Compositions For Delivering A Drug

• US 20100202986A1
• Filed: 07/11/2008
• Published: 08/12/2010
• Est. Priority Date: 07/11/2007
• Status: Abandoned Application

• Current Assignee: Dow Corning Corporation (Dow, Inc.)
• Original Assignee: Dow Corning Corporation (Dow, Inc.)
• Inventors: Huber, Robert O., Nartker, Linda Sue, Raul, Victor Albert
• Application Number:
  US12/668,555
• Publication Number:
  US 20100202986A1
• Time in Patent Office: Days
• US Class Current: 424/59
• CPC Class Codes: A61K 47/20 containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
• CPC Class Codes: A61K 47/24 containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• 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 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 17/06 Antipsoriatics
• CPC Class Codes: A61P 17/10 Anti-acne agents

Abstract

A composition comprises a mixture of a silicone and a solvent. The composition further comprises a drug selected from the group of retinoids, retinyls, vitamin A esters, vitamin D analogues, and combinations thereof. The composition further comprises a salt of a dialkyl sulfosuccinate, such as dioctyl sodium sulfosuccinate (DOSS). The composition yet further comprises and a solubilizer. The salt of a dialkyl sulfosuccinate solubilizes the drug. The solubilizer solubilizes the salt of a dialkyl sulfosuccinate. The composition can be topically applied to a substrate, such as skin, for delivering the drug. Drugs with a wide solubility range are soluble and compatible in the composition without separation or crystallization of the drugs occurring.

Claims

1. A composition comprising:

a mixture of a silicone and a solvent;

a drug selected from the group of retinoids, retinyls, vitamin A esters, vitamin D analogues, and combinations thereof;

a salt of a dialkyl sulfosuccinate for solubilizing said drug; and

a solubilizer for solubilizing said salt of a dialkyl sulfosuccinate.

2. A composition as set forth in claim 1 wherein said solubilizer comprises a surfactant.

3. A composition as set forth in claim 2 wherein said surfactant is a nonionic surfactant.

4. A composition as set forth in claim 2 wherein said surfactant is a liquid.

5. A composition as set forth in claim 2 wherein said surfactant has a hydrophilic-lipophilic balance (HLB) of less than 15.

6. A composition as set forth in claim 1 wherein said solubilizer comprises a glycol.

7. A composition as set forth in claim 6 wherein said glycol is selected from the group of propylene glycol, dipropylene glycol, butylene glycol, and combinations thereof.

8. A composition as set forth in claim 1 substantially free of water.

9. A composition as set forth in claim 1 substantially free of an alcohol having the formula C_nH_2n+1OH wherein n is from 1 to 5.

10. A composition as set forth in claim 1 wherein said silicone is a silicone elastomer.

11. A composition as set forth in claim 10 wherein said solvent comprises a polysiloxane for swelling said silicone elastomer.

12. A composition as set forth in claim 11 wherein said polysiloxane is selected from the group of hexamethyldisiloxane, hexamethylcyclotrisiloxane, hexadecamethylheptasiloxane, octamethyltrisiloxane, octamethylcyclotetrasiloxane, decamethyltetrasiloxane, decamethylcyclopentasiloxane, dodecamethylpentasiloxane, dodecamethylcyclohexasiloxane, tetradecamethylhexasiloxane, and combinations thereof.

13. A composition as set forth in claim 11 wherein said polysiloxane and said silicone elastomer are present in a weight ratio of 5:

1 to 9;

1.

14. A composition as set forth in claim 1 wherein said salt of a dialkyl sulfosuccinate comprises dioctyl sodium sulfosuccinate (DOSS).

15. A composition as set forth in claim 10 wherein said silicone elastomer comprises the reaction product of;

an ≡

Si—

H containing polysiloxane, and

an alpha, omega-diene,

in the presence of a metal catalyst.

16. A composition as set forth in claim 15 wherein said ≡

Si—

H containing polysiloxane has the formula

R₃SiO(R′

₂SiO)_a(R″

₂HSiO)_bSiR₃

wherein R, R′

, and R″

are each independently alkyl groups with 1 to 6 carbon atoms, a is 0 to 250, and b is 1 to 250.

17. A composition as set forth in claim 15 wherein said alpha, omega-diene has the formula

CH₂═

CH(CH₂)_xCH═

CH₂

wherein x is 1 to 20.

18. A composition as set forth in claim 1 wherein said mixture comprises a cyclomethicone and dimethicone crosspolymer.

19. A composition as set forth in claim 1 wherein said mixture comprises a dimethicone and dimethicone crosspolymer.

20. A composition as set forth in claim 1 wherein said silicone is a silicone adhesive comprising the reaction product of;

a polydialkylsiloxane end blocked with silanols, and

a silicate resin.

21. A composition as set forth in claim 20 wherein said polydialkylsiloxane is a polydimethylsiloxane.

22. A composition as set forth in claim 20 wherein said solvent is selected from the group of alkanes, arenes, esters, and combinations thereof.

23. A composition as set forth in claim 1 wherein said drug is selected from the group of trans-retinoic acid, cis-retinoic acid, adapalene, tazarotene, calciprotriene, calcitriol, calciprotiol, vitamin D₃, and combinations thereof.

24. A composition as set forth in claim 1 wherein said drug is present in an amount of no greater than 1 part by weight based on 100 parts by weight of said composition.

25. A composition as set forth in claim 1 further comprising an additive selected from the group of an emollient, a penetration enhancer, a fragrance, an antioxidant, UV light blockers, steroids, pH adjusters, and combinations thereof.

26. A composition as set forth in claim 1 wherein said salt of a dialkyl sulfosuccinate and said solubilizer are present in a weight ratio of from 2:

1 to 1;

10.

27. A method of delivering a drug to a substrate, said method comprising the step of applying the composition of claim 1 to the substrate.

28. A method of forming the composition of claim 1, said method comprising the steps of:

dissolving the salt of a dialkyl sulfosuccinate in the solubilizer to form a first blend;

dissolving the drug in the first blend to form a second blend; and

mixing the mixture and the second blend to form the composition.

29. A composition as set forth in claim 2 wherein said solubilizer further comprises a glycol.