Compositions For Delivering A Drug

• US 20100184714A1
• Filed: 07/11/2008
• Published: 07/22/2010
• Est. Priority Date: 07/11/2007
• Status: Abandoned Application

• Current Assignee: Dow Corning Corporation (Dow, Inc.)
• Original Assignee: Dow Corning Corporation (Dow, Inc.)
• Inventors: Raul, Victor Albert, Nartker, Linda Sue
• Application Number:
  US12/668,492
• Publication Number:
  US 20100184714A1
• Time in Patent Office: Days
• US Class Current: 514/29
• 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 first solvent, a drug, such as a hydrophilic or lipophilic pharmaceutical agent, a salt of a dialkyl sulfosuccinate, such as dioctyl sodium sulfosuccinate (DOSS), and a second solvent, such as an alcohol. The salt of a dialkyl sulfosuccinate solubilizes the drug. 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 first solvent;

a drug;

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

a second solvent different from said first solvent.

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

3. A composition as set forth in claim 2 wherein said first solvent comprises a polysiloxane for swelling said silicone elastomer.

4. A composition as set forth in claim 3 wherein said polysiloxane is selected from the group of hexamethyldisiloxane, hexamethylcyclotrisiloxane, hexadecamethylheptasiloxane, octamethyltrisiloxane, octamethylcyclotetrasiloxane, decamethyltetrasiloxane, decamethylcyclopentasiloxane, dodecamethylpentasiloxane, dodecamethylcyclohexasiloxane, tetradecamethylhexasiloxane, and combinations thereof.

5. A composition as set forth in claim 3 wherein said polysiloxane and said silicone elastomer are present in a weight ratio of 5:

1 to 9;

1.

6. A composition as set forth in claim 2 wherein said silicone elastomer is present in an amount of 5 to 20, said first solvent is present in an amount of 45 to 90, said drug is present in an amount of 0.0001 to 15, said salt of a dialkyl sulfosuccinate is present in an amount of 0.1 to 5, and said second solvent is present in an amount of 0.1 to 20, parts by weight, all based on 100 parts by weight of said composition.

7. A composition as set forth in claim 1 wherein said salt of a dialkyl sulfosuccinate comprises dioctyl sodium sulfosuccinate.

8. A composition as set forth in claim 1 wherein said second solvent comprises an alcohol.

9. A composition as set forth in claim 8 wherein said alcohol is a monomeric alcohol.

10. A composition as set forth in claim 9 wherein said monomeric alcohol is selected from the group of methanol, ethanol, propanol, butanol, pentanol, hexanol, heptanol, octanol, nonanol, decanol, and combinations thereof.

11. A composition as set forth in claim 8 wherein said salt of a dialkyl sulfosuccinate and said alcohol are present in a weight ratio of 1:

1 to 1;

4.

12. A composition as set forth in claim 1 wherein said drug is selected from the group of tetracycline, clindamycin phosphate, erythromycin, ciprofloxacin, norfloxacin, salicylic acid, benzoyl peroxide, alprostadil, terbinafine, clobetasol propionate, ketoconazole, progesterone, niacinamide, calcipotriol, retinoids, vitamin D analogues, vitamin A esters, dapsone, doxycycline, and combinations thereof.

13. A composition as set forth in claim 2 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.

14. A composition as set forth in claim 13 wherein said silicone elastomer is present in an amount of 75 to 95, said first solvent is present in an amount of 1 to 50, said drug is present in an amount of 0.0001 to 15, said salt of a dialkyl sulfosuccinate is present in an amount of 0.1 to 5, and said second solvent is present in an amount of 0.1 to 20, parts by weight, all based on 100 parts by weight of said composition.

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

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

17. 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.

18. A composition as set forth in claim 17 wherein said polydialkylsiloxane is a polydimethylsiloxane.

19. A composition as set forth in claim 17 wherein said first solvent is selected from the group of alkanes, arenes, esters, and combinations thereof.

20. A composition as set forth in claim 17 wherein said silicone adhesive is present in an amount of 40 to 80, said first solvent is present in an amount of 1 to 40, said drug is present in an amount of 0.0001 to 15, said salt of a dialkyl sulfosuccinate is present in an amount of 0.1 to 5, and said second solvent is present in an amount of 0.1 to 20, parts by weight, based on 100 parts by weight of said composition.

21. A composition as set forth in claim 1 further comprising an additive selected from the group of an emollient, a penetration enhancer, a fragrance, a drug solubilizer, a surfactant, an antioxidant, an antioxidant, a UV light blocker, a steroid, a pH adjuster, and combinations thereof.

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

23. A composition comprising:

a silicone elastomer comprising the reaction product of;

an ≡

Si—

H containing polysiloxane having the formula

R₃SiO(R′

₂SiO)_a(R″

HSiO)_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, and

an alpha,omega-diene having the formula

CH₂═

CH(CH₂)_xCH═

CH₂

wherein x is 1 to 20,

in the presence of a metal catalyst and a polysiloxane,

a drug;

dioctyl sodium sulfosuccinate for solubilizing said drug; and

an alcohol for solubilizing said dioctyl sodium sulfosuccinate.

24. A composition as set forth in claim 23 wherein said polysiloxane is selected from the group of hexamethyldisiloxane, hexamethylcyclotrisiloxane, hexadecamethylheptasiloxane, octamethyltrisiloxane, octamethylcyclotetrasiloxane, decamethyltetrasiloxane, decamethylcyclopentasiloxane, dodecamethylpentasiloxane, dodecamethylcyclohexasiloxane, tetradecamethylhexasiloxane, and combinations thereof.

25. A composition comprising:

a silicone adhesive comprising the reaction product of;

a polydimethylsiloxane end blocked with silanols, and

a silicate resin,

a first solvent;

a drug; and

dioctyl sodium sulfosuccinate for solubilizing said drug.

26. A composition as set forth in claim 25 further comprising an alcohol different from said first solvent for solubilizing said dioctyl sodium sulfosuccinate.