交泰丸中4种生物碱与人血浆蛋白结合率的测定  

Determination of the protein-binding rates of four compounds in Jiaotai pills with human plasma proteins

作　　者：朱立静[1] 何书芬[1] 宗阳[1] 张倩[1] 戴国梁[1] 居文政[1] 

机构地区：[1]南京中医药大学附属医院,江苏南京210029

出　　处：《中国医院药学杂志》2017年第22期2222-2225,2235,共5页Chinese Journal of Hospital Pharmacy

基　　金：国家自然科学基金资助项目(编号:81573685);重大新药创制(编号:2012ZX09303009-002)

摘　　要：目的:研究交泰丸中表小檗碱,盐酸黄连碱,盐酸巴马汀,盐酸小檗碱与人血浆蛋白的结合率。方法:采用平衡透析法测定交泰丸中4种生物碱与人血浆蛋白的结合率,用高效液相色谱(HPLC)法测定透析内、外液中4种成分的质量浓度,计算血浆蛋白结合率。结果:表小檗碱,盐酸黄连碱,盐酸巴马汀和盐酸小檗碱的线性关系、精密度、提取回收率和稳定性均符合方法学要求;交泰丸低、中、高(0.5,1,1.5 mg·mL-1)浓度中,表小檗碱与人血浆蛋白结合率分别为40.28%±3.02%,42.41%±2.61%,33.76%±2.19%,盐酸黄连碱与人血浆蛋白结合率分别为46.60%±3.47%,58.49%±6.47%,47.00%±1.3%,盐酸巴马汀与人血浆蛋白结合率分别为40.17%±3.26%,33.71%±3.74%,24.05%±1.81%,盐酸小檗碱与人血浆蛋白的结合率分别为29.41%±4.99%,25.35%±1.37%,18.07%±1.61%。结论:交泰丸中表小檗碱,盐酸巴马汀和盐酸小檗碱属于低等结合型成分,盐酸黄连碱属于中等结合型成分。OBJECtIVE To study the protein-binding rates of epiberberine, coptisine hydrochloride, palmatine chloride, berberine hydrochloride in Jiaotai pills with human plasma proteins. METHODS Equilibrium dialysis method was carried to de- termine the binding rates of 4 alkaloids in Jiaotai pills in vitro. A HPLC method for the determination of the four compounds both in inner and outer dialysis was established and then the protein-binding rate with human plasma proteins was calculated. RESULTS Linear relationship, precision, extraction recovery and stability of epiberberine, coptisine hydrochloride, palmatine chloride, berberine hydrochloride all complied with the methodological requirements. At the low, middle and high concentra- tion （0. 5, 1, 1.5 mg·mL^-1） of Jiaotai pills, the human plasma protein-binding rates were 40. 28% ±3.02%, 42. 41% ± 2. 61% and 33.76% ± 2. 19% for epiberberine, 46. 60% ± 3.47%, 58. 49% ± 6. 47% and 47. 00% ± 1.3% for coptisine hydro- chloride, 40. 17% ±3. 26±33. 71% ± 3.74% and 24. 05% ± 1.81% for palmatine chloride, 29. 44%± 4. 99%, 25. 35%0 ± 1.37% and 18. 07% ±1.61% for berberine hydroehloride. CONCLUSION Epiberberine, palmatine chloride, berberine hydro chloride in Jiaotai pills have low capacity in binding to human plasma proteins in vitro, while coptisine hydrochloride has a mid- dle capacity.

关 键 词：交泰丸 黄连 生物碱 蛋白结合率 高效液相色谱 

分 类 号：R927.2[医药卫生—药学]