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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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Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs
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Atorvastatin solid dispersion for bioavailability enhancement.

Shamsuddin1, Mohammad Fazil2, Shahid H Ansari3

  • 1Department of Pharmacy, OPJS University, Churu, Rajasthan, India.

Journal of Advanced Pharmaceutical Technology & Research
|March 9, 2016
PubMed
Summary
This summary is machine-generated.

This study improved atorvastatin calcium

Keywords:
Atorvastatin calciumbioavailability enhancementconventional fusion methodsolid dispersion

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems

Background:

  • Atorvastatin calcium, a lipid-lowering agent, exhibits low bioavailability (approx. 15%).
  • Poor solubility and dissolution limit the therapeutic efficacy of atorvastatin calcium.
  • Undesirable adverse effects can arise from the unabsorbed portion of the drug.

Purpose of the Study:

  • To enhance the solubility and dissolution profile of atorvastatin (AT) calcium.
  • To develop an improved drug delivery system for atorvastatin calcium.

Main Methods:

  • Solid dispersion (SD) technique was employed to improve atorvastatin calcium's properties.
  • Conventional fusion method using polyethylene glycol 4000 (PEG 4000) as a hydrophilic carrier was utilized.
  • Solubility and dissolution rates were evaluated using phosphate buffer (pH 6.8).
  • Fourier transform infrared (FTIR) and differential scanning calorimetry (DSC) were used for characterization.

Main Results:

  • Solubility of atorvastatin calcium significantly increased in solid dispersion (93.66 ± 1.35%) compared to pure drug (55.33 ± 0.66%) and physical mixture (81.89 ± 2.35%).
  • Solid dispersion formulation converted atorvastatin calcium from crystalline to amorphous form, confirmed by FTIR and DSC.
  • Dissolution rate was significantly enhanced, with 91.66 ± 1.65% drug release at 1 hour for SD, compared to 28.92 ± 1.66% for pure drug and 72.16 ± 1.33% for a marketed tablet.

Conclusions:

  • Solid dispersion formulation effectively enhances the solubility and dissolution profile of atorvastatin calcium.
  • The developed solid dispersion shows superior performance compared to existing marketed preparations.
  • This approach offers a promising strategy for improving the bioavailability and therapeutic outcomes of poorly soluble drugs like atorvastatin calcium.