Pharmaceutical compositions comprising silica microspheres

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.

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.