Patent ID: 7893040
Filing Date: 2011-02-22
Classification: A61K,A61P,B82Y,Y10S

Abstract:
1. An ophthalmic composition which is an aqueous suspension comprising drug, cyclodextrin and water, the composition having an aqueous phase of from about 5% (w/v) to about 50% (w/v) of the drug in solution, as dissolved free drug and as dissolved drug/cyclodextrin complex(es), and a solid phase of from about 50% (w/v) to about 95% (w/v) of the drug as solid drug/cyclodextrin complex particles, the size of the particles in the solid phase being from about 0.1 μm to about 500 μm, the drug/cyclodextrin complex particles being capable of dissolving in tear fluid, the cyclodextrin comprising at least one natural cyclodextrin selected from the group consisting of α-cyclodextrin, β-cyclodextrin and γ-cyclodextrin, the total concentration of the drug/cyclodextrin complex in the composition being above the aqueous solubility of the complex; the drug being a carbonic anhydrase inhibitor selected from the group consisting of acetazolamide, dorzolamide, methazolamide, ethoxyzolamide and brinzolamide; or the drug being a GABAergic benzodiazepine selected from the group consisting of alprazolam, diazepam, brotizolam, chlordiazepoxide, clobazam, clonazepam, clorazepam, demoxazepam, flumazenil, fluazepam, halazepam, midazolam, nordazepam, mebazepam, nitrazepam, oxazepam, medazepam, lorazepam, prazepam, quazepam, timezepam, lorazelam and triazolam; or the drug being an anti-inflammatory steroid selected from the group consisting of 21-acetoxypregnenolone, alclometasone, algestone, amcinonide, beclomethasone, betamethasone, budesonide, chloroprednisone, clobetasol, clobetasone, clocortolone, cloprednol, corticosterone, cortisone, cortivazol, deflazacort, desonide, desoximetasone, dexamethasone, diflorasone, diflucortolone, difluprednate, enoxolone, etiprednol dicloacetate, fluazacort, flucloronide, flumethasone, flunisolide, fluocinolone acetonide, fluocinonide, fluocortin butyl, fluocortolone, fluorometholone, fluperolone acetate, fluprednidene acetate, fluprednisolone, flurandrenolide, fluticasone propionate, formocortal, halcinonide, haiobetasol propionate, halometasone, halopredone acetate, hydrocortamate, hydrocortisone, loteprednol etabonate, mazipredone, medrysone, meprednisone, methylprednisolone, mometasone furoate, paramethasone, prednicarbate, prednisolone, prednisolone 25-diethylamino-acetate, prednisolone sodium phosphate, prednisone, prednival, prednylidene, rimexolone, tixocortol, triamcinolone, triamcinolone acetonide, triamcinolone benetonide and triamcinolone hexacetonide.