JPS59163319A - Antimycotic agent - Google Patents

Abstract

PURPOSE:To provide a low-toxic antimycotic agent effective to the mycete of mammal, especially to dermatophyte, having higher activity than griseofulvin, and containing dihydrotanshinone I known as a component of TANSHIN (root of Salvia miltiorrhiza) as an active component. CONSTITUTION:The objective antimycotic agent contains dihydrotanshinone I of formula as an active component. Dihydrotanshinone has higher activity than griseofulvin in terms of the minimum inhibitory concentration to mycete. The titled antimycotic agent is useful for the prevention and remedy of diseases caused especially by dermatophyte (e.g. superficial trichophytosis capitis, vesicobullous trichophytosis, eczema marginatum, etc.) by oral administration or external application.

Description

[Detailed description of the invention] The present invention relates to a novel antifungal agent.

The present inventors have conducted extensive research on the components of Danshen, and have completed the present invention by discovering that among the many components of Danshen, dihydrotandinone I exhibits excellent antifungal activity.

That is, the present invention is an antifungal agent containing dihydrocundinone I as an active ingredient.

Dihydrocundinone I used in the present invention is already known as a component of Danshen, and its structure is as follows: The antifungal agent of the present invention is usually administered orally or externally. administered to mammals, including humans, especially diseases caused by dermatophytes (e.g., superficial cephalic vigilantism, vesicular patchy albinism, obstinacy, white-snoring feet, and hidrotic albinism). It is used for the prevention and treatment of conditions such as nail baldness, baldness, and albinism. The dosage forms include oral preparations such as tablets, capsules, granules, and powders, and external preparations such as ointments. These preparations are mixed with appropriate pharmacologically acceptable excipients, carriers, diluents, etc., and manufactured according to known methods.

The dosage of dihydrocundinone I may vary depending on the subject's disease, symptoms, body weight, gender, etc., but for example, when administered orally to adult humans, the dose is 250 to 500 μ per day, divided into one or several doses. do.

The bactericidal activity of dihydrotandinone I and the control Tera lyseofulvin against various (skin) fungi was reported in Journal of Antibiotics, Vol. 28 (1970).
The results of the investigation according to the method described in 2010, page 131 are consistent with those shown in table m1, and the minimum inhibitory concentration of dihydrocundinone I is superior to that of theofulvin.

Table 1 Note that dihydrotandinone is a component of Danshen, and the extract of Danshen itself is commonly used orally as a herbal medicine, so its low toxicity has already been established.

Reference Example Danshen (Hong Kong market product 2.5 to 4) was extracted with methanol 201, the methanol extract obtained was shaken with a mixture of ether and water, and the ether layer was mixed with 7 ml. Dihydrocundinone 1158Ing was obtained by recolumn chromatography.

Example 1. (capsules) Dihydrotandinone 1250r, lactose 119.4r.

After weighing 5.62 kg of magnesium stearate, the mixed powder was mixed uniformly, and 875 kuna of the mixed powder was filled into Jf62 hard gelatin capsules to form capsules.

Example 2. (Tablet) 5.1? After weighing each dihydrotandinone 1
, lactose, corn starch 82ft evenly mixed. Cut 8 f of corn starch into 10 pieces using hot water.
% corn starch, add the mixture of the three components mentioned above, and prepare granules by a general wet granulation method. This granule) is mixed with magnesium stearate,
Compress the tablets with a tablet machine using a % I Q nm punch and MIA
840'9 tablets.

Example 3 (External ointment) A hydrophobic ointment base (melting point 45°C) containing white petrolatum, white wax, and olive oil was liquefied by heating, and dihydrocundinone 1 was formulated at 1% a degree. , apply to skin fungal disease areas.

Patent applicant: Sawai Pharmaceutical Co., Ltd. Procedural amendment (voluntary) Date of Showa: September 1A, 2015 Director-General of the Japan Patent Office 1 Indication of the case: 1982 Patent Application No. 037060 2, Title of the invention: Antifungal agent 3 Person making the amendment Relationship to the incident: Mr. Junto Utsuide Name: Sawai? ! ! Yakuhin Co., Ltd. 6 Number of inventions increased by amendment 7, subject of amendment 3 Detailed explanation of the invention column (1) Chemical formula 7 on page 2 of the specification Correct as follows 0 [ ( 2) "Washino" on page 3 of the same book? ” Corrected.

(3) Doso, page 4, line 1, ``1 dihydrotandinone'', followed by ``technical'' τ added, 0 (Jun Circular 4th negative, line 19, Vcr starch) and Amebon ``
Corrected to ``Tengua.''

(5) On page 5 of the same book, in the third line, ``nori'' is added after ``starch''.

Claims (1)

[Claims] Antifungal agent containing dihydrotandinone I as an active ingredient