Niwano Y, Koga H, Kanai K, Hamaguchi H, Yamaguchi H
Pharmaceutical Research Center, Nihon Nohyaku Co., Ltd., Osaka, Japan.
Arzneimittelforschung. 1996 Feb;46(2):218-23.
The wound healing effect of cream preparations of lanoconazole (CAS 101530-10-3, NND-318), an antimycotic imidazole compound, was examined using an excisional open skin-wound model produced on the back of rats. The rapid decrease in the size of wounded areas showed that 0.5% and 1% lanoconazole creams accelerated spontaneous healing. The effectiveness was almost similar to that of an ointment containing 5% deproteinized calf blood extract (DCBE), a wound healing agent on the market. In contrast, neither 1% clotrimazole cream nor 1% bifonazole cream, both of which are imidazole antimycotics, showed an accelerative effect. The wound healing effect of lanoconazole was further confirmed by histological evaluation; a thicker and more cellular granulation tissue was formed, and epidermal regeneration was more stimulated by lanoconazole than by non-treatment or vehicle alone. The effect of lanoconazole on the formation of granulation tissue in rats was also studied using a cotton pellet implantation method. Lanoconazole accelerated the formation of this tissue in terms of dry weight in a dose dependent manner (0.5-4 mg/pellet), and collagen content and angiogenesis also increased in the stimulated tissue, indicating that these accompany the compound-induced acceleration of tissue formation. These results suggest that lanoconazole has a distinctive wound healing effect which is a feature no other imidazole antimycotic is known to possess to date.
使用在大鼠背部制作的切除性开放性皮肤伤口模型,研究了抗真菌咪唑化合物氯康唑(CAS 101530-10-3,NND-318)乳膏制剂的伤口愈合效果。伤口面积的迅速减小表明,0.5%和1%的氯康唑乳膏可加速自发愈合。其效果与市售伤口愈合剂、含5%脱蛋白小牛血提取物(DCBE)的软膏几乎相似。相比之下,同为咪唑类抗真菌药的1%克霉唑乳膏和1%联苯苄唑乳膏均未显示出加速作用。通过组织学评估进一步证实了氯康唑的伤口愈合效果;形成了更厚且细胞更多的肉芽组织,与未治疗或仅使用赋形剂相比,氯康唑对表皮再生的刺激作用更强。还使用棉球植入法研究了氯康唑对大鼠肉芽组织形成的影响。氯康唑以剂量依赖方式(0.5 - 4mg/棉球)加速了该组织的干重形成,并且在受刺激组织中胶原蛋白含量和血管生成也增加,表明这些与化合物诱导的组织形成加速相伴。这些结果表明,氯康唑具有独特的伤口愈合效果,这是迄今为止已知的其他咪唑类抗真菌药所不具备的特征。