OBJECTIVE: To prepare Carvedilol microemulsion-based nasal gels, and to investigate its properties. METHODS: The surfactant, the ratio of surfactant to cosurfactant (Km) and oil phase of microemulsion prescription were screened by using solubility and pseudo-ternary phase diagram. The amounts of gel matrix as poloxamer and carbomer were screened by using gelation temperature, gel strength, pH, adhesion and appearance. The nasal gels was inspected in respects of the content of main component, release rate in vitro, gel stability and the cilia toxicity. RESULTS: The emulsifier was tween-80; Km of tween-80-diethylene glycol monoethyl ether was 1 ∶ 1; oil phase was labrafil M-1944; gel matrix were 19% poloxamer and 1% carbomer. The parameters of prepared nasal gel were as follows as gelation temperature of (33.4±0.4) ℃, gel strength of (37.5±1.2) s, pH of (5.71±0.03), adhesion of (64.4±0.5) mg/cm2, white transparent appearance (n=5). The content of main component was 99.48% (n=3), and 8 h accumulative release rate in vitro was 87.11% (n=5). RSDs were all lower than 5% and no stratification or demulsification was found under the condition of centrifugation, low temperature, high temperature and light (n=3). There was no difference in cilia toxicity and normal saline, and they conformed to claim of drug use. CONCLUSIONS: Prepared Carvedilol microemulsion gels show the characteristics of quality stabilization, low cilia toxicity and biological adhensive. Prepared gels can be released completely compared to tablet and in line with the standard of nasal preparations.
关键词
卡维地洛微乳伪三元相图鼻用凝胶体外释放度
Keywords
CarvedilolMicroemulsionPseudo-ternary phase diagramNasal gelRelease degree in vitro