Preparation and evaluation of progesterone injection with different particle size
10.13220/j.cnki.jipr.2017.06.027
- VernacularTitle:不同粒径黄体酮的制备及评价
- Author:
Li LI
;
Wanqing LI
;
Ying LI
;
Jing GAO
;
Hui ZHANG
;
Jianxu SUN
;
Aiping ZHENG
- Keywords:
progesterone;
nanocrystal;
release rate;
pharmacokinetics
- From:
Journal of International Pharmaceutical Research
2017;44(6):609-615
- CountryChina
- Language:Chinese
-
Abstract:
Objective To compare the release rate and bioavailability of progesterone injection with different particle sizes. Methods The preparation of progesterone nano sized injection and micron sized injection were performed by power X-ray diffraction (PXRD)and Fourier trensform infrared spectooscory(FTIR). The dissolution rate of two preparations and progesterone was compared by dialysis Method. HPLC-MS method was used to determine the progesterone concentration of plasma in rats after intramuscular injec-tion of different preparations,and the main pharmacokinetic parameters were calculated and analyzed statistically. Results Based on the analysis of PXRD and FTIR,there were no crystal structure changes between the two preparations and progesterone. The complete release of progesterone nano sized injection and micron sized injection required 2 and 4 h in the PBS solution,respectively,while the release of progesterone required nearly 40 h. In the pharmacokinetic experiment,compared with progesterone injection,the Cmax of pro-gesterone nano sized injection and micron sized injection were increased by 1.8 and 1.7 times,respectively;the AUC0-t were increased by 2.95 and 1.63 times,respectively. The bioavailability of both was higher than that of progesterone injection. Conclusion The re-lease rate bioavailability of progesterone nano sized injection and micron sized injection is higher than that of progesterone and proges-terone injection. Bioavailability of progesterone nano sized injection is higher than that of progesterone micron sized injection.
