Journal: JPR:BioMedRx:An International Journal

Article Id: JPRS-Ph-0000284
Title: Factorial Studies on Enhancement of Solubility and Dissolution Rate and Formulation Development of Efavirenz Tablets Employing β Cyclodextrin and Soluplus
Category: Pharmaceutics
Section: Research Article
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    Efavirenz, a widely prescribed anti retroviral drug belongs to class II under BCS and exhibit low and variable oral bioavailability due to its poor aqueous solubility. Its oral absorption is dissolution rate limited and it requires enhancement in the solubility and dissolution rate for increasing its oral bioavailability. The objective of the study is to enhance the solubility and dissolution rate of efavirenz by cyclodextrin complexation along with Soluplus and to evaluate the individual main effects and combined (or interaction) effects of β cyclodextrin (βCD) and surfactant (Soluplus) on the solubility and dissolution rate of efavirenz in a series of 22 factorial experiments. The solubility of efavirenz in four selected fluids containing βCD and Soluplus as per 22 factorial study was determined. Solid inclusion complexes of efavirenz-βCD were prepared with and without Soluplus by kneading method as per 22-factorial design and were evaluated. The feasibility of formulating the drug- βCD- Soluplus complexes into compressed tablets was also evaluated in a 22 factorial study . The individual and combined effects of βCD and Soluplus in enhancing the solubility, dissolution rate and dissolution efficiency of efavirenz were highly significant (P < 0.01).βCD alone gave a 2.14 fold increase in the solubility of efavirenz. Combination of âCD with Soluplus resulted in a much higher enhancement in the solubility of efavirenz, 86.96 fold than with âCD alone. Soluplus alone gave a much higher enhancement (289.49 folds) in the solubility of efavirenz. Combination of βCD with Soluplus also gave significantly higher dissolution rates (K1) and dissolution efficiency (DE20) when compared to βCD alone. βCD alone gave 2.00 fold increase and in combination with Soluplus, it gave 7.34 fold increase in the dissolution rate of efavirenz. Efavirenz – βCD, Efavirenz – Soluplus and efavirenz –βCD – Soluplus inclusion complexes could be formulated into compressed tablets by direct compression method. Efavirenz dissolution was rapid and higher from the tablets formulated employing drug- βCD- Soluplus inclusion complexes when compared to the tablets containing efavirenz alone. The tablets formulated employing drug- βCD- Soluplus inclusion complexes fulfilled the official (I.P 2010) dissolution rate test specification of NLT 70 % in 30 min prescribed for efavirenz tablets. The individual as well as combined effects of the two factors involved i.e., βCD (factor A) and Soluplus (factor B) were highly significant (P< 0.01) in enhancing the dissolution rate (K1) and dissolution efficiency (DE 30) of efavirenz. Soluplus alone also gave a higher enhancement in the dissolution rate and dissolution efficiency of efavirenz and efavirenz tablets. Hence a combination of βCD with Soluplus and / or Soluplus alone is recommended to enhance the solubility, dissolution rate and dissolution efficiency of efavirenz, a BCS class II drug and its tablet formulations.

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    Author(s) Name:

    K. Ravi Shankar1 and K. P. R. Chowdary* 2

    Affiliation(s) Name:

    1A.KR.G College of Pharmacy, Nallajerla - 534112, Andhra Pradesh, India
    *2Former Principal, A. U. College of Pharmaceutical Sciences, Andhra University, Visakhapatnam - 530003, Andhra Pradesh, India

    *Corresponding author.
    Prof. K.P.R. Chowdary
    Former Principal,
    A. U. College of Pharmaceutical Sciences,
    Andhra University,
    Visakhapatnam – 530003 ,
    Andhra Pradesh, India


    Received on:17-01-2012; Revised on: 19-02-2013; Accepted on:27-02-2013

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    Author:

    K. Ravi Shankar1 and K. P. R. Chowdary* 2

    Title:Factorial Studies on Enhancement of Solubility and Dissolution Rate and Formulation Development of Efavirenz Tablets Employing β Cyclodextrin and Soluplus
    Journal:JPR:BioMedRx:An International Journal
    Vol(issue):1 (March)
    Year:2013
    Page No: (299-303)
  • Experimental Methods Keywords

    Methodology:Solubility, Dissolution Rate, Efavirenz Tablets, Formulation development.
    Research Materials:Efavirenz

Keywords

Efavirenz β Cyclodextrin Soluplus Solubility Dissolution Rate Efavirenz Tablets Formulation development.

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