Garala Kevin, Joshi Parth, Shah Malay, Ramkishan A, Patel Jaydeep
Department of Pharmaceutics, Atmiya Institute of Pharmacy, Kalawad Road, Rajkot, Gujarat, India.
Int J Pharm Investig. 2013 Jan;3(1):29-41. doi: 10.4103/2230-973X.108961.
The present study was aimed to develop and optimize in situ gel for the treatment of periodontal disease.
Temperature-sensitive in situ gel containing 0.1% w/v Chlorhexidine hydrochloride was formulated by cold method using different polymers. Preliminary study was carried out to optimize different types and concentration of polymers such as Poloxamer 188, Poloxamer 407, Gellan gum, and Carbopol 934P. Central composite design was employed for optimization of the effect of independent variables such as Poloxamer 407 and Carbopol 934P on responses such as gelation temperature, spreadability, cumulative percentage release at 2 h, and time for 50% drug release (t50 %). Each formulations were evaluated for clarity, pH, gelation temperature, spreadability, drug content, in vitro drug release, t50 %, and cumulative percentage drug release at 2 h.
Results of evaluation parameters revealed that the drug release, gelation temperature was considerably decreased with increasing t50 % as the concentration of each polymer was increased. The desirability function was utilized to find out optimized formulation of the factorial design. Formulation F6 showed the highest overall desirability of 0.6283 and, therefore, this formulation was considered to be the optimized formulation. The % relative error was calculated, which showed that observed responses were in close agreement with the predicted values calculated from the generated regression equations.
The clarity, pH, drug content of all formulations was found to be satisfactory. Further, all the formulations showed sustained drug release for a period of 6 h, which satisfied to treat periodontal disease.
本研究旨在开发并优化用于治疗牙周疾病的原位凝胶。
采用不同聚合物通过冷法制备含0.1%（w/v）盐酸氯己定的温度敏感型原位凝胶。开展初步研究以优化不同类型和浓度的聚合物，如泊洛沙姆188、泊洛沙姆407、结冷胶和卡波姆934P。采用中心复合设计来优化自变量（如泊洛沙姆407和卡波姆934P）对响应变量（如胶凝温度、铺展性、2小时累积释放百分比和50%药物释放时间（t50%））的影响。对每种制剂的澄清度、pH值、胶凝温度、铺展性、药物含量、体外药物释放、t50%以及2小时药物累积释放百分比进行评估。
评估参数结果显示，随着每种聚合物浓度增加，药物释放和胶凝温度随t50%的增加而显著降低。利用合意性函数找出析因设计的优化制剂。制剂F6的总体合意性最高，为0.6283，因此该制剂被认为是优化制剂。计算了相对误差百分比，结果表明观察到的响应与根据生成的回归方程计算出的预测值非常吻合。
发现所有制剂的澄清度、pH值和药物含量均令人满意。此外，所有制剂均显示出6小时的持续药物释放，足以满足治疗牙周疾病的需求。
