FORMULATION AND EVALUATION OF DOLUTEGRAVIR SODIUM SOLID DISPERSIONS AND FAST DISSOLVING TABLETS USING POLOXAMER-188 AND JACK FRUIT SEED STARCH AS EXCIPIENTS

  • SUNDEEP MUPPARAJU Department of Pharmaceutics, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chandramoulipuram, Guntur, Andhra Pradesh, India.
  • VIDYADHARA SURYADEVARA Department of Pharmaceutics, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chandramoulipuram, Guntur, Andhra Pradesh, India.
  • SAILAJA YALLAM Department of Pharmaceutics, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chandramoulipuram, Guntur, Andhra Pradesh, India.
  • SANDEEP DOPPALAPUDI Department of Pharmaceutics, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chandramoulipuram, Guntur, Andhra Pradesh, India.
  • SASIDHAR REDDYVALLAM LC Department of Pharmaceutics, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chandramoulipuram, Guntur, Andhra Pradesh, India.
  • RAMU ANNE Department of Pharmaceutics, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chandramoulipuram, Guntur, Andhra Pradesh, India.

Abstract

Objective: The current work mainly focuses on solubility enhancement of dolutegravir which is a biopharmaceutical classification system Class-II drug using jack fruit seed starch (JFS2) as excipient which improves the drug release.


Materials and Methods: Starches were extracted using aqueous and alkali methods (sodium hydroxide at 0.1%, 0.25%, and 0.5% concentrations) from jack fruit seed powder. These starches were evaluated for phytochemical and physicochemical parameters. Fast dissolving tablets were prepared using dolutegravir sodium solid dispersion, JFS2, and croscarmellose sodium (CCS) in various concentrations using wet granulation technique. Various pre- and post-compression parameters were evaluated along with in vitro drug release studies; characterization studies such as Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), scanning electron microscopy, X-ray diffraction (XRD), and stability studies.


Results: Phytochemical tests revealed the presence of only starch in all extracts. Starch prepared from 0.1% sodium hydroxide (JFS2) showed best physicochemical properties. From in vitro dissolution studies, it was observed that solid dispersion formulation DF3 containing dolutegravir sodium and poloxamer-188 in 1:1.5 ratios showed a better dissolution rate. From in vitro dissolution studies, tablet formulations DFT6 and DFT9 containing 12.5% w/w of JFS2 and 12.5% w/w of CCS showed enhanced dissolution rate compared with other formulations. FTIR and DSC studies revealed that there were no major interactions between drug and excipients. XRD studies revealed the nature of formulations. Accelerated stability studies showed that all tablets were stable.


Conclusion: The tablets prepared using jack fruit starch seed starch revealed the superdisintegrant property of starch.

Keywords: Jack fruit seed starch,, Dolutegravir,, Poloxamer-188,, Solid dispersions,, Fast dissolving tablets.

Author Biographies

SUNDEEP MUPPARAJU, Department of Pharmaceutics, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chandramoulipuram, Guntur, Andhra Pradesh, India.

Department of Pharmaceutics,

Research Scholar

VIDYADHARA SURYADEVARA, Department of Pharmaceutics, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chandramoulipuram, Guntur, Andhra Pradesh, India.

Departmnet of Pharmaceutics,

Professor and Principal

SAILAJA YALLAM, Department of Pharmaceutics, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chandramoulipuram, Guntur, Andhra Pradesh, India.

Department of Pharmaceutics,

Lecturer

SANDEEP DOPPALAPUDI, Department of Pharmaceutics, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chandramoulipuram, Guntur, Andhra Pradesh, India.

Department of Pharmacology,

Assistant Professor and PhD Scholar

SASIDHAR REDDYVALLAM LC, Department of Pharmaceutics, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chandramoulipuram, Guntur, Andhra Pradesh, India.

Department of Pharmaceutics,

Associate Professor

RAMU ANNE, Department of Pharmaceutics, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chandramoulipuram, Guntur, Andhra Pradesh, India.

Department of Pharmaceutics,

Associate Professor

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SUNDEEP MUPPARAJU, VIDYADHARA SURYADEVARA, SAILAJA YALLAM, SANDEEP DOPPALAPUDI, SASIDHAR REDDYVALLAM LC, and RAMU ANNE. “FORMULATION AND EVALUATION OF DOLUTEGRAVIR SODIUM SOLID DISPERSIONS AND FAST DISSOLVING TABLETS USING POLOXAMER-188 AND JACK FRUIT SEED STARCH AS EXCIPIENTS”. Asian Journal of Pharmaceutical and Clinical Research, Vol. 12, no. 6, Apr. 2019, pp. 181-90, https://innovareacademics.in/journals/index.php/ajpcr/article/view/33302.
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