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Nimodipine semi-solid capsules containing solid dispersion for improving dissolution.

Yunzhe Sun1, Yang Rui, Zhou Wenliang

  • 1School of Pharmacy, Department of Pharmaceutics, Shenyang Pharmaceutical University, No. 103 Wenhua Road, Shenyang 110016, PR China.

International Journal of Pharmaceutics
|May 24, 2008
PubMed
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This study enhanced nimodipine (NMD) dissolution and bioavailability using solid dispersions and semi-solid capsules. The new nimodipine semi-solid capsules (NMD-SSC) showed faster absorption rates compared to the reference drug.

Area of Science:

  • Pharmaceutical Technology
  • Drug Delivery Systems
  • Pharmacokinetics

Background:

  • Nimodipine (NMD) is a poorly water-soluble drug with high permeability.
  • Improving NMD's dissolution and bioavailability is crucial for effective therapeutic outcomes.
  • Current formulations may not fully exploit NMD's absorption potential.

Purpose of the Study:

  • To enhance the dissolution and bioavailability of nimodipine (NMD).
  • To develop a novel nimodipine semi-solid capsule (NMD-SSC) formulation.
  • To compare the pharmacokinetic profile of NMD-SSC with a reference product.

Main Methods:

  • Preparation of nimodipine solid dispersion (NMD-SD) using Eudragit-E100 and Plasdone-S630 via hot-melt extrusion (HME).
  • Formulation of nimodipine semi-solid capsules (NMD-SSC) incorporating NMD-SD, Plasdone-S630, and PEG400 in HPMC capsules.

Related Experiment Videos

  • In vivo pharmacokinetic study in beagle dogs comparing NMD-SSC to Nimotop (reference) after a single oral dose.

    • Main Results:

    • NMD dissolution was significantly enhanced from the solid dispersion (SD) and further improved in the semi-solid capsules (SSC).
    • NMD-SSC demonstrated a markedly faster rate of absorption (tmax=1.3h) compared to Nimotop (tmax=3.1h).
    • No significant difference was observed in the overall exposure (AUC) and peak concentration (Cmax) between NMD-SSC and Nimotop.

    Conclusions:

    • Hot-melt extrusion and semi-solid capsule formulation effectively improved nimodipine dissolution and absorption.
    • NMD-SSC represents a promising fast-release formulation with comparable overall bioavailability to the reference product.
    • The developed NMD-SSC formulation enhances the therapeutic potential of nimodipine through improved drug delivery.