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Related Concept Videos

Oral Drug Delivery Systems: Continuous-Release Systems01:26

Oral Drug Delivery Systems: Continuous-Release Systems

Continuous-release drug delivery systems offer a strategic approach to maintaining therapeutic drug levels over extended periods following oral administration. By modulating the release rate of active pharmaceutical ingredients, these systems minimize fluctuations in plasma concentrations, which enhances clinical efficacy and reduces the need for frequent dosing. Such characteristics make them particularly advantageous in managing chronic diseases where patient adherence and stable drug...
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Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence

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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Factors Influencing Drug Absorption: Pharmaceutical Parameters

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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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).
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Adrenergic agonists' structure-activity relationship (SAR) determines their selectivity and efficacy. These agonists comprise a phenylethylamine moiety with an aromatic ring and an ethylamine side chain.
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Oral drug delivery is the most common route of administration due to its convenience, cost-effectiveness, and high patient compliance. It enables precise formulation to ensure proper drug dosage and bioavailability. The development of oral dosage forms considers drug properties such as solubility, stability, and absorption to optimize therapeutic efficacy.Tablets, capsules, liquids, and chewable formulations enhance drug stability, mask undesirable tastes, and improve patient experience.

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Synthesis of a Borylated Ibuprofen Derivative Through Suzuki Cross-Coupling and Alkene Boracarboxylation Reactions
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Structures from powders: bupropion hydrochloride.

Elisabetta Maccaroni1, Luciana Malpezzi, Norberto Masciocchi

  • 1Dipartimento di Scienze Chimiche e Ambientali, Università dell'Insubria, Via Valleggio 11, I-22100 Como, Italy. emaccaroni@gmail.com

Journal of Pharmaceutical and Biomedical Analysis
|May 26, 2009
PubMed
Summary

This study fully characterized the crystal structure of bupropion hydrochloride using ab-initio X-ray powder diffraction. The research determined its crystal system, space group, and lattice parameters, revealing specific molecular interactions.

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Area of Science:

  • Crystallography
  • Solid-state chemistry
  • Pharmaceutical science

Background:

  • Bupropion hydrochloride is an antidepressant medication.
  • Understanding its crystal structure is crucial for formulation and stability.
  • Previous structural data may have been limited or incomplete.

Purpose of the Study:

  • To fully characterize the crystal structure of bupropion hydrochloride.
  • To elucidate the intermolecular interactions within the crystal lattice.
  • To compare the crystal structure with its ethanol solvate.

Main Methods:

  • Ab initio X-ray powder diffraction (XRPD) technique.
  • Global optimization strategy (simulated annealing).
  • Differential scanning calorimetry (DSC) for thermal analysis.

Main Results:

  • Bupropion hydrochloride crystallizes as a racemate in the monoclinic system, space group P2(1)/c.
  • Detailed lattice parameters (a, b, c, beta) and unit cell volume were determined.
  • Strong NH[...]Cl contacts form dimeric entities, with CH[...]O contacts further stabilizing the structure.

Conclusions:

  • The crystal structure of bupropion hydrochloride has been definitively determined.
  • Specific intermolecular interactions dictate the packing and stability of the crystalline form.
  • The structural findings provide a foundation for further pharmaceutical development and quality control.