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Bioavailability Enhancement: Drug Solubility Enhancement01:16

Bioavailability Enhancement: Drug Solubility Enhancement

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...
Bioavailability Enhancement: Drug Stability Enhancement and GI Retention01:05

Bioavailability Enhancement: Drug Stability Enhancement and GI Retention

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...
Bioavailability Enhancement: Drug Permeability Enhancement01:27

Bioavailability Enhancement: Drug Permeability Enhancement

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Factors Affecting Dissolution: Particle Size and Effective Surface Area01:23

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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 employed to...
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Updated: Jul 16, 2026

Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs
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Rosuvastatin-Metformin Co-Processing: Enhanced Dissolution, Oral Bioavailability, and Therapeutic Efficacy through a

Soha M El-Masry1, Shaimaa K Mostafa2, Shaimaa M Khedr3

  • 1Department of Pharmaceutics, Faculty of Pharmacy, Damanhour University, Damanhour, P.O. Box 22516, Egypt.

Drug Development and Industrial Pharmacy
|July 15, 2026
PubMed
Summary

This study developed a novel co-processed fixed-dose combination of rosuvastatin (ROS) and metformin (MET) using a solvent-minimized wet co-grinding method. The enhanced formulation significantly improved ROS dissolution, bioavailability, and anti-hyperlipidemic efficacy, offering a promising treatment for dyslipidemia and type 2 diabetes.

Keywords:
MetforminRosuvastatindissolution ratedyslipidemiapharmacokineticswet co-grinding

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Last Updated: Jul 16, 2026

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Published on: July 27, 2022

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07:58

Formulation and Characterization of Bioactive Agent Containing Nanodisks

Published on: March 17, 2023

Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Biopharmaceutics

Background:

  • Rosuvastatin calcium (ROS) exhibits poor aqueous solubility, limiting its oral absorption and therapeutic effectiveness.
  • Developing fixed-dose combinations (FDCs) for managing comorbid conditions like dyslipidemia and type 2 diabetes is clinically relevant.

Purpose of the Study:

  • To develop an oral co-processed fixed-dose combination of rosuvastatin (ROS) and metformin hydrochloride (MET) to enhance ROS dissolution and oral bioavailability.
  • To evaluate the biopharmaceutical performance and therapeutic efficacy of the co-processed ROS/MET system.

Main Methods:

  • Co-processed ROS/MET systems were prepared using a solvent-minimized wet co-processing approach.
  • Formulations were characterized using FTIR, PXRD, DSC/TGA, and SEM.
  • In vitro dissolution, in vivo pharmacokinetic studies in rats, and anti-hyperlipidemic efficacy assessments were conducted.

Main Results:

  • The co-processed ROS/MET formulation (F2) significantly enhanced rosuvastatin dissolution across various pH conditions compared to unprocessed ROS.
  • Pharmacokinetic studies showed a 21.5% increase in relative bioavailability and a 1.34-fold increase in Cmax for co-processed ROS.
  • The co-processed formulation demonstrated improved liver drug distribution and superior anti-hyperlipidemic effects in hyperlipidemic rats.

Conclusions:

  • Co-processing rosuvastatin with metformin via a solvent-minimized wet co-grinding method is an effective strategy to improve ROS dissolution, bioavailability, and therapeutic efficacy.
  • This approach offers a promising avenue for the clinical management of dyslipidemia and type 2 diabetes mellitus.