Tsujiyama T, Suzuki N, Kawata M, Uchida T, Goto S
Pharma Research Laboratories, Hoechst Japan Limited, Saitama.
J Pharmacobiodyn. 1989 Jun;12(6):311-23. doi: 10.1248/bpb1978.12.311.
Hydroxy propyl cellulose (HPC)-ethyl cellulose (EC) microcapsules containing piretanide were newly by a solvent evaporation technique and their slow-release properties were evaluated on dissolution properties in vitro and pharmacokinetic and pharmacodynamic parameters in beagle dogs. The dissolution behavior of piretanide from the microcapsules in dissolution media of pH 1.2-6.8 and the plasma piretanide level in beagle dogs varied dependently on the contents of HPC and EC. As compared with ordinary piretanide tablet on the market, the HPC-EC10 (5:3) microcapsule showed the controlled dissolution behavior, sustained plasma piretanide level, almost same AUC (area under curve), slow urinary piretanide excretion, decreased urine excretion maximum rate, and no difference in the cumulative urine volume and cumulative urinary electrolytes (Na+, K+, Cl-) excretion. HPC-EC microcapsules containing piretanide sufficiently satisfied the conditions which slow-release preparations must have.
采用溶剂蒸发技术新制备了含吡咯他尼的羟丙基纤维素（HPC）-乙基纤维素（EC）微胶囊，并通过体外溶出特性以及比格犬的药代动力学和药效学参数对其缓释性能进行了评价。吡咯他尼从微胶囊在pH 1.2 - 6.8溶出介质中的溶出行为以及比格犬血浆中吡咯他尼水平随HPC和EC含量的变化而有所不同。与市售普通吡咯他尼片剂相比，HPC - EC10（5:3）微胶囊表现出可控的溶出行为、血浆中吡咯他尼水平持续稳定、曲线下面积（AUC）几乎相同、吡咯他尼尿排泄缓慢、尿排泄最大速率降低，且累积尿量和累积尿电解质（Na +、K +、Cl -）排泄无差异。含吡咯他尼的HPC - EC微胶囊充分满足了缓释制剂必须具备的条件。
