Preparation and in vitro Evaluation of Inclusion Complexes of Nelfinavir with Chemically Modified ?-cyclodextrins

Authors

  • Shivanand Hiremath Department of Pharmaceutics, PRES?S College of Pharmacy, Sinnar, Nashik- 422101, Maharashtra
  • Ganesh Godge Department of Pharmaceutics, P.D.V.V.P.F?S College of Pharmacy, Vilad Ghat, Ahmednagar-414111, Maharashtra

DOI:

https://doi.org/10.3329/dujps.v11i2.14558

Keywords:

Nelfinavir, Hydroxypropyl- ? -cyclodextrin, inclusion complex, kneading method, freeze drying

Abstract

Nelfinavir is a poorly water-soluble antiretroviral drug with relatively low bioavailability. In the present study, the practically insoluble drug, nelfinavir (NFV) and its inclusion complexes with hydroxypropyl-?-cyclodextrin (HP-?-CD) were investigated to improve the aqueous solubility and the dissolution rate of the drug, thus enhancing its bioavailability. The phase solubility diagram with HP-?-CD was classified as AL-type at all temperatures investigated, indicating the formation of higher order complexes. The apparent complexation constants (K1:1) calculated from phase solubility diagram were 145.49, 188.45 and 255.54 M-1 at 25, 37 and 45 ± 0.5°C, respectively. Aqueous solubility and dissolution studies indicated that the dissolution rates were remarkably increased; this could be mainly attributed to the improved solubility and dissolution associated with inclusion complex between drug and HP- ? -CD. Absence of endothermic and characteristic diffraction peaks corresponding to NFV was observed for the inclusion complex in DSC and PXRD. FT-IR study indicated that the presence of intermolecular hydrogen bonds between NFV and HP-?-CD in inclusion complex, resulting in the formation of amorphous form.

DOI: http://dx.doi.org/10.3329/dujps.v11i2.14558

Dhaka Univ. J. Pharm. Sci. 11(2): 107-116, 2012 (December)

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Published

2013-04-14

How to Cite

Hiremath, S., & Godge, G. (2013). Preparation and in vitro Evaluation of Inclusion Complexes of Nelfinavir with Chemically Modified ?-cyclodextrins. Dhaka University Journal of Pharmaceutical Sciences, 11(2), 107–116. https://doi.org/10.3329/dujps.v11i2.14558

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