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Bioavailability Enhancement: Drug Solubility Enhancement01:16

Bioavailability Enhancement: Drug Solubility Enhancement

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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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Bioavailability Enhancement: Drug Stability Enhancement and GI Retention01:05

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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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Bioavailability Enhancement: Drug Permeability Enhancement01:27

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After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt secretion,...
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Factors Influencing Drug Absorption: Drug Dissolution01:27

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The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...
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Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

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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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Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism01:21

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism

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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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Enhancement of docetaxel solubility using binary and ternary solid dispersion systems.

Sue May Lim1, Zyu Wenn Pang1, Hwei Yuin Tan1

  • 1a International Medical University , Kuala Lumpur , Malaysia and.

Drug Development and Industrial Pharmacy
|February 28, 2015
PubMed
Summary

Oral docetaxel (DTX) solid dispersions (SDs) were developed to improve drug solubility. Soluplus significantly enhanced DTX solubility, showing promise for oral drug delivery.

Keywords:
Anti-cancerSoluplusapparent solubilityfreeze-dryingsolubility parameter

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Formulation Development

Background:

  • Intravenous docetaxel (DTX) faces challenges with poor biopharmaceutical properties and toxicity.
  • Development of an oral DTX formulation is crucial for improved patient compliance and reduced side effects.

Purpose of the Study:

  • To enhance the solubility of poorly soluble docetaxel (DTX) using solid dispersion (SD) technology.
  • To explore novel oral drug delivery systems for docetaxel.

Main Methods:

  • Formulation of DTX solid dispersions (SDs) with various solubilizers including Soluplus, Kollidon 12PF, Lutrol F68, and Hydroxypropyl-β-cyclodextrin.
  • Utilized freeze-drying technique for SD preparation and evaluated kinetic solubility for optimal drug-solubilizer combinations.
  • Characterized promising SD formulations using DSC, PXRD, FTIR, and SEM.

Main Results:

  • Soluplus demonstrated superior performance among all tested excipients in enhancing DTX solubility.
  • A binary SD of DTX and Soluplus (1:10 ratio) achieved a 93-fold increase in solubility, reaching 362.93 ± 11.01 µg/mL.
  • The enhanced solubility is attributed to solid-state transformation and micellization effects.

Conclusions:

  • Soluplus solid dispersion is a highly promising excipient for developing oral docetaxel formulations.
  • The developed SD approach offers a viable strategy for improving the oral bioavailability of poorly soluble drugs like docetaxel.