International Journal of Pharmaceutical Sciences and Drug Research

199-203

Authors: J. S. Shah1*, J. B. Patel2, S. Dani3

Coronary Artery Disease (CAD) occurs when the arteries of the heart that normally provide blood and oxygen to the heart are narrowed or even completely blocked due to clot formation. The Stenting implantation composes 84.2% of all Percutaneous coronary intervention (PCI). Despite the widespread use of these devices, bare metal stents (BMS) have been associated with a 20-30% restenosis rate which requires reintervention. In December 2006, US Food and Drug Administration cardiovascular experts concluded that for many patients, such as those with uncomplicated medical histories who undergo elective stenting of simple coronary blockages, drug-eluting stents remain a safe and appropriate therapy. Previously reports are suggestive of similar clinical outcomes for stainless steel and cobalt chromium bare metal stent. No reports are available for comparison of sirolimus eluting stainless steel stent and sirolimus eluting cobalt chromium stent. The present study was undertaken with the objective of comparative evaluation of Stainless Steel Stent (Sirolimus) and Cobalt Chromium Stent (Sirolimus) in Patient with Coronary Artery Disease. A single centric, retrospective, non-randomized study involving 118 patients who have undergone PCI from January 2011 to March 2012 implanted with either Sirolimus Stainless Steel Stent (SSSS) or Sirolimus Cobalt Chromium Stents (SCCS) were included in the study. Primary objective was to determine and compare the clinical outcome and rates of target vessel revascularization (TVR) in patients undergoing primary PCI for CAD patients who were treated with Sirolimus cobalt-chromium stents and Sirolimus stainless steel stents. The secondary outcomes of study were Major Adverse Cardiac Events, mortality at the end of 1 month, 6 month and 1 year of outcomes. At 1 month follow up there was no significant difference between two groups (p = 0.96). The individual clinical component showed no difference in occurrence of death (p = 0.29), MI (p = 0.29) and TLR (p = 0.96) at end of 6 month. The cumulative clinical outcome at 1 year rate of target vessel revascularization TVR (SSSS 1.75% versus SCCS 0%, p = 0.29), target lesion revascularization (SSSS 5.27% versus SCCS 1.63%, p = 0.27), and Major Adverse Cardiac Events (SSSS 22.80% versus SCCS 13.11%, p = 0.16). This study showed that among Coronary artery disease (CAD) patients undergoing primary percutaneous coronary intervention, sirolimus stainless steel stent showed similar efficacy and safety to sirolimus cobalt chromium stent.

210-217

Authors: CM Detroja1*, LD Patel2, PR Vasanani3

Factorial design enables researchers to study and understand how multiple factors affect a dependent variable, both independently and jointly. In present report, 33 factorial design was used to study the combined influence of three independent variables in preparation of Simvastatin loaded Poly (D, L Lactide -co- Glycolide) (PLGA) nanoparticles. Nanoparticles were prepared by nanoprecipitation method. The process variables like rate of addition of organic phase to aqueous phase, temperature, speed of magnetic stirrer and time to evaporate organic phase were kept constant throughout the investigation. The formulation variables like concentration of stabilizer (Polyvinyl alcohol), drug (Simvastatin): polymer ratio (PLGA), and organic (acetone): aqueous phase ratio were selected as independent variables. Prepared nanoparticles were evaluated for particle size (PS) and entrapment efficiency (EE). PS and EE were selected as dependent variables. The coded values of independent variables were subjected to multiple regressions to derive a second order polynomial equation (full model). After neglecting the non-significant terms from full model, F-Statistics was applied to set up reduce polynomial equation. Among the three independent variables, value of coefficient of drug: polymer ratio was found to be maximum. This revealed that major contributing variable for PS and EE in nanoparticles is drug: polymer ratio. Two dimensional contour plots and three dimensional response surface plots were established by varying levels of two factors and keeping the third factor at fixed level at a time. Thus the derived equation, surface response plot and contour plot helps in predicting the value of independent variables for optimum PS and EE in preparation of Simvastatin loaded PLGA nanoparticles.

223-228

Authors: Paras R. Vasanani1*, L. D. Patel2, Chetan M. Detroja3

Nanosuspensions are the dispersions of nanosized particles in a suitable vehicle prepared using surfactants or solubilizers to aid in nanosize distribution. Nanosuspension is best suited for dosage form development of poorly soluble drugs. According to the biopharmaceutical classification system, drugs with poor solubility fall either in BCS class II or BCS class IV. BCS class II drugs show poor solubility and good permeability; hence their bioavailability problems can be overcome by improving their solubility. Metaxalone is one such BCS class II drug from an oxazolidin-2-one class of centrally acting muscle relaxant drugs, indicated for relief of discomforts associated with acute, painful musculoskeletal conditions. Therefore, in present investigation, nanosuspension of Metaxalone has been formulated as an attempt to improve solubility and hence the overall bioavailability of Metaxalone. Media milling technique has been employed for nanosuspension preparation. Surfactant concentration (Poloxamer 407) and stirring time has been optimized using 32 factorial design to achieve desired particle size and saturation solubility responses as dependent variables. The particle size (PS) of 215.3 nm and maximum saturation solubility (SS) of 2805μg/ml was obtained as suggested solutions from factorial design which was further confirmed using check point analysis. Interaction of surfactant concentration and stirring time and their effect on particle size and saturation solubility was predicted using the contour plots and response surface plots. The optimized formulation showed around 99% metaxalone in vitro dissolution in comparison to around 46% dissolution from SKELAXIN® tablet at 30 minutes. These methodologies could therefore be employed successfully to improve solubility of any BCS class II drug and to predict effects and interactions of many experimental variables at the same time.

235-239

Authors: G. Prakash Williams1*, Anju Anand1, Parvathy A1, Rakky C. Raj1, Robert Raju1, S. Krishna Kumar2

Living organisms can be found over a wide range of extreme conditions. Most of the organisms living in extreme environments (i.e, extremophiles) belong to the prokaryotes. Halophiles are interesting class of extremophilic organisms that have adapted to harsh, hypersaline conditions. They are able to compete successfully for water and resist the denaturing effects of salts. The present study was an investigation on the in vitro antibacterial effect of secondary metabolites from halophilic bacteria isolated from salted fish samples. The cured salted fish samples were collected and enumerated using halophilic Nutrient Agar supplemented with 4% NaCl. The isolated and purified bacterial cultures are numbered as SF1, SF2, SF3, SF4 and SF5 are further identified using VITEK 2 system as Bacillus vallismortis, Ralstonia mannitolytica, Bacillus subtilis, Rhizoboum radiobacter and Kocuria kristina. Growth kinetics of halobacterial isolates were determined by spectrophotometric assay. The antibiotic resistance pattern of tested pathogenic microorganisms using the commercial antibiotics was screened and almost all the tested microorganisms are resistant to Penicillin. The antimicrobial activity of secondary metabolites of halophilic bacteria against drug resistant microbes was assessed using the Agar well diffusion assay. Among the different extracts of the halophilic bacteria, the chloroform extracts of R. mannitolytica showed maximum antibacterial activity against Bacillus subtilis MTCC 441 and Xanthomonas campestris MTCC 2286. The results of antimicrobial activity are considerable because it enables the identification of potential secondary metabolites present in marine halophilic bacteria, which act as source of innumerable therapeutic agents. Further research is highly warranted to find out the active principle responsible for the antibacterial property and to elucidate the structure of particular compound.