reducing the risk of NSAIDs induced gastric ulcer. Only the frequency of NSAIDs prescription was considered significant determinant for the co-prescription with GPAs in patients who are < 65 years and ≥ 65 years old.

Keywords: gastro protective agents, non steridol anti inlfammatory agents

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Authors: Kalimullah Khan, Samina Roohi, Mohammad Rafi, Rizwana Zahoor

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Labeling of 5-Aminolevulinic acid (5-ALA) with 99 mTc was achieved by using tin chloride dihydrate (Sncl2.2H2O) as reducing agent. Radiochemical purity and labeling efficiency was determined by Whattman paper No.3 and instant thin layer chromatographic strips impregnated with silica gel (ITLC/SG). Labeling efficiency was dependent on many parameters such as amount of ligand, reducing agent, pH, and incubation time. Therefore, optimum conditions for maximum labeling were selected. Stability of 99 mTc- 5-ALA was also checked in fresh human serum. Tissue bio-distribution of 99 mTc-5-ALA was evaluated in Spargue Dawley rats. 5-ALA was 98% labeled with 99 mTc under optimum conditions, i.e. 100µg of 5-ALA, pH: 4, 10µg of Sncl2.2H2O and 30 minutes incubation at room temperature. 99 mTc labelled 5- ALA remained stable for 24 hours in human serum. Bio-distribution study (%ID/gm) in rats revealed that maximum accumulation of 99 mTc-5-ALA was in liver, spleen, stomach and intestine after half hour, 4 hours, and 24 hours. Significant activity in bladder and urine indicated urinary mode of excretion.

Keywords: 99mTc-ALA, aminolevulinic acid, quality control, radiopharmaceuticals

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Authors: M. Kumpugdee-Vollrath, M. Tabatabaeifar, M. Helmis

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Shellac is a natural polyester resin secreted by insects. Pectins are natural, non-toxic and water-soluble polysaccharides extracted from the peels of citrus fruits or the leftovers of apples. Both polymers are allowed for the use in the pharmaceutical industry and as a food additive. SSB Aquagold® is the aqueous solution of shellac and can be used for a coating process as an enteric or controlled drug release polymer. In this study, tablets containing 10 mg methylene blue as a model drug were prepared with a rotary press. Those tablets were coated with mixtures of shellac and one of the pectin different types (i.e. CU 201, CU 501, CU 701 and CU 020) mostly in a 2:1 ratio or with pure shellac in a small scale fluidized bed apparatus. A stable, simple and reproducible three-stage coating process was successfully developed. The drug contents of the coated tablets were determined using UV-VIS spectrophotometer. The characterization of the surface and the film thickness were performed with the scanning electron microscopy (SEM) and the light microscopy. Release studies were performed in a dissolution apparatus with a basket. Most of the formulations were enteric coated. The dissolution profiles showed a delayed or sustained release with a lagtime of at least 4 h. Dissolution profiles of coated tablets with pure shellac had a very long lagtime ranging from 13 to 17.5 h and the slopes were quite high. The duration of the lagtime and the slope of the dissolution profiles could be adjusted by adding the proper type of pectin to the shellac formulation and by variation of the coating amount. In order to apply a coating formulation as a colon delivery system, the prepared film should be resistant against gastric fluid for at least 2 h and against intestinal fluid for 4-6 h. The required delay time was gained with most of the shellac-pectin polymer mixtures. The release profiles were fitted with the modified model of the Korsmeyer-Peppas equation and the Hixson-Crowell model. A correlation coefficient (R²) > 0.99 was obtained by Korsmeyer-Peppas equation.

Keywords: shellac, pectin, coating, fluidized bed, release, colon delivery system, kinetic, SEM, methylene blue

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Authors: Amina Unis, Samah S. El Basateeny, Noha A. H. Nassef

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Introduction: Acute Renal Failure (ARF) is one of the most common problems encountered in hospitalized critically ill patients. In recent years great effort has been focused on the introduction of herbal medicine as a novel therapeutic agent for prevention of ARF. Hence, the current study was designed to investigate the effect of Green Coffee Bean Extract (GCBE) on gentamicin induced ARF in rats. Methods: The study was conducted on 60 male rats divided into six equal groups. Group 1 served as normal control group and GCBE was administered for 7 days at a dose of 20 mg/kg/day in group 2 and 40 mg/kg/day in group 3 to test the effect of GCBE on normal kidneys. ARF was induced by a daily intraperitoneal injection of gentamicin (80 mg/kg) for 7 days in group 4 (model group), group 5 (GCBE 20 mg/kg/day) and group 6 (GCBE 20 mg/kg/day). All rats were sacrificed after 7 days and blood was withdrawn for kidney function tests. Kidneys were removed for determination of renal oxidative stress markers and histopathological examination. Results: The present study showed that rats that received oral GCBE for 7 days without induction of ARF showed no significant change in all the assessed parameters in comparison to the normal control group, while rats in the groups that received oral GCBE for 7 days with induction of ARF showed a significant improvement in kidney functions tests (decrease in serum urea, serum creatinine, and blood urea nitrogen) when compared to the ARF model group. Moreover, there was significant amelioration in renal oxidative stress markers (renal malondialdehyde, renal superoxide dismutase) and renal histopathological changes in the GCBE treated groups along induction of ARF when compared to ARF model group. The most significant improvement was reported in the group where GCBE was administered for 7 days in a dose 40 mg/kg/day, along with induction of ARF. Conclusion: GCBE has a potential role in ameliorating renal damage involved in ARF mostly through its antioxidant effect.

Keywords: green coffee bean extract, gentamicin, acute renal failure, pharmacology

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Authors: Anan Jarab, Riham Almrayat, Salam Alqudah, Maher Khdour, Tareq Mukattash, Sharell Pinto

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Background: The prevalence of diabetes in Jordan is among the highest in the world, making it a particularly alarming health problem there. It has been indicated that poor adherence to the prescribed therapy lead to poor glycemic control and enhance the development of diabetes complications and unnecessary hospitalization. Purpose: To explore factors associated with medication non-adherence in patients with type 2 diabetes in Jordan. Materials and Methods: Variables including socio-demographics, disease and therapy factors, diabetes knowledge, and health-related quality of life in addition to adherence assessment were collected for 171 patients with type 2 diabetes using custom-designed and validated questionnaires. Logistic regression was performed to develop a model with variables that best predicted medication non-adherence in patients with type 2 diabetes in Jordan. Results: The majority of the patients (72.5%) were non-adherent. Patients were found four times less likely to adhere to their medications with each unit increase in the number of prescribed medications (OR = 0.244, CI = 0.08-0.63) and nine times less likely to adhere to their medications with each unit increase in the frequency of administration of diabetic medication (OR = 0.111, CI = 0.04-2.01). Patients in the present study were also approximately three times less likely (OR = 0.362, CI = 0.24-0.87) to adhere to their medications if they reported having concerns about side effects and twice more likely to adhere to medications (OR = 0.493, CI = 0.08-1.16) if they had one or more micro-vascular complication. Conclusion: The current study revealed low adherence rate to the prescribed therapy among Jordanians with type 2 diabetes. Simplifying dosage regimen, selecting treatments with lower side effects along with an emphasis on diabetes complications should be taken into account when developing care plans for patients with type 2 diabetes.

Keywords: type 2 diabetes, adherence, glycemic control, clinical pharmacist, Jordan

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Authors: Soad Ali Yehia, Mohamed Shafik El-Ridi, Mina Ibrahim Tadros, Nolwa Gamal El-Sherif

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Fexofenadine hydrochloride (FXD) is a slightly soluble, bitter-tasting, drug having an oral bioavailability of 35%. The maximum plasma concentration is reached 2.6 hours (Tmax) post-dose. The current work aimed to develop taste-masked FXD orodispersible tablets (ODTs) to increase extent of drug absorption and reduce Tmax. Taste masking was achieved via solid dispersion (SD) with chitosan (CS) or sodium alginate (ALG). FT-IR, DSC and XRD were performed to identify physicochemical interactions and FXD crystallinity. Taste-masked FXD-ODTs were developed via addition of superdisintegrants (crosscarmelose sodium or sodium starch glycolate, 5% and 10%, w/w) or sublimable agents (camphor, menthol or thymol; 10% and 20%, w/w) to FXD-SDs. ODTs were evaluated for weight variation, drug-content, friability, wetting time, disintegration time and drug release. Camphor-based (20%, w/w) FXD-ODT (F12) was optimized (F23) by incorporation of a more hydrophilic lubricant, sodium stearyl fumarate (Pruv®). The topography of the latter formula was examined via scanning electron microscopy (SEM). The in vivo estimation of FXD pharmacokinetics, relative to Allegra® tablets, was evaluated in healthy human volunteers. Based on the gustatory sensation test in healthy volunteers, FXD:CS (1:1) and FXD:ALG (1:0.5) SDs were selected. Taste-masked FXD-ODTs had appropriate physicochemical properties and showed short wetting and disintegration times. Drug release profiles of F23 and phenylalanine-containing Allegra® ODT were similar (f2 = 96) showing a complete release in two minutes. SEM micrographs revealed pores following camphor sublimation. Compared to Allegra® tablets, pharmacokinetic studies in healthy volunteers proved F23 ability to increase extent of FXD absorption (14%) and reduce Tmax to 1.83 h.

Keywords: fexofenadine hydrochloride, taste masking, chitosan, orodispersible

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Authors: Nagat M. Saeed, Mabruka S. Elashheb, Fatma M. Ben Rabaha, Aisha M Edrah

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The aim of the study was to determine the type and pattern of antibiotic susceptibility of the pathogenic microorganisms causing chronic suppurative otitis media (CSOM), which could lead to better therapeutic decisions and consequently avoidance of appearance of resistance to specific antibiotics. Most frequently isolated agents were Pseudomonas aeruginosa 28.5%; followed by Staphylococcus aureus 18.2%; proteus mirabilis 13.9%; Providencia stuartti 6.7%; Bacteroides melaninogenicus, Aspergillus sp., candida sp., 4.2% each; and other microorganisms were represented in 3-0.2%. Drug sensitivities pattern of Pseudomonas aeruginosa showed that ciprofloxacin was active against the majority of isolates (93.9%) followed by ceftazidime 86.2%, amikacin 76.2% and gentamicin 40.8%. However, Staphylococcus aureus isolates were resistant to penicillin 72.7%, erythromycin 28.6%, cephalothin 18.2%, cloxacillin 8.3% and ciprofloxacin was active against 96.2% of isolates. The resistance pattern of proteus mirabilis was 55.6% to ampicillin, 47.1% to carbencillin, 29.4% to cephalothin, 14.3% to gentamicin and 4.8% to amikacin while 100% were sensitive to ciprofloxacin. We conclude that ciprofloxacin is the best drug of choice in the treatment of CSOM caused by the common microorganisms.

Keywords: otitis media, chronic suppurative otitis media (CSOM), microorganisms, drug sensitivity

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Authors: Abdelkader H. El Debani, Huda Gargoum, Awad G. Abdellatif

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The aim of this study is to investigate analgesic and the anti-inflammatory effects Camel Thorn Extract (CTE) in rodents. Male albino mice weighing 20-25 gm. were divided into different groups each of 8 mice. The control was given normal saline i. p., the first group was given normal saline i. p. the 2nd, 3rd, 4th, groups received different doses of CTE (330, 660, and 1300 mg/kg) respectively and the 6th group received 5mg/kg of morphine i. p. All groups (except the control group) were given acetic acid 40 min after receiving the different treatment. The number of writhes was recorded 5 min after acetic acid injection for 15 min and the % of inhibition of writhing were calculated. Different groups of rats weighing 180- 220 gm., were divided into three groups each of 5 rats. At the beginning, the volumes of the right and left paw in animals were measured by using of the plethysmometer. The 1st group was given 660 mg /kg i. p. of CTE, the 2nd group received indomethacin (5 mg/kg i. p.). One hour later, edema was induced by sub planter injection of 0.1 ml of 1 % freshly prepared suspension of carrageenan into the right hind paws of the rats. The volume of the injected paws and contra-lateral paws were measured at 0, 0.5, 1, 2, 3, 4, and 5 hours using plethysmometer. The volume of the left paw of the rat was subtracted from the volume of the right paw of the same animal. Our results showed that 330,660 and 1300 mg/kg produced 14, 49 and 84%of inhibition of writhes, indicating that CTE has a strong analgesic activity. Our data also showed that the % of inhibition of edema at 30, 60, 120, 180, and 240 min was 14,51,71,61, and 56% in the animals given camel thorn extract whereas these figures in animals given endomethacin were 14, 24, 54, 52, and 54%. These results indicate that camel thorn has anti-inflammatory activities. The mechanism of analgesic and anti-inflammatory activities needs further investigations.

Keywords: camel thorn, imdomethacin, morphine, pharmaceutical medicine

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Authors: Steffen Happel

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Non-standard isotopes such as Sc-44/47, Zr-89, and Sn-117mare finding interest is increasing in radiopharmaceutical applications. Methods for the separation of these elements from typical target materials were developed. The methods used in this paper are based on the use of extraction chromatographic resins such as UTEVA, TBP, and DGA resin. Information on the selectivity of the resins (Dw values of selected elements in HCl and HNO3 of varying concentration) will be presented as well as results of the method development such as elution studies, chemical recoveries, and decontamination factors. Developed methods are based on the use of vacuum supported separation allowing for fast and selective separation.

Keywords: elution, extraction chromatography, radiopharmacy, decontamination factors

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Authors: J. P. Lavande, A. V.Chandewar

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Mouth dissolving tablet is the speedily growing and highly accepted drug delivery system. This study was aimed at development of Ketorolac Tromethamine mouth dissolving tablet (MDTs), which can disintegrate or dissolve rapidly once placed in the mouth. Conventional Ketorolac tromethamine tablet requires water to swallow it and has limitation like low disintegration rate, low solubility etc. Ketorolac Tromethamine mouth dissolving tablets (formulation) consist of super-disintegrate like Heat Modified Karaya Gum, Co-treated Heat Modified Agar & Filler microcrystalline cellulose (MCC). The tablets were evaluated for weight variation, friability, hardness, in vitro disintegration time, wetting time, in vitro drug release profile, content uniformity. The obtained results showed that low weight variation, good hardness, acceptable friability, fast wetting time. Tablets in all batches disintegrated within 15-50 sec. The formulation containing superdisintegrants namely heat modified karaya gum and heat modified agar showed better performance in disintegration and drug release profile.

Keywords: mouth dissolving tablet, Ketorolac tromethamine, disintegration time, heat modified karaya gum, co-treated heat modified agar

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Authors: Thitaporn Thoopputra, Tipaporn Pongmesa, Shuchuen Li

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Aims: To evaluate the application of non-invasive diabetes risk assessment tool in community pharmacy setting. Methods: Thai diabetes risk score was applied to assess individuals at risk of developing type 2 diabetes. Interactive computer-based risk screening (IT) and paper-based risk screening (PT) tools were applied. Participants aged over 25 years with no known diabetes were recruited in six participating pharmacies. Results: A total of 187 clients, mean aged (+SD) was 48.6 (+10.9) years. 35% were at high risk. The mean value of willingness-to-pay for the service fee in IT group was significantly higher than PT group (p=0.013). No significant difference observed for the satisfaction between groups. Conclusions: Non-invasive risk assessment tool, whether paper-based or computerized-based can be applied in community pharmacy to support the enhancing role of pharmacists in chronic disease management. Long term follow up is needed to determine the impact of its application in clinical, humanistic and economic outcomes.

Keywords: community pharmacy, intervention, prevention, risk assessment, type 2 diabetes

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Authors: Chih-Chang Yeh, Min-Fang Yang, Hsin-I Chang

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Chitosan is a cationic polysaccharide derived from the partial deacetylation of chitin. Hyaluronic acid (HA), chondroitin sulfate (CS) and heparin (HP) are anionic glycosaminoglycans (GCGs) which can regulate osteogenic activity. In this study, chitosan membranes were prepared by glutaraldehyde crosslinking reaction and then complexed with three different types of GCGs. 7F2 osteoblasts-like cells and macrophages Raw264.7 were used as models to study the influence of chitosan membranes on osteometabolism. Although chitosan membranes are highly hydrophilic, the membranes associated with GCG-chitosan complexes showed about 60-70% cell attachment. Furthermore, the membranes associated with HP-chitosan complexes could increase ALP activity in comparison with chitosan films only. Three types of the membranes associated with GCG-chitosan complexes could significantly inhibit LPS induced-nitric oxide expression. In addition, chitosan membranes associated with HP and HA can down-regulate tartrate-resistant acid phosphatase (TRAP) activity but not CS-chitosan complexes. Based on these results, we conclude that chitosan membranes associated with HP can increase ALP activity in osteoblasts and chitosan membranes associated with HP and HA reduce TRAP activity in osteoclasts.

Keywords: osteoblast, osteoclast, chitosan, glycosaminoglycan

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Authors: Madhusudan Purohit, Stephen Philip, Bharathkumar Inturi

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In this paper we report the quantitative structure activity relationship of novel bis-triazole derivatives for predicting the activity profile. The full model encompassed a dataset of 46 Bis- triazoles. Tripos Sybyl X 2.0 program was used to conduct CoMSIA QSAR modeling. The Partial Least-Squares (PLS) analysis method was used to conduct statistical analysis and to derive a QSAR model based on the field values of CoMSIA descriptor. The compounds were divided into test and training set. The compounds were evaluated by various CoMSIA parameters to predict the best QSAR model. An optimum numbers of components were first determined separately by cross-validation regression for CoMSIA model, which were then applied in the final analysis. A series of parameters were used for the study and the best fit model was obtained using donor, partition coefficient and steric parameters. The CoMSIA models demonstrated good statistical results with regression coefficient (r2) and the cross-validated coefficient (q2) of 0.575 and 0.830 respectively. The standard error for the predicted model was 0.16322. In the CoMSIA model, the steric descriptors make a marginally larger contribution than the electrostatic descriptors. The finding that the steric descriptor is the largest contributor for the CoMSIA QSAR models is consistent with the observation that more than half of the binding site area is occupied by steric regions.

Keywords: 3D QSAR, CoMSIA, triazoles, novel heterocycles

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Authors: Arpa Petchsomrit, Namfa Sermkaew, Ruedeekorn Wiwattanapatapee

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Oil entrapped floating alginate beads of curcumin were developed and characterized. Cremophor EL, Cremophor RH and Tween 80 were utilized to improve the solubility of the drug. The oil-loaded floating gel beads prepared by emulsion gelation method contained sodium alginate, mineral oil and surfactant. The drug content and % encapsulation declined as the ratio of surfactant was increased. The release of curcumin from 1% alginate beads was significantly more than for the 2% alginate beads. The drug released from the beads containing 25% of tween 80 was about 70% while a higher drug release was observed with the beads containing Cremophor EL or Cremohor RH (approximately 90%). The developed floating beads of curcumin powder with surfactant provided a superior drug release than those without surfactant. Floating beads based on oil entrapment containing the drug solubilized in surfactants is a new delivery system to enhance the dissolution of poorly soluble drugs.

Keywords: alginate, curcumin, floating drug delivery, oil entrapped bead

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Authors: Yaowaporn Sangsen, Kittisak Likhitwitayawuid, Boonchoo Sritularak, Kamonthip Wiwattanawongsa, Ruedeekorn Wiwattanapatapee

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Novel solid lipid nanoparticles (SLNs) were developed to improve oral bioavailability of oxyresveratrol (OXY). The SLNs were prepared by a high speed homogenization technique, at an effective speed and time, using Compritol® 888 ATO (5% w/w) as the solid lipid. The appropriate weight proportions (0.3% w/w) of OXY affected the physicochemical properties of blank SLNs. The effects of surfactant types on the properties of the formulations such as particle size and entrapment efficacy were also investigated. Conclusively, Tween 80 combined with soy lecithin was the most appropriate surfactant to stabilize OXY-loaded SLNs. The mean particle size of the optimized formulation was 134.40 ± 0.57 nm. In vitro drug release study, the selected S2 formulation showed a retarded release profile for OXY with no initial burst release compared to OXY suspension in the simulated gastrointestinal fluids. Therefore, these SLNs could provide a suitable system to develop for the oral OXY delivery.

Keywords: solid lipid nanoparticles, physicochemical properties, in vitro drug release, oxyresveratrol

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Authors: Rawia M. Khalil, Ahmed A. Abd El Rahman, Mahfouz A. Kassem, Mohamed S. El Ridi, Mona M. Abou Samra, Ghada E. A. Awad, Soheir S. Mansy

Abstract:

Solid lipid nanoparticles (SLNs) have gained great attention for the topical treatment of skin associated fungal infection as they facilitate the skin penetration of loaded drugs. Our work deals with the preparation of nystatin loaded solid lipid nanoparticles (NystSLNs) using the hot homogenization and ultrasonication method. The prepared NystSLNs were characterized in terms of entrapment efficiency, particle size, zeta potential, transmission electron microscopy, differential scanning calorimetry, rheological behavior and in vitro drug release. A stability study for 6 months was performed. A microbiological study was conducted in male rats infected with Candida albicans, by counting the colonies and examining the histopathological changes induced on the skin of infected rats. The results showed that SLNs dispersions are spherical in shape with particle size ranging from 83.26±11.33 to 955.04±1.09 nm. The entrapment efficiencies are ranging from 19.73±1.21 to 72.46±0.66% with zeta potential ranging from -18.9 to -38.8 mV and shear-thinning rheological Behavior. The stability studies done for 6 months showed that nystatin (Nyst) is a good candidate for topical SLN formulations. A least number of colony forming unit/ ml (cfu/ml) was recorded for the selected NystSLN compared to the drug solution and the commercial Nystatin® cream present in the market. It can be fulfilled from this work that SLNs provide a good skin targeting effect and may represent promising carrier for topical delivery of Nyst offering the sustained release and maintaining the localized effect, resulting in an effective treatment of cutaneous fungal infection.

Keywords: candida infections, hot homogenization, nystatin, solid lipid nanoparticles, stability, topical delivery

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Authors: Ibraheem Husain, Abul Kalam Najmi, Karishma Chester

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First-in-human (FIH) studies are a critical step in clinical development of any molecule that has shown therapeutic promise in preclinical evaluations, since preclinical research and safety studies into clinical development is a crucial step for successful development of monoclonal antibodies for guidance in pharmaceutical industry for the treatment of human diseases. Therefore, comparison between USFDA and nine pharmacologically guided approaches (PGA) (simple allometry, maximum life span potential, brain weight, rule of exponent (ROE), two species methods and one species methods) were made to determine maximum recommended starting dose (MRSD) for first in human clinical trials using four drugs namely Denosumab, Bevacizumab, Anakinra and Omalizumab. In our study, the predicted pharmacokinetic (pk) parameters and the estimated first-in-human dose of antibodies were compared with the observed human values. The study indicated that the clearance and volume of distribution of antibodies can be predicted with reasonable accuracy in human and a good estimate of first human dose can be obtained from the predicted human clearance and volume of distribution. A pictorial method evaluation chart was also developed based on fold errors for simultaneous evaluation of various methods.

Keywords: clinical pharmacology (CPH), clinical research (CRE), clinical trials (CTR), maximum recommended starting dose (MRSD), clearance and volume of distribution

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Authors: Karishma Chester, Sarvesh Paliwal, Sayeed Ahmad

Abstract:

Solanumnigrum L. (Family: Solanaceae), is an important Indian medicinal plant and have been used in various traditional formulations for hepato-protection. It has been reported to contain significant amount of steroidal glycosides such as solamargine and solasonine as well as their aglycone part solasodine. Being important pharmacologically active metabolites of several members of Solanaceae these markers have been attempted various times for their extraction and quantification but separately for glycoside and aglycone part because of their opposite polarity. Here, we propose for the first time simultaneous extraction and quantification of aglycone (solasodine)and glycosides (solamargine and solasonine) inleaves and berries of S.nigrumusing solvent extraction followed by HPTLC analysis. Simultaneous extraction was carried out by sonication in mixture of chloroform and methanol as solvent. The quantification was done using silica gel 60F254HPTLC plates as stationary phase and chloroform: methanol: acetone: 0.5 % ammonia (7: 2.5: 1: 0.4 v/v/v/v) as mobile phaseat 400 nm, after derivatization with an isaldehydesul furic acid reagent. The method was validated as per ICH guideline for calibration, linearity, precision, recovery, robustness, specificity, LOD, and LOQ. The statistical data obtained for validation showed that method can be used routinely for quality control of various solanaceous drugs reported for these markers as well as traditional formulations containing those plants as an ingredient.

Keywords: solanumnigrum, solasodine, solamargine, solasonine, quantification

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Authors: Pei-Hsiu Chiang, Ling Hong Huang, Hsin-I Chang

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In this research, we used UVA irradiation, which can penetrate into dermis and fibroblasts, the most abundant cells in dermis, to investigate the effect of UV light on dermis, such as inflammation, ECM degradation and elasticity loss. Moreover, this research is focused on the influence of hyaluronic acid (HA) on UVA treated dermal fibroblasts. We aim to establish whether HA can effectively relief ECM degradation, and restore the elasticity of UVA-damaged fibroblasts. Prolonged exposure to UVA radiation can damage fibroblasts and led variation in cell morphology and reduction in cell viability. Besides, UVA radiation can induce IL-1β expression on fibroblasts and then promote MMP-1 and MMP-3 expression, which can accelerate ECM degradation. On the other hand, prolonged exposure to UVA radiation reduced collagen and elastin synthesis on fibroblasts. Due to the acceleration of ECM degradation and the reduction of ECM synthesis, Atomic force microscope (AFM) was used to analyze the elasticity reduction on UVA-damaged fibroblasts. UVA irradiation causes photoaging on fibroblasts. UVA damaged fibroblasts with HA treatment can down-regulate the gene expression of MMP-1, MMP-3, and then slow down ECM degradation. On the other hand, HA may restore elastin and collagen synthesis in UV-damaged fibroblasts. Based on the slowdown of ECM degradation, UVA-damaged fibroblast elasticity can be effectively restored by HA treatment. In summary, HA can relief the photoaging conditions on fibroblasts, but may not be able to return fibroblasts to normal, healthy state. Although HA cannot fully recover UVA-damaged fibroblasts, HA is still potential for repairing photoaging skin.

Keywords: atomic force microscope, hyaluronic acid, UVA radiation, dermal fibroblasts

Procedia PDF Downloads 395

Authors: A. Elmajdoub, A. El-Mahmoudy

Abstract:

The present study was designed to investigate the neurotransmitters that mediate the excitatory response of the circular muscle of final branches of mesenteric artery in bovine calves. Mesentery was dissected and the iliac branches were separated and used. The final mesenteric branches of diameter 400 micrometers and less responded strongly to norepinephrine and moderately to ATP. However, the mesenteric branches of wider diameters were gradually less responsive to norepinephrine and those of diameter 700 micrometers were exclusively nonresponsive. These arteries were strongly responsive to ATP (100 µM). Norepinephrine response was sensitive to phentolamine (3 µM) and prazosin (5 µM) indicating that it is mediated by α1 receptor; while ATP response was sensitive to suramin (200 µM), PPADS (50 µM), but not to cibacron blue (100 µM) indicating that it is mediated via P2X receptor. Further confirmatory experiments were performed including application of α1 and P2X receptor specific agonists which are methoxamine and α,β-methylene ATP. Methoxamine (1 µM) showed effects similar to norepinephrine in final branches and was without effect in wider branches. α,β-methylene ATP (1 µM), exhibited more pronounced effects on both wide and narrow branches but in parallel manner to that of ATP. Agonists for α2 and P2Y receptors as clonidine (10 µM) and 2-meThio ATP (10 µM), respectively, were without effect indicating that involvement of these receptors is unlikely. The neuropeptide-Y (200 nM) did not have any effects on either the narrow or the wide rings. Conclusion: These data may imply that in the most peripheral mesenteric arteries a strong vasopressor power represented by norepinephrine and ATP integration is needed for maintaining peripheral resistance; on the other hand a mild vasopressor power mediated only by ATP is enough to maintain the vascular tone in the relatively central mesenteric branches.

Keywords: ATP, calves, mesenteric artery, norepinephrine

Procedia PDF Downloads 309