10.1 SUMMARY
The aim of the present investigation was to formulate Raloxifene Hydrochloride Liquisolid compacts, with coadministration of a bioenhancer, for oral bioavailability enhancement. The reason for poor bioavailability (2%) of Raloxifene Hydrochloride is low solubility (100μg/mL) and high hepatic first pass metabolism. According to BCS, Raloxifene Hydrochloride is considered as Class II drug, lipophilic and highly permeable compound. Therefore, formulating Liquisolid Compacts bearing bioenhancer would enhance its bioavailability by increasing solubility and avoiding first pass metabolism.
10.1.1 Analytical Method Development
Calibration Plots for Raloxifene Hydrochloride, Piperine and Naringin, were developed in Methanol:Water (8:2) …show more content…
Calibration Plots for Raloxifene Hydrochloride were developed in Blood Plasma for in-vivo studies and Rat Liver Homogenate for ex-vivo studies, using HPLC. R2 values of both the calibration plots were nearer to 1, which indicated that the methods developed were following Beer-Lambert’s law and could be used for further estimation.
Analytical Interference Study of Raloxifene Hydrochloride with tablet excipients was done for assay and dissolution purposes, and no interference was observed at λmax of Raloxifene Hydrochloride.
10.1.2 Preformulation …show more content…
Evaluation was done for formulation as per Indian Pharmacopoeia 2010. The results are given in Table 10.3.
Table 10.3 Evaluation Results of Formulation
Evaluation Tests Liquisolid Compacts bearing Naringin
Hardness 3.167±0.288kg/cm2
Friability 1.34%
Tablet Thickness and Diameter Thickness 4.52±0.085mm Diameter 6.26±0.073mm
Weight Variation All the tablets have deviation less than 5%
Tablet Disintegration Time 5.6±1.15 min
Assay Raloxifene Hydrochloride 95.61% Naringin 92.4%
In-Vitro Release study was performed in Phosphate Buffer Saline pH 7.4 with 0.1% Tween 80 for comparison with marketed formulation and to check for release kinetics, in which best goodness-of-fit test (R2) was taken as criteria for selecting the most appropriate model. Release of optimised batch fitted to Korsemeyer-Peppas model, with R2 value
The aim of the present investigation was to formulate Raloxifene Hydrochloride Liquisolid compacts, with coadministration of a bioenhancer, for oral bioavailability enhancement. The reason for poor bioavailability (2%) of Raloxifene Hydrochloride is low solubility (100μg/mL) and high hepatic first pass metabolism. According to BCS, Raloxifene Hydrochloride is considered as Class II drug, lipophilic and highly permeable compound. Therefore, formulating Liquisolid Compacts bearing bioenhancer would enhance its bioavailability by increasing solubility and avoiding first pass metabolism.
10.1.1 Analytical Method Development
Calibration Plots for Raloxifene Hydrochloride, Piperine and Naringin, were developed in Methanol:Water (8:2) …show more content…
Calibration Plots for Raloxifene Hydrochloride were developed in Blood Plasma for in-vivo studies and Rat Liver Homogenate for ex-vivo studies, using HPLC. R2 values of both the calibration plots were nearer to 1, which indicated that the methods developed were following Beer-Lambert’s law and could be used for further estimation.
Analytical Interference Study of Raloxifene Hydrochloride with tablet excipients was done for assay and dissolution purposes, and no interference was observed at λmax of Raloxifene Hydrochloride.
10.1.2 Preformulation …show more content…
Evaluation was done for formulation as per Indian Pharmacopoeia 2010. The results are given in Table 10.3.
Table 10.3 Evaluation Results of Formulation
Evaluation Tests Liquisolid Compacts bearing Naringin
Hardness 3.167±0.288kg/cm2
Friability 1.34%
Tablet Thickness and Diameter Thickness 4.52±0.085mm Diameter 6.26±0.073mm
Weight Variation All the tablets have deviation less than 5%
Tablet Disintegration Time 5.6±1.15 min
Assay Raloxifene Hydrochloride 95.61% Naringin 92.4%
In-Vitro Release study was performed in Phosphate Buffer Saline pH 7.4 with 0.1% Tween 80 for comparison with marketed formulation and to check for release kinetics, in which best goodness-of-fit test (R2) was taken as criteria for selecting the most appropriate model. Release of optimised batch fitted to Korsemeyer-Peppas model, with R2 value