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Related Experiment Videos

[Studies on heart-protecting musk pH-dependent gradient-release pellets].

Hong-tao Song1, Tao Guo, Ru-hua Zhang

  • 1Department of Pharmacy, Shenyang Military General Hospital, Shenyang 110016, China. sohoto@sohu.com

Yao Xue Xue Bao = Acta Pharmaceutica Sinica
|February 6, 2003
PubMed
Summary

This study developed pH-dependent gradient-release pellets for heart-protecting musk, demonstrating simultaneous release of borneol and total ginsenoside. The novel formulation showed sustained release and improved bioavailability in vivo.

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Pharmacokinetics

Background:

  • Heart-protecting musk contains lipidsoluble borneol and watersoluble total ginsenoside.
  • Traditional formulations may not optimize the release of these components.
  • Developing advanced drug delivery systems is crucial for enhancing therapeutic efficacy.

Purpose of the Study:

  • To prepare pH-dependent gradient-release pellets of heart-protecting musk.
  • To investigate the in vitro drug release characteristics.
  • To evaluate the in vivo gastrointestinal transit, pharmacokinetics, and bioavailability.

Main Methods:

  • Pellets were coated with combinations of HPMC and Eudragit polymers (L-30D-55, L100-S100).
  • In vitro release studies were conducted under simulated gastrointestinal pH conditions.

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  • Gamma-scintigraphy was used to track pellet transit and disintegration in volunteers.
  • Pharmacokinetic analysis of borneol was performed using GC methods in healthy volunteers.

    • Main Results:

    • The pellets exhibited pH-dependent gradient release of borneol and total ginsenoside (f2 value = 79.6).
    • Gamma-scintigraphy confirmed disintegration in the stomach and intestines, with transit times of approximately 5-6 hours.
    • Borneol demonstrated a two-compartment pharmacokinetic model with a mean residence time (MRT) of 2.61 hours.
    • The sustained-release capsule formulation achieved a steadier plasma concentration, lower Cmax, and 96% relative bioavailability with an MRT of 4.0 hours.

    Conclusions:

    • The developed heart-protecting musk pellets achieve simultaneous, sustained release of both lipidsoluble and watersoluble components.
    • The formulation exhibits pH-dependent gradient-releasing and disintegration properties throughout the gastrointestinal tract.
    • The sustained-release capsule formulation offers improved pharmacokinetic profiles and bioavailability compared to traditional pills.