扑热息痛直肠胶囊剂的溶出度和生物利用度研究

Studies on the dissolution and bioavailability of the rectal capsule of acetaminophene

作者制备的扑热息痛直肠胶囊剂，可根据小儿体重分装成不同规格，便于临床实现个体化给药。本品与市售栓剂在家兔体内的达峰时分别为１．８７，１．６７ｈ；峰浓度及ＡＵＣ分别为５４．８６，４６．０９（ｍｇ／Ｌ）和１９８．９４，１８８．９４（ｍｇ·ｈ／Ｌ）。直肠胶囊剂用自行设计的“转筒膜法”测定，体外累积溶出百分率与体内吸收百分率间有显著相关性（ｒ＝０．９９２９，ｎ＝７）。

The rectal capsule of acetaminophene was prepared, it can be formed several sizes by children' s weight so as to administrate in personal. Tmax, Cmax and AUC of the capsule and the suppository commercial were 1. 87, 1. 67h; 54. 86, 46. 69(μg/ml); 198. 94, 188. 94 (μg·h/ml) in rabbits respectively, the results showed that the suppository of acetaminophene can be substitued by the rectal capsule, it was a new dosage form in rectal administration, it's dissolution in vitro was determined by the method of rotating- cylinder with millipore memberane(RCMM) established by ourself. There are a significant correlation between the cumulative dissolution rates in vitro and the absorption rates in vivo , and the both meets zero-order kinetics, the results showed that RCMM could simulated the dissolution of rectal capsule in rectal, it provided a new method of determing dissolution of soluble suppositories , RCMM can simulated the conditions of poor liquid , pH≈7, temperature higher than body temperature but cann' t simulated the larger absorption area and the pressure of rectal acting on preparations in rectal, it has several advantages such as simple operating, fixed diffusion area, regulating millipore memberane and non-ignoring the differances of preparations.