A Novel Copovidone Binder for Dry Granulation and

(a) DC Lactose filler (b) DCP filler
Hardness (KPa)
Ejection force (lb)
20
15
10
5
S-630 10%MCC 28%
MCC 28%
0
0 2000 4000 6000 8000
Compression force (lb)
100
80
60
40
20
0
S-630 10%MCC 18%
MCC 28%
0 2000 4000 6000 8000
Compression force (lb)
Hardness (KPa)
(c) DC Lactose filler (d) DCP filler
Ejection force (lb)
(e) DC Lactose filler (f) DCP filler
Friability (%)
4
3
2
1
S-630 10%MCC 18%
MCC 28%
Friability (%)
20
15
10
5
S-630 10%MCC 18%
MCC 28%
0
0 2000 4000 6000 8000
Compression force (lb)
100
80
60
40
20
0
S-630 10%MCC 18%
MCC 28%
0 2000 4000 6000 8000
Compression force (lb)
0
0
0 2000 4000 6000 8000 0 2000 4000 6000 8000
Compression force (lb)
Compression force (lb)
3
2.5
2
1.5
1
0.5
S-630 10%MCC 18%
MCC 28%
Figure 6: Characteristics of directly compressed HCTZ formulations in which Plasdone S-630 has
replaced 10% MCC: hardness of HCTZ tablets for (a) DC lactose filler and (b) DCP filler; ejection force of
HCTZ tablets for (c) DC lactose filler and (d) DCP filler; and friability of HCTZ tablets for (e) DC lactose
filler and (f) DCP filler.
% Dissolved
120
100
80
60
40
20
Plasdone S-630
HPMC 15 cps
MCC
0
0 20 40
Time (min)
60 80
Figure 7: Dissolution profiles of roller-compacted ASA formulations
(6000 lb, 4 rpm) with 5% of Plasdone S-630 copovidone, MCC 101, or
HPMC 15 cps binder.
were prepared at higher drug loading,
and the binding performance
of Plasdone S-630 copovidone was
compared with those of commonly
used binders such as MCC
or hydroxypropylmethyl cellulose
(HPMC) 15 cps.
Results obtained show the following
trends (3):
● Effect of compaction parameters
on final tablet hardness. The
use of a lower roll speed produced
harder tablets with both
drugs, a confirmation of the
plastic behavior of the three
binders. Feed-screw rate and roll
pressure did not have a significant
effect on final hardness.
● Hardness. As shown in Table V,
HCTZ tablets made with Plasdone
S-630 copovidone show a
substantially improved hardness
in comparison with tablets
made with HPMC or MCC.
ASA tablets made with Plasdone
S-630 copovidone showed similar
hardness to tablets made
with both MCC and HPMC 15
cps.
● Dissolution. HCTZ tablets made
with all three binders showed
similar dissolution profiles. ASA
tablets made with MCC showed
slower dissolution profiles than
did tablets made with either
Plasdone S-630 copovidone or
HPMC 15 cps (see Figure 7).
Conclusion
Plasdone S-630 copovidone has been shown to be a good rollercompaction
binder, and its addition to directly compressed formulations
has been shown to improve tablet hardness substantially.
Tablets made with Plasdone S-630 copovidone show
higher hardness and/or better drug dissolution profiles than
those made with other binders. For additional information
about Plasdone S-630 copovidone, contact the author.
References
1. ISP technical bulletin, Pharma/PLASS630.0800.
2. A. Moroni, M. Nerella, and G. DuBrowny, “Plasdone S-630 as High-
Performance Binder for Dry Granulation,” presented at the 2000 AAPS
meeting, Indianapolis, Indiana, 29 October–2 November 2000.
3. A. Moroni, M. Nerella, and G. DuBrowny, “Plasdone S-630 Mixes as
Dry Granulation Binders with Improved Performance,” presented at
the AAPS Pharmaceutical Congress of the Americas, Orlando, Florida,
24–29 March 2001. PT
12 Pharmaceutical Technology DRUG DELIVERY 2001 www.pharmtech.com