摘要
目的:研究盐酸小檗碱羧甲基魔芋胶小丸在大鼠体内的药物吸收及胃,小肠和结肠组织中药物浓度经时变化,评价其结肠定位释药特性。方法:将盐酸小檗碱羧甲基魔芋胶小丸(小丸组)和盐酸小檗碱羧甲基纤维素混悬液(对照组)大鼠灌胃给药(以盐酸小檗碱计,给药剂量50 mg·kg^(-1)),采用HPLC测定大鼠体内盐酸小檗碱在血浆,胃,小肠和结肠组织中的浓度,计算药物相对靶向释药指数。结果:盐酸小檗碱在血浆和组织匀浆中线性范围分别为0.0252～2.52 mg·L^(-1)(r=0.999 2)和0.126～25.22 mg·L^(-1)(r>0.99),血浆和组织匀浆中检测限分别为10,8 mg·L^(-1),小丸组血浆中药时曲线下面积(AUC_(0→∞))是对照组的0.477倍;小丸组胃,小肠,结肠组织AUC_(0→∞)分别是对照组的0.187,0.228,2.00倍;小丸组在大鼠胃,小肠,结肠组织的药物相对靶向释药指数分别为0.392 4,0.478 6,4.193。结论:盐酸小檗碱羧甲基魔芋胶小丸具有较好的结肠定位释药特性。
Objective： To observe the absorption and concentration of berberine hydrochloride （BH） in gastric, entric, colonic tissue after intragastric administration of BH-containing carboxymethyl konjac glucomannan pellets for evaluating colon-specific drug delivery characteristics of the pellets. Method： BH-containing carboxymethyl konjac glucomannan pellets （pellets group） and BH-containing carboxymethyl cellulose suspension （control group） were intragastric administrated to rats at the dose of 50 mg·kg^-1, respectively. A high performance liquid chromatography method determinated BH concentration in rat plasma and tissue. Drug delivery index （DDI） was calculated. Result： The range of BH in plasma and tissue in rats were 0. 025 2-2. 52 mg·L^-1（ r = 0. 999 2） and 0. 126- 25.22 mg·L^-1 （R 〉0. 99） ,respectively. The detection of BH in plasma and tissue were 10 μg·L^-1 and 8μg· L^-1 , respectively. The area under the curve （ AUC0→∞ ） in the plasma samples of pellets group was 0. 477 times that of the control group ; in the gastric, entric, colonic tissue, the AUC0→∞ of pellets group was as much as 0. 187, 0. 228, 2.00 times that of the control group, respectively. The DDI of the pellets was 0. 392 4, 0. 478 6, 4. 193 in the gastric, entric, colonic tissue of the rat, respectively. Conclusion： Carboxymethyl konjac glucomannan pellets may be a useful carrier of BH for colon-specific delivery.
出处
《中国中药杂志》
CAS
CSCD
北大核心
2008年第13期1591-1595,共5页
China Journal of Chinese Materia Medica
关键词
盐酸小檗碱
羧甲基魔芋胶
体内药物释放
结肠定位给药系统
berberine hydrochloride
carbexymethyl konjac glucomannan
in vivo drug release
colon-specific drug delivery system
