Table 1.
Composition of various DL-CDDS formulations
| Ingredient (mg/tablet) | CA-free DL-CDDS
|
CA-supplemented DL-CDDS
|
||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| CA0-CTN0/EE10 | CA0-CTN1/EE9 | CA0-CTN3/EE7 | CA0-CTN0/EE21 | CA0-CTN3/EE18 | CA0-CTN6/EE15 | CA15-CTN3/EE18 | CA15-CTN6/EE15 | CA30-CTN3/EE18 | CA30-CTN6/EE15 | |
| Core tablet | ||||||||||
| LXP | 60 | 60 | 60 | 60 | 60 | 60 | 60 | 60 | 60 | 60 |
| Lactose | 145 | 145 | 145 | 145 | 145 | 145 | 130 | 130 | 115 | 115 |
| L-HPC | 25 | 25 | 25 | 25 | 25 | 25 | 25 | 25 | 25 | 25 |
| Povidone | 8 | 8 | 8 | 8 | 8 | 8 | 8 | 8 | 8 | 8 |
| Croscarmellose sodium | 7 | 7 | 7 | 7 | 7 | 7 | 7 | 7 | 7 | 7 |
| Colloidal silicon dioxide | 1 | 1 | 1 | 1 | 1 | 1 | 1 | 1 | 1 | 1 |
| Magnesium stearate | 4 | 4 | 4 | 4 | 4 | 4 | 4 | 4 | 4 | 4 |
| CA | – | – | – | – | – | – | 15 | 15 | 30 | 30 |
| Subtotal | 250 | 250 | 250 | 250 | 250 | 250 | 250 | 250 | 250 | 250 |
| Subcoatinga | ||||||||||
| EE | 10.8 | 9.3 | 7.8 | 21.6 | 18.6 | 15.6 | 18.6 | 15.6 | 18.6 | 15.6 |
| CTN | 0 | 1.5 | 3 | 0 | 3 | 6 | 3 | 6 | 3 | 6 |
| Triethyl citrate | 0.6 | 0.6 | 0.6 | 1.2 | 1.2 | 1.2 | 1.2 | 1.2 | 1.2 | 1.2 |
| Talc | 3.6 | 3.6 | 3.6 | 7.2 | 7.2 | 7.2 | 7.2 | 7.2 | 7.2 | 7.2 |
| Subtotal | 15 | 15 | 15 | 30 | 30 | 30 | 30 | 30 | 30 | 30 |
| Enteric coatingb | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 |
| Total | 280 | 280 | 280 | 295 | 295 | 295 | 295 | 295 | 295 | 295 |
Notes:
a
CTN/EE subcoating was further modified with EC addition, designated as CTN/EC/EE coating;
b
the layered enteric coating was maintained with 6% of the core tablet weight, composed of EL, triethyl citrate, and talc (6:0.5:1 in weight ratio).
Abbreviations: CA, citric acid; CTN, chitosan; DL-CDDS, double layer-coated colon-specific drug delivery system; EC, ethyl cellulose; EE, Eudragit E100; EL, Eudragit L100-55; L-HPC, low-substituted hydroxypropyl cellulose; LXP, loxoprofen sodium; CA0, citric acid-free tablet; CA15, CA 15 mg; CA30, CA 30 mg.