Samanta Arnab, Ghosal Saroj K
Division of Pharmaceutics, Department of Pharmaceutical Technology, Jadavpur University, Jadavpur, Kolkata, PIN 700 032, INDIA.
Acta Pol Pharm. 2004 Sep-Oct;61(5):343-9.
Ocular inserts were developed with prolonged release of drug and minimum swelling within cul-de-sac using ciprofloxacin (CPF) hydrochloride as a model drug. The ocular inserts were fahricated with sodium alginate films loaded with drug and then treated with calcium chloride. A 4% w/v solution of calcium chloride and an exposure of 15 s to this solution was found to be the optimum treatment combination of inserts. Four types of inserts were produced: type-I contained CPF hydrochloride and alginate, type-II contained CPF crystals and alginate, type-III contained CPF hydrochloride inalginate and hydroxypropylmethylcellulose (HPMC) matrix and type-IV contained CPF crystals entrapped inalginate and HPMC matrix. In vitro release profile of drug from the inserts followed Higuchi and first-order kinetic models. Longer duration for 90% drug release were obtained from types-II and IV inserts than from types I and III, although type III had a longer duration than type-I inserts. In vivo studies were carried out in rabbit eyes by measuring the tear concentrations against time. From the pharmacokinctic parameters obtained types II and IV were found to prolong the duration of action more than 2 days while types I and II inserts the duration of action lasted for about 1.5 days.
以盐酸环丙沙星（CPF）为模型药物，开发了一种眼用植入剂，该植入剂能在泪囊内实现药物的长效释放且肿胀最小。眼用植入剂由负载药物的海藻酸钠薄膜制成，然后用氯化钙处理。发现4%（w/v）的氯化钙溶液以及将植入剂在此溶液中暴露15秒是植入剂的最佳处理组合。制备了四种类型的植入剂：I型包含盐酸环丙沙星和海藻酸盐，II型包含环丙沙星晶体和海藻酸盐，III型包含盐酸环丙沙星在海藻酸盐和羟丙基甲基纤维素（HPMC）基质中，IV型包含包裹在海藻酸盐和HPMC基质中的环丙沙星晶体。植入剂中药物的体外释放曲线符合Higuchi模型和一级动力学模型。II型和IV型植入剂的药物释放90%所需时间比I型和III型更长，尽管III型的持续时间比I型植入剂长。通过测量兔眼泪液浓度随时间的变化进行体内研究。从获得的药代动力学参数来看，II型和IV型植入剂的作用持续时间延长超过2天，而I型和III型植入剂的作用持续时间约为1.5天。
