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Mahapatra, Anjan Kumar
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Medicine & Pharmacology

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Solubility enhancement of etoricoxib using inclusion complexation with cyclodextrins: formulation of oro dispersible tablets by QbD approach Mahapatra, Anjan Kumar; Dora, Siddharth; Parida, Sanatan; Bal, Usharani; Jena, Bandana Rani; Lenka, Madhusmita
Journal of Applied Pharmaceutical Research Vol. 12 No. 4 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i4.603

Abstract

Background: The work was intended to enhance etoricoxib's solubility and dissolution rate and then develop oro-dispersible tablets for faster onset of action. Methodology: Inclusion complexes (ICs) of the drug were obtained with β-cyclodextrin (β-CD) and hydroxypropyl β-cyclodextrin (HP β-CD) at ratios of 1:0.125, 1:0.25, 1:0.5, 1:1, and 1:2 (w/w). The selected cyclodextrin at appropriate drug carrier proportion was used to develop oro-dispersible tablets (ODTs) by direct compression, adding crospovidone as a super disintegrant. Phase solubility studies of etoricoxib were carried out by using multiple concentrations of β-cyclodextrin and hydroxypropyl β-cyclodextrin, i.e., 1 %, 2 %, 3 % w/v in distilled water at 37±2°C. Spectroscopic (FT-IR) and thermal analysis (DSC) techniques were employed to identify the drug-carrier interactions. Result: It showed that etoricoxib solubility improves with increasing hydrophilic carrier concentration. The Gibbs free energy values (ΔG˚tr) are consistently negative, showing the solubility of etoricoxib. Significant drug carrier interaction in spectroscopic or thermal analysis was not found. Discussion: The ICs of drugs with β-CD and HP β-CD have successfully addressed the challenges of solubility enhancement and taste masking for etoricoxib. Conclusions: It is observed that the inclusion complexes formed by the kneading method using β-cyclodextrin (β-CD) at a 1:1 ratio and hydroxypropyl β-cyclodextrin (HP β-CD) at a 1:2 ratio can be used to improve dissolution. Hence β-CD (at a 1:1 ratio) is selected for the formulation of oro-dispersible tablets. ODTs offer more patient compliance and an alternative to available conventional tablets.
Rivaroxaban solid dispersions for dissolution enhancement and formulation of mouth disintegrating tablets Priyadarshan, Kalki Ranjan; Sahu, Asish; Mahapatra, Anjan Kumar; Chowdary, K. A; Nahak, Ajit; Patra, Ruchita Kumari
Journal of Applied Pharmaceutical Research Vol. 12 No. 4 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i4.647

Abstract

Background: Work is carried out to improve rivaroxaban's dissolution rate (DR) and develop mouth-disintegrating tablets for rapid onset of action. Objectives: The work objective was to improve the dissolution rate of rivaroxaban using PEG 6000 by preparing its solid dispersions (SDs) further to prepare mouth-disintegrating tablets (MDTs). Methods: Methods like physical mixing, melting, and solvent evaporation were used to prepare SDs at 1:0.5, 1:1, and 1:1.5 w/w ratios of rivaroxaban with PEG 6000 were prepared. Differential scanning calorimetry (DSC) and Infrared spectroscopy (IR) were used to characterize the SDs. The selected solid dispersion at an appropriate drug: carrier ratio was used to develop MDTs by direct compression, using super disintegrants. Results: The SDs show improved solubility and rate of dissolution. SDs developed using a melting or solvent evaporation technique showed a more than two-fold increase in dissolution rate. In the dissolution study, after 60 min, the pure drug dissolved 45 %, while the prepared SDs showed almost more than 90 % within the same period. No significant drug carrier interaction was observed in the IR and DSC studies. However, minor shifts in peak values were observed for the characterization of functional groups in the drug structure. Conclusions: Formulation of solid dispersions of the drug with PEG 6000 is a successful approach for the dissolution rate improvement of rivaroxaban. This work for dissolution rate improvement of rivaroxaban using PEG 6000 showed significant improvement in dissolution rate at a 1:1 w/w ratio prepared by solvent evaporation method, which was further selected for mouth disintegrating tablet formulation.
Co-Authors Bal, Usharani Chowdary, K. A Dora, Siddharth Jena, Bandana Rani Lenka, Madhusmita Nahak, Ajit Parida, Sanatan Patra, Ruchita Kumari Priyadarshan, Kalki Ranjan Sahu, Asish