Foam-forming pharmaceutical composition

• US 6,258,374 B1
• Filed: 09/24/1998
• Issued: 07/10/2001
• Est. Priority Date: 09/08/1997
• Status: Expired due to Term

• Current Assignee: Astra AB (Astrazeneca PLC)
• Original Assignee: Astra AB (Astrazeneca PLC)
• Inventors: Friess, Stefan, Kublik, Heike, Heckenmüller, Harald, Szambien, Oliver
• Primary Examiner(s): Azpuru, Carlos A.
• Application Number:
  US09/155,250
• Time in Patent Office: 1,020 Days
• Field of Search: 424/430, 424/433, 424/436
• US Class Current: 424/436
• CPC Class Codes: A61K 9/0031 Rectum, anus
• CPC Class Codes: A61K 9/0034 Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
• CPC Class Codes: A61P 15/18 Feminine contraceptives
• CPC Class Codes: A61P 23/02 Local anaesthetics
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 29/02 without antiinflammatory effect
• CPC Class Codes: A61P 31/00 Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• CPC Class Codes: A61P 31/04 Antibacterial agents
• CPC Class Codes: A61P 9/14 Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

Abstract

The invention provides a pharmaceutical composition for rectal or vaginal administration which comprises at least two parts wherein the composition comprises

(i) two or more physiologically acceptable substances each in separate parts of the composition which are such that on admixture they react to produce a physiologically acceptable gas;

(ii) in at least one part of the composition a polymer stabiliser which is adapted to facilitate the formation of a water-soluble collapsible foam structure; and

(iii) in at least one part of the composition a pharmaceutically active substance; an its use in the treatment or prophylaxis of disorders of the intestines, rectum or vagina.

Claims

1. A pharmaceutical composition for rectal or vaginal administration which comprises at least two parts wherein the composition comprises

(i) two or more physiologically acceptable substances each in separate parts of the composition which are such that on admixture they react to produce a physiologically acceptable gas;

(ii) in at least one part of the composition a polymer stabiliser which is adapted to facilitate the formation of a water-soluble collapsible foam structure; and

(iii) in at least one part of the composition a pharmaceutically active substance.

2. A composition according to claim 1 wherein the two or more substances defined in (i) are one or more acids and one or more effervescent compounds.

3. A composition according to claim 2 wherein the acid is a water-soluble acid.

4. A composition according to claim 1, wherein the polymer stabiliser is a hydrogel thickener.

5. A composition according to claim 1 wherein the pharmaceutically active substance is one or more of an anti-inflammatory drug, analgesic, local anaesthetic, anti-infection drug, contraceptive or vaso-active drug.

6. A method of treatment or prophylaxis of a disorder of the intestines, rectum or vagina which comprises administering a therapeutically effective amount of a composition according to claim 1 to a patient suffering from or liable to suffer from said disorder.

7. A composition according to claim 2, wherein the polymer stabiliser is a hydrogel thickener.

8. A composition according to claim 3, wherein the polymer stabiliser is a hydrogel thickener.

9. A composition according to claim 2, wherein the pharmaceutically active substance is one or more of an anti-inflammatory drug, analgesic, local anaesthetic, anti-infection drug, contraceptive or vaso-active drug.

10. A composition according to claim 3, wherein the pharmaceutically active substance is one or more of an anti-inflammatory drug, analgesic, local anaesthetic, anti-infection drug, contraceptive or vaso-active drug.

11. A method of treatment or prophylaxis of a disorder of the intestines, rectum or vagina which comprises administering a therapeutically effective amount of a composition according to claim 2 to a patient suffering from or liable to suffer from said disorder.

12. The method of claim 11, wherein the pharmaceutically active substance is one or more of an anti-inflammatory drug, analgesic, local anaesthetic, anti-infection drug, contraceptive or vaso-active drug.

13. The method of claim 11, wherein the two or more substances defined in (i) are one or more acids and one or more effervescent compounds.

14. The method of claim 13, wherein the acid is a water-soluble acid.

15. The method of claim 11, wherein the polymer stabiliser is a hydrogel thickener.

16. The composition of claim 5, wherein the pharmaceutically active substance is an anti-inflammatory drug selected from the group consisting of steroids and non-steroidal anti-inflammatory drugs.

17. The composition of claim 16, wherein the pharmaceutically active substance is a steroid selected from the group consisting of budesonide, esters of beclomethasone, rofleponide, esters of rofleponide, hydrocortisone, betamethasone, prednisolone, dexamethasone, fluocinolone, amcinonide, bufexamac, and flunisolide.

18. The composition of claim 16, wherein the pharmaceutically active substance is a non-steroidal anti-inflammatory drug selected from the group consisting of 4-aminosalicylic acid, 5-aminosalicylic acid, and sulphasalazine.

19. The composition of claim 5, wherein the pharmaceutically active substance is an analgesic selected from the group consisting of lidocaine, morphine, and codeine.

20. The composition of claim 5, wherein the pharmaceutically active substance is an anti-infection drug is an anti-microbial agent, antiseptic, fungicide, or antiviral agent.

21. The composition of claim 20, wherein the pharmaceutically active substance is selected from the group consisting of bacitracine, iodine, cetrimide, clotrimazole, metonidazole, cyclosporine, acyclovir, and idoxuridin.

22. The composition of claim 5, wherein the vaso-active drug is isosorbicle-5-mononitrate or isosorbide dinitrate.

23. A method of administering a pharmaceutical composition to the rectum or vagina, comprising:

(a) providing a multi-chamber syringe containing the pharmaceutical composition, the composition comprising two or more parts, each part containing a physiologically acceptable substance, the substances being selected so that on admixture they react to produce a physiologically acceptable gas, at least one part of the composition including a polymer stabilizer that is adapted to facilitate the formation of a water-soluble collapsible foam structure, and at least one part of the composition including a pharmaceutically active substance, each of the parts being disposed in a separate chamber of the syringe;

(b) delivering the parts of the composition from the chambers of the syringe to the rectum or vagina.

24. The method of claim 23 wherein the parts of the composition are mixed during delivery.

25. The method of claim 23 wherein the parts react to form a water-soluble collapsible foam.