Back to results
US 5,346,703 AGranted
Body cavity drug delivery with thermo-irreversible polyoxyalkylene and ionic polysaccharide gels
AssigneeMediventures, Inc.
InventorsTacey X. Viegas, Lorraine E. Reeve, Raymond L. Henry
Life of this patent
Estimating the term…
Abstract
Balanced pH, thermo-irreversible gels are ideal vehicles for drug delivery to a body cavity of a mammal. The gels contain a mixture of a polyoxyalkylene block copolymer or polyether together with an ionic polysaccharide which is thermo-irreversibly gelled in the presence of a counter-ion.
Claims28
A pharamaceutical aqueous gel composition, said composition comprising
- (1) about 0.2% to about 2.5% by weight of an ionic polysaccharide;
- (2) about 10% to about 50% by weight of a polyoxyalkylene block copolymer of general formula
- Y[(A).sub.n - - - E - - - H].sub.x
- where A is a polyoxyalkylene moiety having an oxygen/carbon atom ratio of less than 0.5, x is at least 2, Y is derived from water or an organic compound containing x reactive hydrogen atoms, E is a polyoxyethylene moiety constituting at least 60 percent by weight of the polyoxyalkylene block copolymer, n has a value such that the minimum molecular weight of A is between about 500 and about 900, as determined by the hydroxyl number of an intermediate of general formula
- Y [(A).sub.n - - - H].sub.x
- and the average molecular weight of the polyoxyalkylene block copolymer is between about 5000 and about 50,000;
- (3) about 0.01% to about 60% by weight of a pharmacologically effective amount of a drug selected from the group consisting of antibacterials, antihistamines, decongestants, antiinflammatories, antiparasitics, antivirals, local anesthetics, antifungals, analgesics, antiarthritics, antiastrunatics, anticoagulants, anticonvulsants, antidepressants, antidiabetics, antieoplastics, antipsychotics, antihypertensives, spermicidals, and muscle relaxants;
- (4) a pharmaceutically acceptable buffer sufficient to maintain the p.sub.H of the aqueous gel composition at a desired level;
- and
- (5) optionally, a latent form of a counter-ion capable of cross-linking the ionic polysaccharide,
- wherein the aqueous gel composition is a liquid at room temperature or below and a gel at mammalian body temperature.
8 more elements
A hyperosomotic, iso-osmotic, or hypoosmotic aqueous gel composition comprising
- (1) about 0.2% to about 2.5% by weight of an ionic polysaccharide;
- (2) about 10% to about 50% by weight of a polyoxyalkylene block copolymer of general formula
- Y[(A).sub.n - - - E - - - H].sub.x
- where A is a polyoxyalkylene moiety having an oxygen/carbon atom ratio of less than 0.5, x is at least 2, Y is derived from water or an organic compound containing x reactive hydrogen atoms, E is a polyoxyethylene moiety constituting at least 60 percent by weight of the polyoxyalkylene block copolymer, n has a value such that the minimum molecular weight of A is between about 500 and about 900, as determined by the hydroxyl number of an intermediate of general formula
- Y[(A).sub.n - - - H].sub.x
- and the average molecular weight of the polyoxyalkylene block copolymer is between about 5000 and about 50,000;
- and
- (3) optionally, a latent form of a counter-ion capable of cross-linking the ionic polysaccharide, wherein the aqueous gel composition is a liquid at room temperature or below and a gel at mammalian body temperature.
5 more elements
A hyperosmottc, iso-osmotic, or hypoosmotic aqueous gel composition having a desired osmolality and pH, said composition comprising
- (1) about 0,2% to about 2.5% by weight of an ionic polysaccharide;
- (2) about 0.1% to about ! 0% by weight of a combination of a surfactant and a polyoxyalkylene polyether, wherein sais polyether having a molecular weight of about 10,000 to about 100,000 which is selected from the group consisting of
- (A) a polyoxalkylene polyether 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 heretic or block copolymer intermediate and further reacting the copolymer intermediate with at least one alpha-olefin oxide having an average carbon chain length of about 20 to about 45 aliphatic carbon atoms, wherein the alpha-olefin oxide is present in the amount of about 0.3 to about 10 percent by weight based on the total weight of the polyether;
- and
- (B) a polyoxalkylene polyether 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 the homopolymer intermediate with at least one alpha-olefin oxide having an average carbon chain length of about 20 to 45 aliphatic carbon atoms, wherein the alpha-olefin oxide is present in the amount of about 0.3 to 10 percent by weight based on the total weight of the polyether;
- and
- (3) optionally, a latent form of a counter-ion capable of cross-linking the ionic polysaccharide.
4 more elements
Dependencies are inferred from the claim text.