氢溴酸高乌甲素亲水凝胶骨架片的制备及体外释放

Hydrophilic Matrix Sustained Release Tablets of Lappaconite Hydrobromide: Preparation and Release in Vitro

关键词:  氢溴酸高乌甲素  凝胶骨架片  体外释放

Key words:  lappaconite hydrobromide  hydrophilic matrix sustained release tablets  release in vitro

摘要:

目的 为了减少给药次数，方便患者，并提高镇痛效果，制备氢溴酸高乌甲素亲水凝胶骨架片，优化制剂处方，并探讨释放机制。方法 以羟丙甲纤维素(HPMC)为骨架材料，乳糖、微晶纤维素(MCC)、淀粉为填充剂，硬脂酸镁为润滑剂制备氢溴酸高乌甲素骨架片，考察各因素对药物释放度的影响，筛选优化处方，并拟合讨论其释放机制。结果 HPMC的用量及分子量，微晶纤维素和硬脂酸镁的用量对药物释放有显著影响。所制缓释片无突释现象，缓释周期12 h，根据拟合方程，药物释放符合一级释放模型，其释放既有扩散，又有骨架溶蚀。结论 本方法制备的氢溴酸高乌甲素缓释片工艺简单，生产成本低，且具有良好的释放性能。

Abstract:

OBJECTIVE To reduce the frequency of administration, enhance patient compliance, increase antinociceptive effect of lappoconitine hydrobromide, hydrophilic matrix sustained release tablets of lappaconite hydrobromide were prepared. The formulations of the tablets were optimized. Then the in vitro release models were also evaluated in present study. METHODS The effects of various molecular masses and contents of HPMC(using as hydrophilic matrix), various contents of lactose(filling agent), microcrystalline cellulose(filling agent), starch(filling agent) and magnesium stearate(lubricant) on drug release from the matrix tablets in vitro were investigated, respectively. The in vitro release mechanism of the optimal formulation was discussed by fitting various models. RESULTS The results showed that the molecular mass and the content of HPMC, the contents of microcrystalline cellulose and magnesium stearate influenced greatly on drug release in vitro from the tablets. No burst drug release from the obtained matrix tablets was observed. Drug release in vitro sustained up to 12 h. It was better agreed with first-order kinetics model, which indicated that drug release from the tablets was controlled by drug diffusion from the hydrophilic gel and degradation of the matrix. CONCLUSION The obtained hydrophilic matrix tablets of lappaconite hydrobromide in present study had many advantages, such as ease of manufacturing, low production costs and good performance of drug release, etc.