Patel Vipul P, Damasiya Harshad M, Kapupara Pankaj, Ashara Kalpesh C
School of Pharmacy, RK University, Tramba, Rajkot, Gujarat,India.
Folia Med (Plovdiv). 2019 Jun 1;61(2):266-276. doi: 10.2478/folmed-2018-0073.
The in-situ gel-forming polymeric formulations offer sustained and prolonged action in comparison to conventional drug delivery systems.
To formulate and evaluate in situ vaginal gel of clotrimazole.
Poloxamer 407 (20%) was slowly added to freezing water (5°C) with constant stirring. The prepared dispersion was refrigerated for 5 h, the different concentrations of polymers were added for preliminary batches. Differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR) were performed for clotrimazole-excipients compatibility study. The final batch was prepared and evaluated for physicochemical parameters, in vitro clotrimazole release, in vitro antifungal activity, and in vivo vaginal tissue irritation test.
The compatibility study showed no chemical interaction between clotrimazole and excipients used. The evaluation parameters showed that clotrimazole release was in the range of 8 to 10 h, gelling temperature was in the range of 27-35°C, gelling time was in the range of 28-34 sec, pH was in the range of 4.4-4.8, and viscosities were in the range of 16.4-182.6 cP (solution form) and 10,500-20,756 cP (gel form). The zone of inhibitions for clotrimazole pure drug, the marketed vaginal gel of clotrimazole, and optimized gel formulation was 9.15±0.75 mm, 14.35±1.12 mm, and 18.85±1.56 mm, respectively (p < 0.0001, q = 5.98). An optimized gel formulation was not irritant to vaginal tissue.
It was possible to formulate effective in situ vaginal gel for control release action of clotrimazole.
IIC.
与传统药物递送系统相比，原位凝胶形成聚合物制剂具有持续和延长的作用。
制备并评价克霉唑原位阴道凝胶。
在持续搅拌下，将泊洛沙姆407（20%）缓慢加入冷冻水（5℃）中。将制得的分散体冷藏5小时，加入不同浓度的聚合物用于初步批次。进行差示扫描量热法（DSC）和傅里叶变换红外光谱法（FTIR）以研究克霉唑与辅料的相容性。制备最终批次并对其进行理化参数、体外克霉唑释放、体外抗真菌活性和体内阴道组织刺激性试验的评价。
相容性研究表明克霉唑与所用辅料之间无化学相互作用。评价参数显示克霉唑释放时间为8至10小时，胶凝温度为27 - 35℃，胶凝时间为28 - 34秒，pH值为4.4 - 4.8，粘度在溶液形式下为16.4 - 182.6厘泊，在凝胶形式下为10500 - 20756厘泊。克霉唑纯药物、市售克霉唑阴道凝胶和优化凝胶制剂的抑菌圈分别为9.15±0.75毫米、14.35±1.12毫米和18.85±1.56毫米（p < 0.0001，q = 5.98）。优化的凝胶制剂对阴道组织无刺激性。
有可能制备出用于克霉唑控释作用的有效原位阴道凝胶。
IIC。
