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Claims for Patent: 4,873,080

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Claims for Patent: 4,873,080

Title: Oral anti-diabetic pharmaceutical compositions and the preparation thereof
Abstract:Galenic compositions containing an oral antidiabetic agent and having an improved release of active substance as well as processes for producing these compositions are provided. The pharmaceutical compositions are characterized in that the onset of the activity and the duration of activity are adapted to the particular needs of diabetics with regard to proper control of metabolism and the associated proper release of insulin. A basic or acidic excipient in a solvent is added to the anti-diabetically active substance in a quantity such that the active substance is made soluble, and then a solubilizing agent is added. The solution is applied to a water-insoluble carrier, the solvent is evaporated, and the residue is further processed to yield the various compositions.
Inventor(s): Brickl; Rolf (Warthausen, DE), Schepky; Gottfried (Biberach, DE), Rupprecht; Eckhard (Aulendorf-Tannhausen, DE), Greischel; Andreas (Biberach, DE)
Assignee: Dr. Karl Thomae GmbH (Biberach an der Riss, DE)
Application Number:07/103,524
Patent Claims: 1. The method of preparing an oral antidiabetic pharmaceutical composition containing an antidiabetic benzoic acid as the active ingredient, which comprises dissolving or emulsifying

(a) an acid antidiabetic benzoic acid with a basic excipient, or

(b) an amphoteric antidiabetic benzoic acid with a basic or acid excipient, or

(c) a basic antidiabetic benzoic acid with an acid excipient in an inert polar solvent in the presence of at least one solubilizing or emulsifying substance, where the molar ratio of benzoic acid to basic or acid excipient is less than 1:1 and the ratio of benzoic acid to the total of solubilizing or emulsifying substance is from about 1:0.5 to 1:10 parts by weight, applying the resulting solution or emulsion to the surface of at least one water-insoluble carrier, where the ratio of benzoic acid to the total of water-insoluble carrier is from 1:1 to 1:12 parts by weight, and drying the thus treated water-insoluble carrier.

2. The method of claim 1, wherein the dry treated water-insoluble carrier is combined with a conventional pharmaceutical excipient to produce the desired oral antidiabetic pharmaceutical composition.

3. The method of claim 1, where said benzoic acid is 2-Ethoxy-4-[2-oxo-2-[(.alpha.-isobutyl-2-piperidino-benzyl)-amino]-ethyl]b enzoic acid.

4. The method of claim 1, where said basic excipient is sodium hydroxide, potassium hydroxide, ammonia, tert.sodium phosphate, diethanolamine, ethylenediamine, N-methyl-glucamine or L-lysine, and said acid excipient is sulfuric acid, phosphoric acid or tartaric acid.

5. The method of claim 1, where the molar ratio of benzoic acid to basic or acid excipient is 1:1.8 to 1:10.

6. The method of claim 1, wherein the water-insoluble carrier is selected from the group consisting of highly dispersed silicon dioxide, microcrystalline cellulose, basic aluminum oxide, magnesium-aluminum-trisilicate, cross-linked polyvinylpyrrolidone, sodium carboxymethyl starch, tricalcium phosphate, calcium biphosphate and mixtures thereof, and the solubilizing or emulsifying substance is selected from the group consisting of polyvinylpyrrolidone, polyethylene glycol, polyethoxylated sorbitan monooleate, sorbitol, polyoxyethylene polyoxypropylene polymer, polyoxyethylene fatty alcohol ether, glycerol polyethylene glycoloxy stearate, and mixtures thereof.

7. The method of claim 1, wherein the solubilizing substance is polyvinylpyrrolidone, polyoxyethylene polyoxypropylene polymer or a mixture thereof.

8. The method of claim 1, wherein the basic excipient is selected from the group consisting of a pharmacologically acceptable inorganic and organic base.

9. An oral antidiabetic pharmaceutical composition consisting essentially of a conventional pharmaceutical excipient and a dry water-insoluble carrier having applied to the surface thereof the evaporation residue of a solution or emulsion of an effective antidiabetic amount of an acid, amphoteric or basic antidiabetic benzoic acid, a basic or acid excipient, and at least one solubilizing or emulsifying substance in an inert polar solvent, where the molar ratio of benzoic acid to basic or acid excipient is less than 1:1, the ratio of benzoic acid to the total of solubilizing or emulsifying substance is from 1:0.5 to 1:10 by weight, and the ratio of benzoic acid to the total of water-insoluble carrier is from 1:1 to 1:12 parts by weight.

10. A composition of claim 9, where said benzoic acid is 2-Ethoxy-4-[2-oxo-2-[(.alpha.-isobutyl-2-piperidino-benzyl)-amino]-ethyl]b enzoic acid.

11. A composition of claim 9, where said basic excipient is sodium hydroxide, potassium hydroxide, ammonia, tert.sodium phosphate, diethanolamine, ethylenediamine, N-methyl-glucamine or L-lysine, and said acid excipient is sulfuric acid, phosphoric acid or tartaric acid.

12. A composition of claim 9, where the molar ratio of benzoic acid to basic or acid excipient is from 1:1.8 to 1:10.

13. A composition of claim 9, wherein the basic excipient is selected from the group consisting of a pharmacologically acceptable inorganic or organic base, the acid excipient is sulfuric acid or tartaric acid, the water-insoluble carrier is selected from the group consisting of highly dispersed silicon dioxide, microcrystalline cellulose, basic aluminum oxide, magnesium-aluminum-trisilicate, cross-linked polyvinylpyrrolidone, sodium carboxymethyl starch, tricalcium phosphate, calcium biphosphate and mixtures thereof, and the solubilitizing or emulsifying substance is selected from the group consisting of polyvinylpyrrolidone, polyethylene glycol, polyethoxylated sorbitan monooleate, sorbitol, polyoxyethylene polyoxypropylene polymer, glycerol polyethylene glycoloxy stearate and mixtures thereof.

14. A method for the treatment of diabetes in a warmblooded host in need of such treatment, which comprises orally administering to said warm-blooded host a composition of claim 9.
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