Bioavailability study of self-microemulsifying drug delivery system of a novel anti-stroke compound TID-101 in rats
10.13220/j.cnki.jipr.2016.04.027
- Author:
Guang-Yu GAO
1
Author Information
1. Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences
- Publication Type:Journal Article
- Keywords:
Bioavailability;
LC-MS/MS;
Pharmacokinetics;
Self-(micro)emulsifying drug delivery system(SMEDDS);
Stroke
- From:
Journal of International Pharmaceutical Research
2016;43(4):731-735
- CountryChina
- Language:Chinese
-
Abstract:
Objective: To establish and validate a LC-MS/MS method for quantitative analysis of a new anti-stroke compound TID-101 in rat plasma and to study the pharmacokinetics and bioavailability of TID-101 self-(micro)emulsified drug delivery system(SMEDDS). Methods: The plasma samples were treated with methanol for precipitating protein. The chromatographic separation was achieved with a acetonitrile-water mobile phase. Detection of TID-101 and the internal standard (IS) dexamethasone acetate was achieved by electrospray ionization (ESI) source in the negative ion mode at m/z 353.4→323.2 and m/z 433.4→353.4. The method was applied for pharmacokinetics study of TID-101 between SMEDDS in rats. Results: The method was linear over TID-101 concentration range from 10-95 000 ng/ml with the correlation coefficients (r) of 0.9998. The intra-run and inter-run relative standard deviations(RSD) were less than 15% and the average absolute recovery values were 83.4-87.0%. The validated method was applied to a pharmacokinetic study in rats after intravenous administration of TID-101 fat emulsion injection and oral administration of TID-101 suspension and SMEDDS. The bioavailability of TID-101 API and SMEDDS was 2.8% and 14.9%, respectively. Conclusion: The analysis method is simple, accurate, and sensitive for assaying the in vivo pharmacokinetic study of TID-101 in rats. SMEDDS could effectively enhance the oral bioavailability of TID-101.
