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Biodistribution and Pharmacokinetics of O-Palmitoyl Tilisolol, a Lipophilic Prodrug of Tilisolol, after Intravenous Administration in Rats.
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- Kawakami Shigeru
- School of Pharmaceutical Sciences, Nagasaki University
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- Ohshima Nao
- Department of Hospital Pharmacy, Nagasaki University School of Medicine
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- Hirayama Ryu
- School of Pharmaceutical Sciences, Nagasaki University
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- Hirai Masami
- Department of Hospital Pharmacy, Nagasaki University School of Medicine
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- Kitahara Takashi
- Department of Hospital Pharmacy, Nagasaki University School of Medicine
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- Sakaeda Toshiyuki
- Department of Hospital Pharmacy, School of Medicine, Kobe University
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- Mukai Takahiro
- School of Pharmaceutical Sciences, Nagasaki University
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- Nishida Koyo
- School of Pharmaceutical Sciences, Nagasaki University
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- Nakamura Junzo
- School of Pharmaceutical Sciences, Nagasaki University
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- Nakashima Mikiro
- Department of Hospital Pharmacy, Nagasaki University School of Medicine
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- Sasaki Hitoshi
- Department of Hospital Pharmacy, Nagasaki University School of Medicine
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Description
The purpose of this study was to modify the biodistribution and pharmacokinetics of tilisolol, a β-blocker, using the palmitoyl prodrug approach. After intravenous administration of tilisolol and O-palmitoyl tilisolol in rats, drug concentrations were determined in blood, bile, urine, and several tissues. The concentration-time profiles of tilisolol and O-palmitoyl tilisolol were analyzed pharmacokinetically. The blood concentrations of O-palmitoyl tilisolol after intravenous administration of O-palmitoyl tilisolol were about 10-fold higher than those of tilisolol after intravenous administration of tilisolol. The biliary excretion rates of O-palmitoyl tilisolol and tilisolol after intravenous administration of O-palmitoyl tilisolol were about 10- to 100-fold larger than those of tilisolol after intravenous administration of tilisolol. In addition, the hepatic uptake clearance of O-palmitoyl tilisolol after intravenous administration of O-palmitoyl tilisolol was 3.6-fold higher than that of tilisolol after the intravenous administration of tilisolol. In the in vitro experiments, it was demonstrated that the distribution ratios between blood cells and plasma (blood/plasma) of O-palmitoyl tilisolol and tilisolol was 95.7 and 55.5%, respectively. These findings suggest that O-palmitoyl tilisolol exists as a binding form with biological components, especially blood cells, in systemic circulation. In conclusion, the palmitoyl prodrug approach is useful as a drug delivery system to deliver the parent drug to the liver.
Journal
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- Biological and Pharmaceutical Bulletin
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Biological and Pharmaceutical Bulletin 25 (8), 1072-1076, 2002
The Pharmaceutical Society of Japan
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Keywords
Details 詳細情報について
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- CRID
- 1390282679605047424
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- NII Article ID
- 110003638877
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- NII Book ID
- AA10885497
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- COI
- 1:CAS:528:DC%2BD38Xmt1SjtLY%3D
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- ISSN
- 13475215
- 09186158
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- HANDLE
- 10069/8376
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- NDL BIB ID
- 6243328
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- PubMed
- 12186412
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- Text Lang
- en
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- Article Type
- journal article
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- Data Source
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- JaLC
- IRDB
- NDL Search
- Crossref
- PubMed
- CiNii Articles
- OpenAIRE
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- Abstract License Flag
- Disallowed