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Related Concept Videos

Factors Influencing Drug Absorption: Pharmaceutical Parameters01:28

Factors Influencing Drug Absorption: Pharmaceutical Parameters

129
Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
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Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism01:21

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism

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Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
295

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Computer-driven formulation development of Ginsenoside Rh2 ternary solid dispersion.

Tianshu Lu1,2, Tongchuan Wu3, Hao Zhong2

  • 1Institute of Applied Physics and Materials Engineering, University of Macau, Macau, 999078, China.

Drug Delivery and Translational Research
|June 24, 2024
PubMed
Summary

This study developed an improved formulation for (20 S)-Ginsenoside Rh2, enhancing its solubility and bioavailability for better anticancer drug delivery. Advanced computational and experimental methods were used to create a novel solid dispersion.

Keywords:
(20S)-Ginsenoside Rh2Dissolution rateGelucire 44/14Molecular dynamics simulationTernary solid dispersion

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Computational Chemistry

Background:

  • (20 S)-Ginsenoside Rh2, a potent anticancer saponin from Panax ginseng, suffers from poor water solubility and bioavailability, limiting its therapeutic use.
  • Developing advanced formulations is crucial to overcome these limitations and unlock the full potential of Ginsenoside Rh2 in cancer treatment.

Purpose of the Study:

  • To engineer a modified (20 S)-Ginsenoside Rh2 formulation with significantly enhanced solubility, dissolution rate, and bioavailability.
  • To utilize a combined computational and experimental approach for optimizing solid dispersion formulation development.

Main Methods:

  • Utilized the 'PharmSD' model to predict optimal polymers for solid dispersion, followed by experimental assessment of solubility and dissolution.
  • Employed Powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR), and molecular dynamics simulations for characterization and mechanism elucidation.
  • Conducted in vitro cell and in vivo animal experiments to evaluate the efficacy and absorption of the developed formulation.

Main Results:

  • Gelucire 44/14 was identified as the optimal polymer, with a ternary solid dispersion including sodium dodecyl sulfate (SDS) further enhancing dissolution rates.
  • Characterization confirmed the amorphous state of (20 S)-Ginsenoside Rh2 within the solid dispersion, with hydrogen bonding interactions observed between the drug and excipients.
  • The modified formulation exhibited reduced efflux ratio in cell studies and significantly improved in vivo absorption in rats compared to pure (20 S)-Ginsenoside Rh2.

Conclusions:

  • Successfully developed an optimized ternary solid dispersion of (20 S)-Ginsenoside Rh2 with superior solubility, dissolution, and bioavailability.
  • The integration of Artificial Intelligence (AI) and molecular dynamics simulation proved effective in guiding formulation development for poorly soluble drugs.
  • This approach offers a promising strategy for enhancing the pharmaceutical applications of natural compounds like Ginsenoside Rh2.