Synergistic binder composition, method for making same, and tablets of an active and said binder having advantageous hardness and friability
View Patent ↗Tablets of a pharmaceutical, nutritional or vitamin active compound or composition, e.g. a poorly compressible drug are made by direct compression using a synergistic binder composition of co-processed (a) copolymer of vinylpyrrolidone (VP) and vinyl acetate (VA) and (b) microcrystalline cellulose (MCC), in a wt. ratio of (a):(b) of 1-30:99-70, which is spray dried to provide a readily compressible excipient binder powder for such active. The tablets obtained herein have advantageous hardness and friability at an acceptable compression force.
1. A process for making tablets of a pharmaceutical, nutritional or vitamin active compound or composition by direct compression, which comprises providing an aqueous dispersion of (a) a copolymer of vinylpyrrolidone (VP) and vinyl acetate (VA) and (b) microcrystalline cellulose (MCC), in a wt. ratio of (a) to (b) of 1-30:99-70, spray drying said aqueous dispersion to form powders thereof, admixing said powders and said active, and forming a tablet thereof by direct compression.
2. A process according to claim 1 wherein (a) has a wt. ratio of 30-90 VP and 70-10 VA.
3. A process according to claim 1 wherein said copolymer comprises about 60 wt. % VP and about 40% wt. VA.
4. A process according to claim 1 wherein the binder powders have an average particle size of about 20-120 μ (0.79-4.72 mils).
5. A process according to claim 1 wherein said active is present in said tablet in an amount of 1-85 wt. % and said binder composition is present in an amount of 99-15 wt. %.
6. A process according to claim 1 wherein direct compression is carried out at 2000-7000 lbs. (8.9-31.1 kN) and the tablet has a hardness of at least 6 kP (59N; 13 lbf) and a friability of less than 2%.
7. A process according to claim 6 wherein said tablet hardness is about 8-30 kP (79-294N; 18-66 lbf) and said friability is about 1-2%.
8. A process according to claim 5 wherein said active is present in an amount of 50 to 70 wt. % in said mixture of binder composition and drug.
9. A process according to claim 1 in which said tablet also includes other excipients.
10. A process according to claim 1 wherein said active is a drug.
11. A free-flowing, co-processed powdered binder composition obtained by spray drying an aqueous dispersion of (a) a copolymer of VP and VA and (b) MCC, in a wt. ratio of (a):(b) of 1-30:99-70.
12. The free-flowing co-processed powdered binder composition according to claim 11 having a mean particle size of 20-120 μ (0.79-4.72 mils).
13. The free-flowing co-processed powdered binder composition according to claim 11 wherein (a) comprises 30-90% VP and 10-70% VA.
14. The free-flowing, co-processed powdered binder composition according to claim 11 wherein spray drying is carried out on an aqueous dispersion of said copolymer and MCC at an inlet temperature of about 200-300° C. (392-572° F.) and an outlet temperature of about 75-95° C. (167-203° F.), at an atomizer speed rate of about 12,000 to 24,000 rpm.
15. The free-flowing, co-processed powdered binder composition according to claim 13 wherein said copolymer comprises about 60 wt. % VP and about 40 wt. % VA.
16. The free-flowing, co-processed powdered binder composition according to claim 13 wherein the wt. ratio of (a):(b) is from about 5-15:85-95.
17. A process according to claim 3 wherein the wt. ratio of (a):(b) is from about 5-15:85-95.