不同中药物料对丸剂溶出的影响及其体内外评价(1)
摘要：目的 研究5类不同中药物料对丸剂溶出的影响，评价其体内外相关性，并对中药物料的辅料功能进行探索。方法 采用均匀设计法，自拟8个处方，用淀粉类、纤维类、蛋白类、油脂类、多糖类中药物料制备不同模型丸剂，HPLC测定丸剂中盐酸小檗碱体外累积释放度、家兔体内血药浓度，考察中药物料对丸剂体内外释药行为的影响，并进行丸剂体内外相关性评价。结果 淀粉、纤维类物料对丸剂溶出有促进作用，蛋白、油脂类物料对丸剂溶出有阻滞作用，多糖类物料对丸剂溶出无显著作用；丸剂体内外相关性显著。结论 中药物料具有“药辅统一”的性质，可通过调节处方中物料细粉比例控制丸剂溶出度及生物有效性；丸剂的体内外相关性良好。
关键词：中药物料；盐酸小檗碱；丸剂；溶出；体内外相关性
DOI：10.3969/j.issn.1005-5304.2018.02.019
中图分类号：R285.5 文献标识码：A 文章编号：1005-5304(2018)02-0083-06
Effects of Different Chinese Medicine Materials on Dissolution of Pills
and Their in Vitro - in vivo Evaluation
CHEN Tian-chao1，2， HU Yu-qing1， LIU Rui-xia3， YU Lan-lan4， MA Yan-jiang2， CHANG Qian-qian1， LI Rui-ying1
1. Henan University of Traditional Chinese Medicine， Zhengzhou 450008， China； 2. The First Affiliated Hospital of Henan University of Traditional Chinese Medicine， Zhengzhou 450000， China； 3. Zhongmou County Hospital， Zhengzhou 451450， China； 4. Henan Province Third People's Hospital， Zhengzhou 450000， China
Abstract： Objective To study the effects of five different kinds of Chinese medicine materials on dissolution of pills； To evaluate their in vitro - in vivo correlation. Methods Five different types of traditional Chinese medicine materials， such as starch， fiber， protein， grease and polysaccharide materials， were selected by uniform design to the proposed 8 model formulation and preparation of pills， and the cumulative release rate and in vivo plasma concentration of berberine hydrochloride were determined by HPLC. The effects of Chinese medicine materials on the drug release behavior of pills in vitro - in vivo were investigated. And the in vitro - in vivo correlation of the pills was evaluated. Results Starch and fiber materials could promote the release of the pills， and protein and grease materials has a blocking effect on the pills dissolution. Polysaccharide materials have no significant effect on the dissolution of the pills. Pills in vitro - in vivo correlation was significant. Conclusion Chinese medicine materials have the characteristics of medicine-assisted unity， which can control the dissolution and bioavailability of pills by adjusting the proportion of powder in the prescription. And the pills have good correlation in vitro - in vivo.
Keywords： Chinese medicine materials； berberine hydrochloride； pill； dissolution； correlation in vivo - in vitro
中藥丸剂是指药材细粉或药材提取物加适宜粘合剂或其他辅料制成的球形或类球形制剂。研究表明，辅料是药物制剂的基础材料及重要的组成部分，在制剂剂型和生产中起着关键作用，它不仅赋予药物一定剂型，并且与提高药物疗效、降低毒副作用有很大的关系[1]。但长期以来，药用辅料导致的不良反应、药用辅料质量标准水平参差不齐等影响了药品质量、溶出度、生物利用度和工艺稳定性[2]。有研究显示，丸剂中所含中药物料(药物细粉)既是药物成分，又具有制剂辅料功能，即中药物料具有“药辅统一”性质[3]。发掘中药的“药辅统一”功能，可减少药用辅料的用量和不良反应，提高丸剂的载药量、稳定性和质量可控性[4]，为丸剂处方及制备工艺的优化提供依据。本研究通过调整中药物料比例(药物细粉与提取物比例)制备不同模型丸剂，测定其体内外释放度，探讨中药物料是否具有辅料功能，能否改变中药丸剂溶出过程，实现速释或缓释，达到控制药效的目的。, http://www.100md.com(陈天朝 胡玉青 刘瑞霞 于兰兰 马彦江 常倩倩 李瑞颖)
关键词：中药物料；盐酸小檗碱；丸剂；溶出；体内外相关性
DOI：10.3969/j.issn.1005-5304.2018.02.019
中图分类号：R285.5 文献标识码：A 文章编号：1005-5304(2018)02-0083-06
Effects of Different Chinese Medicine Materials on Dissolution of Pills
and Their in Vitro - in vivo Evaluation
CHEN Tian-chao1，2， HU Yu-qing1， LIU Rui-xia3， YU Lan-lan4， MA Yan-jiang2， CHANG Qian-qian1， LI Rui-ying1
1. Henan University of Traditional Chinese Medicine， Zhengzhou 450008， China； 2. The First Affiliated Hospital of Henan University of Traditional Chinese Medicine， Zhengzhou 450000， China； 3. Zhongmou County Hospital， Zhengzhou 451450， China； 4. Henan Province Third People's Hospital， Zhengzhou 450000， China
Abstract： Objective To study the effects of five different kinds of Chinese medicine materials on dissolution of pills； To evaluate their in vitro - in vivo correlation. Methods Five different types of traditional Chinese medicine materials， such as starch， fiber， protein， grease and polysaccharide materials， were selected by uniform design to the proposed 8 model formulation and preparation of pills， and the cumulative release rate and in vivo plasma concentration of berberine hydrochloride were determined by HPLC. The effects of Chinese medicine materials on the drug release behavior of pills in vitro - in vivo were investigated. And the in vitro - in vivo correlation of the pills was evaluated. Results Starch and fiber materials could promote the release of the pills， and protein and grease materials has a blocking effect on the pills dissolution. Polysaccharide materials have no significant effect on the dissolution of the pills. Pills in vitro - in vivo correlation was significant. Conclusion Chinese medicine materials have the characteristics of medicine-assisted unity， which can control the dissolution and bioavailability of pills by adjusting the proportion of powder in the prescription. And the pills have good correlation in vitro - in vivo.
Keywords： Chinese medicine materials； berberine hydrochloride； pill； dissolution； correlation in vivo - in vitro
中藥丸剂是指药材细粉或药材提取物加适宜粘合剂或其他辅料制成的球形或类球形制剂。研究表明，辅料是药物制剂的基础材料及重要的组成部分，在制剂剂型和生产中起着关键作用，它不仅赋予药物一定剂型，并且与提高药物疗效、降低毒副作用有很大的关系[1]。但长期以来，药用辅料导致的不良反应、药用辅料质量标准水平参差不齐等影响了药品质量、溶出度、生物利用度和工艺稳定性[2]。有研究显示，丸剂中所含中药物料(药物细粉)既是药物成分，又具有制剂辅料功能，即中药物料具有“药辅统一”性质[3]。发掘中药的“药辅统一”功能，可减少药用辅料的用量和不良反应，提高丸剂的载药量、稳定性和质量可控性[4]，为丸剂处方及制备工艺的优化提供依据。本研究通过调整中药物料比例(药物细粉与提取物比例)制备不同模型丸剂，测定其体内外释放度，探讨中药物料是否具有辅料功能，能否改变中药丸剂溶出过程，实现速释或缓释，达到控制药效的目的。, http://www.100md.com(陈天朝 胡玉青 刘瑞霞 于兰兰 马彦江 常倩倩 李瑞颖)