阿司匹林─聚天冬酰胺共价复合体“爆释”现象研究  

STUDIES ON THE PHENOMENON OF INITIAL BURST RELEASE OF ASPIRIN-POLYASARAMIDE CONJUGATE

作　　者：章志坚[1] 王斌[1] 汤谷平[1] 陈启琪[1] 

机构地区：[1]浙江大学药学院,310006

出　　处：《健康研究》1999年第2期8-12,共5页Health Research

基　　金：国家自然科学基金!9502319

摘　　要：目的：针对阿司匹林－αβ－聚－（羟丙基）－DL－天冬酰胺共价更合体（ASA－PHPA）在释放中存在的"爆释"现象，希望以改变剂型来控制或消除该现象，并对"爆释"现象产生的原因进行探讨。方法：将ASA－PHPA制备成三种剂型：粉末型、理植型和微囊型，并对微囊的载药率及包封率进行测定。以0．02mol／L磷酸盐缓冲液（pH＝7．4）作为释放介质，释放液用RP－HPLC法进行测定，分别对三种剂型进行体外释药研究。结果：粉末型ASA－PHPA在释药初期存在着显著的"爆释"现象，理植型也有一定程度的"爆释"，而微囊型的释放最为平稳。结果：微囊型ASA-PHPA能有效地控制该共价复合体的"爆释"现象。objective To investigate the effect of initial burst release of Acetylsalicylic acid - poly - α, β - (hydroxypropyl) - DL - aspartamide conjugates(ASA - PHPA) in vitro Methods Acetylsalicylic acid (ASA), as a model drug, was conjugated to the biocompatible polymer poly - α, β - (hydroxypropyl) - DL - aspartamide(PHPA) to make up ASA - PHPA conjugate. Three dosage forms, powder, microcapsule and stili medicament - torum, were prepared to compare the phenomenon of initial burst release. In-vitro release tests were performed in phosphatebuffered saline (pH 7. 4) and the release solutions were determined by RP - HPLC. Results Experimental data indicated that burst effect was decreased to a certain extent in stili medicamen - torum, and completely decreased in microcapsule. Conclusion: The microcapsule would control the the effect of initial burst release of ASA - PHPA.

关 键 词：爆释"现象 ASA-PHPA 体外释药 RP-HPLC法 

分 类 号：R96[医药卫生—药理学]