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Bioavailability Enhancement: Drug Stability Enhancement and GI Retention01:05

Bioavailability Enhancement: Drug Stability Enhancement and GI Retention

Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
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The long-term stability of drug products is critical to ensuring their quality, safety, and effectiveness over time. Stability directly influences a product's ability to maintain its intended characteristics, ensuring it performs as expected during its intended shelf life. Key attributes such as drug potency, impurities, dissolution, and other physicochemical measures of performance are tested to assess stability. These parameters indicate how well the product retains its quality over time and...
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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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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...
In Vitro Drug Release Testing: Overview, Development and Validation01:10

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Related Experiment Video

Updated: May 16, 2026

Process Development for the Spray-Drying of Probiotic Bacteria and Evaluation of the Product Quality
05:45

Process Development for the Spray-Drying of Probiotic Bacteria and Evaluation of the Product Quality

Published on: April 7, 2023

Development of probiotic tablets using microparticles: viability studies and stability studies.

J P Sousa e Silva1, Sérgio C Sousa, Paulo Costa

  • 1Department of Drug Sciences, Faculty of Pharmacy, University of Porto, Rua Jorge Viterbo Ferreira, 228, 4050-313, Porto, Portugal. paulo.silva@ff.up.pt

AAPS Pharmscitech
|December 13, 2012
PubMed
Summary

New probiotic tablets protect Lactobacillus paracasei L26 from stomach acid, improving delivery to the colon. These easily manufactured tablets offer a promising way to deliver beneficial bacteria for probiotic therapy.

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Area of Science:

  • Microbiology
  • Pharmaceutical Sciences
  • Food Science

Background:

  • Probiotics require effective delivery systems to survive gastrointestinal conditions.
  • Existing vectors often lack sufficient resistance to gastric acidity.
  • Development of scalable dosage forms for probiotic delivery is crucial.

Purpose of the Study:

  • To develop a tablet formulation for protecting entrapped probiotic bacteria, specifically Lactobacillus paracasei L26.
  • To create an easily manufactured, scalable dosage form for enhanced probiotic delivery to the colon.
  • To evaluate the viability, gastric resistance, and release profile of encapsulated L. paracasei L26.

Main Methods:

  • Spray-drying of whey protein concentrate microparticles containing L. paracasei L26.
  • Incorporation of microparticles into tablets with cellulose acetate phthalate and sodium croscarmellose.
  • Assessment of bacterial viability during tableting, gastric resistance, release kinetics, and storage stability.

Main Results:

  • Probiotic tablets demonstrated protection against gastric acidity, with a one logarithmic cycle decrease post-acid exposure.
  • Release of L. paracasei L26 from tablets occurred after 4 hours under tested conditions.
  • Viability decreased by 2 log cycles after 60 days of storage, but remained stable for 45 days under simulated gastrointestinal conditions.

Conclusions:

  • Developed probiotic tablets serve as effective vectors for delivering viable L. paracasei L26.
  • The formulation offers a scalable and potentially beneficial approach for probiotic therapy.
  • Further research may extend this technology to other probiotic strains for enhanced gut health.