首页|基于溶解性与渗透性评价盐酸小檗碱的生物药剂学分类研究

基于溶解性与渗透性评价盐酸小檗碱的生物药剂学分类研究

Biopharmaceutics Classification of Berberine Hydrochloride Based on Solubility and Permeability Evaluation

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目的 对盐酸小檗碱在生物药剂学分类系统中的归属进行研究,并确定其分类属性.方法 考察盐酸小檗碱在pH 1.0～8.0介质中的溶解度;通过在体原位肠灌流模型得出其在大鼠十二指肠、空肠、回肠和结肠中的相关吸收参数,确定其渗透性.结果 通过在不同pH值溶解介质中的药物剂量数D0值和药典规定发现盐酸小檗碱属于低溶解度药物;从渗透性实验结果发现盐酸小檗碱在大鼠各肠段的渗透系数Peff(rat)均超过5.0×10-5 cm·s-1,转化成人体吸收百分率Fa(human)均超过85％,故判定其属于高渗透性药物.结论 结合溶解性与渗透性实验结果证明盐酸小檗碱属于低溶解性、高渗透性药物,即属于BCS Ⅱ类药物.
OBJECTIVE To investigate the attribution of berberine hydrochloride in the biological pharmaceutics classification system(BCS)and to determine its taxonomic properties.METHODS The solubility of berberine hydrochloride was investigated in pH 1.0-8.0 medium;its absorption parameters related to the rat duodenum,jejunum,ileum and colon were derived from in-situ intestinal perfusion model in vivo to determine its permeability.RESULTS The solubility in different pH dissolution media with the value of drug metering number(D0)and combined with the pharmacopoeia regulations found that berberine hydrochloride belonged to the low solubility drugs.From the results of permeability experiments,it was found that the permeability coefficient Peff(rat)of berberine hydrochloride in each intestinal segments was exceeded than 5.0 × 10-5 cm·s-1in rats,and the conversion into human absorption Fa(human)was exceeded than 85％,therefore,it was determined to be the high permeability drug.CONCLUSION The combination of solubility and permeability test results proves that berberine hydrochloride is a low solubility and high permeability drug,which belongs to BCS class Ⅱ.

berberine hydrochloridesolubilitypermeabilityBCS classificationin-situ single pass intestinal perfusion

罗文慧、温艳艳、崩淑娟、韩海伦、阚家义、彭灿

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安徽中医药大学药学院,合肥 230012

安徽中医药大学药物制剂技术与应用安徽省重点实验室,合肥 230012

安徽省食品药品检验研究院,合肥 230051

安徽中医药大学省部共建安徽道地中药材品质提升协同创新中心,合肥 230012

安徽中医药大学安徽省乡村振兴协同技术服务中心,合肥 230012

安徽中医药大学安徽省现代中药产业共性技术研究中心,合肥 230012

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盐酸小檗碱 溶解度 渗透性 生物药剂学分类系统 在体单向原位肠灌流

安徽省科技重大专项资助安徽省高校协同创新项目资助安徽省高校协同创新项目资助安徽省高校协同创新项目资助

202103a07020001GXXT-2022-084GXXT-2022-075GXXT-2020-025

2024

10.11669/cpj.2024.13.007

中国药学杂志
中国药学会

中国药学杂志

CSTPCD北大核心
影响因子：0.957
ISSN：1001-2494
年,卷(期)：2024.59(13)