The aim of the present study was to improve the dissolution and flow properties of lurasidone hydrochloride (LH) by solid dispersion adsorbate (SDA) technique. Solid dispersions (SDs) of LH were prepared by fusion method using Poloxamer P188. The melt dispersion was adsorbed onto the porous carrier Florite (calcium silicate). A 3 factorial design was employed to quantify the effect of two independent variables, namely ratio of carrier (Poloxamer 188) and LH in SD and ratio of adsorbent (Florite) to SD. SDA granules of LH were studied for flow properties and characterized using differential scanning calorimetry, scanning electron microscopy, and X-ray diffraction. Tablets of optimized composition of SDA granules (equivalent to 20 mg of drug) and plain tablets were prepared by direct compression method. The dissolution studies were carried out in Mcllvaine buffer (pH 3.8) as per USFDA guidelines and characterized for parameters such as percent dissolution efficiency, t, and Q. Tablets prepared from SDA granules showed almost four-fold increase in cumulative percentage drug release as compared to tablets prepared from plain LH. The value of dissolution efficiency was enhanced from 49.60% for plain tablets to 94.15% for SDA tablets. SDA granules did not show any change in drug release and X-ray diffraction pattern after storage at 40 °C/75% of RH for 3 months, which confirms that Florite prevented conversion of drug from amorphous form to crystalline form improving physical stability of the amorphous state of LH.
Background
A sensitive, precise, and stability-indicating high-performance thin-layer chromatographic (HPTLC) method has been developed for the analysis of Remogliflozin etabonate in tablet formulation. HPTLC plates precoated with silica gel 60 F254 were used as the stationary phase; methanol: ethyl acetate: toluene: NH3 (2:4:4:0.1, v/v/v) was used as mobile phase, and densitometry was used for the quantitative estimation of the drug. The proposed method was validated with respect to linearity, accuracy, precision, and robustness and applied for the estimation of drug in tablet dosage form.
Results
The Rf value of Remogliflozin etabonate was observed to be 0.61. The densitometric estimation was performed in reflectance mode at 229 nm. The method was found to be linear in the range of 500–8000 ng/band for Remogliflozin etabonate. The possible degradation pathway was estimated by performing forced degradation studies. The degradant peaks were well resolved from the drug peak with acceptable resolution in their Rf value.
Conclusion
An accurate and precise high-performance thin-layer chromatographic method has been developed for the quantification of Remogliflozin etabonate in tablets. Forced degradation studies were performed, and drug was found to be highly susceptible to acid, base hydrolysis, and oxidative stress degradation and gets converted into active drug Remogliflozin. Both Remogliflozin etabonate and Remogliflozin bands were well resolved. The method was applied for the analysis of drug in tablet formulation, and it can be used for routine quality control analysis, as well as for the analysis of stability samples.
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