Oestradiol Release from Self-setting Apatitic Bone Cement Responsive to Plasma-calcium Level in Ovariectomized Rats, and its Physicochemical Mechanism

Author:

Otsuka Makoto1,Yoneoka Kazuki1,Matsuda Yoshihisa1,Fox Jeffrey L2,Higuchi William I2,Sugiyama Yuichi3

Affiliation:

1. Department of Pharmaceutical Technology, Kobe Pharmaceutical University, Higashi-Nada, Kobe 658

2. Department of Pharmaceutics and Pharmaceutical Chemistry, University of Utah, Salt Lake City, Utah 84112, USA

3. Department of Biopharmaceutics, University of Tokyo, Bunkyo, Tokyo 113, Japan

Abstract

Abstract The effect of plasma calcium levels on the release of oestradiol from a self-setting apatite bone cement containing 0.5% oestradiol was investigated in ovariectomized rats. The profiles of in-vitro release from the cements in simulated body fluid containing 0, 5 or 10 mg calcium per 100 mL indicated that the rate of release of oestradiol decreased with increasing calcium concentration in the dissolution media. After subcutaneous implantation of oestradiol-loaded cement in healthy and vitamin D-deficient rats, oestradiol release in diseased rats with low plasma calcium levels was significantly higher than that in healthy rats. These results suggest that in-vitro release of oestradiol from apatite bone cement was dependent on the calcium concentration in the buffer and that the in-vivo release of oestradiol from apatite bone cement was dependent on plasma calcium levels.

Publisher

Oxford University Press (OUP)

Subject

Pharmaceutical Science,Pharmacology

Reference21 articles.

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