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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/05/08 11:15:32」(JST)
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English Journal
- Transport of timolol and tilisolol in rabbit corneal epithelium.
- Sakanaka K, Kawazu K, Nishida K, Nakamura J, Nakashima M, Nakamura T, Oshita A, Ichikawa N, Sasaki H.Author information Department of Hospital Pharmacy, Nagasaki University Hospital of Medicine and Dentistry, Nagasaki, Japan.AbstractThe purpose of this study is to characterize the transport of tilisolol and timolol through the corneal epithelium, which is believed to be a tight barrier of ocular drug absorption. Cultured normal rabbit corneal epithelial cells (RCEC) were used to investigate drug transport. Primary RCEC were seeded on a filter membrane of Transwell-COL insert coated with fibronectin and grown in Dulbecco's modified Eagle's medium/nutrient mixture F-12 with various supplements. Beta-blocker permeability through the RCEC layer was measured to assess the transcellular permeability coefficient (P(transcell)) in the absence or presence of inhibitors. The transcellular permeability of tilisolol was dependent on drug concentration although timolol showed no concentration dependency. Tilisolol flux from the apical to the basal side was larger than in the opposite direction although timolol showed no direction dependency. The transcellular permeability of tilisolol from the apical to the basal side was inhibited by sodium azide, tetraethylammonium, quinidine, taurocholic acid, guanidine and carnitine. Tilisolol had an active mechanism in uptake to the corneal epithelium, probably by the organic cation transporter family, although timolol predominantly permeated via passive diffusion. This RCEC system was useful to characterize the ocular permeation mechanism of drugs.
- Biological & pharmaceutical bulletin.Biol Pharm Bull.2006 Oct;29(10):2143-7.
- The purpose of this study is to characterize the transport of tilisolol and timolol through the corneal epithelium, which is believed to be a tight barrier of ocular drug absorption. Cultured normal rabbit corneal epithelial cells (RCEC) were used to investigate drug transport. Primary RCEC were see
- PMID 17015968
- One-side-coated insert as a unique ophthalmic drug delivery system.
- Sasaki H, Nagano T, Sakanaka K, Kawakami S, Nishida K, Nakamura J, Ichikawa N, Iwashita J, Nakamura T, Nakashima M.Author information Department of Hospital Pharmacy, Nagasaki University School of Medicine, 1-7-1 Sakamoto, Nagasaki 852-8501, Japan. sasaki@net.nagasaki-u.ac.jpAbstractWe newly prepared a unique one-side-coated insert that releases drug from only uncoated side. The purpose of this study is to determine whether ocular and systemic absorption of ophthalmic drug could be altered by an inserting direction of the insert in rabbit eyes. One-side-coated insert was prepared by attaching a polypropylene tape on the one side of the polymer disc of poly(2-hydroxypropyl methacrylate) (HPM) containing tilisolol as a model ophthalmic drug. The insert was applied in the lower conjunctival cul-de-sac of albino rabbits with the uncoated side facing bulbar conjunctiva/sclera (SC insert) or palpebral conjunctiva (CJ insert). At the adequate intervals, the tear fluid, plasma, aqueous humor, conjunctiva, and sclera were collected and the drug concentrations were determined by an HPLC. A release of tilisolol from the one-side-coated insert was twice slower than from the uncoated insert. Ocular application of the one-side-coated insert produced the constant concentrations of tilisolol in the tear fluid over 180 min. SC insert showed higher drug concentrations in the aqueous humor and sclera, and lower drug concentrations in the plasma and conjunctiva than CJ insert.The one-side-coated insert can alter the ocular and systemic absorption of drug by an inserting direction.
- Journal of controlled release : official journal of the Controlled Release Society.J Control Release.2003 Oct 30;92(3):241-7.
- We newly prepared a unique one-side-coated insert that releases drug from only uncoated side. The purpose of this study is to determine whether ocular and systemic absorption of ophthalmic drug could be altered by an inserting direction of the insert in rabbit eyes. One-side-coated insert was prepar
- PMID 14568405
- Biodistribution and pharmacokinetics of O-palmitoyl tilisolol, a lipophilic prodrug of tilisolol, after intravenous administration in rats.
- Kawakami S, Ohshima N, Hirayama R, Al MH, Kitahara T, Sakaeda T, Mukai T, Nishida K, Nakamura J, Nakashima M, Sasaki H.Author information School of Pharmaceutical Sciences, Nagasaki University, Japan. kawakami@net.nagasaki-u.ac.jpAbstractThe purpose of this study was to modify the biodistribution and pharmacokinetics of tilisolol, a beta-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.
- Biological & pharmaceutical bulletin.Biol Pharm Bull.2002 Aug;25(8):1072-6.
- The purpose of this study was to modify the biodistribution and pharmacokinetics of tilisolol, a beta-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
- PMID 12186412
Japanese Journal
- Transport of Timolol and Tilisolol in Rabbit Corneal Epithelium
- SAKANAKA Koji,KAWAZU Kouichi,NISHIDA Koyo,NAKAMURA Junzo,NAKASHIMA Mikiro,NAKAMURA Tadahiro,OSHITA Akemi,ICHIKAWA Nobuhiro,SASAKI Hitoshi
- Biological & pharmaceutical bulletin 29(10), 2143-2147, 2006-10-01
- … The purpose of this study is to characterize the transport of tilisolol and timolol through the corneal epithelium, which is believed to be a tight barrier of ocular drug absorption. … The transcellular permeability of tilisolol was dependent on drug concentration although timolol showed no concentration dependency. … Tilisolol flux from the apical to the basal side was larger than in the opposite direction although timolol showed no direction dependency. …
- NAID 110004810309
- Biodistribution and Pharmacokinetics of O-Palmitoyl Tilisolol, a Lipophilic Prodrug of Tilisolol, after Intravenous Administration in Rats
- KAWAKAMI Shigeru,OHSHIMA Nao,HIRAYAMA Ryu,HIRAI Masami,KITAHARA Takashi,SAKAEDA Toshiyuki,MUKAI Takahiro,NISHIDA Koyo,NAKAMURA Junzo,NAKASHIMA Mikiro,SASAKI Hitoshi
- Biological & pharmaceutical bulletin 25(8), 1072-1076, 2002-08-01
- … 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. …
- NAID 110003638877
Related Links
- 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 ...
- タイトル: Biodistribution and Pharmacokinetics of O-Palmitoyl Tilisolol, a Lipophilic Prodrug of Tilisolol, after Intravenous Administration in Rats 著者: Kawakami, Shigeru / Ohshima, Nao / Hirayama, Ryu / Hirai, Masami / Kitahara ...
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| リンク元 | 「チリソロール」 |
| 拡張検索 | 「tilisolol hydrochloride」 |