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Published on: July 27, 2022
Bioavailability and pharmacokinetic studies of rofecoxib solid dispersion
Y Prasannaraju1, V Harini Chowdary, V Jayasri
1Department. of Pharmaceutics, Sree Vidyanikethan College of Pharmacy, A. Rangampet, Tirupati, 517102, Andhra Pradesh, India. kanishka9002@gmail.com.
Current Drug Delivery
|June 19, 2013
Summary
This study compared the bioavailability of Rofecoxib solid dispersion to pure Rofecoxib (RFB) in healthy volunteers. The solid dispersion formulation significantly enhanced Rofecoxib bioavailability, showing higher peak plasma concentrations.
Area of Science:
- Pharmacokinetics
- Drug Delivery Systems
- Medicinal Chemistry
Background:
- Rofecoxib (RFB) is a non-steroidal anti-inflammatory drug (NSAID).
- Improving the bioavailability of Rofecoxib is crucial for its therapeutic efficacy.
- Solid dispersion technology offers a promising approach for enhancing drug absorption.
Purpose of the Study:
- To determine and compare the bioavailability of Rofecoxib solid dispersion versus pure Rofecoxib.
- To evaluate the pharmacokinetic profile of Rofecoxib formulations in healthy volunteers.
Main Methods:
- A non-blinded, open-label, crossover study was conducted in six healthy volunteers.
- Blood samples were collected over 12 hours post-administration and analyzed using High-Performance Liquid Chromatography (HPLC).
- Key pharmacokinetic parameters including Cmax, tmax, Kel, t1/2, Ka, and AUC were determined.
Main Results:
- The Rofecoxib solid dispersion, utilizing hupu gum as a carrier, demonstrated significantly higher bioavailability compared to pure Rofecoxib.
- Peak plasma concentrations (Cmax) were 76.84 ng/mL at 3 hours for the solid dispersion, versus 8.34 ng/mL at 4 hours for pure Rofecoxib.
- The study indicated a marked enhancement in Rofecoxib bioavailability with the solid mixture preparation.
Conclusions:
- Rofecoxib solid dispersion formulated with hupu gum significantly enhances Rofecoxib bioavailability.
- This formulation strategy holds potential for improving the therapeutic outcomes of Rofecoxib.
- Solid dispersion is an effective method for improving the pharmacokinetic profile of poorly soluble drugs like Rofecoxib.
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