Abstract：【Objective】To study the pharmacokinetics profiles and relative bioavailability of berberine hydrochloride and berberine hydrochloride solid dispersion in rats. 【Methods】A total of 18 SD rats were randomly divided into A, B, C groups. Rats in group A, B and C were administrated with 200 mg/kg (calculated as berberine hydrochloride) of berberine hydrochloride APIs, berberine hydrochloride photysome and berberine hydrochloride solid dispersion, respectively. Then blood samples were taken at 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 10, 12, 24h to determine the plasma concentration of berberine hydrochloride by HPLC. 【Results】The t1/2 of group A, group B and group C were 2.53±0.64h, 4.15±0.58h and 2.24±0.44h, respectively. The Cmax were 211.0±31.2 ng/mL, 318.5±42.6 ng/mL and 541.3±55.3 ng/mL,respectively and AUC0~24h were 1392.6±367.6 ng/(h?mL), 2638.5±630.7 ng/(h?mL), 3081.9±751.4 ng/(h?mL), respectively. With group A as reference, group B and C were Fr(B)=189.5%, Fr(C)=221.3%.【Conclusion】The photysome and solid dispersion can highly improve the bioavailability of berberine hydrochloride. Further,, the blood sample processing and HPLC method can accurately determine the plasma concentration of berberine hydrochloride.
陈佰青, 叶剑波, 王汝上. 盐酸小檗碱及其制剂中间体在大鼠体内的药动学及生物利用度研究[J]. 医学临床研究, 2019, 36(3): 463-465.
CHENG Bai-qing, YE Jian-bo, WANG Nu-shang. Pharmacokinetics and Bioavailability of Berberine Hydrochloride and Its Preparation Intermediates in Rats. JOURNAL OF CLINICAL RESEARCH, 2019, 36(3): 463-465.
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