Multiphase pharmaceutical formulations

Details Multiphase pharmaceutical formulations Multiphase pharmaceutical formulations

1992-12-18

1995-06-06

Page, Thurman K.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Implant or insert

424489, 424DIG15, 514966, A61F 902, A61K 914

Patent

active

054221170

DESCRIPTION:

BRIEF SUMMARY
This invention concerns pharmaceutical formulation for the treatment of skin and anorectal conditions.
Skin diseases commonly require the frequent application of medicaments. It is commonly preferably to leave the site of application uncovered although there is then a tendency for the medicament to be removed by contact with moisture. This is particularly true in the cases of anorectal diseases such as haemorrhoids and anal fissures which are commonly treated with combinations of astringents, antiseptics, topical analgesics, vasoconstrictors, antispasmodics and antiinflammatory steroids. However, the healing of the lesions is commonly inhibited by the mucous environment which, for example, leads to maceration of moist perianal skin.
One possible solution to this problem would be to apply medicaments in an occlusive layer which would repel water from the treated area. However, such conditions tend also to cause retention of fluids produced by the tissues, so that such an occlusive layer, by producing maceration of the affected area would thereby exacerbate the problem.
Furthermore, it is difficult to ensure that the occlusive layer does not form a barrier to prevent the medicaments from reaching the intended site of application.
On the other hand, at internal sites a deposited occlusive layer, for example of suppository base containing medicaments, is subject to erosion by aqueous media which can quickly reduce the beneficial effect of the medicament(s).
Our copending International Patent Application No. PCT/GB89/01545 describes and claims a multiphase pharmaceutical composition for combatting an anorectal disease comprising at least one phase containing one or more medicaments for combatting said disease and at least one phase adapted for delayed release of a silicone oil whereby application of said composition at a region affected by said disease deposits said medicament or medicaments thereon and a layer of silicone oil is formed thereover, so protecting the medicaments from erosion by aqueous media.
In our above International application, the means for delayed release of silicone oil include microcapsules containing the silicone oil which release the latter on rupture of the microcapsule shell, for example by pressure, dissolving or melting. The present invention is based on the concept of using, as the means for delayed release of silicone oil, one or more porous phases having silicone oil absorbed therein.
According to the present invention therefore we provide a multiphase pharmaceutical composition for combatting skin and anorectal conditions requiring medication comprising at least one phase containing one or more medicaments for combatting said disease and at least one porous phase containing a silicone oil absorbed therein and adapted for release, preferably delayed release, of the silicone oil whereby application of said composition at a region affected by said skin or anorectal condition deposits said medicament or medicaments thereon and a layer of silicone oil is formed thereover thus protecting the medicaments from erosion by aqueous media.
It will be appreciated that by being released after the application of the medicament, the silicone oil does not form a barrier between the medicament and the skin but forms a layer over the medicament which protects it from erosion while allowing the passage of water vapour and thus avoiding some of the problems of occlusive layers.
Skin conditions which may usefully be treated by compositions according to the invention include eczema, dermatitis, dry skin, chapped skin, napkin rash, pruritis and mild burns such as sunburn.
The porous phase(s) may be adapted to release the silicone oil by diffusion, possibly aided by the action of pressure to compress the particles, dissolution or melting.
In general, the porous phase(s) comprise porous particles.
A wide range of porous particles are available, as described in International Patent Applications WO088/01164 and W089/10132, U.S. Pat. Nos 4,873,091 and 4,690,825 and European Patent Application 306236A, the c

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