首页> 外国专利> Use of a controlled release losartan oral dosage form, to decrease the inter individual gap of standard deviation of maximum concentration of the losartan, independent of administration of losartan before or after the meals

Use of a controlled release losartan oral dosage form, to decrease the inter individual gap of standard deviation of maximum concentration of the losartan, independent of administration of losartan before or after the meals

机译:控释氯沙坦口服剂型的使用,以减少氯沙坦最大浓度的标准偏差的个体间差距,与饭前或饭后服用洛沙坦无关

摘要

Use of a oral dosage form (A) comprising a coating or a matrix containing losartan (I) and allowing controlled release of (I), before or after meals, to decrease the inter individual gap of standard deviation of maximum concentration of (I) (C max), which results in a low variability of effectiveness of (A), when compared to a dosage form with immediate release of (I). Independent claims are included for: (1) a modified release oral dosage form (A) of losartan (I), comprising micro-units (II) containing (I), where (II) has an average diameter of 50-1000 (preferably 150-500) mu m, and carboxylic acid metabolite of (I) (E3174) has a specific plasma profile (i.e. C18h(i)=C18h (preferably 2.0 C18h(i)=C18h=C max(i)/2), where C18h is the plasma concentration of E3174 after 18 hour of administering (A), C18h(i) is the plasma concentration of E3174 obtained after administering immediate release form, C max is the maximum plasma concentration of E3174 after the administration of (A) and C max(i) is the maximum plasma concentration of E3174 obtained after administering immediate release form); and (2) a micro particle.
机译:包含剂型或基质的口服剂型(A)的使用,该涂层或基质含有losartan(I)并允许在饭前或饭后控释(I),以减少(I)最大浓度的标准偏差之间的个体差异(C max),与立即释放(I)的剂型相比,导致(A)有效性的可变性低。包括以下方面的独立权利要求:(1)氯沙坦(I)的缓释口服剂型(A),其包含含(I)的微单元(II),其中(II)的平均直径为50-1000(优选(I)(E3174)的羧酸代谢物具有150-500)μm的特定血浆分布(即C18h(i)= C18h(最好是2.0 C18h(i)= C18h = C max(i)/ 2),其中C18h是给药(A)18小时后E3174的血浆浓度,C18h(i)是给药即释形式后获得的E3174的血浆浓度,C max是给药(A)后E3174的最大血浆浓度Cmax(i)是立即释放形式给药后得到的E3174的最大血浆浓度。 (2)微粒。

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