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Journal of Chinese Pharmaceutical Sciences ›› 2017, Vol. 26 ›› Issue (6): 413-422.DOI: 10.5246/jcps.2017.06.045

• Original articles • Previous Articles     Next Articles

Lappaconitine solid dispersion monolithic osmotic tablet and lappaconitine push-pull osmotic pump: preparation and comparison of their release performance in vitro

Xianchuang Wu1, Jiaojiao Wang2, Haijun Hao2*, Xiaoyong Song1*, Yongzhou Zhang1, Yuxin Liu1, Hongqin Zhang3   

  1. 1. Department of Pharmacy, Huai He Hospital of Henan University, Kaifeng 475000
    2. Shanghai Institute of Pharmaceutical Industry, Shanghai 200437
    3. Shanghai Advanced Vehicle Technology Pharmaceutical L.T.D. Co, Shanghai 201203
  • Received:2017-02-15 Revised:2017-04-20 Online:2017-06-29 Published:2017-04-25
  • Contact: Tel.: +86-021-50272000-1041; +86-0371-23906970, E-mail: haohj2007@126.com; sxyyjk@sina.com
  • Supported by:
    Science and Technology Department of Henan Province Fund Project (Grant No. 144300510019).

Abstract:

Lappaconitine is a water-insoluble drug, which was used as model drug in this study. Currently, two osmotically controlleddelivery systems that are widely used for water-insoluble drug are monolithic osmotic tablet (MOT) and push–pull osmotic pump (PPOP). In the present study, lappaconitine solid dispersion monolithic osmotic tablet (lappaconitine-SD-MOT) and lappaconitine-PPOP were developed. The prepared lappaconitine-PPOP was able to delivery drug at the rate of approximate zero-order (r = 0.9931), and the cumulative release was above 95.0%. The lappaconitine-SD-MOT showed a comparatively poor linearity when the data were plotted according to the zero-order equation (r = 0.9798), and the cumulative release was 84.69%. Lappaconitine-PPOP exhibited better controlled drug release (higher regression value) compared with lappaconitine-SD-MOT. The similarity index (f2) between lappaconitine-PPOP and lappaconitine-SD-MOT was 49.1 (<50). A clear difference of drug release characteristics between the lappaconitine-SD-MOT and lappaconitine-PPOP was revealed. It indicated that the drug release performance of lappaconitine-PPOPcould gain favorable zero-order kinetics and higher cumulative release compared with lappaconitine-SD-MOT. Therefore, these results suggested that PPOP was still a very effective device for the delivery of poorly water-soluble drug with zero-order pattern.

Key words: Lappaconitine, Solid dispersion, Monolithic osmotic tablet, Push-pull osmotic pumps

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