作者: Kira, Hitomi ; Utoguchi, Naoki ; Iino, Hayato ; Hashizaki, Kaname ; Fujino, Manami ; Fujii, Makiko ; Kohara, Shizuka ; Koizumi, Naoya ; Watanabe, Yoshiteru

Skin penetration amounts of a highly lipophilic drug, ufenamate, prepared in four oily vehicles, including white petrolatum (WP), liquid paraffin (LP), isopropyl myristate (IPM), and isocetyl stearate (ICS), were compared. Ufenamate was mixed in each vehicle at 5% and applied at a rate of 2 mg/cm² to intact, stripped, and delipidized Yucatan micropig skin. The amounts of ufenamate and IPM in the stratum corneum (SC), epidermis, and dermis were determined. The skin penetration amounts of ufenamate from liquid oils were significantly higher than those from WP; the amounts of ufenamate were in the order WP

2015-01-01·Biological & Pharmaceutical Bulletin4区 · 医学

Penetration of Ufenamate into Intact, Stripped, or Delipidized Skin Using Different Vehicles

4区 · 医学

Article

作者: Watanabe, Yoshiteru ; Iino, Hayato ; Fujii, Makiko ; Koizumi, Naoya ; Fujino, Manami

The purpose of this study was to clarify the effect of skin condition on skin penetration of the very high lipophilic drug, ufenamate (UF). UF was applied to stripped or delipidized skin using liquid paraffin (LP) or purified water containing polysorbate 80 at a dose of 2 µL/cm(2). We found that UF penetration into intact and stripped skin using a water vehicle was respectively 5 and 10 times higher than that using LP. UF is freely soluble in oil and insoluble in water; thus, activity in water is higher than that in LP. Therefore, it is useful to use a water-based vehicle for both intact sites and those with defective stratum corneum (SC). Conversely, we found that delipidization of SC decreased the penetration of UF significantly with both LP and water, and the amount measured in the epidermis was 1 µg/cm(2) with both vehicles. This indicates that UF is not suitable for so-called "dry skin." This study revealed clinically relevant differences in the penetration of UF into intact, stripped, or delipidized skin conditions.

2011-06-01·Journal of Drug Targeting3区 · 医学

Evaluation of dextran-flufenamic acid ester as a polymeric colon-specific prodrug of flufenamic acid, an anti-inflammatory drug, for chronotherapy

3区 · 医学

Article

作者: In Ho Kim ; Yunjin Jung ; Jeong Hyun Yoon ; Young Hee Shin ; Young Mi Kim ; Jeongyun Kim ; Yonghyun Lee

Dextran-flufenamic acid ester (Dex-FFA) with varied degree of substitution (DS) was prepared by imidazolide method. Dex-FFA was stable in pH 1.2 or pH 6.8 buffer. The depolymerization degree of Dex-FFA by dextranase decreased as DS increased. Dex-FFA with DS of 13 or 20 released FFA up to 70% or 21% of the dose, respectively, on 24 h-incubation with the 10% cecal contents. FFA was liberated up to 29% of the dose on 24 h-incubation of dextranase pre-treated Dex-FFA with the homogenates of the upper intestine, whereas no FFA was detected devoid of dextranse-pretreatment. Upon oral administration of Dex-FFA (DS 13, 20 mg equivalent of FFA/kg) or FFA (10 mg/kg) to rats, t(max) for FFA with Dex-FFA administration delayed approximately 6 h compared with that of free FFA administration, while C(max) for FFA was similar. The plasma level for FFA became greater around 6 h after administration of Dex-FFA than free FFA and it was maintained throughout the period of 24 h-experiment. Dex-FFA markedly attenuated gastric ulcerogenicity of FFA. Taken together, Dex-FFA could be useful as a colon-specific prodrug which possesses anti-inflammatory properties and offers opportunities as a chronotherapeutic approach for the treatment of arthritis.

100 项与乌芬那酯相关的药物交易

登录后查看更多信息

外链

KEGG	Wiki	ATC	Drug Bank
D01823	乌芬那酯	M01AG03	-

研发状态

10 条最早获批的记录,

后查看更多信息

适应症	国家/地区	公司	日期
急性湿疹	日本	Viatris Pharmaceutical GK	1983-02-01
慢性湿疹	日本	Viatris Pharmaceutical GK	1983-02-01
口周皮炎	日本	Viatris Pharmaceutical GK	1983-02-01
酒渣鼻样皮炎	日本	Viatris Pharmaceutical GK	1983-02-01
特应性皮炎	日本	Mitsubishi Tanabe Pharma Corp.	1982-10-07
接触性皮炎	日本	Mitsubishi Tanabe Pharma Corp.	1982-10-07
脂溢性皮炎	日本	Mitsubishi Tanabe Pharma Corp.	1982-10-07
带状疱疹	日本	Mitsubishi Tanabe Pharma Corp.	1982-10-07
湿疹	中国	沈阳抗生素厂	-