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Titolo:
Effect of lipophilicity on in vivo iontophoretic delivery. II. beta-blockers
Autore:
Tashiro, Y; Sami, M; Shichibe, S; Kato, Y; Hayakawa, E; Itoh, K;
Indirizzi:
Kyowa Hakko Kogyo Co Ltd, Pharmaceut Res Inst, Drug Formulat Res Labs, Nagaizumi, Shizuoka 4118731, Japan Kyowa Hakko Kogyo Co Ltd Nagaizumi Shizuoka Japan 4118731 4118731, Japan
Titolo Testata:
BIOLOGICAL & PHARMACEUTICAL BULLETIN
fascicolo: 6, volume: 24, anno: 2001,
pagine: 671 - 677
SICI:
0918-6158(200106)24:6<671:EOLOIV>2.0.ZU;2-L
Fonte:
ISI
Lingua:
ENG
Soggetto:
TRANSDERMAL DELIVERY; TOPICAL APPLICATION; STRATUM-CORNEUM; BLOCKING-AGENTS; PH GRADIENT; HUMAN SKIN; IN-VIVO; ABSORPTION; PROPRANOLOL; PENETRATION;
Keywords:
transdermal delivery; iontophoresis; lipophilicity; beta-blocker;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
42
Recensione:
Indirizzi per estratti:
Indirizzo: Tashiro, Y Kyowa Hakko Kogyo Co Ltd, Pharmaceut Res Inst, Drug Formulat Res Labs, 1188 Shimotogari, Nagaizumi, Shizuoka 4118731, Japan Kyowa Hakko Kogyo Co Ltd 1188 Shimotogari Nagaizumi Shizuoka Japan 4118731
Citazione:
Y. Tashiro et al., "Effect of lipophilicity on in vivo iontophoretic delivery. II. beta-blockers", BIOL PHAR B, 24(6), 2001, pp. 671-677

Abstract

The objective of this study was to investigate the relationship between drug lipophilicity and the transdermal absorption processes in the iontophoretic delivery in vivo. Anodal iontophoresis of beta -blockers as model drugshaving different lipophilicity (atenolol, pindolol, metoprolol, acebutolol, oxprenolol and propranolol) was performed with rats (electrical current, 0.625 mA/cm(2); application period, 90 min), and the drug concentrations inskin, cutaneous vein and systemic vein were determined. Increasing the lipophilicity of beta -blockers caused a greater absorption into the skin. Exceptionally; it was found that pindolol had high skin absorption, irrespective of its hydrophilic nature, Further, the drug transfer rate from skin to cutaneous vein (R-SC) was evaluated from the arterio-venous plasma concentration difference of drug in the skin. Normalized R-SC by skin concentrationshowed a negative correlation with the logarithm of n-octanol/buffer partition coefficient (Log P, pH 7.4), suggesting the partitioning between stratum corneum and viable epidermis was a primary process to determine the transfer properties of beta -blockers to local blood circulation. Pindolol exhibited both high skin absorption and high transfer from skin to cutaneous vein. These characteristics of pindolol could be explained by the chemical structure, molecular size and hydrophilicity, These findings for pindolol should be valuable for the optimal design of drug candidates for iontophoretictransdermal delivery.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 31/03/20 alle ore 10:27:11