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不同种属动物皮肤体外研究 0.1% 盐酸奥替尼啶和 2% 2-苯氧乙醇(奥替尼啶®)复方制剂的经皮渗透。

The percutaneous permeation of a combination of 0.1% octenidine dihydrochloride and 2% 2-phenoxyethanol (octenisept®) through skin of different species in vitro.

机构信息

Department of Pharmacology, Toxicology and Pharmacy, University of Veterinary Medicine Hannover, Foundation, Buenteweg 17, 30559 Hannover, Germany.

出版信息

BMC Vet Res. 2011 Aug 11;7:44. doi: 10.1186/1746-6148-7-44.

Abstract

BACKGROUND

A water based combination of 0.1% octenidine dihydrochloride and 2% 2 - phenoxyethanol is registered in many European countries as an antiseptic solution (octenisept®) for topical treatment with high antimicrobial activity for human use, but octenidine based products have not been registered for veterinary use yet. The aim of the present study was to investigate whether octenidine dihydrochloride or 2 -phenoxyethanol, the two main components of this disinfectant, permeate through animal skin in vitro. Therefore, permeation studies were conducted using Franz-type diffusion cells. 2 ml of the test compound were applied onto 1.77 cm2 split skin of cats, dogs, cows and horses. To simulate wounded skin, cattle skin was treated with adhesive tapes 100 times, as well. Up to an incubation time of 28 hours samples of the acceptor chamber were taken and were analysed by UV-HPLC. Using the method of the external standard, the apparent permeability coefficient, the flux Jmax, and the recovery were calculated. Furthermore, the residues of both components in the skin samples were determined after completion of the diffusion experiment.

RESULTS

After 28 hours no octenidine dihydrochloride was found in the receptor chamber of intact skin samples, while 2.7% of the topical applied octenidine dihydrochloride permeated through barrier disrupted cattle skin. 2 - phenoxyethanol permeated through all skin samples with the highest permeability in equine, followed by bovine, canine to feline skin. Furthermore, both components were found in the stratum corneum and the dermis of all split skin samples with different amounts in the examined species.

CONCLUSION

For 2-phenoxyethanol the systemic impact of the high absorption rate and a potential toxicological risk have to be investigated in further studies. Due to its low absorption rates through the skin, octenidine dihydrochloride is suitable for superficial skin treatment in the examined species.

摘要

背景

一种 0.1%盐酸奥替尼啶和 2%2-苯氧乙醇的水基混合物在许多欧洲国家被注册为一种具有高抗菌活性的局部用消毒剂溶液(奥替尼啶®),可用于人体,但基于奥替尼啶的产品尚未在兽医领域注册。本研究的目的是研究这种消毒剂的两种主要成分盐酸奥替尼啶和 2-苯氧乙醇是否会穿透动物皮肤。因此,进行了渗透研究使用 Franz 型扩散池。将 2 ml 测试化合物应用于猫、狗、牛和马的 1.77 cm2 分裂皮上。为了模拟创伤皮肤,牛皮用胶带处理了 100 次。在 28 小时的孵育时间内,从接受室中取出样品,并通过 UV-HPLC 进行分析。使用外标法,计算表观渗透系数、通量 Jmax 和回收率。此外,在扩散实验完成后,测定了两种成分在皮肤样品中的残留量。

结果

28 小时后,完整皮肤样品的受体室中未发现盐酸奥替尼啶,而经破坏的牛皮肤穿透了 2.7%的局部应用盐酸奥替尼啶。2-苯氧乙醇通过所有皮肤样品渗透,在马皮中渗透性最高,其次是牛皮、犬皮和猫皮。此外,两种成分都存在于所有分裂皮肤样品的角质层和真皮中,在不同的检查物种中存在不同的数量。

结论

对于 2-苯氧乙醇,必须在进一步的研究中调查其高吸收率的全身影响和潜在的毒理学风险。由于其通过皮肤的吸收率低,盐酸奥替尼啶适合在检查的物种中进行浅表皮肤治疗。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af1e/3180697/c2b2e12bf75b/1746-6148-7-44-1.jpg

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