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Factors Influencing Drug Absorption: Pharmaceutical Parameters01:28

Factors Influencing Drug Absorption: Pharmaceutical Parameters

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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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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).
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
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Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

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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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In Vitro Drug Dissolution: Alternative Methods01:17

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Alternative drug dissolution methods include the rotating bottle, intrinsic dissolution test, peristalsis, and the Franz diffusion cell method. The rotating bottle method involves meticulously rotating tightly capped controlled-release beads in a temperature-controlled bath. Periodic decanting of samples allows for residue assay, followed by refilling with fresh medium and testing at various pH levels to emulate the gastrointestinal tract conditions.In contrast, the intrinsic dissolution test...
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Bioavailability Enhancement: Drug Solubility Enhancement01:16

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Body:Bioavailability is a critical factor in determining a drug's effectiveness. It refers to the proportion of a drug that enters the circulation when introduced into the body and is, as a result, able to have an active effect. Enhancing bioavailability is essential for drugs with poor solubility, as it can significantly impact their therapeutic efficacy. Various methods are employed to increase the solubility of drugs, thereby enhancing their bioavailability.Micronization and nanonization are...
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Developing Multi-Component Solid Formulation Strategies for PROTAC Dissolution Enhancement.

Martin A Screen1, Sean Askin2, James F McCabe3

  • 1Department of Chemistry, Durham University, South Road, Durham DH1 3LE, U.K.

Molecular Pharmaceutics
|October 2, 2025
PubMed
Summary
This summary is machine-generated.

Amorphous solid dispersions (ASDs) enhance the bioavailability of Proteolysis Targeting Chimeras (PROTACs), enabling oral drug delivery. Slurry-prepared ASDs show superior solubility enhancement and stability compared to other formulations.

Keywords:
ASDPROTACsamorphousdissolutionformulation

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery
  • Medicinal Chemistry

Background:

  • Proteolysis Targeting Chimeras (PROTACs) are novel therapeutics for cancer, but their poor solubility and amorphous nature limit bioavailability.
  • Developing oral formulations for PROTACs is challenging due to their physicochemical properties and limited sample availability.

Purpose of the Study:

  • To investigate amorphous solid dispersions (ASDs) using hydroxypropyl methylcellulose acetate succinate (HPMCAS) to enhance the dissolution and bioavailability of PROTACs.
  • To compare formulation strategies, including slurry conversion versus solvent evaporation, and evaluate physical stability.

Main Methods:

  • Preparation of ASDs of four cereblon-recruiting PROTACs (AZ1-4) with HPMCAS.
  • Characterization of ASDs, including drug loading, supersaturation, physical stability (Tg, DSC, FTIR), and dissolution testing.
  • Comparison with coamorphous formulations and pure amorphous active pharmaceutical ingredients (APIs).

Main Results:

  • ASDs of AZ1 demonstrated up to a 2-fold increase in drug supersaturation compared to the pure amorphous API.
  • Slurry-prepared ASDs exhibited greater solubility enhancement and maintained advantages at higher drug loadings than solvent-evaporated ASDs.
  • ASDs showed good physical stability under accelerated conditions, unlike coamorphous formulations which lacked dissolution benefits.

Conclusions:

  • ASDs are a viable strategy for improving PROTAC oral bioavailability and creating commercializable solid forms.
  • Formulation by slurry conversion is superior to solvent evaporation for enhancing PROTAC solubility.
  • Further research is needed to optimize formulation approaches for beyond-rule-of-5 (bRo5) compounds like PROTACs.