Pharmaceutical compositions comprising silica microspheres

Patent metadata

Field	Value
Publication number	US-RE50804-E
Application number	US-202217950597-A
Country	US
Kind code	E1
Filing date	Sep 22, 2022
Priority date	Apr 14, 2006
Publication date	Feb 24, 2026
Grant date	Feb 24, 2026

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:
3% w/w of benzoyl peroxide and 0.1% w/w tretinoin as the active ingredients0.04% w/w to 0.3% w/w of an active ingredient that is an antibiotic, tazarotene, or a combination thereof,
and
silica microspheres, formed prior to contact with the active ingredients ingredient, impregnated with the active ingredients ingredient;
wherein some of the 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 , wherein some of the active ingredients are free in the composition, and the active ingredients impregnated in the silica microspheres provides sustained release of the active ingredients.

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 composition may be used to treat skin disorders and diseases, including atopic dermatitis, psoriasis, rosacea, actinic keratosis, acne, skin pigmentation and other types of skin inflammations or viral, fungal or bacterial skin infections.

Assignees

• Sol Gel Tech Ltd

Inventors

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

Classifications

• A61K31/05

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

• A61K31/192

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

• A61K31/4436

  containing a heterocyclic ring having sulfur as a ring hetero atom · CPC title

• A61K9/143

  with inorganic compounds · 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