Objective:The aim of present investigation is to enhance in vitro dissolution of poorly soluble drug glimepiride by preparing solid dispersions using modified gum karaya.Materials and Methods:Solid dispersions of drug were prepared by solvent evaporation method using modified gum karaya as carrier. Four batches of solid dispersion (SD1, SD4, SD9, and SD14) and physical mixture (PM1, PM4, PM9, and PM14) were prepared and characterized by differential scanning colorimetry (DSC), Fourier transform infrared (FTIR) spectroscopy, powder X-Ray diffraction (X-RD), and scanning electron microscopy (SEM) studies. Equilibrium solubility studies were carried out in shaker incubator for 24 h and in vitro drug release was determined using USP Dissolution Apparatus-II.Results:Maximum solubility and in vitro dissolution were observed with Batch SD4. No significant enhancement of dissolution characteristics were observed in the corresponding physical mixture PM4. Low viscosity with comparable swelling characteristics as compared to GK of modified form of gum karaya may lead to improvement in dissolution behavior of solid dispersion batches. Also, the conversion of crystalline form of drug to amorphous form may be a responsible factor, which was further confirmed by DSC, FTIR studies, and X-RD studies. SEM photographs of batch SD4 revealed porous nature of particle surface.Conclusion:Modified forms of natural carriers prove beneficial in dissolution enhancement of poorly soluble drugs and exhibited a great potential in novel drug delivery systems.
Administration (100 mg/kg body weight/day, for 14 and 21 days) of flutamide induced duration-dependent regressive changes in the male reproductive organs. The seminiferous tubules in drug-treated shrews exhibited marked regressive changes with suppression of spermatogenesis; the tubules were devoid of spermatozoa and contained Sertoli cells and spermatogonia. However, there was no change in testicular weight, Leydig cell appearance and the concentrations of testicular protein, RNA and DNA in drug-treated animals. Epididymal spermatozoa from drug-treated shrews were immotile and fragmented. The drug also induced regressive histological changes in the ampullary gland and prostate accompanied by significant decrease in the weight; the level of fructose in the ampullary gland was also significantly reduced. Flutamide-induced alterations in the reproductive organs were reversible; by 56 days after drug withdrawal the organs returned to their normal state.
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