Patil Sachin, Sharma Sameer, Nimbalkar Anagha, Pawar Atmaram
Department of Pharmaceutics, Poona College of Pharmacy, Bharati Vidyapeeth Deemed University, Erandwane, Maharashtra State, India.
Drug Dev Ind Pharm. 2006 Mar;32(3):315-26. doi: 10.1080/03639040500518930.
The aim of the present study was to obtain cross-linked calcium-gellan beads containing diclofenac sodium as model drug, using full 3(3) factorial design. Drug quantity, pH of cross-linking solution, and speed of agitation were selected as variables for factorial design. The resultant beads were evaluated by scanning electron microscopy (SEM), percent yield, entrapment efficiency, micromeritic properties, swelling and drug release studies. The drug-loaded beads were spherical with size range of 0.85-1.8 mm. Percent yield and entrapment efficiency of various batches were in the range of 86.48-98.28% w/w and 72.52-92.74% w/w, respectively. Calcium-gellan beads containing diclofenac sodium showed pH-dependent swelling and drug release properties. Swelling and drug release were significantly higher in pH 7.4 phosphate buffer than 0.1N HCl. The swelling ratio for beads was up to 22 and 3 for phosphate buffer and 0.1N HCl, respectively. Cumulative diclofenac sodium release from calcium-gellan beads was 12-35% in 0.1N HCl within 2 h, whereas complete drug release was observed within 3-4 h in pH 7.4 phosphate buffer.
本研究的目的是采用全3（3）析因设计，制备含双氯芬酸钠作为模型药物的交联钙-结冷胶珠。药物用量、交联溶液的pH值和搅拌速度被选为析因设计的变量。通过扫描电子显微镜（SEM）、产率百分比、包封率、粉体学性质、溶胀和药物释放研究对所得珠子进行评价。载药珠子呈球形，尺寸范围为0.85 - 1.8毫米。各批次的产率百分比和包封率分别在86.48 - 98.28% w/w和72.52 - 92.74% w/w范围内。含双氯芬酸钠的钙-结冷胶珠表现出pH依赖性溶胀和药物释放特性。在pH 7.4磷酸盐缓冲液中的溶胀和药物释放明显高于0.1N盐酸。珠子在磷酸盐缓冲液和0.1N盐酸中的溶胀率分别高达22和3。双氯芬酸钠从钙-结冷胶珠中的累积释放率在0.1N盐酸中2小时内为12 - 35%，而在pH 7.4磷酸盐缓冲液中3 - 4小时内观察到药物完全释放。
