Topical Compositions for Paediatric Use

• US 20090215753A1
• Filed: 12/07/2006
• Published: 08/27/2009
• Est. Priority Date: 12/07/2005
• Status: Abandoned Application

• Current Assignee: Pharmacodex Ltd.
• Original Assignee: Pharmacodex Ltd.
• Inventors: Staniforth, John, Goggin, Paul
• Application Number:
  US12/086,043
• Publication Number:
  US 20090215753A1
• Time in Patent Office: Days
• US Class Current: 514/221
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/14 Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• CPC Class Codes: A61K 9/0014 Skin, i.e. galenical aspects of topical compositions non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00
• CPC Class Codes: A61P 25/08 Antiepileptics; Anticonvulsants

Abstract

The present invention provides pharmaceutical compositions for treating a paediatric mammal, the compositions comprising a therapeutic agent and a pharmaceutically acceptable carrier, the composition being suitable for topical application resulting in transdermal administration of the therapeutic agent and a systemic therapeutic effect. The invention also provides relates uses of the compositions, applicators and kits.

Claims

1. A pharmaceutical composition for treating a paediatric mammalian subject, comprising a therapeutic agent, and a pharmaceutically acceptable carrier, the composition being suitable for topical application resulting in transdermal administration of the therapeutic agent to provide a systemic effect.

2. A pharmaceutical composition as claimed in claim 1, wherein said mammal is selected from one or more of a human neonate, infant, young child or child.

3. A pharmaceutical composition as claimed in claim 1, wherein the therapeutic agent is a benzodiazepine, such as diazepam.

4. A pharmaceutical composition as claimed in claim 1, wherein the therapeutic agent is a selective serotonin receptor antagonist.

5. A pharmaceutical composition as claimed in claim 1, wherein the therapeutic agent is a proton pump inhibitor.

6. A pharmaceutical composition as claimed in claim 1, further comprising one or more solvents.

7. A pharmaceutical composition as claimed in claim 6, wherein the solvent is selected from the group comprising:

ethanol, menthol, thymol, eucalyptol, eucalyptus oil, benzyl alcohol, isopropyl alcohol, propylene glycol, methylated spirit, phenol, cyclodextrins, ethyl oleate, eugenol, glycerol, levomenol, monoethanolamine oleate, myristyl alcohol, octyldodecanol, methyl alcohol, coconut oil or silicone oil.

8. A pharmaceutical composition as claimed in claim 1, further comprising one or more penetration enhancers.

9. A pharmaceutical composition as claimed in claim 8, wherein the penetration enhancer is selected from the group comprising:

surfactants, alcohols, esters, carboxylates, phenols, glycols, humectants, surfactants, emulsifiers, antioxidants, preservatives, clays, antifoaming agents, spreading agents, emollients, barriers or solubilising agents.

10. A pharmaceutical composition as claimed in claim 1, wherein the composition is in the form of an ointment, cream or gel.

11. A pharmaceutical composition as claimed in claim 1, wherein the composition is a substantially solid dosage form at a temperature of about 25°

C. or less and, upon contact with the skin of the subject, softens to a consistency that allows transdermal absorption of the therapeutic agent.

12. A pharmaceutical composition as claimed in claim 11, wherein the composition has a softening point of not higher than 35°

C.

13. A pharmaceutical composition as claimed in claim 11, wherein the composition softens to a consistency to allow transdermal absorption of the therapeutic agent within a time period of less than 10 minutes upon being placed in continuous contact with the skin of the subject.

14. A pharmaceutical composition as claimed in claim 11, wherein the dosage form has a total weight from about 50 mg to less than 1 g from about 100 mg to about 900 mg or from about 250 mg to about 750 mg.

15. A pharmaceutical composition as claimed in claim 1, comprising a compacted granulate of the therapeutic agent and the pharmaceutically acceptable carrier, the compacted granulate having a softening point of not higher than 35°

C.

16. A pharmaceutical composition as claimed in claim 1, wherein the composition comprises a plurality of substantially discrete substantially solid particles comprising the therapeutic agent admixed with a pharmaceutically acceptable carrier medium, the particles having a softening point of about 30°

C. to about 35°

C.

17. A pharmaceutical composition as claimed in claim 1, wherein the composition provides a therapeutically effective serum concentration of the therapeutic agent within a period of less than 10 minutes from topical application to the skin of the subject.

18. A pharmaceutical composition as claimed in claim 17, wherein the time period is less than 5 minutes, less than 2 minutes or less than 1 minute from topical application to the skin of the subject.

19. A pharmaceutical composition as claimed in claim 1, wherein the composition is free of preservatives.

20. A pharmaceutical composition as claimed in claim 1, further comprising one or more preservatives to prevent or reduce contamination of the composition during preparation.

21. A pharmaceutical composition as claimed in claim 1, wherein the composition is substantially free of antioxidants.

22. A pharmaceutical composition as claimed in claim 1, wherein the composition is for treating epilepsy, status epilepticus, nausea and vomiting, or gastric upset.

23. Use of a therapeutic agent in the manufacture of a medicament for topical application as claimed in any one of the preceding claims, the medicament being suitable for topical application resulting in transdermal administration of the therapeutic agent to provide a systemic effect.

24. An applicator for applying a pharmaceutical composition as claimed in claim 1.

25. An applicator as claimed in claim 24, comprising a receiving means for receiving and carrying the pharmaceutical composition so that the composition may be applied directly to the skin and a grip for enabling a user to hold and manipulate the applicator

27. A method of treating an animal or human body comprising topically applying a pharmaceutical composition as claimed in claim 1.

29. A pharmaceutical composition as claimed in claim 4, wherein the selective serotonin receptor antagonist is ondansetron.

30. A pharmaceutical composition as claimed in claim 5, wherein the proton pump inhibitor is omeprazole.

26. A kit comprising at least one dose of a pharmaceutical composition for treating a paediatric mammalian subject, comprising a therapeutic agent, and a pharmaceutically acceptable carrier, the composition being suitable for topical application resulting in transdermal administration of the therapeutic agent to provide a systemic effect, and an applicator.

28. A pharmaceutical composition or product substantially as described in any one of the Examples.