结肠菌群触发型5-氨基水杨酸壳聚糖胶囊大鼠体内的吸收与分布研究

目的评价口服5-氨基水杨酸(5-ASA)壳聚糖胶囊后在大鼠体内的吸收与在结肠组织中的分布规律。方法在轻度乙醚麻醉下通过聚乙烯管给大鼠口服5-ASA壳聚糖胶囊3粒(1.6mg/粒),对照组口服5-ASA羧甲基纤维素混悬液1ml(4.8mg)。于给定的时间间隔从大鼠心脏取血,并取出结肠组织。用HPLC法测定大鼠血液及结肠中药物的浓度。结果壳聚糖胶囊组血清中的时间-浓度曲线下面积(AUC0~12)是对照组AUC0~12的0.62倍;而结肠组织中壳聚糖胶囊组AUC0~12是对照组AUC0~12的3.62倍。结论5-ASA壳聚糖胶囊具有较好的结肠定位靶向释药特性。

Absorption and distribution of 5-aminosalicylic acid from its chitosan capsule degraded by colon bacteria-released enzymes in rats

Objective To examine the absorption and distribution of 5-am in osalicylic acid (5-ASA) in rat colon after oral administration of its chitosan capsule. Methods5-ASA in chitosan capsules (4.8 mg per 3 capsules) were adminis tered orally in rats via a polyethylene cannula under light ether anest hesia. The rats in control group were given 1 ml 5-ASA carboxymethyl ce llulose suspension (4.8 mg). Blood samples were obtained from the rat hearts and the colon tissues sampled at a given interval to measure the concentration of 5-ASA by HPLC. Results The area under the curve (AUC 0-12 ) in the serum samples of chitosan capsule group was 0.62 times that of the control group, while in the colon tissue, the AUC 0-12 of chitosan capsule group was as much as 3.62 times that of the control gr oup. Conclusions The chitosan capsule may be a useful carrier of 5-ASA for colo n-specific delivery.