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A solid dosage form having a fill composition encased in a shell composition; the fill composition comprising (a) 5-60 mg of nifedipine; (b) a 5-7 membered cyclic pharmaceutically acceptable ingestible carbonate of the formula [Figure] I where A is an alpha,omega-C2-C4 alkylene which is unsubstitute

A solid dosage form having a fill composition encased in a shell composition; the fill composition comprising (a) 5-60 mg of nifedipine; (b) a 5-7 membered cyclic pharmaceutically acceptable ingestible carbonate of the formula [Figure] I where A is an alpha,omega-C2-C4 alkylene which is unsubstituted or substituted by at least one C1-C4 alkyl; and (c) a pharmaceutically acceptable ingestible surfactant having a total of d ring members and being of the formula [Figure] II wherein B is a C1-4-alpha,omega-alkylene; n is an integer from 0 up to d-1; m is an integer from 0 up to (d-n-1); each R is independently H or a C1-4alkyl which is unsubstituted or substituted by at least one R′; each R′is independently a hydroxy which is free, etherified by R2, or esterified by R3; each R2 is a C2-4 straight or branched oxyalkylene or a poly (C2-4 straight or branched oxyalkylene), the terminal oxygen of which is bound to hydrogen or R3; and each R3 is independently an acyl of a C2-24 alkanoic acid or a C4-24 alkeneoic acid; provided that there is at least one free hydroxy group, at least one R3 group, and at least 5 now cyclic etherified oxygen atoms per molecule of formula II; (b) and (c) being present in amounts sufficient to dissolve the nifedipine therein; the shell composition comprising at least gelatin and a dye.

대표청구항 ▼

A gelatin encapsulated liquid fill formulation of nifedipine which is substantially stable against light degradation condition comprising a capsule wall formulation encasing a capsule fill formulation, said capsule wall formulation comprising gelatin in an amount sufficient to encapsulate said capsu

A gelatin encapsulated liquid fill formulation of nifedipine which is substantially stable against light degradation condition comprising a capsule wall formulation encasing a capsule fill formulation, said capsule wall formulation comprising gelatin in an amount sufficient to encapsulate said capsule fill composition, with or without a pharmaceutically acceptable, ingestible, plasticizer for gelatin; said fill formulation comprising 5-60 mg of nifedipine, and a mixture of a carbonate and a surfactant in an amount sufficient to dissolve said nifedipine, and in a ratio of carbonate to surfactant of from 99:1 to 1:99, said carbonate being selected from a di-C1-10 alkyl carbonate and a compound of the formula [Figure] I wherein A is a C1-4-alpha,omega-alkylene which is unsubstituted or substituted by C1-4 alkyl; said surfactant being selected from compounds of formula II, IIa, and IIb, decaglycerol mono-dioleate, glycerol polyethylene glycol ricinoleate, and glycerol polyethylene glycol oxystearate; said formula II being a substituted cyclic ether having d ring members and being [Figure] II wherein B is a C1-4-alpha,omega-alkylene; n is an integer 0 to d-1; m is an integer of from 0 to (d-n-1); each R is each R is independently H or a C1-4 alkyl which is unsubstituted or substituted by at least one R1; each R1 is independently a hydroxy which is free, etherified by R2, or esterified by R3, each R2 is a C2-4 straight or branched oxyalkylene or poly(C2-4 straight or branched oxyalkylene), the terminal oxygen of which is bound to H or R3; and each R3 is independently an acyl of a C2-24 alkanoic acid or a C4-24 alkenoic acid; provided that in each compound of formula II there is at least one free hydroxy group, and at least one R3 group; said formula IIa being Rc－O(CH2CH2O)pRd (IIa) wherein p is, on average, 6-8, Rc is stearoyl or palmitoyl or mixtures thereof, and Rd is hydrogen or the same as Rc; said formula IIb being Re(OCH2CH2)fORg (IIb) wherein Re is C10-18 alkyl, f is an integer of from about 10 to about 60, and Rg is hydrogen or the same as Re; said gelatin encapsulated liquid fill formulation further comprising a dye in at least one of said shell formulation and said capsule fill formulation.