Effect of age on the pharmacokinetics of polymorphic nimodipine in rats after oral administration.
- Author:
Wenli LIU
1
;
Xiaona WANG
1
;
Ruilian CHEN
1
;
Kaixuan ZHANG
1
;
Yao LI
1
;
Yi LI
1
;
Duanyun SI
2
;
Junbo GONG
1
;
Dianshu YIN
3
;
Yongli WANG
1
;
Zhenping WEI
1
;
Mingshi YANG
4
Author Information
1. School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China.
2. State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China.
3. Pharmaceutical Research Institute, Shijiazhuang No. 4 Pharmaceutical Company, Shijiazhuang 052165, China.
4. Faculty of Pharmaceutical Science, University of Copenhagen, Copenhagen, Denmark.
- Publication Type:Journal Article
- Keywords:
Age difference;
Crystal form;
Nimodipine;
Pharmacokinetics;
Polymorphic drug
- From:
Acta Pharmaceutica Sinica B
2016;6(5):468-474
- CountryChina
- Language:English
-
Abstract:
The previous investigation has proved that their existed pharmacokinetic difference between the different crystal forms of the polymorphic drugs after oral administration. However, no systemic investigations have been made on the change of this pharmacokinetic difference, resulted either from the physiological or from the pathological factors. In this paper, we used polymorphic nimodipine (Nim) as a model drug and investigated the effect of age difference (2- and 9-month old) on the pharmacokinetics after oral delivery in rats. As the results shown, for L-form of Nim (L-Nim), the AUCin 2-month-old rats was 343.68±47.15 ng·h/mL, which is 23.36% higher than that in 9-month-old rats. For H-form of Nim (H-Nim), the AUCin 2-month-old rats was 140.91±19.47 ng·h/mL, which is 54.64% higher than that in 9-month-old rats. The AUCratio between H-Nim and L-Nim was 2.44 in 2-month-old rats and 3.06 in 9-month-old rats. Since age difference could result in unparallelled change of the absorption and bioavailability of the polymorphic drugs, the results in this experiment are of value for further investigation of crystal form selection in clinical trials and rational clinical application of the polymorphic drugs.
