Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Capsules
Reexamination Certificate
1997-03-04
2001-06-12
Levy, Neil S. (Department: 1617)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Capsules
C424S462000, C424S495000, C424S497000, C424S480000, C523S122000, C514S282000
Reexamination Certificate
active
06245351
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention relates to a controlled-release composition comprising a drug-containing core coated with a coating composition comprising a water-insoluble substance and a swellable polymer having no basic groups.
2. Description of the Related Art
Controlled-release preparations of drugs, especially sustained-release preparations, are advantageous in that administration frequency can be reduced by maintaining a constant plasma concentration of drug over an extended period of time to ensure sustained effect of the active ingredient. In addition, such preparations are also expected to decrease side effects by suppressing the rapid rise in the blood level of drug. Therefore, a large number of controlled-release systems, including capsular preparations comprising a drug-containing core coated with a release-controlling film (Japanese Patent Unexamined Publication Nos. 145056/1995 and 206679/1995, Canadian Patent Unexamined Publication No. 2,068,366, WO 94/22431, EP0377518, EP0630646, EP0631781, Japanese Patent Examined Publication No. 72130/1995). In such capsular preparation, the release-controlling film is made of the hydrophobic polymer containing a hydrophilic or a water-soluble substance, and release or releasing rate of the drug is designed to control by the formula of the film.
There are many drugs whose absorption rate in the large intestine is not as good as in the small intestine. In view of the fact that controlled-release compositions in the form of oral preparations pass through the small intestine in relatively short time, for example, active ingredient generally reaches the large intestine in about 5-6 hours in such composition, it is difficult to design a sustained-release preparation of such drugs for once- or twice-a-day administration that is required to maintain an effective plasma concentration of drug for 12-24 hours, because the absorption of the drugs would be suppressed after 5-6 hours following administration. Also, even a drug absorbable from the entire gastrointestinal tract often undergoes extremely suppressed drug release in the large intestine due to drug concentration reduction in the release-controlling preparation and water loss in the lower gastrointestinal tract during passage through the gastrointestinal tract. Thus it is difficult to obtain a satisfactory sustained-release preparation, especially those of the drugs mainly absorbed at small intestine.
SUMMARY OF THE INVENTION
With this situation in mind, the present inventors made extensive investigation to develop a controlled-release composition for oral administration coated with a coating composition which is capable of releasing the drug at higher rates in the intestinal tract than in the stomach to maintain an almost constant plasma concentration of drug and ensure effect of drug in the body for an extended period of time. Based on the findings that a controlled-release composition comprising a drug-containing core coated with a coating composition comprising a water-insoluble substance and a swellable polymer having no basic groups shows greater release rates in the small and large intestines than in the stomach through which it passes just after oral administration the present invention is developed.
Accordingly, the present invention relates to;
(1) a controlled-release composition comprising a drug-containing core coated with a coating composition comprising a water-insoluble substance and a swellable polymer having no basic group,
(2) the controlled-release composition of (1), wherein said water-insoluble substance has film-forming ability,
(3) the controlled-release composition of (1), wherein said water-insoluble substance is a cellulose ether or cellulose ester,
(4) the controlled-release composition of (1), wherein said water-insoluble substance is ethyl cellulose.
(5) the controlled-release composition of (1), wherein said swellable polymer has an acidic dissociating group and shows pH-dependent swelling.
(6) the controlled-release composition of (1), wherein said swellable polymer is a crosslinked acrylic polymer.
(7) the controlled-release composition of (5), wherein the molecular weight of said swellable polymer is about 1,000,000 to about 10,000,000.
(8) the controlled-release composition of (1), wherein the viscosity of said swellable polymer is about 1,500 to about 60,000 cp in 0.2% neutral solution.
(9) the controlled-release composition of (1), wherein said coating composition may further contain a hydrophilic substance.
(10) the controlled-release composition of (9), wherein said hydrophilic substance is a polysaccharide having a hydroxyalkyl group or carboxyalkyl group.
(11) the controlled-release composition of (9), wherein said hydrophilic substance is hydroxypropylmethyl cellulose.
(12) the controlled-release composition of (1), wherein the ratio of said coating composition to said core is not lower than 1% (w/w).
(13) the controlled-release composition of (1), wherein the content ratios of the water-insoluble substance and swellable polymer in said coating composition are about 40 to about 95% (w/w) and about 1 to about 40% (w/w), respectively.
(14) the controlled-release composition of (9), wherein the content ratios of the water-insoluble substance, swellable polymer and hydrophilic substance in said coating composition are about 40 to about 95% (w/w), about 1 to about 40% (w/w) and 0 to about 40% (w/w), respectively.
(15) the controlled-release composition of (1), wherein said water-insoluble substance is ethyl cellulose and said swellable polymer is a crosslinked acrylic polymer.
(16) the controlled-release composition of (1), wherein said drug is an opioid compound.
(17) the controlled-release composition of (14), wherein said drug is morphine or a salt thereof.
(18) the controlled-release composition of (1), wherein said drug is a sympathamimetics.
(19) the controlled-release composition of (1), wherein the content of said drug is not lower than 0.5% (w/w).
(20) the controlled-release composition of (1) in the form of granules, fine granules, tablets or capsules.
(21) a coating composition comprising a water-insoluble substance and a swellable polymer having no basic groups.
(22) the coating composition of (21), which further contains a hydrophilic substance.
(23) A method of producing a controlled-release composition which comprises coating a drug-containing core with a coating composition comprising a water-insoluble substance and a swellable polymer having no basic group.
(24) use of a coating composition comprising a water-insoluble substance and a swellable polymer having no basic group for manufacturing a medicament for a once daily oral treatment of a drug.
(25) a method for the treatment of pain-associated condition which comprises administering to a mammal in need thereof an effective amount of medicament containing the controlled-release composition of (17) or (18).
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Akiyama Yohko
Nakamura Kenji
Nara Eiji
Levy Neil S.
Takeda Chemical Industries Ltd.
Wenderoth , Lind & Ponack, L.L.P.
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