Cuff G W, Combs A B, McGinity J W
Drug Dynamics Institute, College of Pharmacy, University of Texas, Austin 78712.
J Microencapsul. 1984 Jan-Mar;1(1):27-32. doi: 10.3109/02652048409031534.
The application of nylon microencapsulation as a drug delivery system inherently demands that the microencapsulated matrix should not cause degradation of the encapsulated drug. The presence of alkaline hexamethylenediamine (HMD) in the microcapsule core will affect the final pH of the microcapsules and may influence the stability of some drugs. To follow the pH within the microcapsule core during manufacture, pH indicators were encapsulated. The final pH was found to depend on the formulation used and could be controlled by the addition of acid. Several other variables affecting the nylon wall formation were examined to determine optimum processing conditions. Increased agitation produced a decrease in microcapsule size. This cause an increase in nylon weight recovered. The increased recovery of nylon was due in part to nylon formation over a larger surface area. Varying the amounts of HMD and sebacyl chloride (SC) used also affected the total weight of nylon formed. In general, more nylon is recovered as the level of each reactant increases. However, the molar ratio of HMD:SC determined the total amount of nylon formed when SC was present in excess.
尼龙微囊作为一种药物递送系统,其应用本质上要求微囊化基质不会导致被包裹药物的降解。微囊核心中存在碱性六亚甲基二胺(HMD)会影响微囊的最终pH值,并可能影响某些药物的稳定性。为了在制造过程中跟踪微囊核心内的pH值,将pH指示剂进行了包裹。发现最终pH值取决于所使用的配方,并且可以通过添加酸来控制。研究了影响尼龙壁形成的其他几个变量,以确定最佳加工条件。搅拌增加会导致微囊尺寸减小。这导致回收的尼龙重量增加。尼龙回收率的提高部分归因于在更大表面积上形成尼龙。改变HMD和癸二酰氯(SC)的用量也会影响形成的尼龙总重量。一般来说,随着每种反应物水平的增加,回收的尼龙更多。然而,当SC过量时,HMD:SC的摩尔比决定了形成的尼龙总量。