Posted by admin on Feb 28, 2018 in |
Olmesartan medoxomil (OLM) is a lipophilic (log P = 4.31) antihypertensive drug suffering from limited oral bioavailability in humans (26%) due to its low aqueous solubility, uncontrolled enzymatic conversion to the active metabolite (Olmesartan; OL) and efflux by drug resistance pumps. Surmounting such limitations via incorporation of OLM into self-nanoemulsifying drug delivery systems (SNEDDS). Based on OLM-equilibrium solubility studies in various oils, surfactants and co-surfactants, Capmul® MCM, Tween® 20, Cremophor® EL and polyethylene glycol – 400 (PEG) were combined in different ratios to plot ternary phase diagrams. OLM-loaded SENDDS were developed and evaluated forparticle size, polydispersity index (PDI), zeta potential, self-emulsification time, morphology, drug released percentages after 5-min (Q5min%), 1 hour (Q1h%) and dissolution efficiency percentages (DE1h%). The OL pharmacokinetics from SNEDDS (F6) and Benicar® tablets were evaluated (LC-MS/MS) in rabbits. Spherical OLM-loaded SNEDDS were developed. The best-achieved SNEDDS (F6) showed short emulsification time (13 s), fine droplet size (60.00nm), low PDI (0.25), negative zeta potential (-14.4mV), promising dissolution parameters; Q5min% (29.78%), Q1h% (66.69%) and DE1h% (47.96%) and enhanced...
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Posted by admin on Feb 28, 2018 in |
Tadalafil belongs to BCS class IV and recommended for treatment of erectile dysfunction. Micronization technique is used by researchers to improve its solubilization and dissolution rate. The conventional tabletting excipients pose challenge especially with micronized drug particles. The current research work aimed to study the effect of some speciality excipients on flow properties of micronized Tadalafil formulated wet granulation approach. Different grades of L-HPC and Lactose were studied. L-HPC grades included L-HPC NBD 21, L-HPC 21 and HPC – LM. The lactose grades included Milled lactose (Pharmatose 200M) and Granulated lactose (Supertab GR and Supertab SD 11). Milled lactose was used in formulation using wet granulation process whereas granulated lactose was used as directly compressible excipient. PVP k-30 added intra-granularly in concentration range of 1 – 3% w/w. All the formulation batches were evaluated for its micromeritics and dissolution. The batch with L-HPC NBD 21 showed ‘Excellent’ flow properties as compared to L-HPC LM and L-HPC 21. Both grades of granulated lactose showed ‘Excellent’ flow of granules but slightly...
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Posted by admin on Feb 28, 2018 in |
Objective: Antimicrobials have become one of the most misused therapeutic agents resulting in resistance. Present study was carried out to evaluate the antimicrobial drug utilization pattern. Method: A retrospective, observational record based study was done in hospitalized patients from medicine and surgery department of tertiary care hospital of central India over a period of one year. Result: Among 385 patients, 53.25% were females and 26.75% were in 41 – 50 years age group. Amongst 775 antimicrobials prescribed, 75% were injectables. Average number of antimicrobials per prescription was 2.01 ± 0.6. Use of antimicrobial monotherapy (39.74%) was common and 25.71% had more than two antimicrobials. About 33.16% drugs were prescribed by generic names and FDCs were prescribed in 37.14%. Culture and sensitivity tests were done in 35.6% cases. Cephalosporins (65.19%) were the most preferred antimicrobials followed by penicillins, aminoglycosides and antiamoebics. Ceftriaxone, amikacin and metronidazole were the most commonly prescribed antimicrobials. Prescribed daily dose (PDD) was greater than defined daily dose (DDD) for ceftriaxone, amikacin, amoxicillin, metronidazole and levofloxacin indicating...
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Posted by admin on Feb 28, 2018 in |
Antibiotics are most important commercially used secondary metabolites, produced by many soil microorganisms i.e., bacteria and fungi and employed in wide range. Most important antibiotics used today are of microbial origin. The emergence of the antibiotic resistance and need of broad spectrum antibiotics is in focus and in demand. In present study, soil samples from different areas were collected i.e., the sampling is classified based on its micro and macro environment (waste polluted soil) (normal street soil) and (agricultural soil), from a local soil and analyzed for the antibiotic production. After primary screening, bacterial isolates were identified as Micrococcus roseus, Brevibacterium sp., Bacillus subtilis, Bacillus anthracis and Bacillus cerus, through biochemical characterization, and fungal isolates were identified as Tricho-cladium opacum, Rhizocotania sp., Epicoccum nipponicum, Aspergillus niger and Cladosporium cladosporides through microscopic and macroscopic identification and checked for antibiotic activity against some common gram positive and negative bacteria namely, Staphylococcus aureus and Escherichia coli. The antibiotic test indicates that Bacillus subtilis, Bacillus anthracis, Epicoccum nipponicum, Aspergillus niger and Cladosporium cladosporides...
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Posted by admin on Feb 28, 2018 in |
Ganoderma is a miracle edible mushroom with unique composition and miraculous health benefits. The investigation aimed to elucidate interactions for the active compounds of Ganoderma lucidum namely Ganoderol A, Ganoderol B, Ganoderal A and Ganoderic Acid Y with Lanosterol 14 alpha demethylase enzyme using molecular docking software Arguslab. The effect of ganomycin1 and 2 as an inhibitor against HIV 1 protease and Tyrosinase were carried out using molecular docking software DOCK 6.3. The in-silico docking analysis of Ganoderma lucidum triterpenes was found to be effective as inhibitors of Lanosterol 14 alpha demethylase. The grid score and best scored conformations of Ganomycin 1 and 2 suggest that both have a significant inhibitory effect on these enzymes, comparable to the known inhibitors. The docking results showed significant inhibitory action of these compounds indicating the possibility that they can be used as potent drugs in the future. Thus these natural compounds have diverse structural and biological properties which can serve them to be utilized as a valuable lead molecule for the treatment...
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