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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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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).
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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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Polymeric carriers enhance targeted drug delivery by increasing efficacy while minimizing off-target effects. These carriers comprise a biodegradable polymeric backbone integrated with functional elements that enable targeting, improve physicochemical properties, and regulate drug release.Targeting MechanismsThe targeting ability of polymeric carriers is mediated by a homing device, which is a molecular recognition component designed to selectively bind to specific tissues or cells. Monoclonal...
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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...
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Acyclovir-Polyethylene Glycol 6000 Binary Dispersions: Mechanistic Insights.

Krishnamoorthy Venkateskumar1, Subramani Parasuraman2, Raju Gunasunderi3

  • 1Department of Pharmaceutical Technology, Faculty of Pharmacy, AIMST University, Semeling, 08100, Bedong, Kedah Darul Aman, Malaysia. venkateskumar@aimst.edu.my.

AAPS Pharmscitech
|December 23, 2016
PubMed
Summary

This study enhances acyclovir (ACY) solubility using polyethylene glycol 6000 (PEG6000), improving oral bioavailability. Solid dispersions significantly boosted ACY

Keywords:
acyclovircrystallinitydrug-polymer miscibilitysolid dispersions

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery
  • Physical Chemistry

Background:

  • Acyclovir (ACY) exhibits poor aqueous solubility, limiting its oral bioavailability.
  • Enhancing ACY solubility is crucial for effective drug formulation.
  • Polyethylene glycol 6000 (PEG6000) is explored as a carrier for solubility enhancement.

Purpose of the Study:

  • To provide mechanistic insights into the solubility and dissolution enhancement of acyclovir (ACY).
  • To investigate the use of polyethylene glycol 6000 (PEG6000) as a carrier for ACY.
  • To evaluate the impact of PEG6000 on ACY's oral bioavailability and formulation properties.

Main Methods:

  • Preparation and evaluation of acyclovir-polyethylene glycol 6000 (ACY-PEG6000) solid dispersions.
  • Phase solubility, in vitro release, kinetic analysis, in situ perfusion, and in vitro permeation studies.
  • Solid-state characterization using XRD, DSC, FTIR, NMR, SEM, and AFM.

Main Results:

  • Solid dispersions significantly increased aqueous solubility and dissolution rate of ACY.
  • Characterization confirmed solid solution formation, reduced crystallinity, and no drug-carrier interaction.
  • Enhanced permeation and stability were observed in ACY-PEG6000 dispersions.

Conclusions:

  • PEG6000 effectively enhances acyclovir solubility and dissolution.
  • Solid dispersions provide a viable strategy for overcoming ACY's poor aqueous solubility.
  • These findings offer a platform for developing improved ACY formulations.