World Academy of Science, Engineering and Technology

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

Abstract:

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.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 2810

Authors: Anil Bhandari, Imran Khan Pathan, Peeyush K. Sharma, Rakesh K. Patel, Suresh Purohit

Abstract:

The purpose of this study was to prepare time and pH dependent release tablets of Ayurvedic Churna formulation and evaluate their advantages as colon targeted drug delivery system. The Vidangadi Churna was selected for this study which contains Embelin and Gallic acid. Embelin is used in Helminthiasis as therapeutic agent. Embelin is insoluble in water and unstable in gastric environment so it was formulated in time and pH dependent tablets coated with combination of two polymers Eudragit L100 and ethyl cellulose. The 150mg of core tablet of dried extract and lactose were prepared by wet granulation method. The compression coating was used in the polymer concentration of 150mg for both the layer as upper and lower coating tablet was investigated. The results showed that no release was found in 0.1 N HCl and pH 6.8 phosphate buffers for initial 5 hours and about 98.97% of the drug was released in pH 7.4 phosphate buffer in total 17 Hours. The in vitro release profiles of drug from the formulation could be best expressed first order kinetics as highest linearity (r²= 0.9943). The results of the present study have demonstrated that the time and pH dependent tablets system is a promising vehicle for preventing rapid hydrolysis in gastric environment and improving oral bioavailability of Embelin and Gallic acid for treatment of Helminthiasis.

Keywords: Embelin, Gallic acid, Vidangadi Churna, Colon targeted drug delivery.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 2385

Authors: Amit Kumar, Peeyush Sharma, Anil Bhandari

Abstract:

The aim of present work was to optimize the effect of Ethyl Cellulose (EC) and Polyvinyl Pyrrolidone (PVP) concentration in extended release solid dispersion of Glibenclamide using combination of hydrophilic and hydrophobic polymers such as Polyvinyl Pyrrolidone and Ethyl cellulose. The advantage of solid dispersion technique provides a unique approach to particle size reduction and increased rates of dissolution. The compatibility studies of the drug and polymers were studied by TLC and results suggested no interaction between drug and polymers. Solid dispersions of Glibenclamide were prepared by common solvent evaporation method using Polyvinyl Pyrrolidone and Ethyl cellulose. The results indicated that homogeneous or heterogeneous conditions during the preparation methods employed governed the internal structures of the polymer matrices while retaining the drug in an amorphous form. F2 formulation prepared by solid dispersion method, displayed extended drug release followed by Higuchi matrix model indicating diffusion release of GLB from polymer matrices.

Keywords: Ethyl Cellulose, Glibenclamide, Polyvinyl Pyrrolidone, Solid Dispersion.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 2526

Authors: Ahmed Abdi Hassan, Mustapha Muhammad Aliyu

Abstract:

Turmeric (Curcuma longa) belongs to the ginger family and is used for food coloring mostly in Asian countries. It has long traditional medicinal value for the treatment of inflammations with excellent antioxidant properties. The purpose of this study is to investigate the efficiency of turmeric powder in the treatment of hyperthyroidism when combined with carbimazole antithyroid drug. The trial was conducted on 20 hyperthyroid patients but only 16 of them were successfully enrolled for the study. The 16 patients were divided into two equal groups where one group was treated with the only carbimazole while the other group was treated with a combined approach of carbimazole plus turmeric for 6 months consecutively. The result obtained is promising showing an average improvement of 99% in Thyroid-stimulating hormone (TSH) and 88%Thyroid Autoantibodies (TPOAb) in patients treated with the combined approach compared to those treated with the only carbimazole with an average of 3% and 18% of TSH and TPOAb improvement respectively. However, no major difference has been observed in both T4 and T3. Therefore, turmeric powder is a promising treatment if carefully and consistently combined with carbimazole antithyroid drug at very low amounts of 1.5 to 2 grams for at least 2 to 3 times a week.

Keywords: Thyroid, curcuminoids, turmeric, thyroxine, triiodothyronine, thyroid stimulating hormone, TPOAb.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 421

Authors: M. Kumpugdee-Vollrath, T. Subongkot, T. Ngawhirunpat

Abstract:

In this project we are interested in studying different kinds of shed snake skins in order to apply them as a model membrane for pharmaceutical purposes instead of human stratum corneum. Many types of shed snake skins as well as model drugs were studied by different techniques. The data will give deeper understanding about the interaction between drugs and model membranes and may allow us to choose the suitable model membrane for studying the effect of pharmaceutical products.

Keywords: DSC, FTIR, permeation, SAXS, shed snake skin.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 2391

Authors: Emma R. Arakelova, Stepan G. Grigoryan, Ashot M. Khachatryan, Karapet E. Avjyan, Lilia M. Savchenko, Flora G. Arsenyan

Abstract:

The paper presents a new drugs delivery system, based on the thin film technology. As a model antitumor drug, highly toxic doxorubicin is chosen. The system is based on the technology of obtaining zinc oxide composite of doxorubicin by deposition of nanosize ZnO films on the surface of doxorubicin coating on glass substrate using DC magnetron sputtering of zinc targets in Ar:O₂ medium at room temperature. For doxorubicin zinc oxide compositions in the form of coatings and gels with 180-200nm thick ZnO films, higher (by a factor 2) in vivo (ascitic Ehrlich's carcinoma) antitumor activity is observed at low doses of doxorubicin in comparison with that of the initial preparation at therapeutic doses. The vector character of the doxorubicin zinc oxide composite transport to tumor tissues ensures the increase in antitumor activity as well as decrease of toxicity in comparison with the initial drug.

Keywords: Antitumor activity, doxorubicin, DC magnetron sputtering, zinc oxide.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 3614

Authors: Arpa Petchsomrit, Namfa Sermkaew, Ruedeekorn Wiwattanapatapee

Abstract:

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.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 4637

Authors: Sunil Kamboj, Vipin Saini, Suman Bala, Gaurav Sharma

Abstract:

The main aim of the present research was to encapsulate mefenamic acid in niosomes andincorporate the prepared niosomes in the carbopol gel base for sustained therapeutic action. Mefenamic acid loaded niosomes were prepared by thin film hydration technique and evaluated for entrapment efficiency, vesicular size and zeta potential. The entrapment efficiency of the prepared niosomes was found to increase with decreasing the HLB values of surfactants and vesicle size was found to increase with increasing the cholesterol concentration. Niosomal vesicles with good entrapment efficiencies were incorporated in carbopol gel base to form the niosomal gel. The prepared niosomal gel was evaluated for pH, viscosity, spreadability, extrudability and skin permeation study across the rat skin. The results of permeation study revealed that the gel formulated with span 60 niosomes sustained the drug release for 12h. Further the in vivo study showed the good inhibition of inflammation by the gel prepared with span 60 niosomes.

Keywords: Mefenamic acid, niosomal gel, nonionic surfactants, sustained release.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 3743

Authors: Y. Sangsen, K. Likhitwitayawuid, B. Sritularak, K. Wiwattanawongsa, R. Wiwattanapatapee

Abstract:

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.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 3089

Authors: Patcharawalai Jaisamut, Kamonthip Wiwattanawongsa, Ruedeekorn Wiwattanapatapee

Abstract:

Supersaturation of drugs in the gastrointestinal tract is one approach to increase the absorption of poorly water-soluble drugs. The stabilization of a supersaturated state was achieved by adding precipitation inhibitors that may act through a variety of mechanisms. In this study, the effect of the natural gums, acacia, gelatin, pectin and tragacanth on curcumin supersaturation in simulated gastric fluid (SGF) (pH 1.2), fasted state simulated gastric fluid (FaSSGF) (pH 1.6), and simulated intestinal fluid (SIF) (pH 6.8) was investigated. The results indicated that all natural gums significantly increased the curcumin solubility (about 1.2-6-fold) when compared to the absence of gum, and assisted in maintaining the supersaturated drug solution. Among the tested gums, pectin at 3% w/w was the best precipitation inhibitor with a significant increase in the degree of supersaturation about 3-fold in SGF, 2.4-fold in FaSSGF and 2-fold in SIF.

Keywords: Curcumin, Solubility, Supersaturation, Precipitation inhibitor.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 2318

Authors: R. S. Chandan, M. Vasudevan, Deecaraman, B. M. Gurupadayya

Abstract:

In Pharmaceutical industries, it is very important to remove drug residues from the equipment and areas used. The cleaning procedure must be validated, so special attention must be devoted to the methods used for analysis of trace amounts of drugs. A rapid, sensitive and specific reverse phase ultra performance liquid chromatographic (UPLC) method was developed for the quantitative determination of Albendazole in cleaning validation swab samples. The method was validated using an ACQUITY HSS C₁₈, 50 x 2.1mm, 1.8μ column with a isocratic mobile phase containing a mixture of 1.36g of Potassium dihydrogenphosphate in 1000mL MilliQ water, 2mL of triethylamine and pH adjusted to 2.3 ± 0.05 with ortho-phosphoric acid, Acetonitrile and Methanol (50:40:10 v/v). The flow rate of the mobile phase was 0.5 mL min^-1 with a column temperature of 35⁰C and detection wavelength at 254nm using PDA detector. The injection volume was 2µl. Cotton swabs, moisten with acetonitrile were used to remove any residue of drug from stainless steel, teflon, rubber and silicon plates which mimic the production equipment surface and the mean extraction-recovery was found to be 91.8. The selected chromatographic condition was found to effectively elute Albendazole with retention time of 0.67min. The proposed method was found to be linear over the range of 0.2 to 150µg/mL and correlation coefficient obtained is 0.9992. The proposed method was found to be accurate, precise, reproducible and specific and it can also be used for routine quality control analysis of these drugs in biological samples either alone or in combined pharmaceutical dosage forms.

Keywords: Cleaning validation, Albendazole, residues, swab analysis, UPLC.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 3105

Authors: Thitaporn Thoopputra, Tipaporn Pongmesa, Shuchuen Li

Abstract:

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.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 2204

Authors: P. S. Bedi, Neayti Thakur, Balvinder Singh

Abstract:

In the present study an attempt has been made to prepare the crude extracts of leaves and stem of ‘Girardinia heterophylla’ by using various solvents like petroleum ether, ethanol and double distilled water. The samples were given the code NGLS 1, NGLS 2, NGLS 3 and NGSS 1, NGSS 2 and NGSS 3 respectively. All the extracts were used to study their antimicrobial activity against gram positive bacteria e.g. Bacillus subtilis, gram negative bacteria e.g. E. coli and K. pneumonia and antifungal activity against Aspergillus niger. The results of the antimicrobial activity showed that all the crude extracts of the plant possesses antibacterial activity. Maximum antibacterial activity was shown by NGLS 2, NGLS 3 and NGSS 3 against K. pneumonia. The growth of fungus A. niger was also inhibited by all the crude extracts. Maximum inhibition was shown by NGSS 2 followed by NGSS 1.

Keywords: Girardinia heterophylla, leaves and stem extracts, antibacterial activity, antifungal activity.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 2383

Authors: K. Obikeze, P. Mugabo, I. Green, D. Dietrich, A. Burger

Abstract:

Leonotisleonurus a shrub indigenous to Southern Africa is widely used in traditional medicine to treat a variety of conditions ranging from skin diseases and cough to epileptic fits and ‘heart problems’. Studies on the aqueous extract of the leaves have indicated cycloxegenase enzyme inhibitory activity and an antihypertensive effect. Five methanol leaf extract fractions (MLEa - MLEe) of L. leonurus were tested on anaesthetized normotensive male Wistar rats (AWR) and isolated perfused working rat hearts (IWH). Fraction MLEc (0.01mg/kg – 0.05mg/kg) induced significant increases in BP and HR in AWR and positive chronotropic and inotropic effects in IWH (1.0mg/ml – 5.0mg/ml). Pre-administration of atenolol (2.0mg/kg) and prazosin (60μg/kg) significantly inhibited MLEc effect on HR and MAP respectively in vivo, while atenolol (7.0mg/ml) pre-perfusion significantly inhibited MLEc effect in vitro. The hypertensive effect of MLEc is probably via β1agonism. Results also indicate the presence of multiple cardioactive compounds in L. leonurus.

Keywords: Cardiovascular effect, in vitro, in vivo, isolated perfused working heart, Leonotis leonurus, rat.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 2092

Authors: Rathapon Asasutjarit, Chayanid Sorrachaitawatwong, Nardauma Tipchuwong, Sirijit Pouthai

Abstract:

This study was conducted to formulate diclofenac sodium-loaded chitosan nanoparticles and to study the effect of formulation compositions on particle size and zeta potential of chitosan nanoparticles (CSN) containing diclofenac sodium (DC) prepared by ionotropic gelation method. It was found that the formulations containing chitosan, DC and tripolyphosphate (TPP) at a weight ratio of 4:1:1, respectively, with various pH provided various systems. At pH 5.0 and 6.0, the obtained systems were turbid because of precipitation of DC and chitosan, respectively. However, the dispersed system of CSN possessing diameter of 108±1 nm and zeta potential of 19±1 mV could be obtained at pH 5.5. These CSN also showed spherical morphology observed via a transmission scanning electron microscope. Change in weight ratio of chitosan:DC:TPP i.e. 1:1:1, 2:1:1, 3:1:1 and 4:1:1 showed that these ratios led to precipitation of particles except for the ratio of 4:1:1 providing CSN properly. The effect of Tween 80 as a stabilizer was also determined. It suggested that increment of Tween 80 concentration to 0.02% w/v could stabilize CSN at least 48 hours. However, increment of Tween 80 to 0.03% w/v led to quick precipitation of particles. The study of effect of TPP suggested that increment of TPP concentration increased particle size but decreased zeta potential. The excess TPP caused precipitation of CSN. Therefore, the optimized CSN was the CSN containing chitosan, DC and TPP at the ratio of 4:1:1and 0.02% w/v Tween 80 prepared at pH 5.5. Their particle size, zeta potential and entrapment efficiency were 128±1 nm, 15±1 mV and 45.8±2.6%, respectively.

Keywords: Chitosan nanoparticles, diclofenac sodium, size, zeta potential.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 4537

Authors: Manish Kumar Gautam, Raj Kumar Goel

Abstract:

Delayed wound healing in diabetes is primarily associated with hyperglycemia, over-expression of inflammatory marker, oxidative stress and delayed collagen synthesis. This unmanaged wound is producing high economic burden on the society. Thus research is required to develop new and effective treatment strategies to deal with this emerging issue. Our present study incorporates the evaluation of wound healing effects of 50% ethanol extract of Ocimum sanctum (OSE) in streptozotocin (45mg/kg)-induced diabetic rats with concurrent wound ulcer. The animals showing diabetes (Blood glucose level >140 and <250 mg/dL) will be selected for wound healing study using standard dead space wound model. Wounds were created by implanting two polypropylene tubes (0.5 x 2.5 cm2 each), one on either side in the lumbar region on the dorsal surface of each rat. On the 10th postwounding day, the animals were sacrificed and granulation tissue formed on the implanted tubes was carefully dissected out and study the status of antioxidants (Superoxide dismutase, SOD and Glutathione, GSH) free radicals (Lipid peroxidation, LPO and nitric oxide, NO) acute inflammatory marker (myeloperoxidase, MPO) connective tissue determinants, hydroxyproline, hexosamine and hexuronic acid, which play a major role in wound healing and diabetes. Besides the anti-diabetic parameters (estimation of serum blood glucose, triglycerides and total cholesterol), the above parameters for wound healing were studied both in normal, untreated and OSE treated diabetic rats. The effects of extract on above parameters will be compared with known standard antioxidant (Vitamin E) and anti-diabetic (Glybenclamide) drugs. OSE 400 mg/kg substantiated by significantly decreased serum blood glucose, triglycerides and total cholesterol. OSE also decrease granulation tissue free radicals (LPO, 58.1% and NO, 52.7%) and myeloperoxidase (MPO, 63.3%), and enhanced antioxidants (GSH, 116.4% and SOD, 201.1%)

Keywords: Wound healing, diabetes, Ocimum sanctum, Antioxidant, Free radical, Myeloperoxidase

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 3160

Authors: Vipin Saini, Sunil Kamboj, Suman Bala, A. Pandurangan

Abstract:

The present invention relates to multiple-unit tablet dosage forms, which is composed of several subunits (multiparticulates/pellets). Each small multiparticulate further composed of many layers. Some layer contains drug substance; others are rate controlling polymer. The resulting multiple-unit tablet dosage forms of pantoprazole were satisfactory fabricated. Pelletization technique has some advantages over coated tablet formulation. In coated tablet the coating may be damaged and a pinhole possibly formed that would result in increased release of drug in stomach and may be deactivated in stomach juices. If the coat of some pellets may be damaged that would not affect the release properties of the multiple-unit tablet. Hence they are beneficial in this aspect. The results confirmed the successful preparation of stable and bioequivalent once daily controlled release multiple-unit tablets of pantoprazole.

Keywords: Controlled release, multiple unit tablets, pantoprazole, pelletization.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 3257

Authors: S. S. Pathak, M. A. Borkar, S. S. Patel

Abstract:

To compare Healing Effects of an Ayurvedic Preparation and Silver Sulfadiazine on burn wounds in Albino Rats. Methods: Albino rats– 30 male / female rats weighing between 150-200 g were used in the study. They were individually housed and maintained on normal diet and water ad libitum. Partial thickness burn wounds were inflicted, on overnight-starved animals under pentobarbitone (30mg/kg, i.p.) anaesthesia, by pouring hot molten wax at 80oC into a plastic cylinder of 300 mm2 circular openings placed on the shaven back of the animal. Apart from the drugs under investigation no local/ systemic chemotherapeutic cover will be provided to animals. All the animals were assessed for the percentage of wound contraction, signs of infection, scab formation and histopathological examination. Results: Percentage of wound healing was significantly better in the test ointment group compared to the standard. Signs of infection were observed in more animals in the test ointment group compared to the standard. Scab formation also took place earlier in the test ointment group compared to standard. Epithelial regeneration and healing profile was better in the test ointment compared to the standard. Moreover the test ointment group did not show any raised margins in the wound or blackish discoloration as was observed in silver sulfadiazine group. Conclusion: The burn wound healing effect of the ayurvedic ointment under study is better in comparison to standard therapy of silver sulfadiazine. The problem of infection encountered with the test ointment can be overcome by changing the concentrations and proportions of the ingredients in the test ointment which constitutes the further plan of the study.

Keywords: Ayurvedic test ointment, burn wounds, Silver sulfadiazine.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 2406

Authors: Raissa A. Muzychkina, Irina M. Korulkina, Dmitriy Yu. Korulkin

Abstract:

In article the data of acute toxicity for pre-clinical researches of Ramon preparation is described. Ramon effects to clinical characteristics of blood, cardio-vascular system, hepatotoxic and diuretic effects were studied.

Keywords: Cancer, toxicity, antitumor activity, pre-clinical testing, anthraquinones, phytopreparation, Ramon.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 1744

Authors: S. Gupta, R. Chadha

Abstract:

Five crystal modifications of water insoluble artesunate were generated by recrystallizing it from various solvents with improved physicochemical properties. These generated crystal forms were characterized to select the most potent and soluble form. SEM of all the forms showed changes in external shape leading them to be different morphologically. DSC thermograms of Form III and Form V showed broad endotherm peaks at 83.04oC and 76.96oC prior to melting fusion of drug respectively. Calculated weight loss in TGA revealed that Form III and Form V are methanol and acetone solvates respectively. However, few additional peaks were appeared in XRPD pattern in these two solvate forms. All forms exhibit exothermic behavior in buffer and two solvates display maximum ease of molecular release from the lattice. Methanol and acetone solvates were found to be most soluble forms and exhibited higher antimalarial efficacy showing higher survival rate (83.3%) after 30 days.

Keywords: Artesunate, Crystal modifications, in vivo studies, Recrystallization.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 3323

Authors: C. Hönnscheidt, R. Krull

Abstract:

Oxidative stress makes up common incidents in eukaryotic metabolism. The presence of diverse components disturbing the equilibrium during oxygen metabolism increases oxidative damage unspecifically in living cells. Body´s own ubiquinone (Q10) seems to be a promising drug in defending the heightened appearance of reactive oxygen species (ROS). Though, its lipophilic properties require a new strategy in drug formulation to overcome their low bioavailability. Consequently, the manufacture of heterogeneous nanodispersions is in focus for medical applications. The composition of conventional nanodispersions is made up of a drug-consisting core and a surfactive agent, also named as surfactant. Long-termed encapsulation of the surfactive components into tissues might be the consequence of the use during medical therapeutics. The potential of provoking side-effects is given by their nonbiodegradable properties. Further improvements during fabrication process use the incorporation of biodegradable components such as modified γ-polyglutamic acid which decreases the potential of prospective side-effects.

Keywords: Biopolymers, γ-Polyglutamic acid, Oxidative stress, Ubiquinone.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 2238

Authors: Dmitriy Yu. Korulkin, Raissa A. Muzychkina

Abstract:

The Ramon preparation is received from a plant; it is destined for external treatment of inflammations in post-surgery period. The Ramon is a biogenic immune stimulator accelerating metabolism, contributing to improvement of blood indexes, having general tonic, anti-inflammatory and bactericidal effect.

Keywords: Anti-inflammatory, anthraquinones, bactericidal activity, Ramon.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 1579

Authors: Dae Hwan Kang, Young-IL Jeong, Chung-Wook Chung

Abstract:

pH-sensitive drug targeting using nanoparticles for cancer chemotherapy have been spotlighted in recent decades. Graft copolymer composed of poly (L-histidine) (PHS) and dextran (DexPHS) was synthesized and pH-sensitive nanoparticles were fabricated for pH-responsive drug delivery of doxorubicin (DOX). Nanoparticles of DexPHS showed pH-sensitive changes in particle sizes and drug release behavior, i.e. particle sizes and drug release rate were increased at acidic pH, indicating that DexPHS nanoparticles have pH-sensitive drug delivery potentials. Antitumor activity of DOX-incorporated DexPHS nanoparticles were studied using CT26 colorectal carcinoma cells. Results indicated that fluorescence intensity was higher at acidic pH than basic pH. These results indicated that DexPHS nanoparticles have pH-responsive drug targeting.

Keywords: pH-sensitive polymer, nanoparticles, block copolymer, poly (L-histidine).

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 2463

Authors: P. Thongmuang

Abstract:

The purposes of this research were 1) to survey the number of drugstores that unlawful dispense of asthma prescription drugs, in form of drug combinations in the Phaya Thai district of Bangkok, 2) to find the steroids contained in that drug combinations, 3) to find a means for informing general public about the dangers of drugs and for a campaign to stop dispensing them. Researcher collected drug combinations from 69 drugstores in Phaya Thai district from Feb 15, 2012 to Mar 15, 2012. The survey found 30.43%, 21, drug stores, sold asthma drug combinations to customers without a prescription. These collected samples were tested for steroid contamination by using Immunochromatography kits. Eleven samples, 52.38%, were found contaminated with steroids. In short, there should be control and inspection of drugstores in the distribution of steroid medications. To improve the knowledge of self health maintenance and drug usage among public, Thai Government and Department of Public Health should educate people about the side effects of using drug combinations and steroids.

Keywords: Dispensing, Drug Combinations, Steroids

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 2058

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

Abstract:

The possible therapeutic effect of cannabidiol, the major non-psychotropic Cannabis constituent, was investigated against acute hepatotoxicity induced by a single oral dose of acetaminophen (500mg/kg) in mice. Cannabidiol (two intraperitoneal injections, 5mg/kg, each) was given 1 hour and 12 hours following acetaminophen administration. Acetaminophen administration caused significant elevations of serum alanine aminotransferase, and hepatic malondialdehyde, and nitric oxide levels, and a significant decrease in hepatic reduced glutathione. Cannabidiol significantly attenuated the deterioration in the measured biochemical parameters resulted from acetaminophen administration. Also, histopathological examination showed that cannabidiol markedly attenuated ameliorated acetaminophen-induced liver tissue damage. These results emphasize that cannabidiol represents a potential therapeutic option to protect against acetaminophen hepartotoxicity which is a common clinical problem.

Keywords: cannabidiol, acetaminophen, liver, mice.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 2868

Authors: B. Michelle Sweeting

Abstract:

Pepper spray use has gained momentum since 1992 and although the active ingredient is readily available, it is considered a weapon with restricted use in many regions, including The Bahamas. In light of controversy in the literature regarding the severity of presenting respiration complaints among individuals postacute exposure of pepper spray inhalation, this descriptive case series study was conducted to assess the respiratory status of persons evaluated during a mass casualty in The Bahamas. Parameters noted were patients- demographics and respiration severity determined via clinical examination findings, disposition and follow-up review of the 20 persons. Their most common complaint was difficulty breathing post exposure. Two required admission and stayed for <24 hours uneventfully. All cases remained without residual complaints upon follow-up. Results showed that although respiration difficulty was perceived as the most detrimental of presenting complaints, it was noted to be mostly subjective with benign outcome.

Keywords: Acute Pepper Spray Inhalation, Capsaicinoids, Oleoresin Capsicum, Pepper spray, Respiratory severity severity.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 2065

Authors: S. Distantina, Rochmadi, M. Fahrurrozi, Wiratni

Abstract:

Preparation of hydrogel based on carrageenan extracted from Kappaphycus alvarezii was conducted with film immersion in glutaraldehyde solution (GA 4%w/w) for 2min and then followed by thermal curing at 110°C for 25min. The method of carrageenan recovery strongly determines the properties of crosslinked carrageenan. Hydrogel obtained from alkali treated carrageenan showed higher swelling ability compared to hydrogel from nonalkali treated carrageenan. Hydrogel from alkali treated showed the ability of sensitive to pH media.

Keywords: Hydrogel, carrageenan, swelling, alkali treated.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 3309

Authors: Minky Son, Chanin Park, Ayoung Baek, Shalini John, Keun Woo Lee

Abstract:

3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR) catalyzes the conversion of HMG-CoA to mevalonate using NADPH and the enzyme is involved in rate-controlling step of mevalonate. Inhibition of HMGR is considered as effective way to lower cholesterol levels so it is drug target to treat hypercholesterolemia, major risk factor of cardiovascular disease. To discover novel HMGR inhibitor, we performed structure-based pharmacophore modeling combined with molecular dynamics (MD) simulation. Four HMGR inhibitors were used for MD simulation and representative structure of each simulation were selected by clustering analysis. Four structure-based pharmacophore models were generated using the representative structure. The generated models were validated used in virtual screening to find novel scaffolds for inhibiting HMGR. The screened compounds were filtered by applying drug-like properties and used in molecular docking. Finally, four hit compounds were obtained and these complexes were refined using energy minimization. These compounds might be potential leads to design novel HMGR inhibitor.

Keywords: Anti-hypercholesterolemia drug, HMGR inhibitor, Molecular dynamics simulation, Structure-based pharmacophore modeling.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 1948

Authors: Peeyush Kumar, Sapna Mishra, Anushree Malik, Santosh Satya

Abstract:

The essential oil of M. × piperita L. was formulated into a topical gel. The prepared gel was characterized for its pH, viscosity, spreadiblity, consistency and extrudiblity, while its stability was evaluated under different temperature conditions. The prepared M. × piperita oil gel was clear and transparent. The pH value of developed gel was 6.6, while its viscosity was 1200 cP. Spreadability and consistency of the M. × piperita oil gel was 10.7 g.cm/sec and 7 mm, respectively. The prepared gel showed good extrudiblity. During the stability studies, no significant change in pH and viscosity as a function of time for gel was observed, indicating stability of prepared formulation. The gel developed in this study is expected to forward the usage of M. × piperita essential towards commercial application.

Keywords: M. × piperita L., formulation, gel, characterization, stability

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 3127

Authors: Diky Mudhakir, M. Fauzi Bostanudin, Fiki Firmawan, Rachmat Mauludin

Abstract:

In the present study, development of salbutamol sulphate nanoparticles that adhere to gastric mucus was investigated. Salbutamol sulphate has low bioavailability due to short transit time in gastric. It also has a positive surface charge that provides hurdles to be encapsulated by the positively strong mucoadhesive polymer of chitosan. To overcome the difficulties, the surface charge of active ingredient was modified using several nonionic and anionic stomach-specific polymers. The nanoparticles were prepared using ionotropic gelation technique. The evaluation involved determination of particle size, zeta potential, entrapment efficiency, in vitro drug release and in vitro mucoadhesion test. Results exhibited that the use of anionic alginate polymer was more satisfactory than that of nonionic polymer. Characteristics of the particles was nano-size, high encapsulation efficiency, fulfilled the drug release requirements and adhesive towards stomach for around 11 hours. This result shows that the salbutamol sulphate nanoparticles can be utilized for improvement its delivery.

Keywords: Mucoadhesive, salbutamol sulphate, nanosize, anionic polymer.

Procedia APA BibTeX Chicago EndNote Harvard JSON MLA RIS XML ISO 690 PDF Downloads 2565