Study on preparation of ligustrazine ocular implant and correlation between in vivo and in vitro drug release.
- Author:
Jun-Hua WEI
1
;
Pei LI
;
Peng-Kai MA
;
Hong-Jie MU
;
Da-Quan CHEN
;
Kao-Xiang SUN
Author Information
- Publication Type:Journal Article
- MeSH: Animals; Biological Availability; Drug Implants; Eye; Female; Male; Polyglycolic Acid; chemistry; Pyrazines; administration & dosage; chemistry; pharmacokinetics; Rabbits; Vitreous Body
- From: China Journal of Chinese Materia Medica 2013;38(8):1160-1164
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVETo prepare ligustrazine (TMPZ) ocular sustained-release implant, and investigate its in vitro drug release, pharmacokinetics in rabbit vitreum and in vitro correlation.
METHODLigustrazine ocular sustained-release implants were prepared by micro-twin conical screw mixers with hot-melting extrusion method, with polyactic-co-glycolic acid (PLGA) as the matrix. HPLC was adopted to determine the concentration in vitreum after ligustrazine was implanted in rabbit eyes, in order to examine its in vivo sustained-release behavior, and study the correlation between in vitro and in vivo.
RESULTLigustrazine implants were prepared with a drug-loading rate between 10% and 30%, which was in conformity to the pharmacopoeia in terms of the content uniformity. Its in vitro release was in conformity to the zero-order release model. With PLGA 5050, 2. 5A as a vector, ligustrazine implants with a drug-loading rate of 30% could slowly release drug for more than 3 weeks, indicating a good correlation between in vitro and in vivo release.
CONCLUSIONLigustrazine ocular implants prepared with hot-melting extrusion method is practicable. Ligustrazine ocular implants release drug smoothly in rabbit vitreous vitreums, suggesting good sustained-release effect.
