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Related Concept Videos

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Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
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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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The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...
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The physicochemical characteristics of drugs play a crucial role in formulating stable and bioavailable drug products. The solubility of a drug, governed by the varying pH along the GI tract and its dissociation constant (pKa), is pivotal in determining its ionization state and absorption rate. Notably, weak acids and bases remain unionized and are absorbed more rapidly.
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Formation of Dispersible Taohong Siwu Tablets
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Stiripentol Enteric Solid Dispersion-Loaded Effervescent Tablets: Enhanced Dissolution, Stability, and Absorption.

Ying Wang1, Siyuan Xu1, Ziyue Xiao1

  • 1Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing, 211198, China.

AAPS Pharmscitech
|May 10, 2022
PubMed
Summary

This study developed effervescent tablets with stiripentol (STP) solid dispersions to overcome poor solubility and acid stability issues. The new formulation significantly enhanced STP bioavailability and absorption, offering a promising oral drug delivery method.

Keywords:
amorphouseffervescent tabletsepilepsysolid dispersionsstiripentol

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Area of Science:

  • Pharmaceutical Technology
  • Drug Delivery Systems
  • Materials Science

Background:

  • Stiripentol (STP) exhibits poor solubility and stability in acidic conditions, hindering effective gastrointestinal administration.
  • Developing stable and soluble oral formulations for acid-labile drugs like STP remains a significant pharmaceutical challenge.

Purpose of the Study:

  • To investigate the use of effervescent tablets containing stiripentol-loaded enteric solid dispersions.
  • To enhance the solubility, stability, and bioavailability of stiripentol for oral delivery.

Main Methods:

  • Preparation of stiripentol-loaded solid dispersions (STP-SDs) via solvent evaporation.
  • Formulation and optimization of effervescent tablets (STP-SD-ETs) using dry granulation technology.
  • Characterization of STP-SDs for solid-state properties, in vitro release, and stability.

Main Results:

  • Enterically coated amorphous STP-SDs were successfully prepared, significantly improving STP solubility and stability.
  • STP-SD-ETs demonstrated a 138.71% bioavailability compared to STP suspensions.
  • The effervescent tablets notably increased the intestinal absorption rate of stiripentol.

Conclusions:

  • The combination of enteric solid dispersion and effervescent tablet technology offers an effective strategy for improving stiripentol's dissolution, stability, and absorption.
  • This approach presents a promising method for enhancing the oral delivery of drugs with poor solubility and acid-labile characteristics.