DEVELOPMENT OF TRETINOIN AQUEOUS GEL FOR TREATMENT OF POSTINFLAMMATORY HYPERPIGMENTATION AND SENILE LENTIGINES

开发用于治疗炎症后色素沉着和老年雀斑的维A酸水凝胶

• 批准号: 15590124
• 负责人: AOYAMA Takao
• 金额: $ 2.24万
• 依托单位: TOKYO UNIVERSITY OF SCIENCE (2004)The University of Tokyo (2003)
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Scientific Research (C)
• 财政年份: 2003
• 资助国家: 日本
• 起止时间: 2003 至 2004
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/en/grant/KAKENHI-PROJECT-15590124/
• 关键词: Tretinoin; Aqueous gel; Skin hyperpigmentation; Cyclodextrin; Inclusion compound; トレチノイン; シロクデキストリン

All-trans retinoic acid(atRA), one of the retinoids, is effective in the treatment for skin hyperpigmentation and acne in dermatology. However, atRA has several drawbacks such as irritation power, poor stability for the air, light and heat, and insoluble water. It is well known that cyclodextrins and their derivatives form inclusion compounds with many kinds of drugs and improve the physicochemical properties of the drugs. The aim of this study was to investigate inclusion compound formation of atRA with hydroxypropyl β-cyclodextrin (HP-β-CD) for solubilization and stabilization of atRA.Inclusion compound was prepared by evaporation of HP-β-CD-atRA ethanol solution at the 1:1 molar ratio. Power X-ray diffractometry, fourier transform infrared spectroscopy(FTIR), differential scanning calorimetry(DSC), solubility test and photostability test were performed to evaluate inclusion compound formation.No diffraction peaks due to atRA crystals were observed on the XRD pattern in the evaporated sample. In the FTIR spectrum, the asymmetric stretching band of the C=C groups in atRA were shifted to higher wavenumber (1600-1604 cm^<-1>). DSC curves of evaporated sample indicated that new endothermic peak at 213.2℃ due to decomposition of HP-β-CD-atRA complex. Aqueous solubility and photostability of atRA in evaporated sample were improved. These results indicated that complexation was occurred between HP-β-CD and atRA in solid and solution.

全反式维甲酸（all-transretinoicacid，atRA）是维甲酸类化合物之一，在皮肤科中对治疗皮肤色素沉着和痤疮有效。然而，atRA具有几个缺点，例如刺激力，对空气、光和热的稳定性差，以及不溶于水。众所周知，环糊精及其衍生物与许多药物形成包合物，改善药物的理化性质。为了研究羟丙基β-环糊精（HP-β-CD）对atRA的增溶和稳定作用，将HP-β-CD与atRA以1：1的摩尔比在乙醇溶液中蒸发制备包合物。采用X射线粉末衍射、傅立叶变换红外光谱（FTIR）、差示扫描量热法（DSC）、溶解性试验和光稳定性试验等方法对包合物的形成进行了研究。在FTIR光谱中，atRA中C=C基团的不对称伸缩带向更高的波数（1600-1604 cm-2）移动<-1>。蒸发样品的DSC曲线表明，HP-β-CD-atRA复合物在213.2℃处有一个新的吸热峰。蒸发样品中atRA的水溶性和光稳定性得到改善。结果表明，HP-β-CD与atRA在固溶体中均发生了络合作用。

项目成果

Combined Therapy Using Q‐Switched Ruby Laser and Bleaching Treatment With Tretinoin and Hydroquinone for Acquired Dermal Melanocytosis

• DOI: 10.1046/j.1524-4725.2003.29291.x
• 发表时间: 2003-10
• 期刊: Dermatologic Surgery
• 影响因子: 2.4
• 作者: Akira Momosawa;K. Yoshimura;G. Uchida;Katsujiro Sato;E. Aiba;Daisuke Matsumoto;Hisayo Yamaoka;S. Mihara;K. Tsukamoto;K. Harii;T. Aoyama;T. Iga

Combined therapy using Q-switched ruby laser and bleaching treatment with tretinoin and hydroquinone for acquired.

使用Q开关红宝石激光和使用维A酸和氢醌进行漂白治疗的联合治疗。

• 发表时间: 2003
• 期刊: Dermatol.Surg. 29
• 作者: Momasawa A;Yoshimura K;Aoyama T;et al.
• 通讯作者: et al.

Clinical trial of bleaching treatment with 10 % all-trans retinal gel.

临床％20试验％20的％20漂白％20治疗％20与％2010％20％％20全反式％20视网膜％20凝胶。

• 发表时间: 2003
• 期刊: Dermatol.Surg. 29(2)
• 作者: Yoshimura K;Momosawa A;Aiba E;Sato K;Matsumoto D;Mitoma Y;Harii K;Aoyama T;Iga T
• 通讯作者: Iga T

Clinical trial of bleaching treatment with 10% all-Tran retinal gel.

临床%20试验%20%20漂白%20​​治疗%20与%2010%%20all-Tran%20视网膜%20凝胶。

• 发表时间: 2003
• 期刊: Dermatol.Surg. 29
• 作者: Yoshimura K;Aoyama T;et al.
• 通讯作者: et al.

Yoshimura K, Aoyama T, et al.: "Clinical trial of bleaching treatment with 10% all-trans retinal gel"Dermatol.Surg.. 29・2. 155-160 (2003)

Yoshimura K、Aoyama T等人：“10％全反式视网膜凝胶漂白治疗的临床试验”Dermatol.Surg..29・2(2003)。