Solid Self-emulsifying Pellets to Improve Oral Absorption of Poorly Water Soluble Drugs: Preparation and in Vitro and in Vivo Evaluation
The oral delivery of poorly water soluble drugs presents a significant challenge to pharmaceutical scientists because of their low solubility in water, which leads to poor oral bioavailability, high intra- and inter-subject variability and lack of dose proportionality. Thus, for such drugs of biopharmaceutical class II (low solubility and high permeability), the absorption rate and degree from the gastrointestinal tract (GIT) are controlled and limited by dissolution process. In recent years, self-emulsifying drug delivery systems (SEDDS) are recognized as a feasible approach to improve the dissolution and bioavailability of poorly soluble drugs. However, conventional SEDDS, which are mostly prepared in a liquid form and orally administered in soft or hard gelatin capsules, can make some disadvantages such as high production costs, low drug incompatibility and stability, drugs leakage and precipitation, capsule ageing. Then incorporation of liquid SEDDS into a solid dosage form is compelling and desirable. Recently, a new drug delivery technology-solid SEDDS (S-SEDDS) which combine the advantages of SEDDS and those of solid dosage forms, have been investigated. As a multiple-unit dosage form, pellets have some desired advantages, such as flexibility in designing and developing solid dosage form, reduction of intra- and inter-subject variability of drug dissolution and plasma profiles, hence improvement of the drug safety and efficacy. To prepare pellets, extrusion/spheronization technique has become popular in pharmaceutical industry because it is easily large-scale, and its products have many features, including spherical shape, narrow modal size distribution, good flow properties, low friability and uniform packing characteristics.
Solid self-emulsifying drug delivery systems Pellets Eztrusion/ spheronization Nitrendipine Oral bioavailability
Jin Sun Zhiyuan Wang Yongjun Wang Xiaohong Liu Yinghua Sun Zhonggui He
Department of pharmaceutics, College of pharmacy, Shenyang pharmaceutical university, Shenyang Liaoning Province 110016
国际会议
International Symposium on Crystal Engineering and Drug Delivery System 2009(2009晶体工程与药物传送系统国际会议)
天津
英文
409-411
2009-09-05（万方平台首次上网日期，不代表论文的发表时间）