In vitro-in vivo correlation of goserelin acetate microspheres
10.16438/j.0513-4870.2018-0859
- VernacularTitle:醋酸戈舍瑞林微球的体内外相关性研究
- Author:
Meng-di WANG
1
;
Ying XUE
2
;
Guang-yi LENG
2
;
Li-xiao XU
1
,
3
;
Jing-jing YAN
2
;
Fei YU
1
,
3
;
Hua-xin YANG
4
;
Wan-hui LIU
1
,
3
Author Information
1. Key Laboratory of Molecular Pharmacology and Drug Evaluation, Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, School of Pharmacy, Yantai University, Yantai 264005, China
2. State Key Laboratory of Long-acting and Targeting Drug Delivery System, Shandong Luye Pharmaceutical Co. Ltd, Yantai 264670, China
3. State Key Laboratory of Long-acting and Targeting Drug Delivery System, Shandong Luye Pharmaceutical Co. Ltd, Yantai 264670, China
4. National Institutes for Food and Drug Control, Beijing 102629, China
- Publication Type:Research Article
- Keywords:
goserelin acetate;
microsphere;
italic>in vitro release profile;
pharmacokinetics;
italic>in vitro-in vivo correlation;
predictive ability
- From:
Acta Pharmaceutica Sinica
2019;54(1):159-165
- CountryChina
- Language:Chinese
-
Abstract:
The objective of this paper was to establish a level A in vitro-in vivo correlation (IVIVC) for goserelin acetate extended release microspheres for injection. Three kinds of goserelin acetate microspheres with different release rates were prepared and the critical physicochemical properties, such as drug loading, particle size, glass transition temperature and morphology were characterized. In vitro dissolution test of the prepared goserelin acetate microspheres was performed using sample-and-separate method at 45 ℃ in 5% (v/v) methanol. The morphology of the microspheres and the molecular weight of poly (lactic-co-glycolic acid) (PLGA) of the prepared goserelin acetate microspheres were investigated to research the release mechanism of microspheres. The plasma concentration of goserelin was detected after intramuscular injection of goserelin acetate microspheres to SD rats, and correlated with the in vitro release profiles after processing by percent AUC method. The pharmacokinetic experimental protocol of goserelin acetate microspheres for injection in SD rats was approved by the Animal Ethics Committee of Shandong Luye Pharmaceutical Co., Ltd. The results indicated that the developed sample and separate method was able to detect differences in the release characteristics of the prepared goserelin acetate microspheres, and the in vitro-in vivo correlation of goserelin acetate microspheres was excellent (r > 0.98) and had good predictive ability in SD rats.
