Otsuka M, Sato M and Matsuda Y Comparative Evaluation of Tableting Compression Behaviors by Methods of Internal and External Lubricant Addition: Inhibition of Enzymatic Activity of Trypsin Preparation by Using External Lubricant Addition During the Tableting Compression Process AAPS PharmSci 2001;
3
(3)
article 20
(https://www.pharmsci.org/scientificjournals/pharmsci/journal/01_20.html).
Figures and Tables
Table 1.
Amount of Magnesium Stearate on Punches and Dies After Tableting Compression of Trypsin Tablets*
|
Amount of Magnesium Stearate on Tool Surface (mg/Compression)
| |
Upper Punch
|
Lower Punch
|
Die
|
Total
| |
0.592 ± 0.78
|
0.430 ± 0.22
|
1.132 ± 0.288
|
2.154
| |
Amount of Magnesium Stearate in Tablet (mg/Tablet)
| |
Upper Tablet Surface
|
Lower Tablet Surface
|
Around Tablet Surface
|
Total
| |
0.172 ± 0.042
|
0.284 ± 0.026
|
0.664 ± 0.116
|
1.12
| |
Transfer Percent of Magnesium Stearate from Tool Surface
| |
From Upper Punch
|
From Lower Punch
|
From Die
|
Total
| |
29.2
|
66.1
|
58.6
|
44.1
|
* The amount of magnesium stearate of the tablet obtained by 0.5% internal lubricant is 1 mg/tablet.
Figure 1.Effect of lubricant addition methods on compression process of trypsin tablet. closed circle, no addition; open triangle, external addition; open circle, internal addition.
Figure 2.Effect of lubricant addition methods on work of compression of trypsin tablet.
Figure 3.Effect of lubricant addition methods on friction energy of trypsin tablet.
Figure 4.Effect of lubricant addition methods on tablet hardness of trypsin tablet.
Figure 5.Effect of lubricant addition methods on availability of work of compression (CEA) of trypsin tablet.
Figure 6.Effect of lubricant addition methods on micropore distribution of trypsin tablet (closed circle no addition tablet; open triangle, external
addition tablet; open circle, internal addition tablet; closed triangle, granules).
Figure 7.Effect of lubricant addition methods on ejection processes of trypsin tablet (closed circle no addition tablet; open triangle, external
addition tablet; open circle, internal addition tablet; closed triangle, granules).
Figure 8. Effect of lubricant addition methods on ejection energy availability of trypsin tablet.
Figure 9.Effect of lubricant addition methods on dissolution of trypsin tablet (closed circle no addition tablet; open triangle, external
addition tablet; open circle, internal addition tablet; closed triangle,
granules).
Table 2.
Effect of Lubricant Additions on the Dissolution Behaviors of Trypsin Tablets
|
Samples
|
MDT (min)
|
MDIT (min)
|
DIT ± SD (min)
| |
Tablet of internal addition
|
214.2
|
213.7
|
35 ± 6
| |
Tablet of external addition
|
2.1
|
1.8
|
0.9 ± 0.8
| |
Granule powder with 0.5% lubricant
|
0.5
|
-
|
-
| |
Granule powder lubricant
|
0.3
|
-
|
-
|
DIT indicates disintegration time for tablet; MDIT, mean disintegration time for tablet; MDT, mean drug release time; SD, standard deviation.
Figure 10.Effect of lubricant addition methods on water absorption of trypsin tablet (closed circle, no addition tablet; open triangle, external addition tablet; open circle, internal addition).
Table 3.
Effect of Lubricant Additions on the Water Penetration Behaviors of Trypsin Tablets
|
Samples
|
r (µm)
|
k (cm3/min1/2)
|
k2/r (cm5/min)
| |
Tablet of internal addition
|
0.150
|
6.1 × 10-3
|
2.5
| |
Tablet of external addition
|
0.280
|
22.3 × 10-3
|
17.8
| |
Tablet of no addition
|
0.299
|
27.2 × 10-3
|
24.7
|
r indicates the radius of the micropore evaluated on the basis
of data in ; k, water-penetration rate constant estimated on the basis
of the data in the initial stage in by the least squares method.
Figure 11.Effect of availability of work of compression (CEA) on enzymatic activity of trypsin tablet (closed circle, no addition tablet; open triangle, external
addition tablet; open circle, internal addition).
Figure 12.Relationship between tablet hardness and enzymatic activity of trypsin tablet (closed circle, no addition tablet; open triangle, external addition tablet; open circle, internal addition).
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