Search results for: drug sensitivity

Authors: Bushra Nabi, Saleha Rehman, Sanjula Baboota, Javed Ali

Abstract:

Aim: The objective of research undertaken is analytical method validation (HPLC method) of an anti-HIV drug Elvitegravir (EVG). Additionally carrying out the forced degradation studies of the drug under different stress conditions to determine its stability. It is envisaged in order to determine the suitable technique for drug estimation, which would be employed in further research. Furthermore, comparative pharmacokinetic profile of the drug from lipid architectonics and drug suspension would be obtained post oral administration. Method: Lipid Architectonics (LA) of EVR was formulated using probe sonication technique and optimized using QbD (Box-Behnken design). For the estimation of drug during further analysis HPLC method has been validation on the parameters (Linearity, Precision, Accuracy, Robustness) and Limit of Detection (LOD) and Limit of Quantification (LOQ) has been determined. Furthermore, HPLC quantification of forced degradation studies was carried out under different stress conditions (acid induced, base induced, oxidative, photolytic and thermal). For pharmacokinetic (PK) study, Albino Wistar rats were used weighing between 200-250g. Different formulations were given per oral route, and blood was collected at designated time intervals. A plasma concentration profile over time was plotted from which the following parameters were determined:

Keywords: AIDS, Elvitegravir, HPLC, nanostructured lipid carriers, pharmacokinetics

Procedia PDF Downloads 131

Authors: Jolanta Pulit-Prociak, Olga Dlugosz, Marcin Banach

Abstract:

The toxicity of bare zinc oxide nanoparticles used as drug carriers may be the result of releasing zinc ions. Thus, zinc oxide nanoparticles modified with galactose were obtained. The process of their formation was conducted in the microwave field. The physicochemical properties of the obtained products were studied. The size and electrokinetic potential were defined by using dynamic light scattering technique. The crystalline properties were assessed by X-ray diffractometry. In order to confirm the formation of the desired products, Fourier-transform infrared spectroscopy was used. The releasing of zinc ions from the prepared products when comparing to the bare oxide was analyzed. It was found out that modification of zinc oxide nanoparticles with galactose limits the releasing of zinc ions which are responsible for the toxic effect of the whole carrier-drug conjugate.

Keywords: nanomaterials, zinc oxide, drug delivery system, toxicity

Procedia PDF Downloads 176

Authors: Meltem Koray, Arda Ozgon, Duygu Ofluoglu, Mehmet Yaltirik

Abstract:

Oral ulcerations can be seen as a side effect of different drugs. These ulcers usually appear within a few weeks following drug treatment. In most of cases, these ulcers resist to conventional treatments, such as anesthetics, antiseptics, anti-inflammatory agents, cauterization, topical tetracycline and corticosteroid treatment. The diagnosis is usually difficult, especially in patients receiving multiple drug therapies. Hyaluronan or hyaluronic acid (HA) is a biomaterial that has been introduced as an alternative approach to enhance wound healing and also used for oral ulcer treatment. The aim of this report is to present the treatment of drug-induced oral ulceration on maxillary mucosa with HA gel. 60-year-old male patient was referred to Department of Oral and Maxillofacial Surgery complaining of oral ulcerations during few weeks. He had received chemotherapy and radiotherapy in 2014 with the diagnosis of nasopharyngeal carcinoma, and he has accompanying systemic diseases such as; cardiological, neurological diseases and gout. He is medicated with Escitalopram (Cipralex® 20mg), Quetiapine (Seroquel® 100mg), Mirtazapine (Zestat® 15mg), Acetylsalicylic acid (Coraspin® 100mg), Ramipril-hydrochlorothiazide (Delix® 2.5mg), Theophylline anhydrous (Teokap Sr® 200mg), Colchicine (Colchicum Dispert® 0.5mg), Spironolactone (Aldactone® 100mg), Levothyroxine sodium (Levotiron® 50mg). He had painful oral ulceration on the right side of maxillary mucosa. The diagnosis was 'drug-induced oral ulceration' and HA oral gel (Aftamed® Oral gel) was prescribed 3 times a day for 2 weeks. Complete healing was achieved within 3 weeks without any side effect and discomfort. We suggest that HA oral gel is a potentially useful local drug which can be an alternative for management of drug-induced oral ulcerations.

Keywords: drug-induced, hyaluronic acid, oral ulceration, maxillary mucosa

Procedia PDF Downloads 257

Authors: Tayaba Dastgeer, Farhan Rasheed, Muhammad Saeed, Maqsood Ahmad, Zia Ashraf, Abdul Waheed, Muhammad Kamran, Mohsin Khurshid

Abstract:

Objectives: The study aimed to determine the efficacy of linezolid against clinical isolates of methicillin-resistant staphylococcus aureus (MRSA). Methodology: This cross-sectional study was conducted in the microbiology department of Allama Iqbal Medical College Lahore from August 2017 to September 2019. Isolates were confirmed as MRSA via the presence of the mec-A gene. Confirmed MRSA isolates were processed for susceptibility testing against different antimicrobials, especially linezolid, via the disc diffusion method. Zone sizes were interpreted according to CLSI guidelines. Results: Various types of clinical samples were included in the study; however, the highest frequency of MRSA isolates was found in pus samples, followed by other clinical samples. Among hospitalized patients, most MRSA isolates were obtained from patients in the surgical ward. Of 243 mec-A gene detected isolates, Vancomycin and linezolid showed 100% susceptibility, chloramphenicol showed declining resistance 78 (32.09%), and emerging sensitivity 165 (67.90%) against MRSA. Conclusion: Linezolid is a very efficient drug against MRSA, but the use of this novel drug must be conserved for vancomycin-resistant Staphylococcus aureus or when more resistant pathogens are suspected.

Keywords: MRSA, chloramphenicol, linezolid, nosocomial infections

Procedia PDF Downloads 86

Authors: Nagasamy Venkatesh Dhandapani

Abstract:

This work aims at investigating the use of β-Cyclodextrin as a cross linker, in an attempt to formulate nanosponges containing ketoconazole. The nanosponges were prepared by cross-linking method. The excipients used in this study did not alter the physicochemical properties of a drug as revealed by FTIR spectroscopy. Studies on various formulation variables revealed that all the variables are inter-related with the formulation. The ideal batch among the formulation was selected based on the higher entrapment efficiency and drug loading. The in vitro release studies of ketoconazole nanosponges in hydrogel exhibited a sustained release over a period of 24 hours. Mathematical analysis of drug release from the formulation followed non-Fickian diffusion obeying first order kinetics. The anti-fungal activity of the formulation exhibited better zone of inhibition when compared to pure drug (ketoconazole) against Tinea corporis.

Keywords: nanosponges, beta-cyclodextrin, ketoconazole, tinea corporis

Procedia PDF Downloads 139

Authors: Venkatalakshmi Ranganathan, Ong Hsin Ju, Tan Yinn Ming, Lim Kien Sin, Wong Man Ting, Venkata Srikanth Meka

Abstract:

The mucoadhesive buccal tablet is an oral drug delivery system which attached to the buccal surface for direct drug absorption into the systemic circulation and the unidirectional drug release is ensured by formulating a hydrophobic backing layer. The objective of present study was to formulate mucoadhesive atenolol bilayer buccal tablets by using sodium alginate, hydroxyethyl cellulose, and xanthan gum as mucoadhesive polymer and the technique applied was direct compression method. Ethyl cellulose was used as backing layer of the tablet. FTIR and DSC analysis were carried out to identify the drug polymer interactions. The prepared tablets were evaluated for physicochemical parameters, ex vivo mucoadhesion time and in-vitro drug release. The formulated tablets showed the average surface pH 6-7 which is favourable for oral mucosa. The formulation containing sodium alginate showed more than 90 % of drug release at the end of the 7 hours in vitro dissolution studies. The formulation containing xanthan gum showed more than 8 hours of mucoadhesion time and all formulation exhibited non fickian release kinetics. The present study indicates enormous potential of erodible mucoadhesive buccal tablet containing atenolol for systemic delivery with an added advantage of circumventing the hepatic first pass metabolism.

Keywords: atenolol, mucoadhesion, in vitro drug release, direct compression, ethyl cellulose

Procedia PDF Downloads 612

Authors: Puntarikorn Rungrattanakasin

Abstract:

Objectives: To develop the trigger tool to warn about the risk of bleeding as an adverse event from warfarin drug usage during admission in Medical Wards of Chumphae Hospital. Methods: A retrospective study was performed by reviewing the medical records for the patients admitted between June 1st,2020- May 31st, 2021. ADEs were evaluated by Naranjo’s algorithm. The international normalized ratio (INR) and events of bleeding during admissions were collected. Statistical analyses, including Chi-square test and Reciever Operating Characteristic (ROC) curve for optimal INR threshold, were used for the study. Results: Among the 139 admissions, the INR range was found to vary between 0.86-14.91, there was a total of 15 bleeding events, out of which 9 were mild, and 6 were severe. The occurrence of bleeding started whenever the INR was greater than 2.5 and reached the statistical significance (p <0.05), which was in concordance with the ROC curve and yielded 100 % sensitivity and 60% specificity in the detection of a bleeding event. In this regard, the INR greater than 2.5 was considered to be an optimal threshold to alert promptly for bleeding tendency. Conclusions: The INR value of greater than 2.5 (>2.5) would be an appropriate trigger tool to warn of the risk of bleeding for patients taking warfarin in Chumphae Hospital.

Keywords: trigger tool, warfarin, risk of bleeding, medical wards

Procedia PDF Downloads 136

Authors: Surendra Agrawal, Pravina Gurjar, Supriya Bhide, Ram Gaud

Abstract:

Levamisole hydrochloride is a prominent anticancer drug in the treatment of colon cancer but resulted in toxic effects due poor bioavailability and poor cellular uptake by tumor cells. Levamisole is an unstable drug. Incorporation of this molecule in solid lipids may minimize their exposure to the aqueous environment and partly immobilize the drug molecules within the lipid matrix-both of which may protect the encapsulated drugs against degradation. The objectives of the study were to enhance bioavailability by sustaining drug release and to reduce the toxicities associated with the therapy. Solubility of the drug was determined in different lipids to select the components of Solid Lipid Nanoparticles (SLN). Pseudoternary phase diagrams were created using aqueous titration method. Formulations were subjected to particle size and stability evaluation to select the final test formulations which were characterized for average particle size, zeta potential, and in-vitro drug release and percentage transmittance to optimize the final formulation. SLN of Levamisole hydrochloride was prepared by Nanoprecipitation method. Glyceryl behenate (Compritol 888 ATO) was used as core comprising of Tween 80 as surfactant and Lecithin as co-surfactant in (1:1) ratio. Entrapment efficiency (EE) was found to be 45.89%. Particle size was found in the range of 100-600 nm. Zeta potential of the formulation was -17.0 mV revealing the stability of the product. In-vitro release study showed that 66 % drug released in 24 hours in pH 7.2 which represent that formulation can give controlled action at the intestinal environment. In pH 5.0 it showed 64% release indicating that it can even release drug in acidic environment of tumor cells. In conclusion, results revealed SLN to be a promising approach to sustain the drug release so as to increase bioavailability and cellular uptake of the drug with reduction in toxic effects as dose has been reduced with controlled delivery.

Keywords: SLN, nanoparticulate delivery of levamisole, pharmacy, pharmaceutical sciences

Procedia PDF Downloads 424

Authors: Zeynep Yazgan, Gökhan Aygün, Reyhan Çalışkan

Abstract:

Objective: Invasive fungal infections are a serious threat in terms of morbidity and mortality, especially in immunocompromised patients. The most frequently isolated agents are Aspergillus genus fungi, and sensitivity to azoles, which are the first choice in treatment, decreases. In our study, we aimed to investigate the use of the agar plate screening method as a fast, easy, and practical method in determining azole resistance in Aspergillus spp. species. Methods: Our study was conducted with 125 Aspergillus spp. isolates produced from various clinical samples. Aspergillus spp. isolates were identified by conventional methods and azole resistance was determined by gradient test and agar plate screening method. Broth microdilution method was applied to resistant isolates, and CypA-L98H and CypA-M220 mutations in the cyp51A gene were investigated. Results: In our study, 55 A. fumigatus complex (44%), 42 A. flavus (33.6%), 6 A. terreus (5%), 4 A. niger (3%) and 18 Aspergillus spp. (14%) were identified. With the gradient test method, resistance to VOR and POS was detected in 1 (1.8%) of A.fumigatus isolates, and resistance to ITR was detected in 3 (5.45%). With the agar plate method, 1 of the A.fumigatus isolates (1.8%) had VOR, ITR, POS, 1 of the A.terreus isolates (16.7%) had VOR, 1 of the A.niger isolates (25%) had ITR. Resistance to VOR and POS was detected in 2 Aspergillus spp. isolates (11%), and resistance to ITR was detected in 1 (5.6%). Sensitivity and specificity were determined as 100% for VOR and POS in A. fumigatus species, 33.3% and 100% for ITR, respectively, 100% for ITR in A. flavus species, and 100% for ITR and POS in A. terreus species. By broth microdilution method in 7 isolates in which resistance was detected by gradient test and/or agar plate screening method; 1 A.fumigatus resistant to ITR, VOR, POS, 2 A.fumigatus resistant to ITR, 2 Aspergillus spp. ITR, VOR, POS MICs were determined as 2µg/ml and 8µg/ml, 8µg/ml and >32µg/ml, 0.5µg/ml and 4µg/ml, respectively. CypA-L98H mutations were detected in 5 of these isolates, CypA-M220 mutations were detected in 6, and no mutation was detected in 1. CypA-L98H and CypA-M220 mutations were detected in 1 isolate for which resistance was not detected. Conclusion: The need for rapid antifungal susceptibility screening tests is increasing in the treatment of aspergillosis. Although the sensitivity of the agar plate method was determined to be 33.3% for A.fumigatus ITR in our study, its sensitivity and specificity were determined to be 100% for ITR, VOR, and POS in other species. The low sensitivity value detected for A.fumigatus showed that agar plate drug concentrations should be updated in accordance with the latest regulations of EUCAST guidelines. The CypA-L98H and CypA-M220 mutations detected in our study suggested that the distribution of azole resistance-related mutations in different regions in our country should be investigated. In conclusion, it is thought that the agar plate method, which can be easily applied to detect azole resistance, is a fast and practical method in routine use and can contribute to both the determination of effective treatment strategies and the generation of epidemiological data.

Keywords: Aspergillus, agar plate, azole resistance, cyp51A, cypA-L98H, cypA-M220

Procedia PDF Downloads 56

Authors: Zohreh Bayat, Dariush Minai-Tehrani

Abstract:

Pseudomonas aeruginosa is a Gram-negative, rode shape and aerobic bacterium that has shown to be resistance to many antibiotics. This resistance makes the bacterium very harmful in some diseases. It can also generate diseases in any part of the gastrointestinal tract from oropharynx to rectum. P. aeruginosa has become an important cause of infection, especially in patients with compromised host defense mechanisms. One of the most important reasons that make P. aeruginosa an emerging opportunistic pathogen in patients is its ability to use various compounds as carbon sources. Lipase is an enzyme that catalyzes the hydrolysis of lipids. Most lipases act at a specific position on the glycerol backbone of lipid substrate. Some lipases are expressed and secreted by pathogenic organisms during the infection. Muscarinic antagonist used as an antispasmodic and in urinary incontinence. The drug has little effect on glandular secretion or the cardiovascular system. It does have some local anesthetic properties and is used in gastrointestinal, biliary, and urinary tract spasms. Aim: In this study the inhibitory effect of a muscarinic antagonist on lipase of P. aeruginosa was investigated. Methods: P. aeruginosa was cultured in minimal salt medium with 1% olive oil as carbon source. The cells were harvested and the supernatant, which contained lipase, was used for enzyme assay. Results: Our results showed that the drug can inhibit P. aeruginosa lipase by competitive manner. In the presence of different concentrations of the drug, the Vmax (2 mmol/min/mg protein) of enzyme did not change, while the Km raised by increasing the drug concentration. The Ki (inhibition constant) and IC50 (the half maximal inhibitory concentration) value of drug was estimated to be about 30 uM and 60 uM which determined that the drug binds to enzyme with high affinity. Maximum activity of the enzyme was observed at pH 8 in the absence and presence of muscarinic antagonist, respectively. The maximum activity of lipase was observed at 600C and the enzyme became inactive at 900C. Conclusion: The muscarinic antagonist drug could inhibit lipase of P. aeruginosa and changed the kinetic parameters of the enzyme. The drug binded to enzyme with high affinity and did not chang the optimum pH of the enzyme. Temperature did not affect the binding of drug to musmuscarinic antagonist.

Keywords: Pseudomonas aeruginosa, drug, enzyme, inhibition

Procedia PDF Downloads 421

Authors: Farzad Khajavi, Farzaneh Jalilfar, Faranak Jafari, Leila Shokrani

Abstract:

Formulation of gliclazide in the form of extended-release tablet in 30 and 60 mg dosage forms was performed using hypromellose (HPMC K4M) as a retarding agent. Drug-release profiles were investigated in comparison with references Diamicron MR 30 and 60 mg tablets. The effect of size of powder particles, the amount of hypromellose in formulation, hardness of tablets, and also the effect of halving the tablets were investigated on drug release profile. A mathematical model which describes hypromellose behavior in initial times of drug release was proposed for the estimation of hypromellose content in modified-release gliclazide 60 mg tablet. This model is based on erosion of hypromellose in dissolution media. The model is applicable to describe release profiles of insoluble drugs. Therefore, by using dissolved amount of drug in initial times of dissolution and the model, the amount of hypromellose in formulation can be predictable. The model was used to predict the HPMC K4M content in modified-release gliclazide 30 mg and extended-release quetiapine 200 mg tablets.

Keywords: Gliclazide, hypromellose, drug release, modified-release tablet, mathematical model

Procedia PDF Downloads 209

Authors: Afia Naheed, Manmohan Singh, David Lucy

Abstract:

This work is based on a mathematical as well as statistical study of an SEIJTR deterministic model for the interpretation of transmission of severe acute respiratory syndrome (SARS). Based on the SARS epidemic in 2003, the parameters are estimated using Runge-Kutta (Dormand-Prince pairs) and least squares methods. Possible graphical and numerical techniques are used to validate the estimates. Then effect of the model parameters on the dynamics of the disease is examined using sensitivity and uncertainty analysis. Sensitivity and uncertainty analytical techniques are used in order to analyze the affect of the uncertainty in the obtained parameter estimates and to determine which parameters have the largest impact on controlling the disease dynamics.

Keywords: infectious disease, severe acute respiratory syndrome (SARS), parameter estimation, sensitivity analysis, uncertainty analysis, Runge-Kutta methods, Levenberg-Marquardt method

Procedia PDF Downloads 347

Authors: Ian Walmsley

Abstract:

The aim of this paper is to explore the influence of time and temporality on the experience of coming off heroin in prison. The presentation draws on qualitative data collected during a small-scale pilot study of the role of self-care in the process of coming off drugs in prison. Time and temporality emerged as a key theme in the interview transcripts. Drug dependent prisoners experience of time in prison has not been recognized in the research literature. Instead, the literature on prison time typically views prisoners as a homogenous group or tends to focus on the influence of aging and gender on prison time. Furthermore, there is a tendency in the literature on prison drug treatment and recovery to conceptualize drug dependent prisoners as passive recipients of prison healthcare, rather than active agents. In building on these gaps, this paper argues that drug dependent prisoners experience multiple temporalities which involve an interaction between the body-times of the drug dependent prisoner and the economy of time in prison. One consequence of this interaction is the feeling that they are doing, at this point in their prison sentence, double prison time. The second part of the argument is that time and temporality were a means through which they governed their withdrawing bodies. In addition, this paper will comment on the challenges of prison research in England.

Keywords: heroin withdrawal, time and temporality, prison, body

Procedia PDF Downloads 265

Authors: Sarika Gupta, Harshika Khanna, Ajay K Verma, Surya Kant

Abstract:

Background: Drug-resistant tuberculosis (DR-TB) is a growing health challenge to global TB control efforts. Pediatric DR-TB is one of the neglected infectious diseases. In our previously published report, we have notified an increased prevalence of DR-TB in the pediatric population at a tertiary health care centre in North India which was estimated as 17.4%, 15.1%, 18.4%, and 20.3% in (%) in the year 2018, 2019, 2020, and 2021. Limited evidence exists about a pattern of drug resistance, side effect profile and programmatic outcomes of Paediatric DR-TB treatment. Therefore, this study was done to find out the pattern of resistance, side effect profile and treatment outcome. Methodology: This was a prospective cohort study conducted at the nodal drug-resistant tuberculosis centre of a tertiary care hospital in North India from January 2021 to December 2022. Subjects included children aged between 0-18 years of age with a diagnosis of DR-TB, on the basis of GeneXpert (rifampicin [RIF] resistance detected), line probe assay and drug sensitivity testing (DST) of M. tuberculosis (MTB) grown on a culture of body fluids. Children were classified as monoresistant TB, polyresistant TB (resistance to more than 1 first-line anti-TB drug, other than both INH and RIF), MDR-TB, pre-XDR-TB and XDR-TB, as per the WHO classification. All the patients were prescribed DR TB treatment as per the standard guidelines, either shorter oral DR-TB regimen or a longer all-oral MDR/XDR-TB regimen (age below five years needed modification). All the patients were followed up for side effects of treatment once per month. The patient outcomes were categorized as good outcomes if they had completed treatment and cured or were improving during the course of treatment, while bad outcomes included death or not improving during the course of treatment. Results: Of the 50 pediatric patients included in the study, 34 were females (66.7%) and 16 were male (31.4%). Around 33 patients (64.7%) were suffering from pulmonary TB, while 17 (33.3%) were suffering from extrapulmonary TB. The proportions of monoresistant TB, polyresistant TB, MDR-TB, pre-XDR-TB and XDR-TB were 2.0%, 0%, 50.0%, 30.0% and 18.0%, respectively. Good outcome was reported in 40 patients (80.0%). The 10 bad outcomes were 7 deaths (14%) and 3 (6.0%) children who were not improving. Adverse events (single or multiple) were reported in all the patients, most of which were mild in nature. The most common adverse events were metallic taste 16(31.4%), rash and allergic reaction 15(29.4%), nausea and vomiting 13(26.0%), arthralgia 11 (21.6%) and alopecia 11 (21.6%). Serious adverse event of QTc prolongation was reported in 4 cases (7.8%), but neither arrhythmias nor symptomatic cardiac side effects occurred. Vestibular toxicity was reported in 2(3.9%), and psychotic symptoms in 4(7.8%). Hepatotoxicity, hypothyroidism, peripheral neuropathy, gynaecomastia, and amenorrhea were reported in 2 (4.0%), 4 (7.8%), 2 (3.9%), 1(2.0%), and 2 (3.9%) respectively. None of the drugs needed to be withdrawn due to uncontrolled adverse events. Conclusion: Paediatric DR TB treatment achieved favorable outcomes in a large proportion of children. DR TB treatment regimen drugs were overall well tolerated in this cohort.

Keywords: pediatric, drug-resistant, tuberculosis, adverse events, treatment

Procedia PDF Downloads 52

Authors: Marcelus U. Ajonina, Deodata B. Ngonga, Kenric B. Ware, Carine K. Nfor

Abstract:

Background: Lack of knowledge of rational use of antimalarial drugs among dispensers is a serious problem, especially in areas of intense transmission, thus increasing the risk of resistance and adverse drug reactions. This study was aimed at assessing the knowledge of malaria as well as perception and dispensing practices of antimalarials among vendors in Buea community. Methods: A community-based cross-sectional survey of a random sample of 140 drug vendors living within the Buea community was conducted between March and June 2017. A questionnaire was designed to obtain information from drug vendors on the general knowledge of malaria as well as dispensing practices. Data were analyzed using SPSS Statistics 20.0 and were considered significant at p ≤ 0.05. Results: Knowledge of malaria symptoms, transmission, and prevention was reasonable among 55.8% (77) of the respondents. Only 33.6% (47) of the respondents could attribute the cause of malaria to protozoan of genus Plasmodium species. Of the 140 vendors, 115 (82.7%) prescribe antimalarial drugs. The knowledge of the national protocol was malaria case management among dispensers was 35.0%. Vendors in hospital/community pharmacies were 2.4 times (OR = 3.14, 95% CI: 4.14 - 8.74, p < 0.001) more knowledgeable about malaria treatment protocol than those of in drugstores. The prevalence of self-prescription of antimalarials was 39.3%. Self-prescription was significantly higher in drugstores than hospital/community pharmacies (p=0.004). In all, 56 (40.6%) of vendors showed good practices regarding antimalarial drug dispensing with the majority (51.7%) from community pharmacies (OR=2.27,95% CI: 1.13-4.56). Conclusion: Findings reveal moderate knowledge of malaria but poor prescription and dispensing practices of antimalarial drugs among vendors, thus indicating a need for routine monitoring and evaluation to prevent the emergence of resistant strains to current efficacious antimalarials.

Keywords: antimalarials, drug retail outlets, dispensing, drug resistance, prescription

Procedia PDF Downloads 124

Authors: Venkata Srikanth Meka, Nur Arthirah Binti Ahmad Tarmizi Tan, Muhammad Syahmi Bin Md Nazir, Adinarayana Gorajana, Senthil Rajan Dharmalingam

Abstract:

Biphasic drug delivery systems are designed to release drug at two different rates, either fast/prolonged or prolonged/fast. A fast/prolonged release system provides a burst drug release at initial stage followed by a slow release over a prolonged period of time and in case of prolonged/fast release system, the release pattern is vice versa. Terminalia catappa gum (TCG) is a natural polymer and was successfully proven as a novel pharmaceutical excipient. The main objective of the present research is to investigate the applicability of natural polymer, Terminalia catappa gum in the design of oral biphasic drug delivery system in the form of mini tablets by using a model drug, buspirone HCl. This investigation aims to produce a biphasic release drug delivery system of buspirone by combining immediate release and prolonged release mini tablets into a capsule. For immediate release mini tablets, a dose of 4.5 mg buspirone was prepared by varying the concentration of superdisintegrant; crospovidone. On the other hand, prolonged release mini tablets were produced by using different concentrations of the natural polymer; TCG with a buspirone dose of 3mg. All mini tablets were characterized for weight variation, hardness, friability, disintegration, content uniformity and dissolution studies. The optimized formulations of immediate and prolonged release mini tablets were finally combined in a capsule and was evaluated for release studies. FTIR and DSC studies were conducted to study the drug-polymer interaction. All formulations of immediate release and prolonged release mini tablets were passed all the in-process quality control tests according to US Pharmacopoeia. The disintegration time of immediate release mini tablets of different formulations was varied from 2-6 min, and maximum drug release was achieved in lesser than 60 min. Whereas prolonged release mini tablets made with TCG have shown good drug retarding properties. Formulations were controlled for about 4-10 hrs with varying concentration of TCG. As the concentration of TCG increased, the drug release retarding property also increased. The optimised mini tablets were packed in capsules and were evaluated for the release mechanism. The capsule dosage form has clearly exhibited the biphasic release of buspirone, indicating that TCG is a suitable natural polymer for this study. FTIR and DSC studies proved that there was no interaction between the drug and polymer. Based on the above positive results, it can be concluded that TCG is a suitable polymer for the biphasic drug delivery systems.

Keywords: Terminalia catappa gum, biphasic release, mini tablets, tablet in capsule, natural polymers

Procedia PDF Downloads 382

Authors: Sharjeel Abid, Tanveer Hussain, Ahsan Nazir, Abdul Zahir, Nabyl Khenoussi

Abstract:

Localized application of drug has various advantages and fewer side effects as compared with other methods. Burn patients suffer from swear pain and the major aspects that are considered for burn victims include pain and infection management. Nano-fibers (NFs) loaded with drug, applied on local wound area, can solve these problems. Therefore, this study dealt with the fabrication of drug loaded NFs for better pain management. Two layers of NFs were fabricated with different drugs. Contact layer was loaded with Gabapentin (a nerve painkiller) and the second layer with acetaminophen. The fabricated dressing was characterized using scanning electron microscope, Fourier Transform Infrared Spectroscopy, X-Ray Diffraction and UV-Vis Spectroscopy. The double layered based NFs dressing was designed to have both initial burst release followed by slow release to cope with pain for two days. The fabricated nanofibers showed diameter < 300 nm. The liquid absorption capacity of the NFs was also checked to deal with the exudate. The fabricated double layered dressing with dual drug loading and release showed promising results that could be used for dealing pain in burn victims. It was observed that by the addition of drug, the size of nanofibers was reduced, on the other hand, the crystallinity %age was increased, and liquid absorption decreased. The combination of fast nerve pain killer release followed by slow release of non-steroidal anti-inflammatory drug could be a good tool to reduce pain in a more secure manner with fewer side effects.

Keywords: pain management, burn wounds, nano-fibers, controlled drug release

Procedia PDF Downloads 239

Authors: Vaibhav Rana, Nicholas Balaresque

Abstract:

The 3-cup anemometer is the most commonly used instrument for wind speed measurement and, consequently, for the wind resource assessment. Though the cup anemometer shows accurate measurement under quasi-static conditions, there is uncertainty in the measurement when subjected to field measurement. Sensitivity to the angle of attacks with respect to horizontal plane, dynamic response, and non-linear behavior in calibration due to friction. The presented work aimed to identify the sensitivity of anemometer to non-horizontal flow. The cup anemometer was investigated under low wind speed wind tunnel, first under the static flow direction changes and second under the dynamic direction changes, at a different angle of attacks, under the similar conditions of reference wind tunnel speeds. The cup anemometer response under both conditions was evaluated and compared. The results showed the anemometer under dynamic wind direction changes is highly sensitive compared to static conditions.

Keywords: wind energy, cup anemometer, directional sensitivity, dynamic behavior, wind tunnel

Procedia PDF Downloads 137

Authors: S. S. Patil, R. M. Mhetre, S. V. Patil

Abstract:

Lisinopril is an angiotensin converting enzyme inhibitor used in the treatment of hypertension and heart failure in prophylactic treatment after myocardial infarction and in diabetic nephropathy. However, it is very poorly absorbed from gastro-intestinal tract. Intranasal administration is an ideal alternative to the parenteral route for systemic drug delivery. Formulating multiparticulate system with mucoadhesive polymers provide a significant increase in the nasal residence time. The aim of the present approach was to overcome the drawbacks of the conventional dosage forms of lisinopril by formulating intranasal microspheres with Carbopol 974P NF and HPMC K4 M along with film forming polymer ethyl cellulose.The microspheres were prepared by emulsion solvent evaporation method. The prepared microspheres were characterized for encapsulation efficiency, drug loading, particle size, and surface morphology, degree of swelling, ex vivo mucoadhesion, drug release, ex vivo diffusion studies. All formulations has shown entrapment efficiency between 80 to more than 95%, mucoadhesion was more than 80 % and drug release up to 90 %. Ex vivo studies revealed tht the improved bioavailability of drug compared to oral drug administration. Both in vitro and in vivo studies conclude that combination of Carbopol and HPMC based microspheres shown better results than single carbopol based microspheres for the delivery of lisinopril.

Keywords: microspheres, lisinopril, nasal delivery, solvent evaporation method

Procedia PDF Downloads 517

Authors: Rashi Rajput, Manisha Singh

Abstract:

Escitalopram oxalate (ETP), an FDA approved antidepressant drug from the category of SSRI (selective serotonin reuptake inhibitor) and is used in treatment of general anxiety disorder (GAD), major depressive disorder (MDD).When taken orally, it is metabolized to S-demethylcitalopram (S-DCT) and S-didemethylcitalopram (S-DDCT) in the liver with the help of enzymes CYP2C19, CYP3A4 and CYP2D6. Hence, causing side effects such as dizziness, fast or irregular heartbeat, headache, nausea etc. Therefore, targeted and sustained drug delivery will be a helpful tool for increasing its efficacy and reducing side effects. The present study is designed for formulating mucoadhesive nanoparticle formulation for the same Escitalopram loaded polymeric nanoparticles were prepared by ionic gelation method and characterization of the optimised formulation was done by zeta average particle size (93.63nm), zeta potential (-1.89mV), TEM (range of 60nm to 115nm) analysis also confirms nanometric size range of the drug loaded nanoparticles along with polydispersibility index of 0.117. In this research, we have studied the in vitro drug release profile for ETP nanoparticles, through a semi permeable dialysis membrane. The three important characteristics affecting the drug release behaviour were – particle size, ionic strength and morphology of the optimised nanoparticles. The data showed that on increasing the particle size of the drug loaded nanoparticles, the initial burst was reduced which was comparatively higher in drug. Whereas, the formulation with 1mg/ml chitosan in 1.5mg/ml tripolyphosphate solution showed steady release over the entire period of drug release. Then this data was further validated through mathematical modelling to establish the mechanism of drug release kinetics, which showed a typical linear diffusion profile in optimised ETP loaded nanoparticles.

Keywords: ionic gelation, mucoadhesive nanoparticle, semi-permeable dialysis membrane, zeta potential

Procedia PDF Downloads 280

Authors: Jichan Jang

Abstract:

Mycobacterium abscessus is a rapidly growing life-threatening mycobacterium with multiple drug-resistance mechanisms. In this study, we screened the library to identify active molecules targeting Mycobacterium abscessus using resazurin live/dead assays. In this screening assay, the Z-factor was 0.7, as an indication of the statistical confidence of the assay. A cut-off of 80% growth inhibition in the screening resulted in the identification of four different compounds at a single concentration (20 μM). Dose-response curves identified three different hit candidates, which generated good inhibitory curves. All hit candidates were expected to have different molecular targets. Thus, we found that compound X, identified, may be a promising candidate in the M. abscessus drug discovery pipeline.

Keywords: Mycobacterium abscessus, antibiotics, drug discovery, emerging Pathogen

Procedia PDF Downloads 194

Authors: T. Padma, Jayashree S. Pillai

Abstract:

Random entities are an essential component in any cryptographic application. The suitability of a number theory based novel pseudorandom sequence called Pseudorandom Partial Quotient Sequence (PPQS) generated from the continued fraction expansion of irrational numbers, in cryptographic applications, is analyzed in this paper. An approach to build the algorithm around a hard mathematical problem has been considered. The PQ sequence is tested for randomness and its suitability as a cryptographic key by performing randomness analysis, key sensitivity and key space analysis, precision analysis and evaluating the correlation properties is established.

Keywords: pseudorandom sequences, key sensitivity, correlation, security analysis, randomness analysis, sensitivity analysis

Procedia PDF Downloads 575

Authors: Umairah Natasya Binti Mohd Omeershffudin, Suresh Kumar

Abstract:

Klebsiella pneumoniae, a Gram-negative enteric bacterium that causes nosocomial and urinary tract infections. Particular concern is the global emergence of multidrug-resistant (MDR) strains of Klebsiella pneumoniae. Characterization of antibiotic resistance determinants at the genomic level plays a critical role in understanding, and potentially controlling, the spread of multidrug-resistant (MDR) pathogens. In this study, drug-resistant Klebsiella pneumoniae strain 825795-1 was investigated with extensive computational approaches aimed at identifying novel drug targets among hypothetical proteins. We have analyzed 1099 hypothetical proteins available in genome. We have used in-silico genome subtraction methodology to design potential and pathogen-specific drug targets against Klebsiella pneumoniae. We employed bioinformatics tools to subtract the strain-specific paralogous and host-specific homologous sequences from the bacterial proteome. The sorted 645 proteins were further refined to identify the essential genes in the pathogenic bacterium using the database of essential genes (DEG). We found 135 unique essential proteins in the target proteome that could be utilized as novel targets to design newer drugs. Further, we identified 49 cytoplasmic protein as potential drug targets through sub-cellular localization prediction. Further, we investigated these proteins in the DrugBank databases, and 11 of the unique essential proteins showed druggability according to the FDA approved drug bank databases with diverse broad-spectrum property. The results of this study will facilitate discovery of new drugs against Klebsiella pneumoniae.

Keywords: pneumonia, drug target, hypothetical protein, subtractive genomics

Procedia PDF Downloads 164

Authors: Umme Hani, Mohammed Rahmatulla, Mohammed Ghazwani, Ali Alqahtani, Yahya Alhamhoom

Abstract:

Background and introduction: Neratinib is a potent anticancer drug used for the treatment of breast cancer. It is poorly soluble at higher pH, which tends to minimize the therapeutic effects in the lower gastrointestinal tract (GIT) leading to poor bioavailability. An attempt has been made to prepare and develop a gastro-retentive system of Neratinib to improve the drug bioavailability in the GIT by enhancing the gastric retention time. Materials and methods: In the present study a three-factor at two-level (23) factorial design based optimization was used to inspect the effects of three independent variables (factors) such as sodium alginate (A), sodium bicarbonate (B) and sodium citrate (C) on the dependent variables like in vitro gelation, in vitro floating, water uptake and percentage drug release. Results: All the formulations showed pH in the range 6.7 ±0.25 to 7.4 ±0.24, percentage drug content was observed to be 96.3±0.27 to 99.5 ±0.28%, in vitro gelation observed as gelation immediate remains for an extended period. Percentage of water uptake was in the range between 9.01±0.15 to 31.01±0.25%, floating lag time was estimated form 7±0.39 to 57±0.36 sec. F4 and F5 showed floating even after 12hrs. All formulations showed a release of around 90% drug release within 12hr. It was observed that the selected independent variables affect the dependent variables. Conclusion: The developed system may be a promising and alternative approach to augment gastric retention of drugs and enhances the therapeutic efficacy of the drug.

Keywords: neratinib, 2³ factorial design, sodium alginate, floating, in situ gelling system

Procedia PDF Downloads 146

Authors: Ajay Kumar, Neha Gupta

Abstract:

This work presents the sensitivity assessment of Gallium Nitride (GaN) material-based FinFET by dielectric modulation in the nanocavity gap for label-free biosensing applications. The significant deflection is observed in the electrical characteristics such as drain current (ID), transconductance (gm), surface potential, energy band profile, electric field, sub-threshold slope (SS), and threshold voltage (Vth) in the presence of biomolecules owing to GaN material. Further, the device sensitivity is evaluated to identify the effectiveness of the proposed biosensor and its capability to detect the biomolecules with high precision or accuracy. Higher sensitivity is observed for Gelatin (k=12) in terms of on-current (SION), threshold voltage (SVth), and switching ratio (SSR) by 104.88%, 82.12%, and 119.73%, respectively. This work is performed using a powerful tool 3D Sentaurus TCAD using a well-calibrated structure. All the results pave the way for GaN-FinFET as a viable candidate for label-free dielectric modulated biosensor applications.

Keywords: biosensor, biomolecules, FinFET, sensitivity

Procedia PDF Downloads 187

Authors: M. Kumpugdee-Vollrath, J.-P. Krause, S. Bürk

Abstract:

Most of the drugs used for pharmaceutical purposes are poorly water-soluble drugs. About 40% of all newly discovered drugs are lipophilic and the numbers of lipophilic drugs seem to increase more and more. Drug delivery systems such as nanoparticles, micelles or liposomes are applied to improve their solubility and thus their bioavailability. Besides various techniques of solubilization, oil-in-water emulsions are often used to incorporate lipophilic drugs into the oil phase. To stabilize emulsions surface active substances (surfactants) are generally used. An alternative method to avoid the application of surfactants was of great interest. One possibility is to develop O/W-emulsion without any addition of surface active agents or the so called “surfactant-free emulsion or SFE”. The aim of this study was to develop and characterize SFE as a drug carrier by varying the production conditions. Lidocaine base was used as a model drug. The injection method was developed. Effects of ultrasound as well as of temperature on the properties of the emulsion were studied. Particle sizes and release were determined. The long-term stability up to 30 days was performed. The results showed that the surfactant-free O/W emulsions with pharmaceutical oil as drug carrier can be produced.

Keywords: emulsion, lidocaine, Miglyol, size, surfactant, light scattering, release, injection, ultrasound, stability

Procedia PDF Downloads 474

Authors: Ismail Seçer

Abstract:

The purpose of this study is to investigate the effects of anxiety sensitivity in adolescents on anxiety disorder and childhood depression. Mood disorders and anxiety disorders in children and adolescents can be given examples of important research topics in recent years. The participants of the study consist of 670 students in Erzurum and Erzincan city centers. The participants of the study were 670 secondary and high school students studying in city centers of Erzurum and Erzincan. The participants were chosen based on convenience sampling. The participants were between the ages of 13 and 18 (M=15.7, Ss= 1.35) and 355 were male and 315 were female. The data were collected through Anxiety Sensitivity Index and Anxiety and Depression Index for Children and Adolescents. For data analysis, Correlation analysis and Structural Equation Model were used. In this study, correlational descriptive survey was used. This model enables the researcher to make predictions related to different variables based on the information obtained from one or more variables. Therefore, the purpose is to make predictions considering anxiety disorder and childhood depression based on anxiety sensitivity. For this purpose, latent variable and structural equation model was used. Structural equation model is an analysis method which enables the identification of direct and indirect effects by determining the relationship between observable and latent variables and testing their effects on a single model. CFI, RMR, RMSEA and SRMR, which are commonly accepted fit indices in structural equation model, were used. The results revealed that anxiety sensitivity impacts anxiety disorder and childhood depression through direct and indirect effects in a positive way. The results are discussed in line with the relevant literature. This finding can be considered that anxiety sensitivity can be a significant risk source in terms of children's and adolescents’ anxiety disorder experience. This finding is consistent with relevant research highlighting that in case the anxiety sensitivity increases then the obsessive compulsive disorder and panic attack increase too. The adolescents’ experience of anxiety can be attributed to anxiety sensitivity.

Keywords: anxiety sensitivity, anxiety, depression, structural equation

Procedia PDF Downloads 292

Authors: Courtney Evans, Yuto Morimitsu, Tsubasa Hisadome, Futo Inomoto, Masahiro Yoshida, Takayuki Takei

Abstract:

Hydrogels are useful biomaterials due to their highly biocompatible nature and their ability to absorb large quantities of liquid and mimic soft tissue. They are often used as therapeutic drug delivery systems. However, it is sometimes difficult to sustain controlled release when using hydrophobic medicines, as hydrogels are frequently hydrophilic. As such, this research shows the success of chitosan hydrogels modified through hydrophobic interaction. This was done through the imide bonding of the alkyl groups in fatty aldehydes and the amino groups in chitosan, followed by reductive animation. The resulting cryogels could be optimized for strength as well as sorption and desorption (of a hydrophobic dye used to mimic hydrophobic medicine) by varying the alkyl chain length and the substitution degree of the fatty aldehyde. Optimized cryogels showed potential as biomedical materials, particularly as drug delivery systems.

Keywords: biomedical materials, chitosan, drug carriers, hydrophobic modification

Procedia PDF Downloads 220

Authors: Elham Ahmadi

Abstract:

This study is conducted with the aim of investigating the effect of moderate physical activity (60% of maximal heart rate-MHR) on blood pressure in an elderly female with hypertension. Hypertension is considered a modifiable risk factor for cardiovascular disease through physical activity. The purpose and significance of this study were to investigate the role of exercise as an alternative therapy since some patients exhibit sensitivity/intolerance to some drugs. Initially, 65 hypertensive females (average age = 49.7 years) (systolic blood pressure, SBP >140 mmHg and/or diastolic blood pressure, DBP>85 mmHg) and 25 hypertensive females as a control group (average age = 50.3 years and systolic blood pressure, SBP >140 mmHg and/or diastolic blood pressure, DBP>85 mmHg) were selected. The subjects were divided based on their age, duration of disease, physical activity, and drug consumption. Then, blood pressure and heart rate (HR) were measured in all of the patients using a sphygmomanometer (pre-test). The exercise sessions consisted of warm-up, aerobic activity, and cooling down (total duration of 20 minutes for the first session up to 55 minutes in the last session). At the end of the 12th session (mid-test) and final session (24th session), blood pressure was measured for the last time (post-test). The control group was without any exercise during the study. The results were analyzed using a t-test. Our results indicated that moderate physical activity was effective in lowering blood pressure by 6.4/5.6–mm Hg for SBP and 2.4/4.3mm Hg for DBP in hypertensive patients, irrespective of age, duration of disease, and drug consumption ( P<.005). The control group indicates no changes in BP. Physical activity programs with moderate intensity (approximately at 60% MHR), three days per week, can be used not only as a preventive measure for diastolic hypertension (DBP>90 mmHg high blood pressure) but also as an alternative to drug therapy in the treatment of hypertension, as well.

Keywords: endurance exercise, elderly female, hypertension, physical activity

Procedia PDF Downloads 86

Authors: Bashar Al-Sabti, Jehad Harbali

Abstract:

Background: Pyridine is a reactive base that might be used in preparing sitagliptin. International Agency for Research on Cancer classifies pyridine in group 2B; this classification means that pyridine is possibly carcinogenic to humans. Therefore, pyridine should be monitored at the allowed limit in sitagliptin pharmaceutical ingredients. Objective: The aim of this study was to develop a novel ultra high performance liquid chromatography mass spectrometry (UHPLC-MS) method to estimate the quantity of pyridine impurity in sitagliptin pharmaceutical ingredients. Methods: The separation was performed on C8 shim-pack (150 mm X 4.6 mm, 5 µm) in reversed phase mode using a mobile phase of water-methanol-acetonitrile containing 4 mM ammonium acetate in gradient mode. Pyridine was detected by mass spectrometer using selected ionization monitoring mode at m/z = 80. The flow rate of the method was 0.75 mL/min. Results: The method showed excellent sensitivity with a quantitation limit of 1.5 ppm of pyridine relative to sitagliptin. The linearity of the method was excellent at the range of 1.5-22.5 ppm with a correlation coefficient of 0.9996. Recoveries values were between 93.59-103.55%. Conclusions: The results showed good linearity, precision, accuracy, sensitivity, selectivity, and robustness. The studied method was applied to test three batches of sitagliptin raw materials. Highlights: This method is useful for monitoring pyridine in sitagliptin during its synthesis and testing sitagliptin raw materials before using them in the production of pharmaceutical products.

Keywords: genotoxic impurity, pyridine, sitagliptin, UHPLC -MS

Procedia PDF Downloads 85