Department of Pharmacology, Manipal College of Pharmaceutical Sciences, Manipal, Karnataka, India.
Indian J Pharmacol. 2008 Aug;40(4):170-4. doi: 10.4103/0253-7613.43164.
To develop topical gel preparations of astemizole and terfenadine and to investigate the actions of the gels on the healing of incision and excision wounds in male albino rats.
Gels containing 1% astemizole, with varying concentrations of carbopol 934 (polymer), were prepared. Similarly, 1% terfenadine gels were made. The formulations were evaluated for release rate and stability. Incision and excision wounds were inflicted on male albino rats under ketamine anesthesia, taking aseptic precautions. The animals were divided into two groups. They were given a topical application of either astemizole or terfenadine gel, at a dose of 100 mg per wound, once daily, for 10 days in the case of incision wounds and till the time of complete closure in the case of excision wounds. On the 11(th) day, breaking strength of the incision wound was measured. In the excision wound model, wound closure rate, epithelization time, scar features and hydroxyproline content of scar tissue were studied from the day of wounding till the day of the scab falling off, with no residual raw area.
Gels prepared using 0.8% carbopol 934 and 1% of drug in gel base were found to be stable. The gels of astemizole and terfenadine significantly (P < 0.05) promoted the phases of healing such as collagenation (in incision wounds), wound contraction and epithelization (in excision wounds).
The gels of astemizole and terfenadine might play an important role in wound management program.
研制阿替美唑和特非那定的局部凝胶制剂，并研究凝胶对雄性白化大鼠切口和切除伤口愈合的作用。
制备含有 1%阿替美唑、不同浓度卡波姆 934（聚合物）的凝胶。同样，也制备了 1%特非那定凝胶。对制剂的释放率和稳定性进行了评价。在氯胺酮麻醉下，雄性白化大鼠在无菌条件下进行切口和切除伤口。将动物分为两组。在切口伤口中，每天一次给予 100mg 阿替美唑或特非那定凝胶局部应用，持续 10 天；在切除伤口中，给予局部应用直至伤口完全闭合。第 11 天，测量切口伤口的断裂强度。在切除伤口模型中，从伤口形成之日起至结痂脱落之日止，研究伤口闭合率、上皮化时间、瘢痕特征和瘢痕组织中的羟脯氨酸含量，无残留的原始创面。
使用 0.8%卡波姆 934 和 1%药物的凝胶稳定。阿替美唑和特非那定凝胶显著（P <0.05）促进了胶原形成（切口伤口）、伤口收缩和上皮化（切除伤口）等愈合阶段。
阿替美唑和特非那定凝胶可能在伤口管理方案中发挥重要作用。
