Skip to content
Research Article Open access CC BY 3.0

Preparation, Characterization and Optimization of Poloxamer Solid Dispersions of a Poorly Water Soluble Drug Aprepitant

Rabia Dhillon, Ritu Ojha, Neena Bedi

Journal of Pharmaceutical Research International · pp. 2436–2454 · Published 23 Oct 2014

10.9734/BJPR/2014/10561

Abstract

Aim: The aim of the present investigation was to enhance the dissolution rate of a poorly water soluble drug, aprepitant, by preparation of solid dispersion with hydrophilic carrier, poloxamer 188, using solvent evaporation method. Place and Duration of Study: Department of Pharmaceutical Sciences and Department of Emerging Life Sciences, Guru Nanak Dev University, Amritsar, Punjab, between August 2012 and July 2013. Study Design: Designs of experiments were carried out with two input variables, drug to carrier ratio (X1) and amount of solvent (X2). A total of 7 experiments were performed (4 factorial runs and 3 centre points) as per full factorial design. Percent dissolution efficiency at 60 min (DE60) was selected as the response variable. Pareto chart along with half probability plot were studied for determining the most significant process variables, which were modelled using ANOVA. Methodology: Solid dispersions of aprepitant with poloxamer 188 were prepared using the solvent evaporation method and studied systematically using an optimization technique. A 22 full factorial design approach was used for the optimization of process variables on dissolution characteristics. The optimized solid dispersion was characterized by dissolution studies, Fourier Transform Infrared Spectroscopy, Differential Scanning Calorimetry, X-ray powder Diffraction studies and Scanning Electron Microscopy. Results: The results of the experimental study confirm that the factors like drug to carrier ratio and solvent amount significantly influence the dependent variable DE60. A high level of drug to carrier ratio and low level of solvent amount were found to be suitable for maximum DE60. The use of factorial design approach helped in the optimization of the solid dispersion. The characterization of optimized solid dispersion (F5) demonstrated that the decrease in crystallinity of aprepitant and poloxamer 188 might be responsible for the enhanced dissolution rate. Analysis of dissolution data indicated the best fitting with first-order model. Conclusion: Dissolution enhancement of aprepitant was successfully obtained by preparing its solid dispersion with poloxamer 188 using solid evaporation method.

Aprepitant poloxamer 188 factorial design dissolution efficiency solid dispersion solvent evaporation.

References (23)

  1. 1 Modeling and comparison of dissolution profiles [DOI]
  2. 2 Mechanism of sustained‐action medication. Theoretical analysis of rate of release of solid drugs dispersed in solid matrices [DOI]
  3. 3 Improving drug solubility for oral delivery using solid dispersions [DOI]
  4. 4 Phase solubility techniques
  5. 5 The concept of dissolution efficiency [DOI]
  6. 6 The current status of solid dispersions.
  7. 7 Solid dispersion of carbamazepine in PVP K30 by conventional solvent evaporation and supercritical methods [DOI]
  8. 8 Studies on dissolution enhancement and mathematical modeling of drug release of a poorly water-soluble drug using water-soluble carriers [DOI]
  9. 9 Amorphous solid dispersions and nano-crystal technologies for poorly water-soluble drug delivery [DOI]
  10. 10 Solid Dispersion as an Approach for Bioavailability Enhancement of Poorly Water-Soluble Drug Ritonavir [DOI]
  11. 11 Improving the solubility of ampelopsin by solid dispersions and inclusion complexes [DOI]
  12. 12 Neurokinin-1 receptor antagonists in the prevention of postoperative nausea and vomiting [DOI]
  13. 13 Phase Behavior of Amorphous Molecular Dispersions I: Determination of the Degree and Mechanism of Solid Solubility [DOI]
  14. 14 Intestinal drug solubility estimation based on simulated intestinal fluids: Comparison with solubility in human intestinal fluids [DOI]
  15. 15 Process optimization and characterization of poloxamer solid dispersions of a poorly water-soluble drug [DOI]
  16. 16 Development of aprepitant, the first neurokinin‐1 receptor antagonist for the prevention of chemotherapy‐induced nausea and vomiting [DOI]
  17. 17 Kneading Technique for Preparation of Binary Solid Dispersion of Meloxicam with Poloxamer 188 [DOI]
  18. 18 Effect of solubilizing and microemulsifying excipients in polyethylene glycol 6000 solid dispersion on enhanced dissolution and bioavailability of ketoconazole [DOI]
  19. 19 Characterization of Ibuproxam Binary and Ternary Dispersions with Hydrophilic Carriers [DOI]
  20. 20 Preparation and In Vitro Evaluation of Solid Dispersions of Total Flavones of Hippophae rhamnoides L. [DOI]
  21. 21 Thermal Behavior and Dissolution Properties of Naproxen From Binary and Ternary Solid Dispersions [DOI]
  22. 22 Inclusion complex of aprepitant with cyclodextrin: evaluation of physico-chemical and pharmacokinetic properties [DOI]
  23. 23 Characterization of olanzapine-solid dispersions.

Cited by 9

Effects of Poloxamers as Excipients on the Physicomechanical Properties, Cellular Biocompatibility, and In Vitro Drug Release of Electrospun Polycaprolactone (PCL) Fibers

Addison Faglie, Rachel Emerine, Shih-Feng Chou · Polymers · 2023

Fabrication of a Double Core–Shell Particle-Based Magnetic Nanocomposite for Effective Adsorption-Controlled Release of Drugs

Manzoor Hussain, Touseef Rehan, K. Goh · Polymers · 2022

Development of a New Aprepitant Liquisolid Formulation with the Aid of Artificial Neural Networks and Genetic Programming

P. Barmpalexis, A. Grypioti, G. Eleftheriadis · AAPS PharmSciTech · 2017

In Situ Hydrogels for Effective Treatment of Cancer: Strategies and Polymers Used

Anshula Mehra, Abhay Tharmatt, Navdeep Saini · Recent Advances in Drug Delivery and Formulation · 2022

Showing 4 of 9 known citations — external sources report more than can currently be individually listed.

Related research

Article metrics

Real usage data collected on this platform.

15

Page views

0

PDF downloads

1

Outbound clicks

9

Citations

Views over time

Views by country

Approximate, from request IP at view time — not citizenship or institution. Countries with fewer than 5 views are grouped as "Other".

Traffic sources

Referring site, by host.

Views and downloads exclude known bots/crawlers. Citations combines this platform's own DOI-resolved index with each external source's own reported total — see Cited by above for individually listed citing works. Last refreshed 0 seconds ago.