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

Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence

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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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Formulation and Manufacturing Process: Physical Attributes of Generic Tablets and Capsules01:18

Formulation and Manufacturing Process: Physical Attributes of Generic Tablets and Capsules

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Bioequivalence in generic drugs, such as tablets and capsules, refers to their pharmaceutical equivalence to the brand-name counterparts. However, for therapeutic equivalence, manufacturers must also consider physical attributes like size, shape, and weight (FDA Guidance for Industry, December 2003). Discrepancies in these aspects could impact patient compliance and cause medication errors. For instance, swallowing difficulties, often experienced with larger tablets or capsules, can lead to...
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Factors Affecting Dissolution: Particle Size and Effective Surface Area01:23

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Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are...
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Upstream Processing01:27

Upstream Processing

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Upstream processing represents a critical phase in biomanufacturing, wherein biological systems such as microorganisms, mammalian cells, or insect cells are cultivated to produce therapeutic proteins, vaccines, enzymes, or other biologically derived products. This phase encompasses all steps from the selection and genetic manipulation of the production organism to the cultivation of cells in bioreactors under tightly controlled environmental conditions.Host Selection and Genetic OptimizationThe...
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Formation of Dispersible Taohong Siwu Tablets
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Downstream processing of polymer-based amorphous solid dispersions to generate tablet formulations.

B Démuth1, Z K Nagy1, A Balogh1

  • 1Department of Organic Chemistry and Technology, Budapest University of Technology and Economics (BUTE), Budafoki út 8, 1111 Budapest, Hungary.

International Journal of Pharmaceutics
|April 2, 2015
PubMed
Summary
This summary is machine-generated.

Amorphous solid dispersions (ASDs) enhance drug bioavailability but face challenges in tableting. This review summarizes strategies to overcome these hurdles for improved drug delivery systems.

Keywords:
Amorphous solid dispersionElectrospinningExtrusionGelling polymer networkSpray-dryingTableting

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Area of Science:

  • Pharmaceutical Sciences
  • Materials Science
  • Drug Delivery

Background:

  • Amorphous solid dispersions (ASDs) are crucial for improving the bioavailability of poorly water-soluble drugs.
  • Challenges include poor powder properties, compression-induced changes, and slow disintegration due to polymer gelation.
  • ASD systems aim to create supersaturated drug solutions, but risk precipitation and crystallization.

Purpose of the Study:

  • To review the conversion of ASDs into tablets.
  • To highlight progress and challenges in ASD tableting.
  • To understand strategies for maintaining drug supersaturation and enhancing bioavailability.

Main Methods:

  • Literature review of ASD formulation and tableting.
  • Analysis of pharmaceutical and technological challenges.
  • Examination of methods to inhibit drug crystallization.

Main Results:

  • ASDs present significant tableting challenges like poor flowability and compressibility.
  • Compression can induce phase changes or separation in ASDs.
  • Maintaining supersaturation during dissolution and storage is key for biopharmaceutical performance.

Conclusions:

  • Effective tableting of ASDs requires addressing powder properties and preventing phase transitions.
  • Inhibiting crystallization is vital for sustained supersaturation and enhanced bioavailability.
  • Further research is needed to optimize ASD-based dosage forms for manufacturing and storage.