Percutaneously absorbable preparation

Details Percutaneously absorbable preparation Percutaneously absorbable preparation

1996-03-15

1998-05-05

Venkat, Jyothsan

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Matrices

514183, 514414, 514469, 514944, A61K 906

Patent

active

057470693

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

This application is a 371 of PCT/JP94/01282 filed Aug. 4, 1994.
This invention relates to a percutaneously absorbable preparation containing a drug and a percutaneous absorption accelerator comprising a monoglyceride and a fatty acid.
More particularly, this invention relates to a percutaneously absorbable preparation containing a monoglyceride as well as a fatty acid for enhanced cutaneous penetration of an insoluble (insoluble or sparingly soluble in water) drug.


BACKGROUND

For the purpose of improving the percutaneous absorption of an insoluble drug, it is common practice to employ a solubilizer such as Polyethylene Glycol 400 or propylene glycol.
It is also known that monoglycerides of medium-chain fatty acids assist in percutaneous absorption. For example, JP Kokai 63-227520 employs monolaurin, that is 1-monolauroylrac-glycerol, as a percutaneous absorption accelerator.
However, the problem remains that even the use of cutaneous penetration aids such as said solubilizers and monoglycerides of medium-length fatty acids generally does not insure a sufficient percutaneous delivery of drug which are inherently more or less insoluble in water.
There accordingly exists a demand for the development of dosage forms providing for still improved percutaneous absorption.


DISCLOSURE OF INVENTION

After much research for solving the above problem and even to their own surprise, the inventors of this invention discovered that a dramatic enhancement of cutaneous penetration can be achieved by causing a fatty acid to be present in conjunction with a monoglyceride and have perfected this invention.
This invention is now described in further detail.
The percutaneously absorbable preparation of this invention is characterized by containing a drug and a percutaneous absorption accelerator comprising a monoglyceride and a fatty acid.
The preferred monoglyceride for use in this preparation can be selected from among those monoglycerides which are conventionally employed in the pharmaceutical field, thus including glycerides of medium-chain or long-chain fatty acids, whether saturated or unsaturated, typically monocaprin, monolaurin, monomyristin, monopalmitin, monostearin, monoolein, etc., and mixtures thereof. In particular, glycerides of saturated or unsaturated fatty acids containing 10 to 20 carbon atoms are preferred, and monocaprin, monolaurin and monoolein are especially useful.
As preferred examples of the fatty acid for use in this invention, those fatty acids which are conventionally employed in the pharmaceutical field can be mentioned. Typically, medium-chain and long-chain fatty acids, whether saturated or unsaturated, such as capric acid, lauric acid, myristic acid, palmitic acid, stearic acid, etc., and mixtures thereof can be mentioned. Particularly preferred are saturated C.sub.12 -C.sub.18 fatty acids, among which stearic acid is especially useful.
Where necessary, the percutaneously absorbable preparation of this invention may further contain the common additives which are generally used in the formulation of drug products, typically an excipient, a coloring agent, a solubilizer, and so on.
As to the solubilizer mentioned above, in particular, hydrophilic solvents such as polyhydric alcohols, e.g. propylene glycol, polyethylene glycol, glycerin, etc., and monohydric alcohols, e.g. ethyl alcohol, isopropyl alcohol, etc., including mixtures thereof can be employed.
Furthermore, long-chain or cyclic esters such as isopropyl myristate, diethyl sebacate, diisopropyl adipate, propylene carbonate, etc. can also be mentioned.
The percutaneously absorbable preparation of this invention can be provided in the form of an ordinary ointment. The ointment base that can be used includes vegetable or animal waxes (e.g. bleached beeswax, carnauba wax, beeswax, etc.), paraffins (e.g. paraffin, liquid paraffin, etc.), and petrolatums (e.g. white petrolatum etc.), among others. These bases can be used in the form of a mixture. Moreover, this preparation can be provided in the form of an ordinary cream,

REFERENCES:
JP 63-227520 (1988).

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