两种液中干燥法制备盐酸多西环素微囊的比较研究

Comparison of doxycycline hyclate microcapsules prepared by the two methods of intra-liquid desiccation

关键词:  液中干燥法  盐酸多西环素  微囊  比较

Key words:  intra-liquid desiccation  doxycycline hyclate  microcapsules  comparison

摘要:

分别用水中干燥法和油中干燥法制备盐酸多西环素微囊,比较各自制得的微囊质量参数及其体外释药特性,为盐酸多西环素缓释制剂提供科学依据。以乙基纤维素为囊材,通过正交设计分别考察各因素对微囊质量的影响,评定微囊的大小、形态、载药量、包封率等质量指标,以溶出实验研究其释药特性。结果水中干燥法所制得微囊粒径20 μm～30 μm,包封率为87.3％；油中干燥法微囊粒径范围为200 μm～400 um,包封率为93.7％。以上结果表明油中干燥法所得微囊粒径较大,包封率、载药量均明显高于水中干燥法制得的微囊；体外释药实验表明,微囊化大大延缓了盐酸多西环素的释放时间。

Abstract:

ABSTRACT:Preparing doxycycline hyclate microcapsules through intra-liquid desiccation,(in W/O/W emulsion and O/W/O emulsion respectively),then comparing their quality parameters and in vitro release characteristics in order to provide a scientific basis for the the doxycycline hyclate sustained-release preparation.Ethylcellulose was used as coating material and Doxycycline hyclate was microcapsulated by the two methods of intra-liquid desiccation. Using orthogonal design to study factors influenced the quality of microcapsules.And then,drug loading(DL),encapsulation efficiency(EE),particle size distribution and drug release were measured. As a Resulte, in W/O/W emulsion, the microcapsule partical size distribution was found in the range of 20 μm～30 μm,and its encapsulation efficiency was 87.3% .But in O/W/O emulsion,the partical size was in the range of 200 μm～400 μm and the encapsulation efficiency was 93.7%. The resultes indicated that microcapsules prepared in O/W/O emulsion had larger diametre ,higher drug loading and encapsulation efficiency than those prepared in W/O/W emulsion. The in vitro release experiment showed that microencapsulation prolonged doxycycline hyclate’s release time.