PHARMACEUTICAL COMPOSITIONS COMPRISING NIACIN AND A PROCESS FOR THEIR PREPARATION
A process for the manufacture of compositions containing niacin, the process including a first compaction step of niacin or a pharmaceutically acceptable salt thereof, then a second compaction step of a dry blend comprising niacin and microcrystalline cellulose and a further compression step into tablets. Stable tablet compositions including niacin are capable of extended release of niacin.
1 . A process for the preparation of tablets comprising:
(i) a first compaction step of niacin or a pharmaceutically acceptable salt thereof; then,
(ii) a second compaction step of a dry blend comprising compacted niacin from step (i) and hydroxypropylcellulose; and
(iii) a further compression step into tablets.
2 . The process according to claim 1 , wherein the first compacted blend is granulated.
3 . The process according to claim 1 , wherein the second compacted blend is granulated and the resulting granules are compressed into tablets.
4 . The process according to claim 1 , wherein additional excipients are added to the blend of compacted niacin and hydroxypropylcellulose before the second compaction step (ii).
5 . The process according to claim 1 , wherein the additional excipients are selected among binders, diluents, lubricants and glidants.
6 . The process according to claim 1 , wherein the additional excipients are selected among colloidal silicon dioxide, sodium stearyl fumarate.
7 . The process according to claim 1 , wherein the tablets are further coated.
8 . The process according to claim 1 , wherein the compaction steps are performed using a roll compactor.
9 . The process according to claim 1 , wherein the compression step is performed using a rotating press.
10 . The process according to claim 1 , wherein the first compaction step is performed at a pressure within the range of 1 to 6 Mpa.
11 . The process according to claim 1 , wherein the second compaction step is performed at a pressure within the range of 1 to 6 Mpa.
12 . A tablet obtainable by the process according to claim 1 .
13 . The tablet according to claim 12 , comprising 200 to 1000 mg of niacin or of a pharmaceutically acceptable salt thereof.
14 . The tablet according to claim 12 , further comprising a binder and/or a diluent and/or a glidant and/or alubricant.
15 . The tablet according to claim 14 , wherein the additional excipients are selected among colloidal silicon dioxide, sodium stearyl fumarate.
16 . A tablet according to claim 12 , having the following composition wherein percentages are by weight of the tablet:
Niacin Granules
Niacin
200-1000.0 mg
Compacted Blend
Hydroxypropyl Cellulose
10-20%
Sodium stearyl fumarate
0.1-0.5%
Colloidal silicon dioxide
0.10-0.30%
Compressed Blend
Sodium stearyl fumarate
0.40-0.55%
Aerosil ®
0.30-0.45%
Coating Layer
Opadry ® II
3-6%
Total
100%
17 . A tablet according to claim 16 , having the following composition:
Niacin Granules
Niacin
1000.0
mg
Compacted Blend
Hydroxypropyl Cellulose
215.0
mg
Sodium stearyl fumarate
5.1
mg
Colloidal silicon dioxide
2.5
mg
Compressed Blend
Sodium stearyl fumarate
6.1
mg
Aerosil ®
4.9
mg
Coating Layer
Opadry ® II
60.0
mg
Total
1293.60
mg
18 . A method for treating or preventing hypercholesterolemia, comprising the step of administering orally to a patient in need thereof, a tablet according to claim 12 .