Table 3. Composition and observed responses from runs.
Mixture number | Formulation composition | Response measured | |||||
---|---|---|---|---|---|---|---|
X1 | X2 | X3 | Y1 | Y2 | Y3 | Y4 | |
(A) Optimized S-SuSMEDDS granules | |||||||
Florite® PS-10 (%) | Vivapur® 105 (%) | N.A.a | CSR (g/mL) | D15 (%) | N.A. | N.A. | |
1 | 0 | 100 | - | 1.8 | 64.3 | - | - |
2 | 25 | 75 | - | 1.45 | 59.3 | - | - |
3 | 50 | 50 | - | 1.1 | 55.5 | - | - |
4 | 75 | 25 | - | 0.8 | 52.7 | - | - |
5 | 100 | 0 | - | 1.4 | 46.6 | - | - |
6 | 0 | 100 | - | 1.8 | 62.8 | - | - |
7 | 50 | 50 | - | 1.15 | 54.4 | - | - |
8 | 100 | 0 | - | 0.42 | 45.7 | - | - |
(B) Optimized S-SuSMEDDS tablets | |||||||
Compression force (%) | Conc. of super-disintegrant (%) | Type of super-disintegrant | Hardness (N) | Disint (%) | DE (%) | Total mass (mg) | |
1 | 500 | 2 | CS | 77 | 23.8 | 3.4 | 466.1 |
2 | 1250 | 2 | CS | 93 | 23.0 | 3.3 | 465.5 |
3 | 2000 | 2 | CS | 66 | 23.0 | 3.1 | 466.2 |
4 | 500 | 5 | CS | 76 | 89.2 | 27.3 | 478.2 |
5 | 1250 | 5 | CS | 72 | 84.9 | 28.8 | 480.5 |
6 | 2000 | 5 | CS | 73 | 87.2 | 28.8 | 476.6 |
7 | 500 | 8 | CS | 75 | 100.0 | 38.6 | 489.6 |
8 | 1250 | 8 | CS | 77 | 100.0 | 39.5 | 489.7 |
9 | 2000 | 8 | CS | 71 | 100.0 | 38.9 | 493.1 |
10 | 500 | 2 | KC | 74 | 16.9 | 3.8 | 464.3 |
11 | 1250 | 2 | KC | 81 | 18.3 | 4.3 | 461.8 |
12 | 2000 | 2 | KC | 69 | 19.1 | 5.3 | 466.5 |
13 | 500 | 5 | KC | 80 | 63.8 | 32.2 | 476.3 |
14 | 1250 | 5 | KC | 88 | 59.8 | 33.8 | 479.3 |
15 | 2000 | 5 | KC | 82 | 62.6 | 31.7 | 480.5 |
16 | 500 | 8 | KC | 74 | 89.5 | 42.8 | 493.8 |
17 | 1250 | 8 | KC | 84 | 90.1 | 41.3 | 490.2 |
18 | 2000 | 8 | KC | 80 | 92.0 | 40.6 | 489.9 |
19 | 500 | 2 | SSG | 68 | 23.8 | 4.5 | 461.3 |
20 | 1250 | 2 | SSG | 86 | 27.3 | 4.8 | 463.7 |
21 | 2000 | 2 | SSG | 69 | 26.4 | 4.8 | 465.8 |
22 | 500 | 5 | SSG | 67 | 41.1 | 12.1 | 476.1 |
23 | 1250 | 5 | SSG | 79 | 44.1 | 12.3 | 479.3 |
24 | 2000 | 5 | SSG | 66 | 49.0 | 11.7 | 480.2 |
25 | 500 | 8 | SSG | 76 | 68.6 | 25.7 | 489.3 |
26 | 1250 | 8 | SSG | 88 | 69.2 | 25.6 | 491.7 |
27 | 2000 | 8 | SSG | 70 | 71.1 | 27.4 | 493.2 |
28 | 1250 | 5 | CS | 76 | 80.1 | 30.1 | 478.6 |
29 | 1250 | 5 | KC | 82 | 64.4 | 35.6 | 479.8 |
30 | 1250 | 5 | SSG | 83 | 48.8 | 26.1 | 476.5 |
aNot applicable
Abbreviations: S-SuSMEDDS, solidified supersaturable self-microemulsifying drug delivery system; CSR, critical solidifying ratio; D15, percentage of drug released in 15 min; Disint%, percentage of disintegration in 30 min; DE, dissolution efficiency; CS, croscarmellose sodium; KC, Kollidon® CL; SSG, Sodium starch glycolate.