Abstract
This study was performed to investigate the in vitro release characteristics of levodropropizine (LDP) from novel dual-coated sustained release (SR) pellets, and evaluate the pharmacokinetics of a novel controlled release (CR) preparation composed of the dual-coated SR pellets and immediate release (IR) LDP pellets. The dual-coated SR pellets composed of a drug-loaded nonpareil core, a sub-coating layer (HPMC 6cps) and an SR-coating layer (Aquacoat ECD, Eudragit RS 30D or Kollicoat SR 30D) were prepared by a bottom-spray fluidized bed-coating method. The drug release from the dual-coated SR pellets coated with Aquacoat ECD followed a zero-order profile in water, and the drug release was not affected by the coating level of the sub-coating layer and stable under the accelerated storage condition (40 C, 75% RH) for 6 months. The CR preparation showed significantly decreased values of maximum drug concentration (Cmax) and elimination rate (K) than the reference product (LEVOTUS SYR) but the similar bioavailability (F95.43%). The novel CR preparation presents promising delivery of LDP with an immediate and sustained release manner, with similar clinical effect as the commercial IR product.
| Original language | English |
|---|---|
| Journal | Pharmaceutical Development and Technology |
| Volume | 19 |
| Issue number | 3 |
| Pages (from-to) | 296-303 |
| ISSN | 1083-7450 |
| DOIs | |
| Publication status | Published - 2014 |