Assessment of the pharmaceutical quality of omeprazole capsule brands marketed in Egypt.

The pharmaceutical quality of 7 local omeprazole capsule brands in Egypt was assessed relative to the proprietary product (Losec). Drug content, content uniformity, drug release (using USP test for enteric coated articles and a modified release test) were determined. Products were subjected to a 3-month stability study. Of the 7 brands, 6 had satisfactory drug content and content uniformity. All brands passed the USP drug release test. The modified release test proved to be more discriminative. After 3 months storage, drug content of 3 brands remained > 90% and 2 of these brands maintained drug release above 75%. Changes in pellet appearance during storage were indicative of omeprazole chemical degradation.

Assessment of the pharmaceutical quality of omeprazole capsule brands marketed in Egypt

The pharmaceutical quality of 7 local omeprazole capsule brands in Egypt was assessed relative to the proprietary product [Losec[R]]. Drug content, content uniformity, drug release [using USP test for enteric coated articles and a modified release test] were determined. Products were subjected to a 3-month stability study. Of the 7 brands, 6 had satisfactory drug content and content uniformity. All brands passed the USP drug release test. The modified release test proved to be more discriminative. After 3 months storage, drug content of 3 brands remained > 90% and 2 of these brands maintained drug release above 75%. Changes in pellet appearance during storage were indicative of omeprazole chemical degradation

Enhancement of dissolution rate of hydrochlorothiazide via solid dispersion.

Solid dispersions of hydrochlorothiazide (1) in mannitol (2) and in dihydroxypropyltheophylline (3) were prepared by melting and solvent methods. For both systems, phase diagrams of simple eutectic type were obtained. A significant increase in dissolution rate was observed for 1/2 and 1/3 physical mixtures and solid dispersion as compared to pure drug. Solubility of 1 in 2 and in 3 solution at 27 degrees C and 37 degrees C was studied. At 37 degrees C the water solubility of the drug increased 3.7 times using 0.4 mol X 1(-1) 3. The solubilization of the drug by 3 in water was due to the formation 1 : 1 soluble complex. 1 tablets from physical mixtures and solid dispersion were prepared. Effect of ageing on the physical properties of the prepared 1 tablets was investigated.

The construction and uses of factorial designs in the preparation of solid dosage forms.

The present experiments were factorially designed to study the effect of particle size (X3), at different levels of both temperature (X1) and time (X2), on the hardness and mechanical strength of sintered tablets. A 2 X 2 X 3 design was constructed for salicylamide tablets with X1, X2 and X3 at 2,2 and 3 levels respectively. For phenobarbital tablets, a 3 X 3 X 3 factorial experiment was run. On the basis of analysis of variance, empirical regression equations have been developed. Within the limits of the factors, it was found that the quadratic effect of X 2/3, on the average, was the most significant. The significance of the linear effects was in the following order: X3 greater than X1 greater than X2 in salicylamide tablets and X1 greater than X3 greater than X2 in phenobarbital tablets. A change of X3 from the high to the low or intermediate levels caused an increase in the mechanical properties of tablets. The only linear interaction was that of X1X3 for the hardness data of phenobarbital tablets, but it was of least significance among the other effects. Other quadratic main effects of X 2/1, X 2/2 and quadratic interaction effects of X 2/3X1 and X 2/1X2 were also found to be significant. The optimum values of the factors studied, that would maximize any given mechanical property, were located.

The construction and uses of factorial designs in the preparation of solid dosage forms. Part 3. Effect of temperature and time on the mechanical properties of sintered tablets.

The present and forecoming series of experiments illustrate the application of factorial design to the study of the sintering phenomena of pharmaceutical tablets. This part was concerned with the effect of temperature (X1) and time (X2) on the mechanical properties of sintered tablets. A 2 X 2 design was developed for salicylamide tablets with the two factors at two levels, and a 3 X 3 design for phenobarbital tablets with the two factors at three levels. Analysis of variance was used to determine the significant effects. Empirical regression equations were obtained which indicated that the hardness of sintered tablets was markedly improved by using the high level of X1 at the low level of X2 in phenobarbital tablets, and the high levels of both X1 and X2 in salicylamide tablets. The tablets tensile strength was a linear function of X1 and X2, but the interaction effect X1X2 was insignificant. Significant quadratic effects of X2/2 and/or X2/1 were also detected for the mechanical properties of phenobarbital tablets.