JPS58162514A - Gel pharmaceutical preparation for external use - Google Patents

Abstract

PURPOSE:An agent for external use, effective for eczema marginatum, tinea unguium, vesicular tinea, etc., well absorbable from the skin, preventing side effect by internal use, comprising griseofulvin, triglyceride of middle chain fatty acid, pure water, and a carboxyvinyl polymer. CONSTITUTION:A base consisting of 1-25wt% trigyceride of 6-12C fatty acid, 70-90wt% pure water and 0.5-3wt% carboxyvinyl polymer is blended with griseofulvin to give an agent for external use in the form of a gel cream. The agent for external use is prepared by adding the carboxyvinyl polymer to a mixture of griseofulvin, triglyceride of fatty acid and pure water, followed by gelatinizing it. The agent has improved stability, and is observed to have griseofulvin transfer to the skin not inferior to an agent for internal use even by applying it to the affected part as an agent for external use.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a gel cream containing griseofulvin as an active ingredient.

Griseofulvin is a compound represented by the structural formula and is known to exhibit antifungal activity against dermatophytes such as Trichophyton, Microsporium, and Epidermophyton. Currently, griseofulvin is widely used as an oral agent, and
It has been confirmed that it can cause symptoms such as nail whitening disorder, headache, and ginseng measles. In addition, griseofulvin is difficult to dissolve in bases that can be used for external preparations, and even when it is present in suspension in commonly used water-soluble and fat-soluble bases, it is poorly absorbed through the skin and cannot be used for the intended purpose. bTherapeutic effect is not obtained.

Therefore, the present inventor has conducted extensive research in an attempt to resolve these drawbacks of griseofulvin, and as a result, it has been found that even when applied locally as an external preparation, griseofulvin transfers into the skin as well as an internal preparation. At the same time, they discovered an external preparation that eliminates the side effects of internal administration, and completed the present invention.

That is, the present invention provides griseofulvin, carbon number 4~/J
This is a gel cream containing medium-chain fatty acid triglyceride, purified water, and h-ruboxyvinyl polymer.

Examples of medium-chain fatty acid triglycerides having 4 to J carbon atoms include caproic acid triglyceride, capric acid triglyceride, and caprylic/capric acid triglyceride.
# can be used. As the carboxyvinyl polymer, for example, t is Hebis Wako IOJμo41. i
os (trade name of crosslinked acrylic acid polymer manufactured by Wako Pure Chemical Industries, Ltd.) can be used.

The blending amount of each base is determined based on the usability, dispersibility, stability, etc. of medium-chain fatty acid triglyceride with a carbon number of t to lλ/-J
It is preferable to mix 3% by weight of purified water, 70% by weight of purified water to 70% by weight of carboxyvinyl polymer, and 0.3% to 3% by weight of carboxyvinyl polymer.

The gel cream of the present invention can be prepared by adding a carboxyvinyl polymer to a mixture of griseofulvin, medium-chain fatty acid triglyceride, and purified water to form a gel. At this time, griseofulvin, medium chain fatty acid triglyceride, and purified water may be mixed in any order.

Depending on the amount of saliva, we added glycerin, propylene glycol, etc., nonionic surfactants such as poliotei, ethylene sorbitan fatty acid ester, and absorption aids such as diisopropyl adipate! Lower alcohols and/or acetone may be added to provide a refreshing sensation. Either of these may be added to the mixture before adding the carboxyvinyl polymer.

The cream of the present invention not only has excellent stability, but also has a high utilization rate, which is clear from the high skin transfer rate shown in Experimental Example/0 Experimental Example/ This Invention The utilization rate of the griseofulvin gel cream shown in Experimental Example/ was compared with the case of oral administration of griseofulvini.
The animals were coated with the cream of the cape, sacrificed 6 hours later, and the griseofulvin in the skin of the Ilk was quantified. For heavy oral administration, griseofulvin was suspended in medium-chain fatty acid triglyceride (concentration was 6%). ), the offspring were killed for 6 hours, the abdominal skin was cut at 0°, and the griseofulvin in the skin was quantified and suspended in triglyceride light (Ilt, Section 6). Examples are shown below for more detailed explanation, but the present invention is not limited thereto.

Example/ Griseofulvin 3F was suspended in glycerin and purified water 741.1. f, polyoxyethylene sorbitan fat acid ester JP, medium chain fatty acid 1. Guu,,i,(.Dp
Japan, Seishinsha,) J.

Add and mix to emulsify. diisopropanolamine θ,
Add and mix the carboxyvinyl polymer/
, /i was added to form a gel to obtain a griseofulvin gel cream.

Example cogriseofulvin! , glycerin jF [11! Cloudy, purified water 6θ・de, ethanolco J, JP・nrubitan fat-ester-0! t, medium chain fatty acid triglyceride (miglyol 1icR).

Dynamite Nobel Co., Ltd. 1ml J, jFt added 1m containing 11. Converting to 0. JP,
Diimprovir adipate was added and mixed, and carboxyvinyl polymer/RiP was added and gelled to obtain a griseofulvin gel cream.

Claims (1)

[Claims] Gel cream agent containing griseofulvin, medium-chain fatty acid triglyceride with 1 to 1 carbon atoms, purified water, and carboxyvinyl polymer and having t1W/P characteristics.