Evaluation of the Carrier Potential for the Lipid Dispersion System with Lipophilic Compound
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- Hosokawa Toshihito
- Pharmaceutical Research Institute, Kyowa Hakko Kogyo Co., Ltd.
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- Yamauchi Masahiro
- Pharmaceutical Research Institute, Kyowa Hakko Kogyo Co., Ltd.
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- Yamamoto Yoshihiko
- Pharmaceutical Research Institute, Kyowa Hakko Kogyo Co., Ltd.
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- Iwata Kenji
- Pharmaceutical Research Institute, Kyowa Hakko Kogyo Co., Ltd.
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- Nakamura Akimasa
- Pharmaceutical Research Institute, Kyowa Hakko Kogyo Co., Ltd.
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- Kato Yasuki
- Pharmaceutical Research Institute, Kyowa Hakko Kogyo Co., Ltd.
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Abstract
KW-3902 (a newly synthesized adenosine A1-receptor antagonist) has potent diuretic and renal protective activities and was formulated in lipid dispersion systems, i.e., lipid emulsions and liposomes. The objective of the present study was to evaluate the carrier potential of these lipid dispersion systems, which is explained here as the ability of the formulation to retain the drug in its dispersed phase. The relative affinity of the drug to the formulation, Kf/b, was defined as a parameter in order to assess the performance of the formulations and was obtained from the in vitro blood component binding study. The results indicated that KW-3902 showed higher relative affinity to the liposome formulation than to the lipid emulsion. Moreover, the total amount of drug retained in the dispersion system depended on both Kf/b and the dosing volume. The usefulness of the parameter, Kf/b, was discussed as an indicator for a carrier potential to understand the properties of the formulations.
Journal
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- Biological and Pharmaceutical Bulletin
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Biological and Pharmaceutical Bulletin 26 (7), 994-999, 2003
The Pharmaceutical Society of Japan
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Details 詳細情報について
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- CRID
- 1390282679601614464
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- NII Article ID
- 110003608561
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- NII Book ID
- AA10885497
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- COI
- 1:CAS:528:DC%2BD3sXmsFWntr4%3D
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- ISSN
- 13475215
- 09186158
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- NDL BIB ID
- 6583546
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- PubMed
- 12843625
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- Text Lang
- en
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- Data Source
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- Abstract License Flag
- Disallowed