High drug load acid labile pharmaceutical composition
AssigneeBristol-Myers Squibb Company
InventorsIsmat Ullah, Gary J Wiley
Life of this patent
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Abstract
A high drug load spheronized beadlet is provided wherein said beadlet comprises about 80% to 100% by weight of an acid labile medicament, preferably didanosine, about 0% to about 10% by weight of a disintegrant, and about 0% to about 10% by weight of a binder selected from the group consisting of sodium carboxymethylcellulose, hydroxypropylmethylcellulose, potassium alginate, and partially pregelatinized corn starch. A high drug load pharmaceutical composition, comprising the beadlet, with an enteric coating disposed thereon, is also provided.
Claims19
A process for preparing spheronized beadlets, comprising:
- a) mixing a granulation solvent, a medicament, optionally a disintegrant, and optionally a binder to form a wet mass;
- b) extruding the wet mass to form an extrudate;
- c) spheronizing the extrudate to form beadlets;
- and
- d) while spheronizing, dusting the extrudate and the forming beadlets with a dry powder containing medicament, the optional disintegrant and the optional binder, which are in the same proportions as contained in the wet mass, to form non-agglomerating beadlets;
- and
- e) drying the non-agglomerating beadlets to form said spheronized beadlets.
A process for preparing a pharmaceutical composition of enterically coated beadlets, comprising:
- (a) mixing a granulation solvent, a medicament which is 2′,3′-dideoxyinosine, optionally a disintegrant, and optionally a binder to form a wet mass;
- (b) extruding the wet mass to form an extrudate;
- (c) spheronizing the extrudate to form beadlets;
- (d) while spheronizing, dusting the extrudate and forming beadlets with a dry powder containing the medicament, the optional disintegrant and the optional binder, which are in the same proportions as contained in the wet mass, to form non-agglomerating beadlets;
- (e) drying the non-agglomerating beadlets to form dry beadlets;
- and
- (f) forming an enteric coating on the dry beadlets, thereby forming the pharmaceutical composition of enterically coated beadlets.
Dependencies are inferred from the claim text.