Preparation technology of supersaturatable self-microemulsifying drug delivery system of etoposide and quality evaluation
10.7501/j.issn.0253-2670.2015.06.008
- Author:
Dan-Dan ZHAO
1
Author Information
1. College of Pharmaceutical Science, Zhejiang Chinese Medical University
- Publication Type:Journal Article
- Keywords:
Etoposide;
Preparation technology;
Pseudo ternary phase diagram;
Psychro-thermal cycles;
Self-microemulsion;
Solubility;
Supersaturatable self-microemulsifying drug delivery system
- From:
Chinese Traditional and Herbal Drugs
2015;46(6):822-831
- CountryChina
- Language:Chinese
-
Abstract:
To prepare supersaturatable self-microemulsifying drug delivery system (S-SMEDDS) of etoposide (VP-16) for increasing the solubility of difficult soluble drug of etoposide, which will provide a scientific basis for improving its bioavailability. To study the prescription and preparation technology of S-SMEDDS of VP-16, according to different oil phases, compatibility of surfactants, and the microemulsion area size in the pseudo ternary phase diagram of different cosurfactants, to determine the basic prescription of self-microemulsifying concentrate, optimize the prescription of VP-16 based on its solubility and crystallization conditions, with filtrating appropriate precipitation inhibitor and the best prescription drug loading. The rate of self-microemulsifying was taken as index to study the preparation technology of VP-16 S-SMEDDS for investigating the influence on the ability of self-microemulsifying. The optimal prescription is: RH40-PEG 400-GTCC-PVP K30 (20∶ 20∶ 10∶ 1), 2% drug content of the mass fraction. The optimum technological conditions are 37 ℃, 20 r/min, and 20 min by magnetic stirring. The average particle size of VP-16 S-SMEDDS is (82.7 ± 3.3) nm and the size distribution of VP-16 S-SMEDDS is relatively concentrated. The average content of VP-16 in three batches of S-SMEDDS is 19.98 mg/g. Results of dissolution test showed that at 60 min the cumulative dissolution is close to 100%. Stability study results show that the high temperature and light could influence the drug stability and micro emulsification ability of VP-16 S-SMEDDS, while the psychro-thermal cycles test has no influence to it. After the preliminary stability test, the results show that the stability of VP-16 S-SMEDDS is good. The optimized prescription of VP-16 S-SMEDDS can significantly increase the solubility of VP-16, and it's quality is stable, which could improve its bioavailability further. The research method is scientific, reliable, and feasible.
