Nootan Pharmacy College, S. P. Vidyadham, Visnagar-384315, India.
Acta Pharm. 2011 Jun;61(2):203-16. doi: 10.2478/v10007-011-0017-3.
Glipizide is mainly absorbed in the proximal areas of the gastrointestinal tract. The purpose of this study was formulation and evaluation of mucoadhesive films to prolong the stay of drug in its absorption area. Glipizide was formulated in a mucoadhesive film that could be retained in the stomach for prolonged intervals. Polymeric films were designed with various compositions of hydroxypropyl cellulose and polyethylene glycol 400 (PEG 400). Properties of the mucoadhesive film such as tensile strength, percentage elongation, swelling index, moisture content, pH and viscosity of polymeric dispersion, film thickness, content uniformity and mucoadhesion in a simulated gastric environment were characterized. In addition, percentage drug retained in stomach mucosa was estimated using a simulated dynamic stomach system as a function of time. Increase in hydroxypropyl cellulose concentration resulted in a higher tensile strength and elongation at break, while increase in concentration of PEG 400 was reflected in a decrease in tensile strength and increase of elongation at break. Glipizide/hydroxypropyl cellulose/PEG 400 (2.5:1:0.5) (GF5) was found to be the optimal composition for a novel mucoadhesive stomach formulation that showed good peelability, relatively high swelling index, moderate tensile strength, and stayed on rat stomach mucosa up to 8 h. In vivo testing of the mucoadhesive films with glipizide demonstrated a potential hypoglycemic effect.
格列吡嗪主要在胃肠道的近端区域被吸收。本研究的目的是开发一种能延长药物在吸收部位停留时间的粘膜粘附性薄膜。我们将格列吡嗪制成一种能在胃中长时间滞留的粘膜粘附性薄膜。聚合物薄膜是由羟丙基纤维素和聚乙二醇 400（PEG 400）的不同比例组成的。研究了粘膜粘附性薄膜的一些特性，如拉伸强度、伸长率、溶胀指数、水分含量、聚合物分散体的 pH 值和粘度、薄膜厚度、含量均匀性和在模拟胃环境中的粘膜粘附性。此外，还使用模拟动态胃系统来估计药物在胃粘膜中的滞留率随时间的变化。随着羟丙基纤维素浓度的增加，拉伸强度和断裂伸长率也随之增加，而 PEG 400 浓度的增加则反映为拉伸强度的降低和断裂伸长率的增加。发现格列吡嗪/羟丙基纤维素/PEG 400（2.5:1:0.5）（GF5）是一种新型粘膜粘附性胃制剂的最佳组成，该制剂具有良好的剥离性、相对较高的溶胀指数、适中的拉伸强度，能在大鼠胃粘膜上停留长达 8 小时。格列吡嗪粘膜粘附性薄膜的体内测试显示出潜在的降血糖作用。
