Pharmaceutical compositions comprising silica microspheres

Patent metadata

Field	Value
Publication number	US-11865208-B2
Application number	US-202017023625-A
Country	US
Kind code	B2
Filing date	Sep 17, 2020
Priority date	Apr 14, 2006
Publication date	Jan 9, 2024
Grant date	Jan 9, 2024

Abstract

Topical vaginal compositions are disclosed herein which include silica microspheres and an active ingredient in the amount of 0.001 to 15.0% w/w selected from estradiol, metronidazole, clindamycin, butoconazole, and combinations thereof. The topical compositions provide sustained release of the active ingredient so as to reduce skin irritation.

First claim

What is claimed is:

1. A sustained release composition for topical application of pharmaceuticals, comprising:
silica microspheres impregnated with benzoyl peroxide, wherein the composition comprises: (a) 0.01 to 15% w/w benzoyl peroxide and (b) silica; and said composition is formulated for sustained release of said benzoyl peroxide.

2. The sustained release composition of claim 1 , wherein some of the benzoyl peroxide is free in the composition, and the benzoyl peroxide impregnated in the silica microspheres provides sustained release of the benzoyl peroxide.

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

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

5. The sustained release composition of claim 4 , wherein the semisolid form is a gel, a cream, a paste, a lotion, an ointment, a shampoo, a semisolid powder or a suspension.

6. 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.

7. 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.

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

9. The sustained release composition of claim 8 , wherein the solvent is selected from the group consisting of isopropanol, oleic acid, glycerol monooleate, oleyl alcohol, propylene glycol, isopropyl myristate, and combinations thereof.

10. The sustained release composition of claim 1 , wherein the silica microspheres were formed prior to contact with the benzoyl peroxide.

11. The sustained release composition of claim 2 , wherein the silica microspheres were formed prior to contact with the benzoyl peroxide.

12. The sustained release composition of claim 1 , wherein the benzoyl peroxide is present in the composition in an amount of about 5% w/w.

13. The sustained release composition of claim 2 , wherein the benzoyl peroxide is present in the composition in an amount of about 5% w/w.

14. The sustained release composition of claim 11 , wherein the benzoyl peroxide is present in the composition in an amount of about 5% w/w.

Assignees

• Sol Gel Tech Ltd

Inventors

• Shevachman Marina
• Ze' Evi Amira
• Asculai Eilon
• Benyaminovich Batella
• Avram Nir
• Aschkenasy Chaim

Classifications

• A61K31/192

  having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid  {(cannabinoids A61K31/658)} · CPC title

• A61K31/05

  Phenols {(cannabinoids A61K31/658)} · CPC title

• A61K9/0034 Primary

  Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants · CPC title

• A61K9/0014

  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 title

• A61K9/06

  Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)} · CPC title