Search

Glimepiride (GMP) is an oral antidiabetic drug classified as BCS class II, demonstrating extremely limited solubility, with a solubility level below 0.00384 mg/mL. Some generic drug manufacturers producing GMP (copy product) tablets encountered bioavailability issues due to poor dissolution, which did not meet the requirements. Therefore, measures were taken to enhance solubility through the modification of polymorphs. It is known that GMP exists in two polymorphic forms, namely Form I and an alternative Form II, which exhibits higher solubility in water. This study aims to produce and characterize the polymorph-modified GMP compared to non-modified GMP, develop an optimal formulation for polymorph-modified GMP tablets that adhere to pharmaceutical requirements as a representative copy drug model, and determine its similarity factor to Amaryl® as the innovator. The research methodology involved initiating the study by examining the polymorph transformation of GMP through the utilization of techniques such as neat grinding, solvent drop grinding, and solvent evaporation. The resulting samples were characterized using DSC, PXRD, and SEM analysis. The performance assessment encompassed the evaluation of flow properties, compressibility index, solubility, and dissolution rate compared to the non-modified GMP. Based on the characterization results, the best polymorph-modified GMP sample was used to produce a tablet formulation containing 4 mg of GMP using the direct compression method as a copy tablet model. In vitro equivalence testing was performed using a comparative dissolution test on the polymorph-modified GMP tablet compared to its innovator, Amaryl® 4 mg, in three different dissolution media, followed by determining the equivalence status using the similarity factor (f2) calculation. Based on the screening results of polymorph transformation, it was determined that the polymorph-modified GMP, using all three techniques, did not undergo a transition from Form I to Form II. Instead, it underwent amorphization, primarily observed in the solvent evaporation technique. Tablets containing polymorph-modified GMP using the solvent evaporation technique were able to enhance the in vitro dissolution rate profile compared to non-modified GMP tablets. The f2 values for the comparative in vitro dissolution test in acetate buffer pH 4.5 and phosphate buffer pH 6.8 were 60.15 ± 0.27 and 88 ± 0.35, respectively within acceptance criteria of 50–100. However, in KCl/HCl buffer pH 1.2, the f2 value was 45.15 ± 0.23. It was concluded that the polymorph-modified GMP tablet was not similar to its innovator, Amaryl®.

Diclofenac sodium is a Non-Steroidal Anti Inflammatory Drugs that if being taken orally have the side effects of peptic ulcers and undergone the first pass metabolism, and also included in the Biopharmaceutics Classification System class 2 which resulted in the low rate of dissolution. This study aims to determine the influence of particle size reduction on the dissolution rate of diclofenac sodium in the form of an FDOF dosage. The formation of diclofenac sodium nanoparticles is carried out by ionic gelation method using chitosan and sodium tripolyphosphate as a crosslinker in various ratios characterized by Particle Size Analyzer and Scanning Electron Microscopy, then it is incorporated into the form of an FDOF that were prepared by solvent casting method at a dose of 12.5 mg using variations concentration of SSG as superdisintegrant and PEG 400 as plasticizer. From the research results, diclofenac sodium nanoparticles are formed in the ratio of chitosan-sodium tripolyphosphate 6:1, have a size of 804 nm and spherical-shaped. The best FDOF dosage formula is F8 containing HPMC E5 LV 35% as the film forming agent, SSG 8% as superdisintegrant and PEG 400 10% as plasticizer. FDOF formula containing diclofenac sodium nanoparticles has a slightly bitter taste, disintegration time less than one minute, surface pH around 7 (neutral), drug content that meets the requirements of the range of determination which is 93.24 ± 0.96, the cumulative amount of drug dissolved in the 28th minute is higher by 88.45% compared to FDOF containing diclofenac sodium raw material, which is only 70.0%.

Jatropha multifida Linn. latex has been reported in many study for its activities to treats wound. Preparation of hydrogels containing 3% of Jatropha multifida Linn. latex with variety of base polymers kappa carrageenan and iota carrageenan was conducted and met good characteristics. This study aimed to evaluate effect of both hydrogels to promote wound healing in Wistar rats. Tests carried out on five groups of rats with 1.5 cm diameter of wound in the back area, consisting of a control group, two test groups were each treated by 2% kappa carrageenan-based hydrogel (kappa-hydrogel group) and 2% iota carrageenan-based hydrogel (iota-hydrogel group) of the latex, and two groups were each given a different hydrogel base according to type of hydrogel tested. Effect on wound healing was assessed by parameters including wound drying period, scab forming period, and the change in diameter of the wound. Results show kappa-hydrogel group achieve the most rapid wound healing compare to the control group significantly (p