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AAPS PharmSciTech

, Volume 19, Issue 3, pp 1308–1319 | Cite as

Controlled Release of the Nimodipine-Loaded Self-Microemulsion Osmotic Pump Capsules: Development and Characterization

  • Yaping Huang
  • Sisi Zhang
  • Huifen Shen
  • Jinqing Li
  • Chongkai Gao
Research Article
  • 173 Downloads

Abstract

The present study was intended to develop a controlled released osmotic pump capsule based on Nimodipine (NM)-loaded self-microemulsifying drug delivery systems (SMEDDSs) in order to improve the low oral bioavailability of NM. To optimize the NM-loaded SMEDDS composition, the experiments of NM solubility in different oils, the pseudo-ternary phase diagram experiments and the different drug loading experiments were conducted in the preliminary screening studies. Controlled release of NM required an osmotic pump capsule comprising a coated semi-permeable capsule shell, plasticizer, and pore-forming agent. NM release follows zero-order kinetics after oral administration. Polyethylene glycol content, used as a pore-forming agent, coating mass, and drug release orifice size were key factors affecting drug release behavior according to the single methods and were optimized through response surface methodology. The NM-loaded SMEDDS droplet size and the 1H NMR mass spectrogram of the novel capsule were determined. The droplet size of the reconstituted microemulsion was 39.9 nm and 1H NMR analysis showed NM dissolution in the microemulsion. The dissolution test performed on three batches of NM-SMEDDS capsules—prepared using optimal preparation methods—indicated the capsule to deliver a qualified drug delivery with a zero-order release rate. The results demonstrated that NM-loaded SMEDDSs were successfully developed and displayed a qualified release rate in vitro.

KEY WORDS

osmotic pump controlled released capsule SMEDDS nimodipine 1H NMR 

Notes

Acknowledgements

The authors are thankful to Prof. Li Ning from Guangdong Pharmaceutical University, for providing equipment used in this project and for consultation on analytical methods.

Compliance with Ethical Standards

Conflict of Interest

The authors declare that they have no conflicts of interest.

Novelty Statement

The use of self-microemulsifying drug delivery system (SMEDDS) solves the water insolubility problem of Nimodipine. Besides, osmotic pump systems (OPSs) can be used as a method to control formulation release by oral administration, whereby the drug release follows zero-order kinetics.

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Copyright information

© American Association of Pharmaceutical Scientists 2018

Authors and Affiliations

  • Yaping Huang
    • 1
  • Sisi Zhang
    • 1
  • Huifen Shen
    • 1
  • Jinqing Li
    • 1
  • Chongkai Gao
    • 2
  1. 1.Guangzhou Higher Education Mega CenterGuangdong Pharmaceutical UniversityGuangzhouChina
  2. 2.Department of Pharmaceutics, School of Pharmacy, Guangzhou Higher Education Mega CenterGuangdong Pharmaceutical UniversityGuangzhouChina

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