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US 5,399,700 AGranted
Method for preparing enteric-coated oral drugs containing acid-unstable compounds
AssigneeSunkyong Industries Co., Ltd.
InventorsDong S. Min, Kee A. Um, Yong S. Kim, Pyong W. Park
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Abstract
The present invention relates to a method for preparing enteric-coated oral drugs containing acid-unstable compound, in particular an enteric-coated oral drug prepared in the form of acid-stable dosage units as inclusion complex formed by reacting benzimidazole derivative, acid-unstable compound, with cyclodextrin in alkaline solution.
Claims12
A method for stabilizing an acid-unstable compound by forming an inclusion complex of omeprazole with cyclodextrin comprising:
- dissolving cyclodextrin in an aqueous alkaline solution at 40.degree.-70.degree. C., and reacting said omeprazole with a cyclodextrin for 1 to 30 minutes in said alkaline solution, the ratio of said acid-unstable compound to said cyclodextrin in said reaction being from about 1:1 to about 1:10, on a number of moles basis.
A method for stabilizing a benzimidazole derivative having the following structural formula:
- ##STR2## wherein:
- R.sub.1 is selected from the group consisting of hydrogen, methoxy, trifluoromethyl and tetrafluoroethoxy radicals;
- R.sub.2 is selected from the group consisting of hydrogen, methylamine and dimethylamine radicals;
- R.sub.3 is selected from the group consisting of hydrogen, methoxy, aryloxy and propaziloxy radicals;
- and
- R.sub.4 is selected from the group consisting of hydrogen and methyl radicals;
- by forming an inclusion complex of said benzimidazole derivative with cyclodextrin comprising:
- A. Dissolving said cyclodextrin in an aqueous alkaline solution at a temperature between about 40.degree. and 70.degree. C.;
- and
- B. Reacting said cyclodextrin with said benzimidazole derivative for 1 to 30 minutes in said aqueous alkaline solution, the ratio of said benzimidazole derivative to said cyclodextrin being from about 1 to 10 moles of said cyclodextrin for each mole of said benzimidazole derivative.
7 more elements
Dependencies are inferred from the claim text.