Formulation and evaluation of famotidine sublingual tablets

Formulation of famotidine, rapidly disintegrated sublingual tablets, by direct compression was carried out. Fifteen tablets formulae were made in order to obtain suitable non-friable formulae, with disintegration time less than one minute and average crushing strength of 2-4 kg/cm2. The excipients used in the different formulae are Avicel pH 101, sorbitol, mannitol, lactose anhydrous, Ac-Di-Sol, magnesium strearate and saccharin sodium. The formulae prepared were tested for the effect of certain excipients on the hardness, friability and disintegration time. Tablets of 20 mg famotidine from the formulated and commercial oral dosage forms were administered to five healthy volunteers participated in the studs using a balanced cross-over design. Comparison of the mean urinary excretion, rats obtained after administration of both dosage forms indicated that in both cases, the rime taken to reach peak occurred at a mid point of 1.5 hours. Comparison of the cumulative amounts excreted in the urine after administration of famotidine in the two different dosage forms, resealed that about 5.49 +/- 1.06 mg of the administered dose [20 mg] was recovered unchanged in the urine during 12 hours following sublingual tablets administration. This value was found to be higher than that excreted after administration of Pepcid [R] oral tablets [4.6 +/- 0.65 mg] during the same period of time. Statistical analysis of the difference at P = 0.05, revealed nun-significant difference in the urinary excretion rate obtained of the two different dosage forms. On the other hand, a significant difference was found to exist in the total cumulative amount of famotidine excreted in the urine at 2 and 6 hours from both dosage forms. The results also indicated that there was no significant difference in AUC [0-12] between the two dosage forms

Effect of B-cyclodextrins of the dissolution behavior and anti-inflammatory activity of quercetin

Quercetin [QUR] is a natural non-toxic flavonol with anti-inflammatory properties. However, formulation problems result from its insolubility in water with low bioavailability. Inclusion complexation of quercetin with beta-cyclodextrin [beta CD] was tried for resolving these problems. An equilibrium phase solubility diagram was obtained for the QUR- beta CD system in water. The solubility of QUR increased on addition of beta CD, displaying an A type phase diagram, which indicates that the soluble complexes contained more than one molecule of ligand at higher beta CD concentration. Stability constant [K[c]] was calculated from the slope of initial straight portion of the curve and found to be 236 M[-1]. The stability constant was also obtained from UV spectra to be 237M[-1] which showed a good agreement with the value of K[c] obtained by the solubility method. The formation of the complex in the solid state was confirmed by infrared spectroscopy [IR]. The amounts of QUR dissolved from inclusion complexes 1:1 [CI] and 1:2 [CII] in water are more 15 and 25 times, respectively, than pure drug solubility. The anti-inflammatory activity of complexed QUR with beta CD was estimated to be increased