Ophthalmic drug delivery with thermo-irreversible gels of polxoxyalkylene polymer and ionic polysaccharide
AssigneeMediventures, Inc.
InventorsTacey X. Viegas, Lorraine E. Reeve, Raymond L. Henry
Life of this patent
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Abstract
Balanced pH, thermo-irreversible gels are ideal vehicles for drug delivery to the eye of a mammal.
Claims22
A process for treating an eye condition requiring the application of a medicament or the administration of a diagnostic agent which comprises administering to the eye of a mammal an osmotically balanced and buffered pH composition, which is a liquid at room temperature or below and a thermo-reversible gel at mammalian body temperature, said composition comprising an ionic polysaccharide and
- A) a polyoxyalkylene block copolymer of the formula
- Y[(a).sub.n --E--H].sub.x (I)
- wherein A is a polyoxyalkylene moiety having an oxygen/carbon atom ratio of less than 0.5, x is at least 1, Y is derived from water or an organic compound containing x reactive hydrogen atoms, E is a polyoxyethylene moiety, n has a value such that the average molecular weight of A is at least about 500 to about 900, as determined by the hydroxyl number of an intermediate,
- Y[(a).sub.n --H].sub.x (II)
- and wherein the total average molecular weight of the copolymer is at least about 5000,
- B) a pharmacologically effective amount of a drug selected from the group consisting of antibacterials, antihistamines and decongestants, antiinflammatories, antiparasitics, miotics and anticholinergics, antivirals, local anethetics, antifungals, amoebicidals, trichomonocidals, analgesics, mydriatics, angiglaucoma drugs, carbonic anhydrase inhibitors, opthalmic diagnostic agents, opthalmic agents used as adjuvants in surgery, chelating agents, antineoplastics, antihypertensives, muscle relaxants, and diagnostics;
- and
- C) optionally, a latent form of a counter-ion capable of thermo-irreversibly gelling said composition.
A process for treating an eye condition requiring the application of a medicament or the administration of a diagnostic agent which comprises administering to the eye of a mammal an osmotically balanced and buffered pH composition comprising an aqueous gel comprising an ionic polysaccharide, a surfactant, and a polyoxyalkylene polyether having a molecular weight of about 10,000 to about 100,000 which is selected from the group consisting of
- A) polyoxyalkylene polyethers prepared by reacting ethylene oxide and at least one lower alkylene oxide having 3 to 4 carbon atoms with at least one active hydrogen-containing compound having from 3 to 10 carbon atoms and from 3 to 6 active hydrogens to prepare a heteric or block copolymer intermediate and further reacting said copolymer intermediate and further reacting said copolymer intermediate with at least one alpha-olefin oxide having an average carbon chain length of about 20 to about 45 aliphatic carbon atoms and wherein said alpha-olefin oxide is present in the amount of about 0.3 to 10 percent by weight based upon the total weight of said polyether and
- B) polyoxyalkylene polyethers prepared by reacting ethylene oxide with at least one active hydrogen-containing compound having from 2 to 10 carbon atoms and from 2 to 6 active hydrogens to prepare a homopolymer intermediate and further reacting said homopolymer with at least one alpha-olefin oxide having an average carbon chain length of about 20 to 45 aliphatic carbon atoms and wherein said alpha-olefin oxide is present in the amount of about 0.3 to 10 percent by weight based on the total weight of said polyether,
- C) a pharmacologically effective amount of a drug selected from the group consisting of antibacterials, antihistamines and decongestants, antiinflammatores, antiparasitics, miotics and anticholinergics, antivirals, local anesthetics, antifungals, amoebicidals, trichomonocidals, analgesics, mydriatics, antiglaucoma drugs, carbonic anhydrase inhibitors, opthalmic diagnostic agents, opthalmic agents used as adjuvants in surgery, chelating agents, antineoplastics, antihypertensives, and muscle relaxants, and diagnostics and
- D) optionally, a latent form of a counter-ion capable of cross-linking the ionic polysaccharide.
The process of claim 11, wherein said polyether is polyether (B) of claim 20.
Dependencies are inferred from the claim text.