Objective: The present study was aimed to enhance the solubility of poorly water-soluble drug (BCS Class II) Febuxostat using water-soluble polymers.Methods: Pre-formulation studies like drug excipient compatibility studies by Fourier-transform infrared spectroscopyDifferential scanning calorimetry and determination of saturation solubility of drug individually in various media like distilled water and pH 7.4 phosphate buffer. Solid dispersions of Febuxostat was prepared using Polyethylene glycol (PEG 6000) (fusion method) and Polyvinyl pyrrolidone (PVP K30) (solvent evaporation method) in various ratios like 1:1, 1:2, 1:3 and 1:4 separately. The formulated solid dispersions were evaluated for percentage yield, drug content and in vitro dissolution studies.Results: From the results of pre-formulation studies it was revealed that there was no interaction between drug and excipients and the pure drug was poorly soluble in water. The percentage yield of all formulations was in the range of 54-78 %, and drug content was in the range of 43-78 mg. The solid dispersion containing polyvinylpyrrolidone K 30 in 1:4 ratio showed the highest amount of drug release at the end of 30 min than other formulations.Conclusion: Finally it was concluded that solid dispersion prepared with PVP K-30 in 1:4 ratio by solvent evaporation method was more soluble than by fusion method.

This study was performed to evaluate the antimicrobial activity of aerial parts of chloroform extract of Cassia auriculata L. The chloroform extract of C. auriculata were shown to possess an antimicrobial activity against two gram positive and two gram negative human pathogenic bacteria and fungi, viz. Bacillus subtilis, Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli and fungus cultures Candida albicans and Aspergillus niger by using disc diffusion method. The extract showed antibacterial activity at all concentrations selected, but only the extract with the concentration of 300µg/ml showed maximum antibacterial activity against all the organisms except Pseudomonas aeruginosa which are comparable with the standard control, amikacin. The anti fungal activity of chloroform extract of C. auriculata revealed significant effect against Candida albicans and Aspergillus niger with the net inhibition zone of 14 and 14 mm, respectively at 300µg/ml concentration, which is almost comparable with standard control, ketokonazole used as an antifungal agent. The phytochemical analysis showed the presence of alkaloids, carbohydrates, fixed oils, fats, tannins, gum & mucilage, flavonoids, saponins, terpenoids, lignin and sterols. It is concluded that the antimicrobial activity showed by the plant was due to the presence of these phytochemicals. Further studies are highly needed for future drug development.DOI: http://dx.doi.org/10.3329/icpj.v2i6.14869 International Current Pharmaceutical Journal, May 2013, 2(6): 105-108

Amukkara curanam, a Siddha formulation, currently used in all types of gastric disorders, rheumatic pain, insomnia and sexual insufficiency, was investigated for the estimation of the marker compounds, withaferine A and piperine contents in a prepared standard formulation and a commercial formulation by using HPTLC method of analysis. The two formulations were subjected to methanol, ethyl acetate and chloroform extractions by using Soxhhlet apparatus The chromatogram was developed using chloroform: methanol (8.5:1.5 v/v) and toluene: ethyl acetate (7:3 v/v) as mobile phases for the estimation of withferine A and piperine respectively. The detection and quantification were performed at a wavelength of 220 nm for withaferine A and 254 nm for piperine. The linear regression analysis of calibration plots of withferine A and piperine exhibited linear relationship in the range of 5 -15 µg and 50 -150 ng respectively, while the % recovery was found to be 94.52% w/w of withaferine A and 98.73%w/w of piperine, thus proving the accuracy and precision of the analysis. Methanol and ethyl acetate were found to be the suitable solvents for the extraction of withaferin A and piperine respectively. The withaferine A content in standard formulation was found to be much higher in all the three extracts than that of the commercial sample. However, the piperine content in all the three extracts of standard formulation was slightly lower than the respective extracts of commercial formulation. The proposed HPTLC method was found to be rapid, simple and accurate for quantitative estimation of withferine A and piperine in different formulation extracts.

The solubility/dissolution behavior of a drug is key factor influencing its oral bioavailability, being the rate-limiting step for absorption of drugs from the gastrointestinal tract. For effective pharmacological action, aqueous solubility is the most important criteria for prompt dissolution and good absorption. The present study was aimed to enhance the solubility of poorly water soluble drug (BCS Class II) Fenofibrate individually using water soluble polymers like Poly ethylene glycol (PEG 6000) (fusion method) and Poly vinyl pyrrolidone (PVP K30) (solvent evaporation method) in various ratios like 1:1, 1:2, 1:3 and 1:4 separately. Initially, pre-formulation studies like drug excipient compatibility studies by FTIR, DSC and determination of saturation solubility of drug individually in various media like distilled water, 0.1N hydrochloric acid and pH 7.4 phosphate buffer. The formulated solid dispersions were evaluated for percentage yield, drug content and in vitro dissolution studies. From the results of pre-formulation studies it was revealed that there was no interaction between drug and excipients and the pure drug was poorly soluble in water. The percentage yield of all formulations was in the range of 60-96 % and drug content was in the range of 56-82 mg. The solid dispersion containing polyvinyl pyrrolidone K 30 in 1:4 ratio showed highest amount of drug release at the end of 30 minutes than other formulations. Finally it was concluded that solid dispersion prepared with PVP K-30 in 1:4 ratio by solvent evaporation method was more soluble than by fusion method.

The objective of the present learns to improve solubility and dissolution of Olmesartan Medoxomil (OM) by improving water solubility by reliable dispersion methods using fusion method (FM) and solvent evaporation (SE) method via hydrophilic polymers PEG 6000 and PVP K30 in different ratios.  Preformulation studies of OM: polymers were carried using DSC and FTIR proves that it is stable without any extra peaks, which implies no interaction among the drug and carrier. For OM in FM drug: polymer ratio was maintained in a range 1:1, 1:3, 1:5 and 1:7 w/w ratio of OM to PEG 6000 and  coded as SDOM1, SDOM2, SDOM3 and SDOM4 whereas for SE method OM to PVP K30  ratio was maintained in a range of 1:1, 1:3, 1:5 and 1:7 w/w ratio  and coded as SDOM5, SDOM6, SDOM7 and SDOM8. SDOM3 by FM and SDOM7 by SE method resulted in the highest production yield. The solubility studies have shown improved drug solubility compared with a pure drug in all medium. Percentage of drug content, flowability characters like the angle of repose and carr's index, bulk density, Hausner's, tapped density were within acceptable limits. In vitro drug release in the intestinal gastric medium of pH 1.2 was improved significantly when compared with pure drug. SDOM3 and SDOM7, selected for accelerated stability studies, had no significant change in physical parameters, drug content, with little changes in the in vitro  drug release pattern. Hence solubility and dissolution rate of OM is increased by using the PEG 6000 and PVP K30 polymers.