Wan L S, Heng P W, Chia C G
Department of Pharmacy, National University of Singapore.
J Microencapsul. 1993 Jan-Mar;10(1):11-23. doi: 10.3109/02652049309015308.
An aqueous spray-drying process was used to coat theophylline particles with a cellulose polymer, sodium carboxymethylcellulose (NaCMC) or hydroxypropylmethylcellulose (HPMC). Effect of a plasticizer, citric acid, was studied. Strength of cast films have a direct relationship to the dissolution T50% values of the respective spray-dried products. With varying plasticizer concentrations, changes in interaction between plasticizer and polymer, and in size of crystallized drug crystals, were observed with HPMC films. The plasticizer content also affected the films of NaCMC by bringing about a change in the form and arrangement of the drug. X-ray diffraction analyses of the different spray-dried products revealed a possibility of the predominance of different crystal forms. Spherical spray-dried microcapsules of NaCMC were formed with a 20-30% w/w plasticizer content. With HPMC, as plasticizer concentration was increased there was a corresponding increase in mean size of the spray-dried products. In terms of drug release and formation of spherical particles, a plasticizer concentration of 30% w/w was found to be suitable for both HPMC and NaCMC.
采用水相喷雾干燥工艺,用纤维素聚合物、羧甲基纤维素钠(NaCMC)或羟丙基甲基纤维素(HPMC)包覆茶碱颗粒。研究了增塑剂柠檬酸的作用。流延膜的强度与相应喷雾干燥产品的溶出T50%值直接相关。对于HPMC膜,随着增塑剂浓度的变化,观察到增塑剂与聚合物之间相互作用以及结晶药物晶体尺寸的变化。增塑剂含量也通过改变药物的形态和排列来影响NaCMC膜。对不同喷雾干燥产品的X射线衍射分析表明,可能存在不同晶型占主导的情况。当增塑剂含量为20 - 30% w/w时,形成了NaCMC球形喷雾干燥微胶囊。对于HPMC,随着增塑剂浓度增加,喷雾干燥产品的平均尺寸相应增大。就药物释放和球形颗粒的形成而言,发现30% w/w的增塑剂浓度对HPMC和NaCMC均适用。