Studies on pharmacokinetics and tissue distribution of oridonin nanosuspensions
详细信息 查看全文
- 作者：Lei Gao ; Dianrui Zhang ; Minghui Chen ; Cunxian Duan ; Wenting Dai ; Lejiao Jia ; Wenfa Zhao
- 关键词：Oridonin ; Nanosuspensions ; High pressure homogenization ; Pharmacokinetics ; Tissue distribution
- 刊名：International Journal of Pharmaceutics
- 出版年：2008
- 出版时间：1 May 2008
- 年：2008
- 卷：355
- 期：1-2
- 页码：321-327
- 全文大小：441 K
文摘
The purpose of the present study was to investigate the effects of particle size on the pharmacokinetics and tissue distribution of oridonin nanosuspensions after intravenous administration. Two oridonin nanosuspensions with markedly different size were prepared by high pressure homogenization method. The particle size of nanosuspension A is 103.3 ± 1.5 nm, while B is 897.2 ± 14.2 nm. Dissolution studies showed that complete dissolution could be obtained within 10 min for nanosuspension A, however, nanosuspension B showed a slower dissolution, only 85.2 % dissolved by 2 h. The pharmacokinetics and tissue distribution of oridonin nanosuspensions A and B were studied after intravenous administration using New Zealand rabbits and Kunming mice as experimental animals, respectively. An Oridonin control solution was studied parallelly. The results showed that oridonin nanosuspension A exhibited pharmacokinetic and biodistribution properties similar to solution due to its rapid dissolution in blood circulation. Oridonin nanosuspension B, however, showed a high uptake in RES organs, meanwhile exhibited a markedly different pharmacokinetic property compared to nanosuspension A. These differences could be attributed to the different particle size of the two nanosuspensions considering their zeta potential had no significant difference. In conclusion, particle size showed obvious effects on pharmacokinetics and tissue distribution of nanosuspensions.