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    • 10. 发明授权
    • Controlled release formulation and method
    • 控释制剂及方法
    • US4505890A
    • 1985-03-19
    • US509493
    • 1983-06-30
    • Nemichand B. JainMahendra R. Patel
    • Nemichand B. JainMahendra R. Patel
    • A61K9/20A61K9/28A61K31/40A61K9/24A61K9/22A61K9/62
    • A61K31/40A61K9/2054A61K9/2866
    • A controlled release pharmaceutical formulation which undergoes substantially zero order release of active drug is provided, preferably in the form of a coated tablet, containing a core portion from which the angiotensin converting enzyme inhibitor (S)-1-[3-(benzoylthio)-2-methyl-1-oxopropyl]-L-proline is slowly released over a controlled length of time. The core also includes one or more hydrocolloid gelling agents having a viscosity of within the range of from about 8000 to about 100,00 centipoises in 2% solution at 20.degree. C., such as hydroxypropylmethyl cellulose and/or methyl cellulose, one or more inert fillers or excipients, one or more lubricants, and optionally one or more anti-adherents such as silicon dioxide and water. The above-described core is coated with a conventional pharmaceutical coating composition. A method of using such controlled release formulations in treating hypertension is also provided.
    • 提供经受基本上零级释放活性药物的控释药物制剂,优选以包衣核心部分的包衣片剂的形式,血管紧张素转化酶抑制剂(S)-1- [3-(苯甲酰硫基) - 2-甲基-1-氧代丙基] -L-脯氨酸在受控的时间内缓慢释放。 核心还包括一种或多种水解胶体凝胶剂,其在20℃的2%溶液中具有约8000至约100,00厘泊范围内的粘度,例如羟丙基甲基纤维素和/或甲基纤维素,一种或多种 惰性填料或赋形剂,一种或多种润滑剂,以及任选的一种或多种抗附着物如二氧化硅和水。 上述核心涂覆有常规的药物涂料组合物。 还提供了使用这种控释制剂治疗高血压的方法。