Design, in vitro release characterization and pharmacokinetics of novel controlled release pellets containing levodropropizine

TY - JOUR

T1 - Design, in vitro release characterization and pharmacokinetics of novel controlled release pellets containing levodropropizine

AU - Cao, Qing-Ri

AU - Piao, Yong-Nan

AU - Choi , Jae-Seung

AU - Liu, Yan

AU - Yang, Mingshi

AU - Cui, Jing-Hao

PY - 2014

Y1 - 2014

N2 - 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.

AB - 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.

U2 - 10.3109/10837450.2013.778871

DO - 10.3109/10837450.2013.778871

M3 - Journal article

C2 - 23509871

SN - 1083-7450

VL - 19

SP - 296

EP - 303

JO - Pharmaceutical Development and Technology

JF - Pharmaceutical Development and Technology

IS - 3

ER -