萘普生缓释片及人体药代动力学研究

A Study on Naproxen Sustained Release Tablets and Its Human Pharmaceutics

萘普生（Ｎａｐｒｃｘｅｎ）缓释片是以羟丙基甲基纤维素（ＨＰＭＣ）为亲的水骨架，加稀释剂、润滑剂压制亲的水凝胶骨架片．该片在体外１２ｈ累积释放量大于９０％，其释放行为（０～８ｈ）可用Ｈｉｇｕｃｈｉ方程描述；人体内血药浓度数据符合一级吸收单室模型，动力学参数Ｋ，Ｃｍａｘ，ｔｍａｘ和ＡｌＣ０—∞分别为０．０２５ｈ－１，２８．２６×１０－５ｍｏｌ／Ｌ，３．７２ｈ和１４．９１×１０－３ｍｏｌ·ｈ／Ｌ．

Sustained release tablets of naproxen(1) were prepared with hydroxypropyl Me cellulose as hydrophilic matrix and with the addition of dilluents and lubricant.The amount of naproxen from I dissolved after 12 h of in vitro release test was >90%.The drug release pattern(0～8) in vitro of I was best described by Higuchi equation.The plasma drug level dada best fit the one compartment model with first order absorption The pharmacokinetic parameters K,C max ,t max and AUC 0～∞ of I were 0 025 h -1 ,28 26×10 5 mol/L,3 72 h and 14 91×10 -3 mol/L respectively.