The objective of this study is to evaluate the feasibility of obtaining extended release of tacrolimus by a novel combination of lipid-based solid dispersion and matrix-type extended release tablet techniques. Tacroli...The objective of this study is to evaluate the feasibility of obtaining extended release of tacrolimus by a novel combination of lipid-based solid dispersion and matrix-type extended release tablet techniques. Tacrolimus solid dispersion was prepared using glycerylbehenate(Compritol~?ATO888) and Pluronic F127 as the carrier materials with hot-melt method, which was then blended with hydrogel matrix materials, such as HPMC and lactose, the powders were directly compressed into tablets. In vitro drug release tests were carried out to evaluate the performance of the solid dispersions and the tablets. The dissolution rate of tacrolimus was significantly improved by the lipid-based solid dispersion, and the incorporation of HPC into the solid dispersion obviously improved its stability after storage. Extended release tablets loaded with tacrolimus solid dispersion showed prolonged drug release patterns over 24 h, the release patterns of the tablets can be tailored by the compositions of the matrix materials, including the types and content of HPMCs. A modified processing method that directly mixed the melted solid dispersion with HPMC powders improved the uniformity of the solid dispersion inside the tablet matrix and release profile. The release data of the extended release tablet fitted well to the Korsmeyer–Peppas model with n value of 0.85, which suggested diffusion-and erosion-controlled release mechanism. The combination of lipid-based solid dispersion and HPMC hydrogel matrix may find wide applications in the extended release dosage forms of high potent, water-insoluble drugs.展开更多
目的:探讨他克莫司联合百令胶囊在儿童原发性肾病综合征(PNS)中的应用价值。方法:选取2022年1月—2023年12月于贵州省人民医院接受治疗的PNS患儿80例为研究对象,随机分为对照组和观察组,各40例。对照组采用他克莫司治疗,观察组采用他克...目的:探讨他克莫司联合百令胶囊在儿童原发性肾病综合征(PNS)中的应用价值。方法:选取2022年1月—2023年12月于贵州省人民医院接受治疗的PNS患儿80例为研究对象,随机分为对照组和观察组,各40例。对照组采用他克莫司治疗,观察组采用他克莫司联合百令胶囊治疗。比较两组临床疗效、肾功能[24 h尿蛋白定量(24 h UTP)、血尿素氮(BUN)、血肌酐(Scr)]、凝血功能[凝血酶原时间(PT)、活化部分凝血活酶时间(APTT)、D-二聚体(D-D)]、免疫指标[免疫球蛋白G(IgG)、免疫球蛋白M(IgM)、免疫球蛋白A(IgA)]。结果:观察组治疗总有效率高于对照组,差异有统计学意义(P=0.043);治疗后,两组24 h UTP、BUN、Scr水平低于治疗前,观察组24 h UTP、BUN水平低于对照组,差异有统计学意义(P<0.05);治疗后,两组Scr水平比较,差异无统计学意义(P>0.05);治疗后,两组PT、APTT水平高于治疗前,D-D水平低于治疗前,观察组PT、APTT水平高于对照组,D-D水平低于对照组,差异有统计学意义(P<0.05);治疗后,两组IgG、IgM、IgA水平高于治疗前,观察组高于对照组,差异有统计学意义(P<0.05)。结论:他克莫司联合百令胶囊治疗PNS的效果较好,可改善患儿凝血功能、肾功能,增强机体免疫力。展开更多
文摘The objective of this study is to evaluate the feasibility of obtaining extended release of tacrolimus by a novel combination of lipid-based solid dispersion and matrix-type extended release tablet techniques. Tacrolimus solid dispersion was prepared using glycerylbehenate(Compritol~?ATO888) and Pluronic F127 as the carrier materials with hot-melt method, which was then blended with hydrogel matrix materials, such as HPMC and lactose, the powders were directly compressed into tablets. In vitro drug release tests were carried out to evaluate the performance of the solid dispersions and the tablets. The dissolution rate of tacrolimus was significantly improved by the lipid-based solid dispersion, and the incorporation of HPC into the solid dispersion obviously improved its stability after storage. Extended release tablets loaded with tacrolimus solid dispersion showed prolonged drug release patterns over 24 h, the release patterns of the tablets can be tailored by the compositions of the matrix materials, including the types and content of HPMCs. A modified processing method that directly mixed the melted solid dispersion with HPMC powders improved the uniformity of the solid dispersion inside the tablet matrix and release profile. The release data of the extended release tablet fitted well to the Korsmeyer–Peppas model with n value of 0.85, which suggested diffusion-and erosion-controlled release mechanism. The combination of lipid-based solid dispersion and HPMC hydrogel matrix may find wide applications in the extended release dosage forms of high potent, water-insoluble drugs.
文摘目的:探讨他克莫司联合百令胶囊在儿童原发性肾病综合征(PNS)中的应用价值。方法:选取2022年1月—2023年12月于贵州省人民医院接受治疗的PNS患儿80例为研究对象,随机分为对照组和观察组,各40例。对照组采用他克莫司治疗,观察组采用他克莫司联合百令胶囊治疗。比较两组临床疗效、肾功能[24 h尿蛋白定量(24 h UTP)、血尿素氮(BUN)、血肌酐(Scr)]、凝血功能[凝血酶原时间(PT)、活化部分凝血活酶时间(APTT)、D-二聚体(D-D)]、免疫指标[免疫球蛋白G(IgG)、免疫球蛋白M(IgM)、免疫球蛋白A(IgA)]。结果:观察组治疗总有效率高于对照组,差异有统计学意义(P=0.043);治疗后,两组24 h UTP、BUN、Scr水平低于治疗前,观察组24 h UTP、BUN水平低于对照组,差异有统计学意义(P<0.05);治疗后,两组Scr水平比较,差异无统计学意义(P>0.05);治疗后,两组PT、APTT水平高于治疗前,D-D水平低于治疗前,观察组PT、APTT水平高于对照组,D-D水平低于对照组,差异有统计学意义(P<0.05);治疗后,两组IgG、IgM、IgA水平高于治疗前,观察组高于对照组,差异有统计学意义(P<0.05)。结论:他克莫司联合百令胶囊治疗PNS的效果较好,可改善患儿凝血功能、肾功能,增强机体免疫力。
