TASTE MASKING OF PRIFINIUM BROMIDE IN ORODISPERSIBLE TABLETS

Objective: In previous work, Prifinium Bromide had been successfully formulated as oro-dispersible tablets. However, Prifinium Bromide, a quaternary ammonium compound, has a bitter taste; therefore, taste masking was necessary to produce acceptable oro-dispersible tablets and enhance patients' compliance. Methods: In this work, several attempts had been made to mask the bitterness of this drug. β-cyclodextrin inclusion complexes, solid dispersions of the drug in ethyl cellulose and methyl cellulose as well as loading the drug on Eudragit E100 have all been used. The selected granules were used to prepare oro-dispersible tablets and were evaluated. Results: Drug-Eudragit granules E3 prepared by mass extrusion method gave less than 10% of drug in simulated saliva fluid and almost complete release in simulated gastric fluid after 2 minutes. Therefore, it was used to prepare oro-dispersible tablets formulas. In vitro disintegration time of formula T2 was 45.5 ± 7.7 seconds showed a complete drug release of Prifinium Bromide in phosphate buffer (pH 6.8) and (94%) in SGF (pH 2.1). Conclusion: Loading of Prifinium Bromide on Eudragit E100 using mass extrusion method was the best method to overcome the disagreeable taste of the drug. They gave the least amount of drug released in simulated saliva fluid and passed the quality control tests of tablets after formulation as oro-dispersible tablets. They also gave good taste when tested in vivo

LIQUORICE BEVERAGE EFFECT ON THE PHARMACOKINETIC PARAMETERS OF ATORVASTATIN, SIMVASTATIN, AND LOVASTATIN BY LIQUID CHROMATOGRAPHY-MASS SPECTROSCOPY/MASS SPECTROSCOPY

ABSTRACTObjective: The objective of this study is to examine the effects of pre-consumption of freshly prepared liquorice beverage (4 ml/kg) on thepharmacokinetic (PK) parameters of (80 mg/kg) oral dose of atorvastatin, simvastatin, and lovastatin in healthy rats plasma.Methods: A simple, rapid, and applicable analytical method was developed for the determination of each statin in rats' plasma. This method usesliquid chromatography-mass spectroscopy/mass spectroscopy. The mobile phase composed of methanol and formic acid in water and glimepiride asan internal standard. 108 rats were used in this study. Liquorice juice was given, and then each of the statins was given to test groups and liquoriceonly to the control groups, and then plasma samples were withdrawn on specific time schedule then PK analysis was performed.Results: The analytical method showed acceptable linearity, recovery, precision, and accuracy. Administration of liquorice resulted in a significantincrease in maximum concentration in plasma (C) of the three statins, also the area under plasma level-time curves (area under curve) was increasedsignificantly. Moreover, the bioavailability of the drugs. On the other hand, the elimination of the three drugs showed no great changes, which suggestsan interaction between liquorice and the transporting system of statins on the gut and biliary wall.maxConclusion: Consumption of liquorice results in increase bioavailability of atorvastatin, simvastatin, and lovastatin.Keywords: Liquorice, Atorvastatin, Liquid chromatography-mass spectroscopy/mass spectroscopy, Simvastatin, Lovastatin, Pharmacokineticparameters

Enhancement of apixaban's solubility and dissolution rate by inclusion complex (β-cyclodextrin and hydroxypropyl β-cyclo¬dextrin) and computational calculation of their inclusion complexes

Background and Purpose: Apixaban (AP) is a factor X inhibitor, an orally active drug that inhibits blood coagulation for better prevention of venous thromboembolism. It has poor solubility, dissolution rate and low bioavailability. The aim of this study was to improve the aqueous solubility and dissolution rate of oral AP as a step to enhance its bioavailability by preparing it as an inclusion complex with beta- and hydroxy propyl beta-cyclodextrin. Experimental Approach: A simple, rapid method of analysis of AP was developed using ultraviolet spectrophotometry (UV) and partially validated in terms of linearity, precision and accuracy, recovery, and robustness. AP was prepared as a complex with beta cyclodextrin (βCD) and hydroxy propyl beta cyclodextrin (HPβCD) in weight ratios 1:1, 1:2, and 1:3 by kneading, solvent evaporation and spray drying methods and characterized by Fourier transfer infra-red (FTIR), differential scanning calorimetry (DSC), and percent drug content in each of the prepared complex. Using the computer simulation, the interactions of AP with βCD and HPβCD were investigated. Key Results: The phase solubility study showed that the solubility of AP was greatly enhanced from 54×10-3 mmol /L to 66 mmol/L using HPβCD with acceptable stability constant. Computer docking supports the formation of a stable 1:1 complex between AP and CD’s. The dissolution test results showed that the complex gave a significantly higher percentage of drug release (95%) over one hour compared to the free AP (60%) (p<0.05). Conclusion: AP- HPβCD complex in the ratio of 1:2 (w/w) can significantly improve the solubility and in vitro dissolution rate of AP

FORMULATION OF LEVOFLOXACIN AS ORODISPERSIBLE TABLETS USING A READY-MADE BLEND OF EXCIPIENTS COMPARED WITH CLASSIC FORMULATION STRATEGIES

Objective: Orodispersible tablets are designed to undergo rapid dispersal when they are placed in the mouth prior to being swallowed. The aim of this study was to compare the performance of a ready-made excipients blend designed for orodispersible tablets with several other conventional methods for the manufacture of tablets using levofloxacin as the active pharmaceutical ingredient.Methods: Several different formulas were prepared to compare the powder characteristics, and the resulting powders were compressed into tablets using the direct compression method. The result compressed tablets was then evaluated in terms of their physical characteristics and drug release properties.Results: The results of these experiments showed that the use of ready-made blend provided several advantages over the conventional methods in terms of physical properties of the powders and tablets, as well as their drug release and dissolution properties.Conclusion: The use of a ready-made powder blend in formulation of ODT of model drug levofloxacin had an advantage over the classic methods of formulation.Â