IP Library Granted Patent US 9,452,137
Granted Patent B2
US 9,452,137 · App. 14/551,155 · Granted Sep 27, 2016

Pharmaceutical compositions comprising silica microspheres

Inventors: Marina Shevachman (Beer-Sheva, IL); Amira Ze' Evi (Omer, IL); Eilon Asculai (Lehavim, IL); Batella Binyaminovich (Beer-Sheva, IL); Nir Avram (Meitar, IL)
Assignee: PERRIGO ISRAEL PHARMACETICALS LTD.
A61K9/143A61K9/0014A61K9/06A61K31/05A61K31/192A61K31/203A61K31/327A61K31/4436A61K45/06A61K47/02
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Quick Facts
Patent No.
US 9,452,137
App. No.
14/551,155
Granted
Sep 27, 2016
Kind
B2
Abstract

A topical composition which includes a silica microspheres and an active ingredient in the amount of 0.01 to 15.0% w/w wherein the active ingredient is selected from adapalene, an antibiotic, tazarotene, tretinoin, a retinoid, or any combination thereof. The topical composition may also include benzoyl peroxide as an active ingredient. The topical compositions provide sustained release of the active ingredient so as to reduce skin irritation.

Claims (18)

1. A sustained release composition for topical application of pharmaceuticals comprising:

0.01 to 15.0% w/w of an active ingredient selected from adapalene, an antibiotic, tazarotene, tretinoin, a retinoid, or any combination thereof; and

silica microspheres, formed prior to contact with the active ingredient, impregnated with the active ingredient;

wherein some of active ingredient is free in the composition, and the active ingredient impregnated in the silica microspheres provides sustained release of the active ingredient.

2. The sustained release composition of claim 1 , further comprising benzoyl peroxide as an active ingredient.

3. The sustained release composition of claim 2 , wherein said active ingredient is a combination of benzoyl peroxide and a retinoid.

4. The sustained release composition of claim 2 , wherein said active ingredient is a combination of benzoyl peroxide and adapalene.

5. The sustained release composition of claim 2 , wherein said active ingredient is a combination of benzoyl peroxide and tazarotene.

6. The sustained release composition of claim 2 , wherein said active ingredient is a combination of benzoyl peroxide and tretinoin.

7. The sustained release composition of claim 2 , wherein said active ingredient is a combination of benzoyl peroxide and clindamycin.

8. The sustained release composition of claim 1 , wherein the composition is formulated as a foam.

9. The sustained release composition of claim 1 , wherein said sustained release composition is formulated in a semisolid form.

10. The sustained release composition of claim 9 , wherein the semisolid form is a gel, a cream, a paste, a lotion, an ointment, a shampoo, a semisolid powder or a suspension.

11. The sustained release composition of claim 1 wherein the silica microspheres have a mean microsphere size in the range of 0.5 micron to 40 microns.

12. The sustained release composition of claim 1 wherein the silica microspheres have a mean microsphere size in the range of 1 micron to 20 microns.

13. The sustained release composition of claim 1 further comprising one or more of a solvent, an antioxidant, an antimicrobial preservative, an emulsifier, and water.

14. The sustained release composition of claim 13 , wherein the solvent is selected from the group consisting of isopropanol, oleic acid, glycerol monooleate, oleyl alcohol, propylene glycol, isopropyl myristate, and combinations thereof.

15. The sustained release composition of claim 1 , wherein the composition may be used to treat skin disorders and diseases, including atopic dermatitis, psoriasis, rosacea, cancer, actinic keratosis, acne, skin pigmentation and other types of skin inflammations or viral, fungal or bacterial skin infections.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 25, 2019
From: PERRIGO ISRAEL PHARMACEUTICALS LTD.
To: SOL-GEL TECHNOLOGIES LTD.
Reel/Frame 048689/0716 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 24, 2014
From: AVRAM, NIR; SHEVACHMAN, MARINA; ZE'EVI, AMIRA; ASCULAI, EILON; BINYAMINOVICH, BATELLA
To: PERRIGO ISRAEL PHARMACEUTICALS LTD.
Reel/Frame 034246/0447 →
Continuity (4)
Continuation 11783895 · Apr 12, 2007
Provisional Application 60791902 · Apr 14, 2006
Provisional Application 60817247 · Jun 29, 2006
Related Publication 20150079182A1 · Mar 19, 2015