Posted by admin on Apr 1, 2014 in |
Zopiclone (ZPC), a cyclopyrrolone derivative, is a short-acting hypnotic agent. Its pharmacological properties include hypnotic, sedative, anxiolytic, anticonvulsant and muscle-relaxant actions. ZPC has a single chiral centre, and its enantiomers are S-zopiclone (S-ZPC) and R-zopiclone (R-ZPC). S-ZPC was adjudge to possess two- fold enhanced pharmacological activity than racemate (ZPC) while its opposite enantiomer R-ZPC appears to have almost zero activity and elevated toxicity. A high performance LC-MS\MS method employing positive electrospray ionization was developed for the simultaneous determination of both S-ZPC and R-ZPC in human plasma samples by using S-Zopiclone d8 as internal standard. Analytes were extracted from plasma samples by employing solid phase extraction technique. After extraction, 5µL of clean sample was injected on to chromatographic system and distinct separation achieved on chiralpak IC-3, 0.46 cm I.D*15 cm L column with the isocratic mobile phase consisting of a mixture of Ammonia in Acetonitrile and Milli Q Water. Detection was performed using API 4000 MS that monitors specific transition per compound in Multi Reaction monitoring mode. Limit of quantitation...
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Posted by admin on Apr 1, 2014 in |
AIDS, a pandemic disease caused by HIV has a high mortality rate. Therapeutic failures have risen due to the emergence of resistant viral strains and adverse side-effects of Anti-HIV drugs. Thus, there arises a need to develop novel and promising anti-HIV drugs. BMS-378806 (BMS-806) inhibits the initial stages of HIV-1 infection by blocking the binding of viral gp120 protein to host-cell CD4 receptor. Protein- Ligand interaction plays a major role in structure-based drug designing. In this study, analogs of BMS-378806 drug for HIV target protein gp120 were virtually designed using Marvin Sketch 4.1.10 and molecular docking studies were carried out using HEX 4.1 docking software. From the results, it was observed that, analog-6 showed better binding affinity to gp120 with Etotal = -102.67 than the original BMS-378806 drug, thus indicating that this compound might be considered as a potential drug candidate against gp120 for controlling HIV-1 infection. Further studies need to be carried out to evaluate the pharmacological efficacy of these...
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Posted by admin on Apr 1, 2014 in |
Solid lipid nanoparticles (SLN) have been reported to be an alternative system to emulsions, liposomes, microparticles and their polymeric counterparts for various application routes since the early 1990s due to their advantages. Solid lipid nanoparticles colloidal drug carrier system gained a lot of popularity among researcher as colloidal drug carriers for incorporating hydrophilic or lipophilic drugs. Solid lipid nanoparticles are the rapidly developing field of nanotechnology with several potential applications in drug delivery, clinical medicine and research, as well as in other varied sciences. Due to their unique size-dependent properties, lipid nanoparticles offer the possibility to develop new therapeutics. The present review focuses on the utility of SLN in terms of their introduction, advantages, disadvantages, general ingredients used, production methodology, characterization and current...
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Posted by admin on Apr 1, 2014 in |
Spondias pinnata is a well-known plant indigenous to South East Asian countries. The plant has been used intensively in many traditional herbal medicines across the globe. This plant has been known to possess antimicrobial, anti-diabetic, ulcer-protective, anti-cancerous, anti-diarrhoeal, anthelmintic, cytotoxic and hepatoprotective activity. It has also been reported that different parts of the plant is used as anti-thirst, anti-emetic and as an anti-tubercular agent. It owes its different pharmacological activities to the wide range of phytoconstituents that are present in the plant. The plant is found to contain sterols, flavonoids, polysaccharides and gums. β-amyrin, oleanolic acid and amino acids—glycine, cystine, serine, alanine and leucine, daucosterol, cycloartanone 24-methylene and lignoceric acid, ellagitannins, galloylgeranin, lignoseric acid and β –carotein are the other constituents that are found to be present in the plant. An attempt has been made to compile these phytoconstituents studies and the different ethnomedicinal and pharmacological properties of Spondias pinnata and provide a full-fledged review in a single document. This review emphasizes the need for more extensive research and...
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Posted by admin on Apr 1, 2014 in |
Niosomes, an emerging class of novel vesicular systems, are non-ionic surfactant vesicles which can entrap both hydrophilic and lipophilic drugs. Niosomes are incorporated into in situ gels for sustained release of drug and to prolong the residence time. The aim of present study is to formulate and evaluate ocular niosomal in situ gels of Linezolid. Linezolid is a potent synthetic oxazolidinone derivative active against a broad range of gram positive and gram-negative aerobic and anaerobic bacteria. Niosomes were prepared using various surfactants (span 20, span 40, span 60 and span 80) in different ratios using thin film hydration technique. They were evaluated for particle size, entrapment efficiency and in vitro drug release. Niosomes prepared using cholesterol and span 60 in the ratio 1:2 showed higher entrapment efficiency and better in vitro drug release. The optimized formulation was formulated as in situ gels using Carbopol 971P and HPMC K4M in different ratios and evaluated for gelling capacity, pH, viscosity, in vitro drug release, drug content, antimicrobial activity and ocular irritation...
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