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Related Concept Videos

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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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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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

Factors Affecting Dissolution: Particle Size and Effective Surface Area

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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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Bioavailability Enhancement: Drug Stability Enhancement and GI Retention01:05

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Body: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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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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Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study
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Scalemic mixtures preparation for optimized composition of ibuprofen solid dosage forms.

Yohann Corvis1, Nicolas Guiblin2, Philippe Négrier3

  • 1Université de Paris, Faculté de Santé, CNRS, Inserm, UTCBS, Chemical and Biological Technologies for Health Group (utcbs.cnrs.fr), 4 avenue de l'Observatoire, 75006 Paris, France.

European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V
|September 27, 2021
PubMed
Summary

Researchers established phase diagrams for ibuprofen enantiomers, proving the existence of a stable solid solution. This finding offers a new method for preparing enantiomeric mixtures to enhance ibuprofen

Keywords:
Drug-drug interactionEnantiomeric mixturesPhase diagramRacemateSolid solutionThermal behaviorX-ray pattern

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Area of Science:

  • Pharmaceutical Science
  • Solid-State Chemistry
  • Crystallography

Background:

  • Ibuprofen exists as two enantiomers: sinister (S) and rectus (R).
  • The rectus enantiomer is pharmacologically inactive but can convert to the active sinister enantiomer in vivo.
  • Understanding the solid-state behavior of ibuprofen enantiomers is crucial for drug formulation.

Purpose of the Study:

  • To establish the stable and metastable phase diagrams of sinister and rectus ibuprofen enantiomers.
  • To investigate the formation of solid solutions between ibuprofen enantiomers.
  • To explore a novel approach for preparing scalemic ibuprofen mixtures for improved therapeutic outcomes.

Main Methods:

  • Thermal analysis (e.g., Differential Scanning Calorimetry).
  • X-ray powder diffraction (XRPD) experiments.
  • Phase diagram determination as a function of temperature.

Main Results:

  • The stable and metastable phase diagrams for ibuprofen enantiomers were successfully established.
  • The existence of a stable solid solution was demonstrated for the first time when mixing racemic ibuprofen with a low concentration of an enantiomer.
  • Characterization of the solid-state behavior under varying temperatures.

Conclusions:

  • This study provides the first evidence of a stable solid solution in ibuprofen enantiomeric mixtures.
  • The findings offer a new strategy for preparing specific scalemic mixtures of ibuprofen.
  • This approach has the potential to optimize the benefit/risk ratio of ibuprofen solid dosage forms.