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US 10,207,002 B2Granted
Sustained release formulation and tablets prepared therefrom
AssigneeMerck Sharp & Dohme Corp.
InventorsPranav Gupta, David Monteith
Life of this patent
Estimating the term…
Abstract
Disclosed are formulations and tablets made therefrom comprising the compound of Formula IA or Formula IB which have sustained-release properties, and the dispersion containing the compounds of Formula IA or IB which facilitates such sustained release: Formula IA, Formula IB.
Claims13
A dispersion comprising a compound of Formula IA or a salt thereof:
- a plasticizer and a matrix polymer, wherein said matrix polymer is:
- (a) a polymer made from free-radical polymerization of methacrylic acid and methylmethacrylate in a 1:2 ratio, and having an average molar mass of approximately 125,000 g/mol;
- or (b) a polymer made from free radical polymerization of a 1:1 mixture of methacrylic acid and ethylacrylate, and having a weight average molecular mass of approximately 320 Kg/mol.
A tablet having the constituent ratio of either Table X, Y or Z:
- TABLE X
- Quantity/
- Amount for
- Tablet
- 3000 g
- Component
- (mg)
- (g)
- Extrudate containing 4% of API (Compound of
- 125.0
- 750.0
- Formula 1)
- Microcrystalline Cellulose
- 88.90
- 533.40
- Polyethylene oxide (~M.W. of 500,000)
- 75.0
- 450.0
- PolyOX WSR Coagulant)
- Polyethylene oxide (~M.W. of 200,000)
- 75.0
- 450.0
- PolyOX WSR 60K
- Hypromellose Acetate Succinate (HPMCAS-
- 204.0
- 1224.0
- MG)
- Croscarmellose Sodium
- 30.0
- 180.0
- Magnesium Stearate
- 1.50
- 9.0
- Butylated Hydroxytoluene (BHT)
- 0.60
- 3.6
- Tablet weight
- 600.0.
- TABLE Y
- Quantity/
- Amount for
- Tablet
- 3450 g
- Component
- (mg)
- (g)
- Extrudate containing 5% of API (Compound of
- 100.00
- 600.00
- Formula 1)
- Microcrystalline Cellulose
- 104.94
- 629.63
- Polyethylene oxide (~M.W. of 500,000)
- 71.90
- 431.40
- PolyOX WSR Coagulant)
- Polyethylene oxide (~M.W. of 200,000)
- 71.90
- 431.40
- PolyOX WSR 60K
- Hypromellose Acetate Succinate (HPMCAS-
- 195.50
- 1173.00
- MG)
- Croscarmellose Sodium
- 28.75
- 172.50
- Magnesium Stearate
- 1.44
- 8.63
- Butylated Hydroxy toluene (BHT)
- 0.58
- 3.45
- Tablet weight
- 575.0.
- TABLE Z
- Quantity/
- Quantity/
- tablet
- 5000 g batch
- Component
- (mg)
- (g)
- (Controlled Release Layer)
- Extrudate containing 5.0% API (Compound of
- 100.00
- 751.90
- Formula 1)
- Microcrystalline Cellulose
- 112.10
- 842.90
- Polyethylene oxide (~M.W. of 500,000)
- 33.25
- 250.00
- Polyethylene oxide (~M.W. of 200,000)
- 38.00
- 285.70
- Hypromellose Acetate Succinate MG
- 166.25
- 1250.00
- Croscarmellose Sodium
- 23.75
- 178.60
- Magnesium Stearate
- 1.19
- 8.90
- Butylated Hydroxytoulene
- 0.47
- 3.50
- Weight of 12-hr controlled release layer
- 475.0
- 3571.50
- (Immediate Release Layer)
- Compound of Formula 1
- 5.0
- 35.7
- Povidone
- 5.0
- 35.7
- Mannitol
- 129.6
- 925.7
- Microcrystalline cellulose
- 50.0
- 357.1
- Croscarmellose Sodium
- 10.0
- 71.4
- Magnesium Stearate
- 0.40
- 2.9
- Weight of immediate release layer
- 200.0
- 1428.5
- Total tablet weight
- 675.00
- 5000.0.
135 more elements
Dependencies are inferred from the claim text.