Famotidine

The objective of the present research was to develop and characterize an olive oil based oral microemulsion systems for famotidine, is a BCS class III drugs which are known to have high solubility but low permeability. An olive oil based microemulsion formulation with Tween-80 as surfactant, and PEG-400 as co-surfactant, was developed for oral delivery of famotidine. Pseudoternary phase diagram was constructed to determine the microemulsion existing zone. Optimized microemulsion was evaluated for its transparency, droplet size, polydispersity index, zeta potential, viscosity, conductivity, DSC studies, SANS studies. The results showed that maximum oil was incorporated in microemulsion system that was contained surfactant to co-surfactant ratio (Km) of 2:1. The optimized microemulsion formulation containing olive oil (7.14%), Tween-80 & PEG-400 [Smix=64.29% (2:1 ratio)], and distilled water (28.57%), had a droplet size (10 times diluted) and zeta potential (10 times diluted) of 170.1 nm and -6.58 mV respectively. Particle size characterization of the resulting microemulsion is essential in ensuring stability and efficient dosage. FTIR and DSC studies revealed the compatibility among the famotidine and microemulsion components. The experimental SANS data of optimized formulation fit well by spherical micelles interacting with hard sphere potential. These results demonstrate microemulsion formulation may be used as an effective and alternative drug delivery system for the antiulcer oral therapy with famotidine.

Two simple, rapid, precise and accurate spectrophotometric methods have been developed for simultaneous analysis of Ibuprofen (IBU) and Famotidine (FAMO) in their combined dosage form. Method A, absorbance correction method involves measurement of amplitudes at 220 nm (for IBU) and 288 nm (for FAMO) in zero derivative spectra. Method B, ratio derivative spectrophotometry, involves division of spectra of IBU by one selected standard spectrum of FAMO and then measuring amplitudes at 234.2 nm in ratio derivative spectra for estimation of IBU. Similarly, spectra of FAMO are divided by one selected standard spectrum of IBU and then amplitudes at 277.8 nm in ratio derivative spectra are measured for estimation of FAMO. Developed methods were validated according to ICH guidelines. The calibration graph follows Beer’s law in the range of 2 to 60 µg/ml for IBU and 3.8 to 4.6 µg/ml for FAMO with R2 value greater than 0.999. Accuracy of all methods was determined by recovery studies and showed % recovery between 98 to 102%. Intraday and Interday precision was checked for both the methods and mean %RSD was found to be less than 2 for these methods. The methods were successfully applied for estimation of IBU and FAMO in marketed formulation.

Conventional drug therapy requires periodic doses of therapeutic agents. These agents are formulated to produce maximum stability, activity and bioavailability.  Floating drug delivery systems (FDDS) have a bulk density less than gastric fluids and so remain buoyant in the stomach without affecting gastric emptying rate for a prolonged period of time. While the system is floating on the gastric contents drug is released slowly at the desired rate from the system. The present study mainly focuses on the development and evaluation effervescent based floating matrix tablet of famotidine. This oral drug delivery offers several advantages over the standard conventional oral dosage forms. Effervescent based floating matrix tablet of famotidine was prepared using sodium bicarbonate as effervescent agent and by incorporating hydrophobic agent stearic acid which retards the drug release and allow the dosage form to float on gastric fluid for several hrs. Then the tablet was evaluated for hardness, friability, drug content and in vitro drug release. On the basis of the preliminary trials, a 32 full factorial design was employed to study the effect of independent variables, HPMC K4M: Carbopol 934P ratio (X1) and concentration of effervescent agent (X2) on dependent variables like floating lag time, Q4 and Q8. The best batch (F3) exhibited optimum floating lag time (16 sec), drug content (98.94%), Q4 (54.36 %), Q8 (93.98%) and similarity factor (83.92). The controlled release of famotidine was observed and good fit to the zero order was demonstrated.