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Claims for Patent: 5,286,497

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Claims for Patent: 5,286,497

Title: Diltiazem formulation
Abstract:The present invention is directed to a diltiazem formulation suitable for one a day administration. The formulation contains a blend of diltiazem beads having two differing dissolution profiles.
Inventor(s): Hendrickson; Dennis L. (Overland Park, KS), Dimmitt; Dan C. (Belton, MO), Williams; Mark S. (Kansas City, MO), Skultety; Paul F. (Leawood, KS), Baltezor; Michael J. (Lees Summit, MO)
Assignee: Carderm Capital L.P. (Thalwil, CH)
Application Number:08/058,534
Patent Claims: 1. A diltiazem formulation suitable for once-a-day oral administration comprising a blend of:

A) a sufficient quantity of rapid release diltiazem beads which further comprise

1) a diltiazem core containing an effective amount of diltiazem of a pharmaceutically acceptable salt thereof, optionally in association with pharmaceutically acceptable excipients and;

2) a sufficient quantity of a first suitable polymeric coating material which substantially envelops said diltiazem core so that said diltiazem bead exhibits the following in-vitro dissolution profile when measured in a type 2 dissolution apparatus (paddle) according to U.S. Pharmacopeia XXII at 37.degree. C. at 100 rpm:

a) from 0-40% of total diltiazem is released after 3 hours of measurement in said apparatus, and;

b) from 30-100% of total diltiazem is released after 6 hours of measurement in said apparatus, and;

B) a sufficient quantity of delayed release diltiazem beads which further comprise:

1) a central core containing an effective amount of diltiazem or a pharmaceutically acceptable salt thereof, optionally in association with pharmaceutically acceptable excipients, and;

2) a sufficient quantity of a second suitable polymeric coating material which substantially envelops said diltiazem core so that said diltiazem bead exhibits the following in-vitro dissolution profile when measured in a type 2 dissolution apparatus (paddle) according to U.S. Pharmacopeia XXII, at 37.degree. C. in 0.1N HCl at 100 rpm:

a) from 0-15% of total diltiazem is released after 12 hours in said apparatus;

b) from 0-45% of total diltiazem is released after 18 hours of measurement in said apparatus, and;

c) not less than 45% of total diltiazem is released after 24 hours of measurement in said apparatus,

wherein said blend exhibits the following in-vitro dissolution pattern when measured in a type 2 dissolution apparatus (paddle), according to U.S. Pharmacopeia XXII, in 0.1N HCl at 100 rpm:

a) from 20-45% of total diltiazem is released after 6 hours of measurement in said apparatus;

b) from 25-50% of total diltiazem is released after 12 hours of measurement in said apparatus;

c) from 35-70% of total diltiazem is released after 18 hours of measurement in said apparatus;

d) not less than 70% of total diltiazem is released after 24 hours of measurement in said apparatus; and

e) not less than 85% of total diltiazem is released after 30 hours of measurement in said apparatus.

2. A diltiazem formulation according to claim 1 in which said second polymeric coating of said delayed release diltiazem bead contains from 10-75 w/w % of polymerized acrylate based upon the total weight of the polymeric coating of a dried delayed release diltiazem bead.

3. A diltiazem formulation according to claim 2 in which said second polymeric coating comprises from 15-50 w/w % of the total weight of a dried delayed release diltiazem bead.

4. A diltiazem formulation according to claim 3 in which said polymerized acrylate is a copolymer of ethyl acrylate and methyl methacrylate which contains trimethylammoniumethyl methacrylate in a range of about 1:40 relative to the neutral monomers.

5. A diltiazem formulation according to claim 4 in which said second polymeric coating contains a plasticizer in the range of 5-15 w/w % based upon the total weight of the polymeric coating of a dried delayed release diltiazem bead.

6. A diltiazem formulation according to claim 5 in which said plasticizer is tributyl citrate and acetyl tributyl citrate.

7. A diltiazem formulation according to claim 6 in which said second polymeric coating comprises about 25 w/w % of the total weight of a dried delayed released diltiazem bead.

8. A diltiazem formulation according to claim 7 in which said second polymeric coating contains

a) a copolymer of ethyl acrylate and methyl methacrylate which contains trimethylammoniumethyl methacrylate in a range of about 1:40 relative to the neutral monomers and

b) a copolymer of ethyl acrylate and methyl methacrylate which contains trimethylammoniumethyl methacrylate in a range of about 1:20 relative to the neutral monomers wherein the ratio of copolymer a) to copolymer b) is 95:5.

9. A diltiazem formulation according to claim 8 wherein said delayed release diltiazem bead exhibits the following in-vitro dissolution profile in 0.1N HCl:

a) from 0-5% of total diltiazem is released after 6 hours of measurement in said apparatus,

b) from 0-10% of total diltiazem is released after 12 hours of measurement in said apparatus,

c) from 0-35% of total diltiazem is released after 18 hours of measurement in said apparatus, and,

d) from 50-90% of total diltiazem is released after 24 hours of measurement in said apparatus.

10. A diltiazem formulation according to claim 1 in which said rapid release diltiazem bead exhibits the following dissolution rate:

a) from 0-20% of total diltiazem is released after 3 hours of measurement in said apparatus, and;

b) from not less than 50% of total diltiazem is released after 6 hours of measurement in said apparatus.

11. A diltiazem formulation according to claim 10 in which said first polymeric coating of said rapid release diltiazem bead contains

a) a copolymer of ethyl acrylate and methyl methacrylate which contains trimethylammoniumethyl methacrylate in a range of about 1:40 relative to the neutral monomers and

b) a copolymer of ethyl acrylate and methyl methacrylate which contains trimethylammoniumethyl methacrylate in a range of about 1:20 relative to the neutral monomers wherein the ratio of copolymer a) to copolymer b) is 95:5.

12. A diltiazem formulation according to claim 11 wherein said first polymeric coating comprises from 10-15 w/w % of the total weight of a dried rapid release diltiazem bead.

13. A diltiazem formulation according to claim 1 wherein said blend exhibits the following in-vitro dissolution profile:

a) from 25-40% of total diltiazem is released after 6 hours of measurement in said apparatus;

b) from 30-45% of total diltiazem is released after 12 hours of measurement in said apparatus;

c) from 40-65% of total diltiazem is released after 18 hours of measurement in said apparatus; and

d) not less than 75% of total diltiazem is released after 24 hours of measurement in said apparatus.
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