Claims
- 1. A pharmaceutical dosage unit composition consisting essentially of a gelatin capsule containing (1) a disintegrating core comprising (i) dipyridamole or an acid addition salt thereof and (ii) an acid substance in an amount sufficient to make the dipyridamole water-soluble and having a readily water-soluble coating, and (2) a plurality of non-disintegrating cores comprising (i) dipyridamole or an acid addition salt thereof and (ii) an acid substance in an amount sufficient to make the dipyridamole water-soluble and having a coating consisting of from 20 to 90 percent by weight of a water-insoluble film former and from 10 to 80 percent by weight of a water-soluble polymer, the diameter of each of the disintegrating and non-disintegrating cores being at least about 5 mm.
- 2. The dosage unit composition of claim 1, wherein the acid substance is selected from the group consisting of citric acid and tartaric acid.
- 3. The dosage unit composition of claim 1, wherein the molar ratio of dipyridamole to acid substance is from about 1:1 to 1:3.
- 4. The dosage unit composition of claim 1, wherein the readily water-soluble coating comprises 90 percent by weight of hydroxypropylmethyl cellulose and 10 percent by weight of polyethylene glycol.
- 5. The dosage unit composition of claim 1, wherein the water-insoluble film former is selected from the group consisting of ethyl cellulose and polymeric lacquer substances based upon acrylate or methacrylate.
- 6. The dosage unit composition of claim 5, wherein the water-insoluble film former is ethyl cellulose.
- 7. The dosage unit composition of claim 1, wherein the water-soluble polymer is selected from the group consisting of polyethylene glycol, methyl cellulose, and polyvinyl pyrrolidone.
- 8. The dosage unit composition of claim 1, wherein the coating on the non-disintegrating cores also contains up to 80 percent by weight of an acid-insoluble polymer.
- 9. The dosage unit composition of claim 8, wherein the acid-insoluble polymer is selected from the group consisting of cellulose acetate phthalate, hydroxypropylmethyl cellulose phthalate, and partially esterified polymethacrylic acid optionally containing a softening agent.
- 10. The dosage unit composition of claim 1, wherein the cores are tablets or pellets.
- 11. The dosage unit composition of claim 1, wherein the cores have a diameter of from about 5 to 6.2 mm.
- 12. The dosage unit composition of claim 1, wherein the dipyridamole or acid addition salt thereof is present in a total amount of from 150 to 400 mgm.
- 13. The dosage unit composition of claim 1 consisting essentially of a gelatin capsule containing (1) a disintegrating tablet comprising dipyridamole and an acid substance selected from the group consisting of citric acid and tartaric acid, the molar ratio of dipyridamole to acid substance being from about 1:1 to 1:3, said tablet having a coating consisting of 90 percent by weight of hydroxypropylmethyl cellulose and 10 percent by weight of polyethylene glycol, and (2) five non-disintegrating tablets comprising dipyridamole and an acid substance selected from the group consisting of citric acid and tartaric acid, the molar ratio of dipyridamole to acid substance being from about 1:1 to 1:3, each of said non-disintegrating tablets having a coating consisting of from about 20 to 90 percent by weight of a water-insoluble film former and from 10 to 80 percent by weight of a water-soluble polymer, the diameter of each of the tablets being about 6.2 mm.
- 14. A method for the treatment of cardiovascular disorders in a host in need of such treatment which comprises administering to said host a cardiovascularly effective amount of a composition of claim 1.
- 15. The method of claim 14, wherein the acid substance is selected from the group consisting of citric acid and tartaric acid.
- 16. The method of claim 14, wherein the molar ratio of dipyridamole to acid substance is from about 1:1 to 1:3.
- 17. The method of claim 14, wherein the readily water-soluble coating comprises 90 percent by weight of hydroxypropylmethyl cellulose and 10 percent by weight of polyethylene glycol.
- 18. The method of claim 14, wherein the water-insoluble film former is selected from the group consisting of ethyl cellulose and polymeric lacquer substances based upon acrylate or methacrylate.
- 19. The method of claim 18, wherein the water-insoluble film former is ethyl cellulose.
- 20. The method of claim 14, wherein the water-soluble polymer is selected from the group consisting of polyethylene glycol, methyl cellulose, and polyvinyl pyrrolidone.
- 21. The method of claim 14, wherein the coating on the non-disintegrating cores also contains up to 80 percent by weight of an acid-insoluble polymer.
- 22. The method of claim 21, wherein the acid-insoluble polymer is selected from the group consisting of cellulose acetate phthalate, hydroxypropylmethyl cellulose phthalate, and partially esterified polymethacrylic acid optionally containing a softening agent.
- 23. The method of claim 14, wherein the cores have a diameter of from about 5 to 6.2 mm.
- 24. The method of claim 14, wherein the dipyridamole or acid addition salt thereof is present in a total amount of from 150 to 400 mgm.
- 25. The method of claim 14, wherein the dosage unit composition consists essentially of a gelatin capsule containing (1) a disintegrating tablet comprising dipyridamole and an acid substance selected from the group consisting of citric acid and tartaric acid, the molar ratio of dipyridamole to acid substance being from about 1:1 to 1:3, and tablet having a coating consisting of 90 percent by weight of hydroxypropylmethyl cellulose and 10 percent by weight of polyethylene glycol, and (2) five non-disintegrating tablets comprising dipyridamole and an acid substance selected from the group consisting of citric acid and tartaric acid, the molar ratio of dipyridamole to acid substance being from about 1:1 to 1:3, each of said non-disintegrating tablets having a coating consisting of from about 20 to 90 percent by weight of a water-insoluble film former and from 10 to 80 percent by weight of a water-soluble polymer, the diameter of each of the tablets being about 6.2 mm.
Priority Claims (10)
Number |
Date |
Country |
Kind |
2831164 |
Jul 1978 |
DEX |
|
2836355 |
Aug 1978 |
DEX |
|
2836356 |
Aug 1978 |
DEX |
|
2836357 |
Aug 1978 |
DEX |
|
2836358 |
Aug 1978 |
DEX |
|
2836387 |
Aug 1978 |
DEX |
|
2836388 |
Aug 1978 |
DEX |
|
2836419 |
Aug 1978 |
DEX |
|
2836477 |
Aug 1978 |
DEX |
|
2905602 |
Feb 1979 |
DEX |
|
Parent Case Info
This is a continuation of Ser. No. 194,852, filed Oct. 7, 1980, now abandoned.
US Referenced Citations (13)
Foreign Referenced Citations (2)
Number |
Date |
Country |
1469133 |
Mar 1977 |
GBX |
1510573 |
Oct 1978 |
GBX |
Non-Patent Literature Citations (1)
Entry |
Spitael et al., Pharmazeutische Industrie 39(5): 502-505 (1977) Factors Affecting the Dissolution Rate of Enterig Coatings. |
Continuations (1)
|
Number |
Date |
Country |
Parent |
194852 |
Oct 1980 |
|