In vitro and in vivo correlation of disintegration and bitter taste masking using orally disintegrating tablet containing ion exchange resin-drug complex

2013 ◽  
Vol 455 (1-2) ◽  
pp. 31-39 ◽  
Author(s):  
Jong-Il Kim ◽  
Sang-Min Cho ◽  
Jing-Hao Cui ◽  
Qing-Ri Cao ◽  
Euichaul Oh ◽  
...  

The bitter taste is one of the most important drug formulation problems. The unpleasant taste leads to noncompliance, which consequently decreases the therapeutic efficacy of the drug. Therefore, masking of bitter taste is very important in drug formulation. In this study an antihypertensive drug, valsartan, which is a weak acid with bitter taste, was used as a model drug to mask its taste with dowex2 (weak base anion exchange resin). The taste masking of a drug using ion exchange resin basically depends on the complex formation between the drug and a specific type of resin. Complex formation under various preparation conditions including; the ratio of drug to resin, mixing time, the pH of the processing medium and the concentration of valsartan was investigated in this study. Optimum conditions for complex formation and maximum drug load were obtained at a drug-resin ratio 1:8, mixing time 4 hours, pH 6.8, temperature 50º C and drug concentration 0.02% w/v. The drug resin ate complex was evaluated for the drug content, taste, drug release and molecular properties. The resinate formation was confirmed using different analytical techniques like thermal analysis using differential scanning calorimetry (DSC), spectroscopic method like Fourier transform infrared spectroscopy (FTIR) and by X-ray powder diffraction analysis (XRPD).


10.32947/358 ◽  
2018 ◽  
Vol 18 (1) ◽  
pp. 11-25

The bitter taste is one of the most important drug formulation problems. The unpleasant taste leads to noncompliance, which consequently decreases the therapeutic efficacy of the drug. Therefore, masking of bitter taste is very important in drug formulation. In this study an antihypertensive drug, valsartan, which is a weak acid with bitter taste, was used as a model drug to mask its taste with dowex2 (weak base anion exchange resin). The taste masking of a drug using ion exchange resin basically depends on the complex formation between the drug and a specific type of resin. Complex formation under various preparation conditions including; the ratio of drug to resin, mixing time, the pH of the processing medium and the concentration of valsartan was investigated in this study. Optimum conditions for complex formation and maximum drug load were obtained at a drug-resin ratio 1:8, mixing time 4 hours, pH 6.8, temperature 50º C and drug concentration 0.02% w/v. The drug resin ate complex was evaluated for the drug content, taste, drug release and molecular properties. The resinate formation was confirmed using different analytical techniques like thermal analysis using differential scanning calorimetry (DSC), spectroscopic method like Fourier transform infrared spectroscopy (FTIR) and by X-ray powder diffraction analysis (XRPD).


2018 ◽  
Vol 547 (1-2) ◽  
pp. 385-394 ◽  
Author(s):  
David Cheng Thiam Tan ◽  
Jeremy Jianming Ong ◽  
Rajeev Gokhale ◽  
Paul Wan Sia Heng

2009 ◽  
Vol 15 (5) ◽  
pp. 511-517 ◽  
Author(s):  
Sradhanjali Patra ◽  
Rakesh Samantaray ◽  
Saswat Pattnaik ◽  
B. B. Barik

Blood ◽  
1964 ◽  
Vol 23 (4) ◽  
pp. 417-426 ◽  
Author(s):  
A. WILLIAM SHAFER

Abstract The phosphorylated carbohydrate intermediates of erythrocytes from normal adults and from five patients with hereditary spherocytosis (HS) were labeled in vitro with P32 orthophosphate and then separated on columns of ion exchange resin. No qualitative or quantitative differences were found between normal and HS erythrocytes. The relative specific activity of each phosphate of 2, 3 DPG was the same; whereas the phosphate attached to ribose in ADP and ATP was not labeled. The nucleotides were labeled at a much faster rate than DPG. When the erythrocytes were washed 6 or more times, the specific activity of Pi approached that of DPG. No definite difference was found in the rate of labeling of the intermediates from normal and HS erythrocytes.


1981 ◽  
Vol 4 (4) ◽  
pp. 192-198 ◽  
Author(s):  
L. Mor. I. Thaler ◽  
J.M. Brandes ◽  
S. Sideman

Removal of bilirubin by hemoperfusion (HP) on a macroreticular ion-exchange resin is suggested as a novel clinical procedure for the treatment of jaundiced newborn babies. The efficiency and biocompatibility of the proposed macroreticular (MR) ion exchange column was tested in vivo with jaundiced dogs. An animal model with a choledocho-suprarenal vein shunting allowed to test the column capacity for the adsorption of conjugated and unconjugated bilirubin. A second animal model, based on infusing unconjugated bilirubin directly into the blood stream, enabled to test the column operation at desired unconjugated bilirubin concentrations. The results of the in vivo hemoperfusion tests are very encouraging and compare favorably with bilirubin removal from babies by exchange transfusion (ET). Operating a column containing 10 ml resin per kg body weight for 3 hours removed over 1.7 times the initial unconjugated bilirubin content. Furthermore, the animals seemed to be unaffected by the HP procedure; the changes due to hemoperfusion on blood chemistry, hematology and some hormone levels were practically insignificant.


Polymers ◽  
2021 ◽  
Vol 13 (24) ◽  
pp. 4394
Author(s):  
Conghui Li ◽  
Xiaolu Han ◽  
Xiaoxuan Hong ◽  
Xianfu Li ◽  
Hui Zhang ◽  
...  

Since the advent of ion exchange resin, it has been widely used in many fields, including drug delivery systems. The drug binds to the resin through an exchange reaction to form a drug–resin complex, which can gradually release drugs through the exchange of physiological ions in the gastrointestinal tract, to realize functions such as taste masking and regulating release. In this study, the complexes of methylphenidate hydrochloride and Amberlite IRP69 were prepared and evaluated to explore the mechanism of complexation, influencing factors and release mechanism at a molecular level. Firstly, with the properties of the selected complexes, molecular dynamics simulation was innovatively used to find that the intermolecular interaction between drug molecules and ion exchange resin molecules is mainly caused by the stacking effect of π and salt bridges. Secondly, with the drug loading status as an indicator, the factors affecting the compounding process of the drug and resin were explored. Finally, the release mechanism of the drug–resin complex was studied by mathematical model fitting. In summary, a variety of methods were used to study the mechanism of complexation and release between drug and resin, providing a theoretical basis for promoting the marketing of ion−exchange resin−mediated oral preparations.


2020 ◽  
Vol 56 (6) ◽  
pp. 722-726
Author(s):  
Vera A. Vil’ ◽  
Ivan A. Yaremenko ◽  
Dmitri I. Fomenkov ◽  
Dmitri O. Levitsky ◽  
Fabrice Fleury ◽  
...  

Author(s):  
NISHANT OZA ◽  
SWATI SAGAR

Objective: The aim of present work was to develop of pediatric cefuroxime axetil 125 mg dispersible tablets by using ion exchange resin as a taste masking agent and quality target product profile was defined based on the properties of the cefuroxime axetil. Methods: Initially, cefuroxime axetil and various resin complexes (DRC) were prepared with different conditions and evaluated for taste masking and drug loading. Optimized DRC was used to formulate the dispersible tablet. A 32 full factorial design was employed to study the effect of mannitol (X1) and microcrystalline cellulose PH-101 (X2) on drug release at 10 min and time taken to 80% drug release. In the present study, the following constraints were arbitrarily used for the selection of an optimized batch: Q10>65% and T80%<30 min. Multiple linear regression analysis, ANOVA and graphical representation of the influence factor by 3D plots were performed by using Sigmaplot 11.0. Checkpoint batch was prepared to validate the evolved model. Results: Among the various drug resins complex DRC-9 was found with less bitter taste which was containing kyron T-114 and among the all factorial batch F7 showed highest drug release at 10 min (Q10) and lowest time taken to 80% drug release (T80) hence batch F7 was selected as an optimized batch and it’s found to be stable in the stability evaluation. Conclusion: The results of full factorial design indicate mannitol and MCC PH-101 have a significant effect on drug release.


Sign in / Sign up

Export Citation Format

Share Document