Controlled release dosage form
AssigneeOsmotica Kereskedelmi Es Szolgaltato Kft
InventorsGlenn A. Meyer, Cristian R. Franco, Gustavo A. Fischbein, Alejandro A. Aguilar, Claude E. Wright
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Abstract
The present invention provides a simple and improved dosage form that is capable of providing a controlled release of GABAB receptor agonist contained in the core thereof. The invention also provides methods of administering the dosage form and of treating conditions that are therapeutically responsive to GABAB receptor agonist.
Claims26
An extended release oral dosage form comprising an active ingredient, wherein said active ingredient consists of arbaclofen (ARBAC), and wherein
- a) the dosage form provides an in vitro release profile for ARBAC as follows under conditions defined in USP <711> using a Type II apparatus with paddles in 0.1 N HCl at a temperature of 37±5° C.:
- about 70 to about 95% wt of the drug is released by six hours, no less than about 80% wt of the drug is released by 8 hours, and no less than about 90% wt of the drug is released by 12 hours, and
- b) the dosage form provides the following pharmacokinetic profile when a single dose comprising 20 mg ARBAC is administered orally to a subject:
- a mean Cmax of about 240 ng/ml±30%, and a mean AUC0-t of about 1460 ng*h/ml±30%.
An extended release dosage form comprising about 2.5 to about 50 mg of arbaclofen (ARBAC) and made according to the following formulation:
- Ingredient
- % wt
- Core
- ARBAC
- 5-11
- NaCl
- 30-40
- MCC
- 2-8
- Copovidone
- 6-16
- Swellable HPMC
- 0.5-5
- Swellable PEO with molecular weight ≤1,000,000
- 30-45
- Optional Antioxidant
- 0.01-0.5
- Optional Glidant
- 0.01-0.5
- Optional Lubricant
- 0.01-0.5
- Semipermeable membrane
- Cellulose acetate Grade 2, 4, or 5
- 0-<10
- Cellulose acetate Grade 1 or 3
- 100-≥90
- Plasticizer
- 1-10
- wherein about 15 to about 35% by weight of the ARBAC is released by 2 hours, about 50 to about 85% wt is released by 4 hours, no less than about 80% wt of the drug is released by 8 hours, and no less than 90% wt of the drug is released by 12 hours after placement in an environment of use.
A controlled or extended release dosage form comprising arbaclofen, wherein following oral administration the dosage form provides a higher AUC0-inf and higher Cmax and a longer Tmax than that provided by an immediate release capsule containing the same amount of arbaclofen.
Dependencies are inferred from the claim text.