PHARMACEUTICAL COMPOSITIONS FOR RELEASE CONTROL OF METHYLPHENIDATE

• US 20110223247A1
• Filed: 11/06/2009
• Published: 09/15/2011
• Est. Priority Date: 11/07/2008
• Status: Active Grant

• Current Assignee: Samyang Holdings Corporation
• Original Assignee: Samyang Corporation (Samyang Holdings Corporation)
• Inventors: Chung, Hojin, Park, Sang Yeob, Pai, Chaul Min
• Granted Patent: US 8,465,768 B2
• Time in Patent Office: Days
• US Class Current: 424/462
• CPC Class Codes: A61K 31/445 Non condensed piperidines, e.g. piperocaine
• CPC Class Codes: A61K 9/0056 Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
• CPC Class Codes: A61K 9/0095 Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006
• CPC Class Codes: A61K 9/5073 having two or more different coatings optionally including drug-containing subcoatings
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/14 for treating abnormal movements, e.g. chorea, dyskinesia

Abstract

Disclosed is a pharmaceutical composition for release control comprising a plurality of particles for release control. The plurality of particles for release control comprise a core material containing methylphenidate and a polymer coating layer for release control formed on the core material. The plurality of particles for release control are divided into two or more groups based on the average thickness of the polymer coating layer for release control. The particle groups are identical in terms of the composition of the polymer in the polymer coating layer, but are different in terms of the average thickness of the coated layer. The pharmaceutical composition for release control according to the present invention may control the release pattern of methylphenidate contained in the core material as desired, and can be used as an oral formulation in a variety of forms such as orally disintegrating tablets, etc.

Claims

1. A pharmaceutical composition for release control comprising a plurality of particles for release control,

the plurality of particles for release control comprise a core material containing methylphenidate and a polymer coating layer for release control formed on the core material,

wherein the plurality of particles for release control are identical in terms of the composition of the polymer in the polymer coating layer, but are divided into two or more groups based on the average thickness of the polymer coating layer for release control.

2. The pharmaceutical composition for release control according to claim 1, wherein the polymer coating layer for release control comprises a single layer or two or more layers.

3. The pharmaceutical composition for release control according to claim 2, wherein, in the polymer coating layer for release control comprising two or more layers, each layer is identical or different in terms of the composition of the polymer.

4. The pharmaceutical composition for release control according to claim 1, wherein the particles for release control further comprise a coating selected from a sub-coating inside the polymer coating layer and an over-coating outside the polymer coating layer.

5. The pharmaceutical composition for release control according to claim 1, wherein the polymer of the polymer coating layer is one or more selected from a group consisting of a water-insoluble polymer, a water-soluble polymer, an enteric polymer and a gastric polymer.

6. The pharmaceutical composition for release control according to claim 1, wherein the particles for release control have an average diameter of 30 to 3500 μ

m.

7. The pharmaceutical composition for release control according to claim 1, wherein, when the number of the particle groups for release control is two, a first particle group has an average coating layer thickness of 1 to 120 μ

m, and a second particle group has an average coating layer thickness of 10 to 250 μ

m.

8. The pharmaceutical composition for release control according to claim 7, wherein, when the number of the particle groups for release control is two, the first particle group has an average coating layer thickness of 2 to 80 μ

m, and the second particle group has an average coating layer thickness of 10 to 120 μ

m.

9. The pharmaceutical composition for release control according to a claim 1, wherein, when the number of the particle groups for release control is three, a first particle group has an average coating layer thickness of 1 to 120 μ

m, a second particle group has an average coating layer thickness of 5 to 200 μ

m, and a third particle group has an average coating layer thickness of 10 to 250 μ

m.

10. The pharmaceutical composition for release control according to claim 9, wherein, when the number of the particle groups for release control is three, the first particle group has an average coating layer thickness of 2 to 90 μ

m, the second particle group has an average coating layer thickness of 5 to 120 μ

m, and the third particle group has an average coating layer thickness of 10 to 150 μ

m.

11. The pharmaceutical composition for release control according to claim 9, wherein, when the number of the particle groups for release control is three, the first particle group has an average coating layer thickness of 2 to 30 μ

m, the second particle group has an average coating layer thickness of 30 to 60 μ

m, and the third particle group has an average coating layer thickness of 45 to 90 μ

m.

12. The pharmaceutical composition for release control according to claim 9, wherein, when the number of the particle groups for release control is three, the weight proportion of the first particle group:

the second particle group;

the third particle group is 1;

0.1-10;

0.1-10.

13. The pharmaceutical composition for release control according to claim 1, wherein the release pattern of the pharmaceutical composition tested according to the method 2(paddle method) of “

36. release test method”

of the Korean Pharmacopoeia, 8th edition (KP VIII) in 500 mL of water at 50 rpm exhibits;

5 to 50% of the total drug is released within 1 hour,

10 to 65% of the total drug is released within 2 hours,

20 to 80% of the total drug is released within 4 hours,

30 to 95% of the total drug is released within 6 hours, and

50% or more of the total drug is released within 8 hours.

14. The pharmaceutical composition for release control according to claim 13, wherein the release pattern of the pharmaceutical composition tested according to the method 2(paddle method) of “

36. release test method”

of KP VIII in 500 mL of water at 50 rpm exhibits;

10 to 40% of the total drug is released within 1 hour,

15 to 50% of the total drug is released within 2 hours,

30 to 75% of the total drug is released within 4 hours,

50 to 90% of the total drug is released within 6 hours, and

70% or more of the total drug is released within 8 hours.

15. The pharmaceutical composition for release control according to claim 1, wherein the core material and the polymer coating layer further comprise one or more selected from a group consisting of a sugar, a sugar alcohol, a polymer material, a colorant, an aromatic, a sweetener, a surfactant, a lubricant, a stabilizer, an antioxidant, a foaming agent, paraffin, wax and a plasticizer.

16. The pharmaceutical composition for release control according to claim 15, wherein the plasticizer is one or more selected from a group consisting of acetyl triethyl citrate, dibutyl phthalate, tributyl citrate, triethyl citrate, acetyl triethyl citrate, propylene glycol, triacetin, polyethylene glycol, diethyl phthalate, dibutyl sebacate, diethyl sebacate, cetyl alcohol, stearyl alcohol and cetostearyl alcohol.

17. The pharmaceutical composition for release control according to claim 1, wherein the pharmaceutical composition is an oral formulation.

18. The pharmaceutical composition for release control according to claim 17, wherein the oral formulation is an orally disintegrating tablet, a chewable tablet, a capsule, a general tablet, a granule or a syrup.