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Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence01:27

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Changes in polymorphic forms can significantly influence the bioavailability of poorly soluble drugs. Although the FDA defines pharmaceutical equivalence based on having the same active ingredient, dosage form, and route of administration, it does not automatically disqualify products with different polymorphic forms. This means two products with different polymorphs can still be deemed pharmaceutically equivalent. However, polymorphic differences can affect properties like wettability,...
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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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Related Experiment Video

Updated: Nov 7, 2025

Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
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Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles

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Statistically optimized pentazocine loaded microsphere for the sustained delivery application: Formulation and

Abdul Jabar1, Asadullah Madni1, Sajid Bashir2

  • 1Department of Pharmacy, The Islamia University of Bahawalpur, Bahawalpur, Pakistan.

Plos One
|April 30, 2021
PubMed
Summary

New ethyl cellulose microspheres effectively deliver pentazocine (PTZ) for sustained pain management. This drug delivery system enhances PTZ bioavailability and provides prolonged release for over 12 hours.

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Area of Science:

  • Pharmaceutics
  • Materials Science

Background:

  • Pentazocine (PTZ) is a key analgesic for moderate to severe pain.
  • Current formulations may have limitations in bioavailability and release duration.

Purpose of the Study:

  • To formulate and characterize pentazocine-loaded ethyl cellulose microspheres.
  • To achieve sustained release and improved bioavailability of pentazocine.

Main Methods:

  • Oil-in-water emulsion solvent evaporation technique was employed.
  • Box-Behnken design was used for optimization.
  • Microspheres were characterized for morphology, physicochemical properties, stability, and drug release.

Main Results:

  • Maximum yield of 98.67% and 98% PTZ entrapment achieved.
  • Microspheres exhibited spherical, porous structures (50-148μm).
  • Sustained release of PTZ for over 12 hours, following zero-order kinetics.

Conclusions:

  • Ethyl cellulose microspheres are a promising drug delivery system for pentazocine.
  • The formulation demonstrates potential for effective pain management.
  • The study validates the stability and controlled-release properties of the microspheres.