Direct compression tabletting composition and pharmaceutical tablets produced therefrom |
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| 申请号 | US40132273 | 申请日 | 1973-09-27 | 公开(公告)号 | US3873694A | 公开(公告)日 | 1975-03-25 |
| 申请人 | CPC INTERNATIONAL INC; | 发明人 | KANIG JOSEPH L; | ||||
| 摘要 | Method for producing a direct compression vehicle for tabletting which involves admixing a crystalline sugar with a maltodextrin and spraying the admixture with an aqueous solution of a maltodextrin. The resulting vehicle may be combined with a pharmaceutically active ingredient wherein the pharmaceutically active ingredient may be present in an amount of up to 80% of the weight of the vehicle. The resulting pharmaceutical composition can be compressed into a tablet having a Strong Cobb Hardness Unit (S.C.H.U.) value of at least about 6. | ||||||
| 权利要求 | 1. A METHOD FOR PRODUCING A DIRECT COMPRESSION VEHICLE FOR TABLETTING COMPRISING: A. ADMIXING A CRYSTALLINE SUGAR WITH FROM ABOUT 10 TO ABOUT 50% BY WEIGHT, BASED UPON THE WEIGHT OF SAID VEHICLE OF A MALTODEXTRIN HAVING A MEASURABLE DEXTROSE EQUIVALENT VALUE NOT SUBSTANTIALLY AOVE ABOUT 20 TO FORM A UNIFORM ADMIXTURE, B. CONCURREENTLY AGITATING AND SPRAYING SAID ADMIXTURE WITH AN AQUEOUS SOLUTION CONTAINING DISSOLVED THEREIN A MALTODEXTRIN HAVING A MEASURABLE DEXTROS EQUIVALENT VALUE NOT SUBSTANTIALLY ABOVE ABOUT 20, SAID AQUEOUS SOLUTION OF DISSOLVED MALTODEXTRIN BEING PRESENT IN AN AMOUNT SUFFICIENT TO PROVIDE A DAMP MASS OF SAID UNIFORM ADMIXTURE AND TO CAUSE GRANULATION OF SAID UNIFORM ADMIXTURE, AND C. DRYING SAID GRANULATION UNIFORM ADMIXTURE TO A MOISTURE CONTENT OF LESS THAN ABOUT 10% BY WEIGHT, BASED UPON THE WEIGHT OF SAID VEHICLE. 2. The process of claim 1, wherein said crystalline sugar is dextrose. 3. The process of claim 2, wherein the dextrose is a centrifuge cake containing up to about 16% by weight moisture, based upon the weight of the centrifuge cake. 4. The process of claim 1, wherein said crystalline sugar is admixed with from about 15 to about 35% by weight of said maltodextrin, based upon the weight of said vehicle. 5. The process of claim 1, wherein said aqueous solution contains from about 5 to about 40% weight/volume solution of said maltodextrin. 6. The process of claim 1, wherein said maltodextrin is a waxy starch hydrolysate having a dextrose equivalent value in the range of from about 9 to about 13 and a descriptive ratio of at least about 2, said descriptive ratio being the sum of the percentages (dry basis) of saccharides of the maltoDextrin with a degree of polymerization of 1 to 6 divided by the dextrose equivalent value. 7. A method for producing a direct compression vehicle for tabletting comprising: a. admixing a crystalline dextrose having a moisture content of up to about 16% by weight with from about 15 to about 35% by weight, based upon the weight of said vehicle, of a maltodextrin having a measurable dextrose equivalent value not substantially above about 20 to form a uniform admixture, b. concurrently agitating and spraying said uniform admixture with an aqueous solution containing dissolved therein from about 10% to about 40% weight/volume of a maltodextrin having a measurable dextrose equivalent value not substantially above about 20, said aqueous solution of dissolved maltodextrin being present in an amount sufficient to provide a damp mass of said uniform admixture, c. agitating said sprayed uniform admixture to uniformly intermingle said crystalline dextrose and maltodextrin with said aqueous solution to cause granulation of said admixture, and d. drying said granulated uniform admixture to a moisture content of less than about 10% by weight. 8. The method of claim 7, wherein the crystalline dextrose is admixed with from about 20 to about 30% by weight, based upon the weight of said vehicle, of said maltodextrin. 9. A directly compressible tabletting vehicle comprising a granulated mixture of a crystalline sugar and from about 10 to about 50% by weight, based upon the weight of said vehicle, of a water soluble maltodextrin having a measurable dextrose equivalent value not substantially above about 20, said granulated mixture containing less than about 10% by weight moisture, based upon the weight of said vehicle, said directly compressible tabletting vehicle in admixture with up to about 80% by weight, based upon the weight of said vehicle, of at least one pharmaceutically active ingredient, being characterized as capable of being formed by direct compression at a pressure as low as about 2000 pounds into hard, substantially non-friable tablets having a Strong Cobb Hardness Unit (S.C.H.U.) value of at least about 6. 10. The directly compressible tabletting vehicle of claim 9, wherein said crystalline sugar is dextrose. 11. The directly compressible vehicle of claim 9, wherein said water soluble maltodextrin is present in an amount ranging from about 15 to about 35% by weight, based upon the weight of said vehicle. 12. The directly compressible vehicle of claim 9, wherein the moisture content of said vehicle is less than about 5% by weight, based upon the weight of said vehicle. 13. A method for preparing tablets comprising forming an admixture of the product of claim 9 and an active material, said product comprising at least about 20% by weight of said vehicle, and compressing the mixture into tablets. 14. A method for preparing tablets comprising forming an admixture of the product of claim 10 and an active material, said product comprising at least 20% of said vehicle, and compressing the mixture into tablets. 15. The method of claim 14, wherein said active material is a pharmaceutically active material. 16. The method of claim 15, wherein said pharmaceutically active material is a member selected from the group consisting of ascorbic acid, sodium salicylate, acetaminophen, sodium bicarbonate, aluminum hydroxide, magnesium trisilicate, Vitamin E acetate, calcium lactate, ferrous sulfate and mixtures thereof. 17. A directly compressed pharmaceutical composition in tablet form, comprising a dry-blended mixture comprising: a. at least one pharmaceutically active ingredient present in an amount up to about 80% by weight, based upon the weight of said directly compressed pharmaceutical composition; and b. a directly compressible vehicle comprising a gRanulated mixture of a crystalline sugar and at least about 10% by weight, based upon the weight of the directly compressible vehicle, of a water soluble maltodextrin having a measurable dextrose equivalent value not substantially above about 20, said directly compressible vehicle containing less than about 10% by weight moisture, said directly compressible vehicle being present in an amount of at least about 20% by weight, based upon the weight of said directly compressed pharmaceutical composition, said directly compressed pharmaceutical composition being characterized as being hard and substantially non-friable, and being further characterized as having a Strong Cobb Hardness Unit (S.C.H.U.) value of at least about 6. 18. The directly compressed pharmaceutical composition of claim 17, wherein said crystalline sugar is dextrose. 19. The directly compressed pharmaceutical composition of claim 17, wherein said directly compressible vehicle comprises a granulated mixture of dextrose monohydrate granulated with 15 to about 35% by weight, based upon the weight of the vehicle, of a maltodextrin having a measurable dextrose equivalent value not substantially above about 20. 20. The directly compressed pharmaceutical composition of claim 17, wherein said pharmaceutically active ingredient is a member selected from the group consisting of ascorbic acid, sodium salicylate, acetaminophen, sodium bicarbonate, aluminum hydroxide, magnesium trisilicate, Vitamin E acetate, calcium lactate, ferrous sulfate and mixtures thereof. 21. The directly compressed pharmaceutical composition of claim 17, which additionally includes a small but effective amount of materials selected from the group consisting of lubricants, coloring aids, disintegrants, binders and mixtures thereof. 22. A directly compressed pharmaceutical composition in tablet form, comprising a dry-blended mixture comprising: a. ascorbic acid in an amount of up to about 80% by weight, based upon the weight of said pharmaceutical composition; and b. a directly compressible vehicle comprising a granulated mixture of dextrose and about 15% to about 35% by weight, based upon the weight of said vehicle, of water soluble maltodextrin having a measurable dextrose equivalent value not substantially above about 20, said vehicle containing less than about 10% by weight moisture. said directly compressed pharmaceutical tablet being characterized as being hard and substantially non-friable such that the tablet has a Strong Cobb Hardness Unit (S.C.H.U.) value of at least about 6. 23. The composition in accordance with claim 22, wherein said composition contains ascorbic acid in an amount from about 15 to about 35% by weight, based upon the weight of the tablet. 24. A directly compressible tabletting vehicle comprising a granulated mixture of dextrose and from about 15 to about 35% by weight, based upon the weight of the vehicle, of a water soluble maltodextrin having a measurable dextrose equivalent value not substantially above about 20, said granulated mixture containing less than about 5% by weight moisture, based upon the weight of said vehicle, said directly compressible tabletting vehicle in admixture with at least one pharmaceutically active ingredient in an amount of from about 15 to about 35% by weight, based upon the weight of the total composition, being characterized as capable of being formed by direct compression at a pressure as low as 2000 pounds into hard, substantially non-friable tablets having a Strong Cobb Hardness Unit (S.C.H.U.) value of at least about 6, said vehicle being further characterized as having a particle size in the range of from about -40 to about +100 mesh screen. 25. The directly compressible tabletting vehicle of claim 24, wherein said vehicle additionally contains a tabLetting lubricant. |
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