A Systematic Study on Processing Problems and In vitro Release of Saraca indica Caesalpiniaceae Bark Powder Tablets

Purpose: To examine the original flowability, compressibility and compactibility of Saraca indica bark powder and its tablet formulations.Methods: Saraca indica bark powder was subjected to various quantitative tests including acid insoluble ash, total ash, foreign organic matter, alcohol soluble extractive and water soluble extractive. Its flowability and compressibility were determined using Kawakita, Heckel and Leuenberger relationships. Tablets were prepared from the powder by direct compression and wet granulation techniques and characterized. Results: Kawakita analysis revealed lower cohesiveness of granules (3.877 ± 0.890) compared to the powder (6.176 ± 1.030), and hence improved flowability. From Heckel analysis, the higher value of intercept (A) for granules (4.38 ± 0.45) implies higher degree of fragmentation than direct compression DC formulation (2.90 ± 0.33) and powders (2.44 ± 0.12). The compression susceptibility parameter obtained from Leuenberger equation for compacts formed by wet granulation technique (0.183 ± 0.045 1/kg/cm2) indicate that maximum crushing strength is reached faster at lower pressures of compression than for Saraca indica bark powder (0.073 ± 0.025 1/kg/cm2) and DC formulation (0.105 ± 0.033 1/kg/cm2). In-vitro dissolution study showed that more than a 90% of tannin was released within 30 and 60 min from tablets prepared by wet granulation and DC, respectively. Brittle fracture index data indicate that tablets prepared from granules showed less fracture, capping and lamination tendencies.Conclusion: It is concluded that the desired flowability, compressibility and compactibility of Saraca indica bark powder can be obtained by direct compression and wet granulation techniques

Improvement in Dissolution Rate of Cefuroxime Axetil by using Poloxamer 188 and Neusilin US2

A combination of fusion and surface adsorption techniques was used to enhance the dissolution rate of cefuroxime axetil. Solid dispersions of cefuroxime axetil were prepared by two methods, namely fusion method using poloxamer 188 alone and combination of poloxamer 188 and Neusilin US2 by fusion and surface adsorption method. Solid dispersions were evaluated for solubility, phase solubility, flowability, compressibility, Kawakita analysis, Fourier transform-infrared spectra, differential scanning calorimetry, powder X-ray diffraction study, in vitro drug release, and stability study. Solubility studies showed 12- and 14-fold increase in solubility for solid dispersions by fusion method, and fusion and surface adsorption method, respectively. Phase solubility studies showed negative values for poloxamer 188 at various concentrations (0, 0.25, 0.5, 0.75 and 1%) indicating spontaneous nature of solubilisation. Fourier transform-infrared spectra and differential scanning calorimetry spectra showed that drug and excipients are compatible with each other. Powder X-ray diffraction study studies indicated that presence of Neusilin US2 is less likely to promote the reversion of the amorphous cefuroxime axetil to crystalline state. In vitro dissolution studies, T50% and mean dissolution time have shown better dissolution rate for solid dispersions by fusion and surface adsorption method. Cefuroxime axetil release at 15 min (Q15) and DE15 exhibited 23- and 20-fold improvement in dissolution rate. The optimized solid dispersion formulation was stable for 6 months of stability study as per ICH guidelines. The stability was ascertained from drug content, in vitro dissolution, Fourier transform-infrared spectra and differential scanning calorimetry study. Hence, this combined approach of fusion and surface adsorption can be used successfully to improve the dissolution rate of poorly soluble biopharmaceutical classification system class II drug cefuroxime axetil