Abstract

ENHANCEMENT OF DISSOLUTION RATE BY SOLID DISPERSION TECHNIQUE FOR ORMELOXIFENE

M. Ramanathan*, L. Subramanian, N. Venkatesan and Dr. P. Solairaj

ABSTRACT

Ormeloxifene is an SERM (selective estrogen receptor modulator) drug which is widely used for the treatment of dysfunctional uterine bleeding, contraceptive, mastalgia and fibroadenoma. One of the major problems with this drug is solubility, which results into low dissolution and poor bioavailability after oral administration. The rationale of this study was to enhance the dissolution rate of Ormeloxifene by solid dispersion technique. It was performed by Kneading technique by using carriers of β-cyclodextrin(BCD), poly vinyl pyrolidine(PVP) and polyethylene glycol 6000 (PEG 6000) in the ratios of 1:1,1:2 & 1:3. The prepared solid dispersion formulation was evaluated for drug content, FTIR, DSC, XRD & In vitro dissolution studies. IR studies indicate drug stability with the carriers; XRD studies depict the conversion of amorphous form and hence more dissolution; In vitro release studies showed enhancement of drug dissolution rate on comparison with pure drug. The Solid dispersion of kneading technique with BCD (BC-3) showed good drug release compared to other carriers used. It can be concluded that the dissolution rate and bioavailability of ormeloxifene can be increased by using BCD in solid dispersion formulation and this technique is useful to improve the drug dissolution rate and subsequently elevate bioavailability of poor water soluble drugs.

Keywords: Ormeloxifene, Bioavailability, Solid dispersion, Kneading technique, dissolution.