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Related Concept Videos

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism01:21

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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).
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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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Prodrugs are a class of pharmaceutical compounds that undergo a biotransformation process within the body to be converted into a pharmacologically active drug. Prodrugs are designed to improve the therapeutic properties of the parent drug, such as enhancing bioavailability, increasing stability, or reducing toxicity. The concept of prodrugs revolves around modifying the chemical structure of the original drug to make it more effective or convenient for administration.
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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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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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Related Experiment Video

Updated: Jun 9, 2025

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Considerations and Challenges to Develop Drug-drug Coamorphous System: A Recent Update.

Madhura Tiwari1, Kavita Singh1, Bappaditya Chatterjee2

  • 1Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKM's NMIMS, Mumbai, 400056, India.

Current Pharmaceutical Biotechnology
|November 1, 2024
PubMed
Summary

Drug-drug coamorphous systems (CAS) enhance solubility for poorly water-soluble medications. Careful drug selection and processing are key to creating stable, effective amorphous drug formulations.

Keywords:
Coamorphousamorphisationconformermolecular interactionpolymeric amorphous systems.solubility

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery
  • Materials Science

Background:

  • Poor water solubility limits oral absorption of many drugs, particularly BCS Class II and IV.
  • Amorphization improves drug solubility and dissolution, but polymeric systems have drawbacks like low drug loading.
  • Coamorphous systems utilize a coformer to stabilize the amorphous drug form.

Purpose of the Study:

  • To explore drug-drug coamorphous systems (CAS) as a strategy for enhancing solubility of poorly water-soluble drugs.
  • To address challenges in drug selection, ratio optimization, and processing stability for CAS.
  • To highlight the importance of molecular-level interactions and excipient selection in CAS development.

Main Methods:

  • In silico prediction of miscibility.
  • Molecular dynamic simulations.
  • Analysis of molecular interactions using techniques like FTIR, Raman spectroscopy, and NMR.

Main Results:

  • Drug-drug coamorphous systems offer a promising approach to overcome solubility limitations.
  • Understanding and analyzing molecular-level interactions are crucial for stable CAS formation.
  • Careful selection of drugs, ratios, and processing methods is essential for therapeutic efficacy and safety.

Conclusions:

  • Drug-drug coamorphous systems represent an advanced strategy for improving oral bioavailability.
  • Further research into rational drug selection and processing optimization is needed for robust CAS development.
  • Excipient choice plays a critical role in the successful formulation of stable and effective CAS.