Pharmaceutical composition

Abstract

A pharmaceutical composition for topical administration, including, as the pharmaceutically active component, at least 5% by weight, based on the total weight of the composition of a piperidinopyrimidine derivative or a pharmaceutically acceptable salt thereof; an acid in an amount to completely solubilise the piperidinopyrimidine derivative or a pharmaceutically acceptable salt thereof; a solvent composition including at least two of water, a lower alcohol and a co-solvent selected from one or more of the group consisting of aromatic and polyhydric alcohols; wherein when the co-solvent includes propylene glycol, it is present in an amount of less than approximately 10% by weight.

Description

BACKGROUND OF THE INVENTION The present invention relates to a vehicle system for a pharmaceutical composition comprising a piperidinopyrimidine derivative. More particularly minoxidil and to a pharmaceutical composition incorporating the vehicle system. Minoxidil is a pharmaceutically active ingredient having several indications including use as a hair growth stimulant. Minoxidil has poor solubility in water and ethanol and pharmaceutical preparations currently marketed only contain a small percentage of minoxidil. That is, below 5%. Numerous formulations comprising minoxidil have been published in the prior art including U.S. Pat. Nos. 4,139,619, 4,820,512, 5,104,646, 5,225,189, 4,938,953, 4,596,812, 5,006,332, 5,156,836 and 5,643,942. Many of the formulations require (or would require where the amount of minoxidil is greater than 5%) a very high percentage (often in the range of 30 to 50%) of propylene glycol or a similar glycol product in order to improve the solubility of mi...

AI Technical Summary

Benefits of technology

"The present invention provides a pharmaceutical composition for topical administration that includes a piperidinopyrimidine derivative or a pharmaceutically acceptable salt thereof, an acid, a solvent composition including water and a lower alcohol, and a co-solvent composition including benzyl alcohol. The composition has improved solubility of the piperidinopyrimidine derivative without the need for large amounts of propylene glycol or optionally excluding propylene glycol. The acid is added in an amount to provide an apparent pH of the composition of approximately 7.0 or less. The ratio of water to ethanol is preferably from approximately 9:1 to 1:3 by volume. The composition may also include benzyl alcohol in an amount of up to 85% by weight. The co-solvent system includes water and benzyl alcohol, wherein the benzyl alcohol is present in an amount of up to (10% by weight. The pharmaceutical composition may also include other ingredients such as preservatives, buffers, stabilizers, propellants, and the like. The composition may be a mousse or gel composition and may contain a skin penetrating agent."

Problems solved by technology

Due to the viscosity and tack of propylene glycol, large amounts of propylene glycol or similar agents in a composition are not pharmaceutically or cosmetically elegant and may be unacceptable to the consumer.

In addition, high concentrations of propylene glycol may cause local irritation and hypersensitivity upon application to the scalp.