Multiphase suppository

Details Multiphase suppository Multiphase suppository

1991-08-28

1995-05-09

Kight, III, John

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Implant or insert

514 63, 514882, 514966, A61K 902, A61K 31695

Patent

active

054137934

DESCRIPTION:

BRIEF SUMMARY
This invention concerns pharmaceutical formulations for the treatment of anorectal diseases.
Anorectal diseases include 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, for example to perianal lesions, 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).
We have found that it is possible at least partially to overcome these problems by formulating medicaments for the treatment of anorectal diseases in a multiphase formulation wherein the medicaments reach the site of intended application first and a layer of silicone oil is released to cover the area to repel liquid water therefrom. Silicones possess the property of repelling liquid water but allowing the passage of water vapour, for example, water vapour formed by insensible perspiration from the skin.
We thus provide 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.


BRIEF DESCRIPTION OF THE DRAWING

FIG. 1 is a cross sectional view of a mold for forming suppositories according to the invention.
In one embodiment of the invention, the composition comprises a cream containing the medicament(s) together with microcapsules containing silicone oil which rupture to release the silicone oil after application of the composition to the affected area.
The microcapsules may comprise silicone oil encapsulated in a material which ruptures (a) on application of pressure, (b) by melting at or just below body temperature, (c) by dissolving in body fluids or by any other means.
Capsules which rupture under pressure include NCR capsules.
Capsule materials which melt at close to body temperature include hard or soft gelatine.
Capsule materials which dissolve in body fluids include polymeric materials e.g. polymethacrylates such as Eudragit which dissolve at the pH of the gut.
The microcapsules may be in the size range 1 to 1000 microns.
The silicone oil will preferably be a polydialkylsiloxane oil, more preferably polydimethylsiloxane. Suitable medical grade silicone oils include Dow Corning 360 Medical Fluid.
The phase in which the medicament(s) are contained may be a conventional cream base, e.g. containing oily or waxy materials such as liquid paraffin, white petroleum or cetyl alcohol, water and one or more surfactants to produce a water-in-oil emulsion. A bactericide such as benzalkonium chloride is conveniently present.
Medicaments which may usefully be present include astringents such as bismuth subgallate, local anaesthetics such as benzocaine or lignocaine and antiinflammatory steroids such as hydrocortisone acetate.
According to a further embodiment of the invention, the composition takes the form of a suppository comprising an outer layer containing the medicament(s) in a suppository base surr

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