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Related Concept Videos

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

Bioavailability Enhancement: Drug Stability Enhancement and GI Retention

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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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Modified-Release Drug Delivery Systems: Bioavailability01:30

Modified-Release Drug Delivery Systems: Bioavailability

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Modified-release (MR) dosage forms are designed to extend drug release over time, thereby maintaining stable plasma concentrations and reducing dosing frequency. However, their bioavailability is typically below 100% due to incomplete drug release and presystemic metabolism, and limitations in drug permeability across the gastrointestinal epithelium, all of which can restrict the fraction of the drug reaching systemic circulation. Consequently, studying the in vivo bioavailability of MR...
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Bioavailability Enhancement: Drug Permeability Enhancement01:27

Bioavailability Enhancement: Drug Permeability Enhancement

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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 Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

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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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Oral Drug Delivery Systems: Continuous-Release Systems01:26

Oral Drug Delivery Systems: Continuous-Release Systems

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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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Related Experiment Video

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Resveratrol cocrystals with enhanced solubility and tabletability.

Zhengzheng Zhou1, Wanying Li2, Wei-Jhe Sun3

  • 1State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao; Hygiene Detection Center, Guangdong Provincial Key Laboratory of Tropical Disease Research, School of Public Health, Southern Medical University, Guangdong, Guangzhou 510515, China.

International Journal of Pharmaceutics
|June 11, 2016
PubMed
Summary

Two novel resveratrol cocrystals with 4-aminobenzamide and isoniazid were developed. These cocrystals demonstrate enhanced solubility and tabletability, making them promising for pharmaceutical tablet formulations.

Keywords:
CocrystalMechanical propertyResveratrol (RES)SolubilityTabletability

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Area of Science:

  • Pharmaceutical Science
  • Materials Science
  • Crystallography

Background:

  • Resveratrol (RES) is a polyphenol with potential health benefits but limited bioavailability.
  • Developing novel formulations to improve RES solubility and delivery is crucial for therapeutic applications.

Purpose of the Study:

  • To synthesize and characterize new resveratrol cocrystals with improved pharmaceutical properties.
  • To evaluate the potential of these cocrystals for enhanced tablet formulation development.

Main Methods:

  • Cocrystal synthesis using liquid-assisted grinding (LAG) and rapid solvent removal (RSR) with ethanol.
  • Physicochemical characterization via PXRD, DSC, NMR, FT-IR, and HPLC.
  • Evaluation of pharmaceutical properties: solubility, dissolution rate, tabletability, and hygroscopicity.

Main Results:

  • Two new 1:1 cocrystals, RES-4ABZ and RES-ISN, were successfully synthesized.
  • Both cocrystals exhibited significantly higher solubility and improved tabletability compared to pure resveratrol.
  • The cocrystals demonstrated phase stability and were non-hygroscopic under high humidity.

Conclusions:

  • The novel resveratrol cocrystals show enhanced solubility and tabletability, addressing key limitations of pure resveratrol.
  • These RES cocrystals are promising candidates for developing advanced tablet formulations.
  • The study highlights the utility of cocrystallization as a strategy for improving drug delivery and formulation characteristics.