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Pharmacodynamics of compound danshen pH-dependent delayed release pellets in dogs

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Author:
No author available
Journal Title:
ACTA PHARMACEUTICA SINICA
Issue:
12
DOI:
10.3321/j.issn:0513-4870.2005.12.004
Key Word:
复方丹参;pH依赖型延迟释药微丸;血清药理学;药效动力学

Abstract: 目的制备复方丹参pH依赖型延迟释药微丸填充胶囊并进行家犬体内药效动力学研究.方法分别用HPMC,Eudragit L-30D-55,Eudragit L100/S100(1:6)包衣制备pH依赖型延迟释药微丸,测定体外释放曲线,并用血清药理学方法进行家犬体内的药效动力学研究.结果制备了复方丹参pH依赖型延迟释药微丸,体外溶出曲线呈pH依赖特征.单剂量给药后自制速释片R的药效动力学参数Tmax为0.58 h,Emax为34.63%,延迟释药胶囊T1和T2的Tmax分别延长至2.42和3.17 h,Emax分别降低至13.57%和14.52%,相对生物利用度分别为99.3%和133.6%.多剂量给药后自制速释片R波动度DF 7.32,延迟释药胶囊T1和T2的波动度DF 3.40和3.03.结论复方丹参pH依赖型延迟释药胶囊体外释放具有pH依赖特征,体内具有明显的延迟释药作用,多剂量达到稳态时,药效动力学波动系数低于普通片.

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