首页> 外国专利> ORAL PHARMACEUTICAL FORMULATION AS AQUEOUS SUSPENSION OF MICROCAPSULES FOR MODIFIED AMOXICILLIN RELEASE

ORAL PHARMACEUTICAL FORMULATION AS AQUEOUS SUSPENSION OF MICROCAPSULES FOR MODIFIED AMOXICILLIN RELEASE

机译:口服药物制剂作为微胶囊水悬浮液用于改良阿莫西林释放的研究

摘要

An orally administered aqueous suspension comprises microcapsules (MC's), each having a core of amoxicillin (A) coated with a release-controlling film (I). (I) consists of (a) film-forming, water-insoluble cellulose derivative, nitrogen-containing polymer and/or plasticizer; (b) hydrophilic polymer; or (c) film-forming polymer, water-soluble polymer, plasticizer and optionally surfactant and/or lubricant. In an orally administered aqueous suspension of MC's, each MC comprises a core of amoxicillin (A) coated with a release-controlling film (I) such that the liquid phase is (or becomes) saturated with (A) in contact with the MC's. (I) consists of : (a) components comprising; (i) film-forming polymer(s) (P1) insoluble in gastro-intestinal fluids, selected from water-insoluble cellulose derivative(s), forming 50-80 (preferably 50-80) wt. % of (I); (ii) nitrogen-containing polymer(s) (P2) selected from polyacrylamide, poly-N-vinyl-amide and/or poly-N-vinyl-lactam, forming 2-20 (preferably 4-15) wt. % of (I); (iii) plasticizer(s) selected from glycerol esters, phthalates, citrates, sebacates, cetyl alcohol esters and castor oil, forming 2-20 (preferably 4-15) wt. % of (I); and (iv) one or more of anionic and/or nonionic surfactants and/or lubricants, forming 2-20 (preferably 4-15) wt. % of (I); (b) components comprising; (i) hydrophilic polymer(s) carrying groups ionized at neutral pH (preferably cellulose derivatives); and (ii) hydrophobic compound(s) (other than (a)); or optionally (c) components comprising; (i) film-forming polymer(s) (P1) insoluble in gastro-intestinal fluids; (ii) water-soluble polymer(s); (iii) plasticizer(s); and (iv) surfactant(s) and/or lubricant(s) (preferably anionic and/or nonionic surfactants). Independent claims are included for: (1) a medicament comprising a suspension as above; and (2) a medicament comprising a kit for the production of a suspension as above, comprising the (A)-containing MC's, optionally (A) in immediate release (non-coated) form and the liquid phase (or at least some of its ingredients and/or instructions for its preparation).
机译:口服给药的水悬浮液包含微囊(MC),每个微囊具有被释放控制膜(I)包裹的阿莫西林(A)的核心。 (I)由(a)成膜的水不溶性纤维素衍生物,含氮聚合物和/或增塑剂组成; (b)亲水性聚合物; (c)成膜聚合物,水溶性聚合物,增塑剂和任选的表面活性剂和/或润滑剂。在口服给予的MC的水性悬浮液中,每个MC包含涂有释放控制膜(I)的阿莫西林(A)的芯,使得液相被与MC接触的(A)饱和(或变得饱和)。 (I)包括:(a)组成; (i)不溶于肠胃液的成膜聚合物(P1),其选自不溶于水的纤维素衍生物,形成50-80(优选50-80)重量%。 (I)的百分比; (ii)选自聚丙烯酰胺,聚-N-乙烯基酰胺和/或聚-N-乙烯基-内酰胺的含氮聚合物(P2),形成2-20重量%(优选4-15重量%)。 (I)的百分比; (iii)选自甘油酯,邻苯二甲酸酯,柠檬酸酯,癸二酸酯,鲸蜡醇酯和蓖麻油的增塑剂,形成2-20重量%(优选4-15重量%)。 (I)的百分比; (iv)一种或多种阴离子和/或非离子表面活性剂和/或润滑剂,形成2-20wt。%(优选4-15wt。%)。 (I)的百分比; (b)组成部分; (i)带有在中性pH下离子化的基团的亲水性聚合物(最好是纤维素衍生物); (ii)疏水性化合物((a)除外);或(c)包含以下成分的成分: (i)不溶于肠胃液的成膜聚合物(P1); (ii)水溶性聚合物; (iii)增塑剂; (iv)表面活性剂和/或润滑剂(优选阴离子和/或非离子表面活性剂)。包括以下方面的独立权利要求:(1)包含上述悬浮液的药物; (2)药物,其包含用于制备上述悬浮液的试剂盒,该试剂盒包含(A)含MC的MC,任选地(A)以立即释放(非包衣的)形式和液相(或至少一些其成分和/或制备说明)。

著录项

  • 公开/公告号FR2843880B1

    专利类型

  • 公开/公告日2006-06-02

    原文格式PDF

  • 申请/专利权人 FLAMEL TECHNOLOGIES;

    申请/专利号FR20020010846

  • 申请日2002-09-02

  • 分类号A61K9/10;A61K9/16;A61K9/50;A61K31/43;A61P31/04;

  • 国家 FR

  • 入库时间 2022-08-21 21:17:40

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