In vivo pharmacokinetics and in vitro-in vivo correlation of silymarin phospholipid complex microporous osmotic pump controlled-release tablets in beagle dogs
10.12206/j.issn.2097-2024.202206052
- VernacularTitle:水飞蓟素磷脂复合物微孔渗透泵控释片比格犬体内药动学及体内外相关性研究
- Author:
Qiping ZENG
1
;
Lina YANG
2
;
Jianqing LIU
3
;
Hongtao SONG
4
Author Information
1. Department of Pharmacy, Zhangzhou Affiliated Hospital of Fujian Medical University, Zhangzhou 363000, China.
2. Department of Pharmacy, No.909 Hospital of Joint Logistic Support Force, Zhangzhou 363000, China.
3. School of pharmacy, Quanzhou Medical College, Quanzhou 362000, China.
4. Department of Pharmacy, No.900 Hospital of Joint Logistic Support Force, Fuzhou 350025, China.
- Keywords:
silymarin;
phospholipid complex;
microporous osmotic pump controlled release tablets;
pharmacokinetics;
in vivo-in vitro correlation;
HPLC;
bioavailability
- From:
Journal of Pharmaceutical Practice
2023;41(12):741-746
- CountryChina
- Language:Chinese
-
Abstract:
Objective To evaluate the release characteristics in vitro, pharmacokinetics in rabbits and in vivo-in vitro correlation of silymarin phospholipid complex microporous osmotic pump controlled release tablets（SM-PC MPOP）. Methods The release characteristics of SM-PC MPOP in vitro were detected by HPLC in the artificial gastric fluid. Six beagle dogs were subjected to double cycle cross control, which were given SM-PC MPOP and Legalon（30 mg/kg）. The concentration of silybin in plasma was determined by HPLC and the data were processed by software. Results The cumulative release rate of SM-PC MPOP in vitro was over 85% in 12 h. The pharmacokinetics in beagle dogs showed that SM-PC MPOP and legalon conformed to double compartment first-order absorption model and the pharmacokinetic parameters were obtained: tmax:（3.2±0.4）and（0.9±0.1）h, Cmax:（0.298 6±0.068 9）and（0.629 9±0.076 5）μg/ml, AUC0→24:（2.996 8±0.583 3）and（2.268 9±0.432 8）h·μg /ml. The relative bioavailability of SM-PC MPOP was（162.21 ± 30.82）%. Conclusion SM-PC MPOP could release slowly, which could increase the relative bioavailability significantly. The correlation between the absorption in vivo and release in vitro was fine（r = 0.839 0）.
