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目的:研究肠溶衣对压力控制结肠定位释放胶囊(Ent-PCDCs)的稳定性及其体内外释放特征。方法:压制法制备含咖啡因半合成脂肪酸脂囊芯,高效包衣机进行乙基纤维素(EC)和肠溶性包衣。测定PCDCs的体外崩解压力后,进行Ent-PC-DCs稳定性、体外释放及恒河猴的口服药动学研究。结果:Ent-PCDCs的稳定性明显提高,其崩解压力与EC厚度呈线性关系;Ent-PCDCs在人工胃液中2h和人工肠液6h的累计释放量低于25%。药动学试验结果,EC厚度为32μm时咖啡因的Tmax和MRT分别为(5.67±1.21)h和(16.80±1.74)h,初步表明药物主要在结肠部位释放和吸收。结论:Ent-PCDC的稳定性符合要求,EC厚度对药物结肠定位释放具有重要影响。
OBJECTIVE: To study the stability of enteric coated colon-controlled release capsules (Ent-PCDCs) and its release in vitro and in vivo. Methods: Preparation of semi-synthetic fatty acid caffeine core with caffeine by pressing, high efficiency coating machine for ethyl cellulose (EC) and enteric coating. After the in vitro disintegration pressure of PCDCs was measured, the stability of Ent-PC-DCs, the release in vitro and the oral pharmacokinetics of rhesus monkeys were studied. Results: The stability of Ent-PCDCs was significantly improved. The disintegration pressure was linear with EC thickness. The cumulative release of Ent-PCDCs in artificial gastric juice for 2 hours and artificial intestinal juice was less than 25%. The results of pharmacokinetics showed that the Tmax and MRT of caffeine were (5.67 ± 1.21) h and (16.80 ± 1.74) h, respectively, at the EC thickness of 32 μm, which indicated that the drug was mainly released and absorbed in the colon. Conclusion: The stability of Ent-PCDC meets the requirement. The thickness of EC has an important influence on the release of drug colon.