Methanediphosphonic acid formulations with ion exchangers
AssigneeCiba-Geigy Corporation
InventorsSatish C. Khanna, Jonathan Green
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Abstract
The invention relates to a novel advantageous oral dosage form for methanediphosphonates, especially the active ingredient disodium pamidronate. A preferred dosage form comprises: a) disodium-3-amino-1-hydroxypropane-1,1-diphosphonate (disodium pamidronate), b) a cationic macroporous ion exchange resin based on a styrene/divinylbenzene copolymer having an exchangeable aminophosphonate group and, where appropriate, c) further pharmaceutically acceptable excipients. The ingredients can be processed to form tablets, dragees, capsules etc.
Claims13
A pharmaceutical composition for the oral administration of methanediphosphonic acid derivatives, comprising
- a) a methanediphosphonic acid derivative of formula:
- ##STR2## wherein one of R.sub.1 and R.sub.2 is hydrogen or hydroxy and the other is amino-C.sub.1-4 alkyl, C.sub.2-6 alkyleneamino-C.sub.1-4 alkyl, N-mono- or N,N-di-C.sub.1-8 alkylamino-C.sub.2-4 alkyl, C.sub.5-7 cycloalkylamino, heteroaryl-C.sub.1-4 alkyl or N-C.sub.1-4 alkyl-N-phenylthio-C.sub.1-4 alkylamino-C.sub.1-4 alkyl, or a pharmaceutically acceptable salt thereof,
- b) a cationic macroporous ion exchange resin based on a styrene/divinylbenzene copolymer having an exchangeable phosphonic acid methylaminomethyl group in the form of the cation-exchangeable mono- or di-sodium salt in an amount which enhances the abosorption of a), and,
- c) pharmaceutically acceptable excipients.
A process for the preparation of a pharmaceutical composition for the oral administration of a methanediphosphonic acid derivative, which comprises mixing together
- a) a compound of formula I, ##STR3## b) resin particles of a cationic ion exchanger based on a styrene/divinylbenzene copolymer having an exchangeable phosphonic acid methylaminomethyl group in the form of the cation-exchangeable mono- or di-sodium salt in an amount which enhances the absorption of a), and
- c) pharmaceutically acceptable excipients, and processing the mixture to produce an oral dosage form.
Dependencies are inferred from the claim text.