Development and evaluation of a buccal bioadhesive system for smoking cessation therapy
Development and evaluation of a buccal bioadhesive system for smoking cessation therapy
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DOI：
10.1691/ph.2007.4.6144
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发表时间：
2007-04-01
期刊：
影响因子：
1.6
通讯作者：
Kumar, G.
中科院分区：
文献类型：
--
作者：
Garg, S.;Kumar, G.
本研究的目的是开发一种用于戒烟治疗的尼古丁氢酒石酸双层口腔生物粘附膜制剂，包括生物粘附药物层和背衬层，其以预定速率释放药物4小时。使用各种生物粘附聚合物制备制剂，并评估物理参数，如可剥离性、柔韧性、柔软度、生物粘附强度、拉伸强度、分散时间和药物参数，如厚度、溶胀、含量均匀性、水蒸气渗透性和药物释放。基于这些参数，选择含有羟丙基甲基纤维素和聚卡波非作为生物粘附聚合物的制剂N-2作为优化制剂。该制剂显示出适当的粘附力，并在前 15 分钟内初始突释 40% 的药物，随后以特征方式释放 80% 的药物，直至 4 小时；这是所需的应用时间。这种释放模式对于遭受紧急渴望的患者是有益的。通过湿气渗透性测试对薄膜的背衬层进行了研究，观察到透过单层薄膜的水分百分比远高于通过双层薄膜的水分百分比，这意味着背衬层可以防止药物被唾液冲走。
The objective of the present study was to develop a bilayered buccal bioadhesive film formulation of nicotine hydrogen tartrate for smoking cessation therapy, comprising a bioadhesive drug layer and a backing layer, which releases the drug at a pre-determined rate for a period of 4 h. Formulations were prepared using various bioadhesive polymers and were evaluated for physical parameters like peelability, flexibility, softness, bioadhesive strength, tensile strength, dispersion time and pharmaceutical parameters such as thickness, swelling, content uniformity, water vapour permeability and drug release. Based on these parameters formulation N-2, containing hydroxypropyl methylcellulose and polycarbophil as the bioadhesive polymers, was selected as the optimized formulation. The formulation showed suitable adhesion and an initial burst release of 40% drug in first 15 min followed by a total 80% drug release in a characteristic manner until 4 h; which is the desired time of application. This release pattern is beneficial for patients suffering from emergent cravings. Backing layers of the films were studied by a moisture vapor permeability test and it was observed that the percentage of moisture which permeated through single layered films was much higher than through bilayered films implying that a backing layer would prevent washing out of drug by the saliva.