他克莫司口服自微乳骨架缓释微丸的制备及其释药机制研究

刘建清; 曾棋平; 刘志宏; 宋洪涛

引用本文:	刘建清,曾棋平,刘志宏,宋洪涛.他克莫司口服自微乳骨架缓释微丸的制备及其释药机制研究[J].中国现代应用药学,2023,40(5):638-645.
	LIU Jianqing,ZENG Qiping,LIU Zhihong,SONG Hongtao.Preparation and Release Mechanism of Tacrolimus Oral Self-microemulsion Matrix Sustained-release Pellets[J].Chin J Mod Appl Pharm(中国现代应用药学),2023,40(5):638-645.

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他克莫司口服自微乳骨架缓释微丸的制备及其释药机制研究
刘建清¹, 曾棋平², 刘志宏³, 宋洪涛³
1.泉州医学高等专科学校, 福建泉州 362000;2.福建医科大学附属漳州市医院药学部, 福建漳州 363000;3.联勤保障部队第九〇〇医院药剂科, 福州 350025

摘要:

目的制备他克莫司自微乳骨架缓释微丸，并探讨其释药机制。方法采用星点设计-效应面法筛选他克莫司自微乳最优处方，在此基础上，采用挤出滚圆技术，以微晶纤维素(microcrystalline cellulose，MCC)为吸附剂和填充剂、乙基纤维素(ethyl cellulose，EC)与硬脂酸(stearic acid，SA)为骨架材料，以5%羟丙基甲基纤维素(hypromellose，HPMC)溶液为黏合剂，制备他克莫司自微乳骨架缓释微丸，并考察其体外溶出情况。结果他克莫司自微乳最优处方为Crodamol EO∶Solutol HS15∶Transcutol P=15%∶52.5%∶32.5%。骨架缓释微丸最优处方为MCC用量为45%，EC∶SA用量比为3∶2，5%HPMC溶液用量为12 mL。制得的他克莫司自微乳骨架缓释微丸符合市售他克莫司缓释胶囊的体外释放标准，释药机制为溶蚀与扩散相结合。结论优选的处方稳定可行，他克莫司自微乳骨架缓释微丸体外释放符合预期目的。

关键词: 他克莫司自微乳骨架缓释微丸释药机制

DOI：10.13748/j.cnki.issn1007-7693.20222093

分类号:R944

基金项目:

Preparation and Release Mechanism of Tacrolimus Oral Self-microemulsion Matrix Sustained-release Pellets

LIU Jianqing¹, ZENG Qiping², LIU Zhihong³, SONG Hongtao³

1.Quanzhou Medical College, Quanzhou 362000, China;2.Department of Pharmacy, Zhangzhou Hospital Affiliated to Fujian Medical University, Zhangzhou 363000, China;3.Department of Pharmacy, No. 900 Hospital of Joint Logistics Support Force, Fuzhou 350025, China

Abstract:

OBJECTIVE To prepare tacrolimus self-microemulsion matrix sustained-release pellets and investigate its the release mechanism. METHODS Optimal formulation of tacrolimus self-microemulsion was screened by the central composite design-response surface methodology, and then the tacrolimus self-microemulsion matrix sustained-release pellets were prepared by extrusion spheronization technology with microcrystalline cellulose(MCC) as adsorbent and filler, ethyl cellulose(EC) and stearic acid(SA) as skeleton materials, 5% hypromellose(HPMC) solution as adhesive. Tacrolimus self-microemulsion matrix sustained-release pellets were prepared, also, their dissolution profiles were investigated in vitro. RESULTS The optimal formula of tacrolimus self-microemulsion was Crodamol EO︰Solutol HS15︰Transcutol P=15%︰52.5%︰32.5%. The optimal formulation of the matrix sustained-release pellets was 45% MCC, 3∶2 of EC∶SA and 12 mL 5% HPMC solution. Tacrolimus self-microemulsion matrix sustained-release pellets met the in vitro release standards of commercially available tacrolimus sustained-release capsules. The release mechanism was a combination of erosion and diffusion. CONCLUSION The optimized formulation of microemulsion matrix sustained-release pellets is stable and feasible, and its in-vitro release fits the intended purpose.

Key words: tacrolimus self-microemulsion matrix sustained-release pellets drug release mechanism