Matrix compositions for controlled delivery of drug substances
First Claim
1. A controlled release pharmaceutical composition for oral use in the form of a coated matrix composition, the matrix composition comprising i) a mixture of a first and a second polymer that have plasticizing properties and which have melting points or melting intervals of a temperature of at the most 200°
- C., the first polymer being selected from the group consisting of polyethylene glycols and polyethylene oxides having a molecular weight of at least about 20,000 in crystalline and/or amorphous form or a mixture such polymers, and the second polymer being selected from poloxamers having a HLB value of at least about 18 ii) a therapeutically, prophylactically and/or diagnostically active substance, wherein the concentration of the second polymer in the matrix composition is from about 5 to about 90% w/w, the matrix composition being provided with a coating having at least one opening exposing at one surface of said matrix, the coating comprising i) a first cellulose derivative which has thermoplastic properties and which is substantially insoluble in the aqueous medium in which the composition is to be used, and at least one of ii) a second cellulose derivative which is soluble or dispersible in water, iii) a plasticizer, and iv) a filler, wherein the active substance is released with a substantially zero order release.
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Accused Products
Abstract
A novel matrix composition for pharmaceutical use. The matrix composition has been designed so that it is especially suitable in those situation where an improved bioavailability is desired and/or in those situation where a slightly or insoluble active substance is employed. Accordingly, a controlled release pharmaceutical composition for oral use is provided in the form of a coated matrix composition, the matrix composition comprising i) a mixture of a first and a second polymer that have plasticizing properties and which have melting points or melting intervals of a temperature of at the most 200° C., the first polymer being selected from the group consisting of polyethylene glycols and polyethylene oxides, and the second polymer being selected form block copolymer of ethylene oxide and propylene oxide including poly(ethylene-glycol-b-(DL-lactic acid-co-glycolic acid)-b-ethylene glycol (PEG-PLGA PEG), poly((DL-lactic acid-co-glycolic acid)-g-ethylene glycol) (PLGA-g-PEG), poloxamers and polyethylene oxide-polypropylene oxide (PEO-PPO), ii) a therapeutically, prophylactically and/or diagnostically active substance, the matrix composition being provided with a coating having at least one opening exposing at one surface of said matrix, wherein the active substance is released with a substantially zero order release.
121 Citations
68 Claims
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1. A controlled release pharmaceutical composition for oral use in the form of a coated matrix composition, the matrix composition comprising
i) a mixture of a first and a second polymer that have plasticizing properties and which have melting points or melting intervals of a temperature of at the most 200° - C.,
the first polymer being selected from the group consisting of polyethylene glycols and polyethylene oxides having a molecular weight of at least about 20,000 in crystalline and/or amorphous form or a mixture such polymers, and the second polymer being selected from poloxamers having a HLB value of at least about 18 ii) a therapeutically, prophylactically and/or diagnostically active substance, wherein the concentration of the second polymer in the matrix composition is from about 5 to about 90% w/w, the matrix composition being provided with a coating having at least one opening exposing at one surface of said matrix, the coating comprising i) a first cellulose derivative which has thermoplastic properties and which is substantially insoluble in the aqueous medium in which the composition is to be used, and at least one of ii) a second cellulose derivative which is soluble or dispersible in water, iii) a plasticizer, and iv) a filler, wherein the active substance is released with a substantially zero order release. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68)
- C.,
Specification