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The Influence of Formula Concentration on the Absorption of Darbepoetin Alfa after Subcutaneous Administration

Tomonori Tayama1*, Kazuki Kawakami1, Hirotaka Takama1, Daisuke Nakashima1, Hideji Tanaka1, Takayuki Tsuji2, Tatsuo Yamamoto3, Sakuo Hoshi4 and Tadao Akizawa5
1Development Division, Kyowa Hakko Kirin Company Ltd., 1-6-1 Ohtemachi, Chiyoda-ku, Tokyo, 100-8185, Japan
21st Department of Internal Medicine, Hamamatsu University School of Medicine, 1-20-1 Handayama, Higashi-ku, Hamamatsu-shi, Shizuoka, 431-3192, Japan
3Faculty of Health Promotional Sciences, Department of Health and Nutritional Science, Hamamatsu University. 1230 Miyakoda-cho, Kita-ku, Hamamatsu-shi, shizuoka, 431-2102, Japan
4Pharmaco-Business Innovation, Graduate School of Pharmaceutical Sciences, Faculty of Pharmaceutical Science, The University of Tokyo. 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-8654, Japan
5Department of Nephrology, Showa University School of Medicine, 1-5-8 Hatanodai, Shinagawa-ku, Tokyo 142-8666, Japan
*Corresponding author:
Dr. Tomonori Tayama, Development Division,
Kyowa Hakko Kirin Company Ltd., 1-6-1 Ohtemachi, Chiyoda-ku, Tokyo,
100-8185, Japan,
Tel: +81-3-3282-0983,
Fax: +81-3-3282-0335,
E-mail: tomonori.tayama@kyowa-kirin.co.jp
Received November 10, 2009; Accepted December 21, 2009; Published December 22, 2009
Citation: Tayama T, Kawakami K, Takama H, Nakashima D, Tanaka H, et al. (2010) The Influence of Formula Concentration on the Absorption of Darbepoetin Alfa after Subcutaneous Administration. J Bioequiv Availab 2: 001-005. doi: 10.4172/jbb.1000021
Copyright:© 2010 Tayama T, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
Abstract

Darbepoetin alfa (DA) is a hyperglycosylated analog of recombinant human erythropoietin (rHuEPO) that stimulates red blood cell production. The aim of this study is to investigate the influence of formula concentration on the absorption of DA after subcutaneous administration. Three separate studies were performed to assess the bioequivalence of four different formula concentrations of DA, 100 μg/ml as reference concentration, comparing with 10, 30, 200 μg/ml as test concentration, by the same dosage (60 μg). The mean values of the pharmacokinetic parameters were similar after subcutaneous administration in each study. The 90% confidence intervals for logtransformed Cmax and AUC0-t were within the bioequivalence criteria (0.8-1.25) in each study. In previous studies, the effect in absorption process of insulin was correlated to the formula concentration, the formula concentration of human growth hormone might not affected its absorption. The molecular weight is thought to be causally related to these results. The absorption rate of DA is not affected by its formula concentration because DA, which has relatively higher molecular weight (36,000 Da), is primarily absorbed slowly via lymph vessels regardless of its concentration.

 
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