Table VI.
Overview: Selection of Formulations and Characteristics
| API | Coating agent | Characteristics/application |
|---|---|---|
| Acetaminophen |
Carnauba wax/sorbitan monostearate Hydrogenated vegetable oils/sodium stearyl lactate or sorbitan monostearate or glyceryl monostearate (46) |
Taste masking, immediate release, storage stability achieved with carnauba wax, formulation with hydrogenated vegetable oils with inferior storage stability |
| Compritol 888 ATO (152) |
Controlled release (Higuchi model) |
|
|
Precirol ATO 5, stearic acid Compritol 888 ATO Several combinations with surfactants and/or release enhancer were tested: CaCO3, PEG 3000, PEG 4000, Amberlite IRP, Tween 20, Cremophor EL, Cremophor A6, Gelucire 50/13, Kollidon CL-M, Kollidon CL, Carbopol 971P NF, Carmellose Sodium, KHCO3, Lactose, Blanose (336) |
Immediate release Taste masking assumed, only study of release profile, no study for taste masking or formulation stability included |
|
| N-acetylcysteine (162) | Tripalmitin/Polysorbate 65 | Immediate release, taste masking (volunteer panel), stability achieved, acceleration of α → β transition due to emulsifier |
| Antibiotics (40) | Carnauba wax/carbomer, xanthan gum, L-HPC | Immediate release, taste masking (electronic tongue), storage stability achieved |
| Bromhexin HCl (33) | Bees wax/cetyl alcohol |
Taste masking (human volunteers) Stability not approved |
| Chloroquine (145) | Compritol 888 ATO | Controlled release |
| Diclofenac sodium (111) | Stearic acid, palmitic acid | Enteric coating |
| Diltiazem HCl (337) | Glyceryl monostearate/bees wax/ white wax/ stearyl alcohol |
Immediate release, taste masking was assumed (drug release after 1 min) Stability not approved |
| Herbal extract (115) | Stearic acid/ PEG 6000 | Immediate release, moisture sorption control, stability not approved |
| Ibuprofen | Precirol ATO 5 (27) | Immediate release, taste masking and stability not approved |
| Compritol 888 ATO (146) |
Controlled release Maturing reduced and stabilized dissolution rate |
|
| Metoprolol tartrate (34) | Bees wax/ethyl cellulose (34) | Sustained release, stable during storage |
| Phenylpropanolamine (146) | Compritol 888 ATO |
Controlled release Maturing reduced and stabilized dissolution rate |
| Theophylline | Hydrogenated castor oil/HPMC, sodium laurel sulphate (52) |
Controlled release Hydrophilic pore formers increased the release, no stability study conducted |
| Compritol 888 ATO (143,144,146) | Controlled release |