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佐米曲普坦温敏型及黏膜黏附性鼻用凝胶流变学评价

Rheological evaluation of thermoreversible and mucoadhesive nasal gels of Zolmitriptan.

机构信息

Department of Pharmaceutical Technology, Meerut Institute of Engineering and Technology, Meerut-250005, India.

出版信息

Eur Rev Med Pharmacol Sci. 2012 Aug;16(8):1022-7.

PMID:22913151
Abstract

BACKGROUND AND OBJECTIVES

Rheological evaluation of thermoreversible mucoadhesive nasal gel of zolmitriptan is done to determine the steady shear behaviour and gelation temperature. The thermoreversible mucoadhesive polymers are sucessesfully used to increase the contact time of the therapeutic compound in the nasal cavity as well as they cause enhancement in permeation of drug through the nasal mucosa.

MATERIAL AND METHODS

Pluronic (F127) and Pluronic (F 68) were used as thermoreversible polymers in combination with a mucoadhesive polymer obtained from natural resource Zolmiriptan anti migraine drug obtained from Cipla Ltd. Rheometer Brookfield R/S- CPS- PI having cone-and-plate geometry was used for steady shear behaviour study and the gelation temperature was determined by Brookfield R/S plus Rheometer (Brookfield viscometer Ltd, Harlow, Essex, UK) fitted with spindle and Eurotherm cone/plate geometry.

RESULTS

Steady shear behaviour study concludes as content of mucoadhesive polymer starts increasing subsequently the viscosity of the solution starts increasing in the same manner. Gelation temperature study suggests that as the mucoadhesive content was increased in formulation the gelation temperature of the formulation was decreased subsequently. So it was concluded from the study that gelation temperature of the formulation was influenced by the mucoadhesive content. Temperature increases the gelation time of the formulation.

CONCLUSIONS

Above studies indicate that even small difference in the composition of the thermoreversible mucoadhesives gel formulations may cause major change in the rheological behaviour. Although the gelation temperatures of all the three formulations L1, L2 and L3 were below the human nasal temperature, they show different responses to the varied shear rates at different temperatures below and above the temperature of nasal cavity.

摘要

背景与目的

对佐米曲普坦的热可逆黏附性鼻凝胶进行流变学评估,以确定稳态剪切行为和胶凝温度。热可逆黏附性聚合物成功地用于增加治疗化合物在鼻腔中的接触时间,并且它们导致药物通过鼻黏膜的渗透增强。

材料与方法

Pluronic(F127)和 Pluronic(F68)用作热可逆聚合物,与天然资源获得的黏附性聚合物(Zolmiriptan 抗偏头痛药物)联合使用,该药物来自 Cipla Ltd。使用具有圆锥-平板几何形状的 Brookfield R/S-CPS-PI 流变仪进行稳态剪切行为研究,并使用配备 spindle 和 Eurotherm 圆锥-平板几何形状的 Brookfield R/S plus Rheometer(Brookfield 黏度计有限公司,Harlow,Essex,英国)确定胶凝温度。

结果

稳态剪切行为研究表明,随着黏附性聚合物含量的增加,溶液的粘度以相同的方式开始增加。胶凝温度研究表明,随着配方中黏附性聚合物含量的增加,配方的胶凝温度随后降低。因此,从研究中得出结论,配方的胶凝温度受黏附性聚合物含量的影响。温度会增加配方的胶凝时间。

结论

上述研究表明,即使热可逆黏附性凝胶配方的组成有微小差异,也可能导致流变行为发生重大变化。尽管所有三种配方(L1、L2 和 L3)的胶凝温度均低于人体鼻腔温度,但它们在鼻腔温度以下和以上的不同温度下对不同剪切速率表现出不同的响应。

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