ABSTRACT
The aim of present work was to enhancing the solubility and dissolution rate of the aquaphobic drug Lafutidine by liquisolid technique. Lafutidine is a H2-receptor antagonist BCS class II drug. Lafutidine compatibility with excipients was evaluated by FT-IR and DSC spectrum. Preliminary trial taken to check the effect of carrier to coating material ratio (R) and non-volatile solvent (PEG- 600) on pre compression and post compression characteristic. Flowable liquid retention potential (Ø -value) and Liquid load factors (Lf) were calculated for required amount of excipients necessary to preparing Lafutidine liquisolid tablet. A 32 full factorial design was employed to check the effect of carrier to coating material ratio R (X1) and PEG- 600 (X2) on hardness (Y1), angle of repose (Y2), % of Cumulative drug release at 5 min Q5 (Y3), and disintegration time (Y4). Multiple linear regression analysis, ANOVA and graphical representation of the influence of factor by 3D plots were performing by using Design expert 7.0. In this study, the following constraints were arbitrarily used for the selection of an optimized batch: Hardness: 3 to 5.5, Angle of repose: 25 to 30, % of Cumulative Drug Release at 5 min (Q5) > 27.09 % and Disintegration time <1.3 min. The desirability value of various dependent variables calculated for determining the optimized batch of tablet and it was also found to be nearer to one. Performance of optimized batch had no shown any significant change at the end of stability study.
ABSTRACT
The present research aimed to improve the dissolution rate and bioavailability of curcumin using the potential of liquisolid technology. Twelve drug-loaded liquisolid systems (LS-1 to LS-12) were prepared using different vehicles (PEG 200, PEG 400 and Tween 80) and curcumin concentrations in vehicle (40%, 50%, 60% and 70%,/). The carrier [microcrystalline cellulose (MCC) PH102] to coat (Aerosil) ratio was 20 in all formulations. The systems were screened for pre-compression properties before being compressed to liquisolid tablets (LT-1 to LT-12). Post compression tests anddissolution of LTs were conducted and the results compared with those obtained for a directly compressed tablet (DCT) made of curcumin, MCC PH102 and Aerosil. LTs exhibited higher cumulative drug release (CDR) than the DCT and the optimum formulation, LT-9 (made using Tween 80), was studied by powder XRD, DSC, SEM and FTIR.permeation of curcumin from LT-9 through goat gastrointestinal mucosa was significantly (<0.05) enhanced and its oral bioavailability was increased 18.6-fold in New Zealand rabbits.cytotoxicity (IC) of LT-9 towards NCL 87 cancer cells was 40.2 µmol/L substantiating its anticancer efficacy. Accelerated stability studies revealed insignificant effects of temperature and humidity on LT-9. In summary, solubility enhancement of curcumin in LTs produced significant improvements in its permeation and bioavailability.