乙肝清HPMC K4M/PVP K30骨架缓释片的研制与体外评价

Preparation and in Vitro Dissolution Behaviors of Yiganqing-HPMC K4M/PVP K30 Matrix Tablet

关键词:  HPMC K4M/PVP K30  缓释片  中药提取物  释药行为

Key words:  HPMC K4M/PVP K30  sustained-release tablet  Chinese medicine extract  dissolution mechanism

摘要:

目的 进行乙肝清HPMC K4M/PVP K30骨架缓释片的研制与体外评价。方法 以中药赶黄草和贯叶连翘的提取物为原料药，以HPMC K4M和PVP K30两种粘度不同，水合行为差异较大的亲水高分子材料联合使用作为骨架材料，制备缓释12 h的“乙肝清骨架缓释片”。 以“HPMC+PVP K30”总量在处方中的百分量和HPMC在“HPMC+PVP K30” 总量中的百分量为考察因素，通过处方单因素考察和星点设计—效应面法进行优化，得到最佳的制剂处方。并通过均一性实验和体外释药行为研究进行体外评价。结果 本片剂优化处方中最低HPMC K4M与PVP K30用量不得低于20%。最佳制剂处方为骨架材料HPMC+PVP K30总量占片剂质量的27.03%，HPMC占HPMC+PVP K30总量的49.04%。本处方具有良好的重现性与稳定性；片剂药物释放符合一级释放模型。结论 制备了载药量40%的乙肝清提取物缓释片，并优化得到了其最佳的制剂处方。

Abstract:

OBJECTIVE To study the preparation and In vitro evaluation of Yiganqing-HPMC K4M/PVP K30 matrix tablet. METHODS Yiganqing- matrix sustained-release tablet, whose release period is 12 hours, was developed with HPMC K4M and PVP K30 as its matrix materials and two Chinese Medicine Catch Huangcao and Hypericum perforatum extract as intermediate drugs. The two matrix materials are both hydrophilic polymer and their hydration behavior are much different. Using single factor of formulation and star point design - response surface methodology to optimize the formulation, and the optimum formulation was obtained. In vitro evaluation was done by the verification tests and the in vitro dissolution data. RESULTS The lowest HPMC K4M and PVP K30 amount in the optimal formulation tablet was not less than 20%, and the matrix material’s ratio is that HPMC + PVP K30 total amount of the tablet mass 27.03% and HPMC of HPMC + PVP K30 total amount 49.04%. This prescription had satisfied reproducibility and stability, and the drug release of this preparation meets first-order model. CONCLUSION The hepatitis B clear extract-release tablets with 40% drug loading are prepared, and the prescription of the best preparations has been obtained by optimization.