Posted by admin on Apr 30, 2016 in |
Postoperative pain management is prerequisite element for care of surgical patient. Objective of this study was to develop and evaluate nefopam hydrochloride loaded poly (meth) acrylates nanospheres (NFH-NS) for post-incisional pain treatment. Nefopam hydrochloride (NFH) is a centrally acting, non-opioid analgesic exclusive for treatment of post-incisional pain. NFH-NS were fabricated using eudragit RL 100: RS 100 by quasi solvent diffusion technique to provide sustained release of NFH. Entrapment efficiency (% EE), drug loading (% DL), z-average, polydispersity index and zeta potential (ζ) of NFH-NS was found 84.972 ± 1.23%, 21.41 ± 2.02 %, 648 ± 4.8 nm, 0.53 and + 4.48 mV, respectively. Scanning electron micrographs asserted smooth morphology and substantial spherical shape of nanospheres. In-vitro dissolution test revealed that NFH-NS followed fickian diffusion for drug transport. Mean dissolution time, dissolution efficiency and difference factor (f1) for NFH-NS was 5.68 h, 68.9 % and 31.83, respectively, which indicated dissimilarity in dissolution profiles as compared to NFH. % EE and % DL of NFH-NS at 25 ± 2°C/60 ± 5...
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Posted by admin on Apr 30, 2016 in |
Glucosamine-6-phosphate synthase (G6PS) (EC 2.6.1.16), is an one of the drug target for the anti microbial species. Systemic anti bacterial and anti fungal infections are of the growing problems in contemporary medicines, however only limited anti bacterial agents are in clinical practice for selective action with low toxicity. Then there is an emergency need for more effective version of existing molecules as well as new potential target specific molecules. In this scenario, our present study is an attempt to find out specific molecules via in silico screening of novel chalcone based series of compounds targeting the glucosamine-6-phosphate synthase. Among the twenty five novel designed chalcones skeleton series of compounds, all of them have found to be successfully docking inside the active binding domain of G6PS target with a binding energy in a range of -7.35 to -9.99 Kcal/mol with predicted IC50 value range of 4.11 micro molar to 47.68 nano molar...
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Posted by admin on Apr 30, 2016 in |
Transdermal drug delivery system (TDDS) involving HPMC-PVA patches were prepared as matrix-dispersion system with Pioglitazone HCl (PH) or Gliclazide (GZ) and drug release pattern from these patches were evaluated in-vitro as well as in-vivo. It has been found that 82.41% of Pioglitazone HCl and 70.12% of Gliclazide were released in-vitro in the period of 12 hours and the release patterns was zero-order. In-vivo skin permeation studies in alloxan-induced diabetic rats showed significant improvement on day-to-day diabetic control. Treatment with the patches induced hypoglycemia in normal rats whereas in diabetic rats blood glucose level returned to normal level within 16 hours. These findings suggest that delivery of these drugs through TDDS may overcome the first-pass effect when administered orally and thus gives better glycemic control in diabetic...
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Posted by admin on Apr 30, 2016 in |
The computational modeling and high throughput screening techniques have been used to identify small molecules that specifically target functional surface sites of the androgen receptor in Prostate cancer. Pharmacophore modeling, Virtual screening, docking based analyses is used for development of new chemical entities. The purpose of the current work is to establish pharmacophore model for the FDA approved anti-androgen receptor drugs of prostate cancer by using the software Ligand Scout 3.1, The data sets for the anti-androgen compounds were downloaded in.sdf format from Pubchem database. The model consists of five hydrogen bond acceptors, and one hydrophobic moieties and one aromatic ring which are defined as essential feature for androgen receptor inhibitors. Then the derived pharmacophore model was compared with the Zinc database of available standard anticancer drugs, Virtual screening of ZINC chemical databases leads to identification of one hit, and this compound can be useful for the design of future targets and development of new drugs to cancer. The newly obtained compound is then docked with androgen receptor with...
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Posted by admin on Apr 30, 2016 in |
The persistent prevalence of poor-quality medicines in resource-limited settings has contributed significantly to the alarming global trends in antibiotic resistance. Antibiotics are among the most used, abused and counterfeited medicines and therefore require regular monitoring and surveillance to provide reliable data for proper healthcare delivery. This study evaluated the quality of a total of 45 samples of Azithromycin, Erythromycin and Clindamycin distributed in Accra and Lagos by HPLC for active pharmaceutical ingredient (API) content and in-vitro dissolution for bioavailability. The results revealed that although all the samples contained the requisite API, only 27% were compliant with US Pharmacopoeia requirements for content. For Azithromycin and Clindamycin samples, the presence of excess API was the cause for non-compliance. Regardless of the high failure rate with respect to content, all Azithromycin samples exhibited good dissolution profiles, while 67% of Clindamycin and 36% of Erythromycin were compliant with in-vitro dissolution. These findings suggest that the population in the study sites and possibly in other parts of the sub regionis exposed to substandard antibiotics....
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