Drugs containing S(+)-ibuprofen
AssigneeSpirig AG, Pharmazeutische Praeparate
InventorsGerd Birrenbach, Rolf-Dieter Juch
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Abstract
Rapid-release S(+)-ibuprofen pellets are proposed whose bioavailability is comparable to that of commercially available racemate formulations. The rapid release of the active substance is promoted by using small amounts of basic inorganic salts, preferably sodium carbonate, or dilute alkali metal hydroxide solutions. Pellets with an active substance content of 90-99% by weight are obtainable in this way. The pellets are suitable for the application of coatings. Pellets with a protective coating can be compressed directly to tablets in this form and with small amounts of suitable tableting adjuncts. The use of the pharmacologically active S(+)-ibuprofen and of the small amounts of adjuncts required makes it possible to prepare compact pharmaceutical forms.
Claims47
S(+)-Ibuprofen pellets containing 90.0-99.0% by weight of S(+)-ibuprofen and 0.1-10.0% by weight of a basic compound selected from the group consisting of basic inorganic salts, dilute alkali metal hydroxide solutions, and mixtures thereof.
S(+)-Ibuprofen pellets containing 90.0-99.0% by weight of S(+)-ibuprofen, 0.1-5.0% by weight of silicon dioxide and 0.1-10.0% by weight of sodium carbonate.
Coated S(+)-ibuprofen pellets containing 90.0-99.0% by weight of S(+)-ibuprofen and 0.1-10.0% by weight of a basic compound selected from the group consisting of basic inorganic salts, dilute alkali metal hydroxide solutions, and mixtures thereof, said coated pellets having a coating selected from the group consisting of protective coatings, coatings resistant to gastric juice, delayed-release coatings, and mixtures thereof.
Tablets comprising coated S(+)-ibuprofen pellets containing 90.0-99.0% by weight of S(+)-ibuprofen and 0.1-10.0% by weight of a basic compound selected from the group consisting of basic inorganic salts, dilute alkali metal hydroxide solutions, and mixtures thereof,
- said coated pellets having a coating selected from the group consisting of protective coatings, coatings resistant to gastric juice, delayed-release coatings, and mixtures thereof,
- said coated tablets further comprising 73.0-410.0 mg of at least one tableting auxiliary per 400.0 mg of S(+)-ibuprofen.
Tablets comprising coated pellets according to claim 10 and 73.0-410.0 mg of at least one tableting auxiliary per 400.0 mg of S(+)-ibuprofen.
A process for the preparation of S(+)-ibuprofen pellets comprising the steps of
- mixing S(+)-ibuprofen with at least one adjunct,
- spraying the mixture with an aqueous solution in a Diosna mixer or a rotary processor until pellets of the desired size are formed, and
- drying said pellets.
A process for the preparation of coated S(+)-ibuprofen pellets comprising the steps of mixing S(+)-ibuprofen with at least one adjunct,
- spraying the mixture with an aqueous solution in a Diosna mixer or a rotary processor until pellets of the desired size are formed,
- drying said pellets, and
- spraying said pellets with a coating.
A method of preparing tablets containing coated S(+)-ibuprofen pellets comprising the step of compressing coated S(+)-ibuprofen pellets directly into tablets with at least one tableting auxiliary.
Dependencies are inferred from the claim text.