transdermal preparation

Abstract

Disclosed is a safe, transdermal absorption preparation useful in the treatment of fungal infections, having excellent skin permeability and strong antifungal activity, and greatly contributing to a patient's quality of life. The disclosed transdermal absorption preparation contains 4-{3-[4-(3-{4-[amino (imino) methyl] phenoxy} propyl)-1-piperidinyl] propoxy} benzamidine, or a salt thereof, and a transdermal absorption enhancer.

Description

technical field [0001] The present invention relates to transdermal absorption preparation of aromatic amidine derivatives effective in treating fungal infection. Background technique [0002] Severe deep mycoses such as invasive candidiasis are often fatal. In the past, it was believed that the main defense mechanism of the host body against fungi such as Candida was the non-specific immunity of neutrophils. When this defense mechanism is functioning properly, the risk of infection with the fungus is minimal. However, in recent years, due to the increase in the number of patients suffering from underlying diseases that lower the immune function of the body such as malignant tumors (especially hematopoietic malignant tumors such as acute leukemia or malignant lymphoma) and AIDS, frequent use of anticancer agents or immunosuppressants, Heavy use of antibiotics or steroid hormones, long-term use of central venous hypertrophy or venous catheterization, etc., increase the risk...

AI Technical Summary

Problems solved by technology

However, the octanol / water partition coefficient of compound A in the pH range of 3 to 9 is less than 0.05, which is very different from the partition coefficient (100 to 1000) of general compounds with high membrane permeability

Compound A tends to be difficult to permeate through membranes, and it is difficult to provide a transdermal preparation of Compound A or a salt thereof having sufficient transdermal absorbability for exerting pharmacological effects

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