کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2485890 | 1114369 | 2007 | 10 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Relative in Vitro Efficacy of the Phosphate Binders Lanthanum Carbonate and Sevelamer Hydrochloride
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Relative in Vitro Efficacy of the Phosphate Binders Lanthanum Carbonate and Sevelamer Hydrochloride Relative in Vitro Efficacy of the Phosphate Binders Lanthanum Carbonate and Sevelamer Hydrochloride](/preview/png/2485890.png)
چکیده انگلیسی
The high tablet burden and poor compliance associated with phosphateâbinding drugs has led to a search for more potent agents. In vitroâbinding studies were performed on the recently introduced binder, lanthanum carbonate (LC; Fosrenol®), to compare its phosphateâbinding affinity with sevelamer hydrochloride (SH; Renagelâ¢). Langmuir equilibrium binding affinities (K1) for LC and SH were established using different phosphorus (5-100 mM) and binder (134-670 mg per 50 mL) concentrations at pH 3-7, with or without salts of bile acids present (30 mM). At all pH levels, LC had a higher binding affinity for phosphate than SH. For LC, K1 was 6.1â±â1.0 mMâ1 and was independent of pH. For SH, K1 was pH dependent, being 1.5â±â0.8 mMâ1 at pH 5-7 and 0.025â±â0.002 mMâ1 at pH 3, that is, >200 times lower than for LC. In the presence of 30 mM bile salts, SH lost 50% of its phosphate, whereas no displacement of phosphate occurred for LC. These findings indicate that LC binds phosphate more effectively than SH across the pH range encountered in the gastrointestinal tract, and has a lower propensity for bound phosphate to be displaced by competing anions in the intestine. © 2007 WileyâLiss, Inc. and the American Pharmacists Association J Pharm Sci 96: 2818-2827, 2007
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 96, Issue 10, October 2007, Pages 2818-2827
Journal: Journal of Pharmaceutical Sciences - Volume 96, Issue 10, October 2007, Pages 2818-2827
نویسندگان
Valerie Autissier, Stephen J.P. Damment, Richard A. Henderson,