Practical Approaches for Taste Masking of Bitter Drug: A Review

Author(s):  
Gupta K. ◽  
Madaan S. ◽  
Dalal M. ◽  
Kumar A. ◽  
Mishra N. ◽  
...  

Taste is most important organoleptic aspects about the acceptance of oral drugs. Bitter and unpalatable taste is a major problem of certain drugs in formulations. In market, there are numbers of pharmaceutical preparations available in which actives are bitter in taste. The improved palatability in these products has prompted the development of numerous formulations, which improved performance and acceptability. The bitterness of preparation also leads to patient incompliance. So masking of bitterness becomes essential and done by masking the bitter taste of drugs by either decreasing its oral solubility on ingestion or decreasing the amount of drug particles exposed to taste buds thereby reducing the perception of bitter taste. Methods commonly used for taste masking involves various physical and chemical method that prevent the interaction of taste bud with drugs and are based on coatings, solid dispersion system and ion exchange resin, entrapment method and masking of taste buds etc. Taste masking of bitter drugs become necessity in case of oral administration and selection of technology depends upon the bitterness of drugs and their compatibility with taste masking agents that does not affect the bioavailability of drug

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).


1992 ◽  
Vol 3 (4) ◽  
pp. 371-393 ◽  
Author(s):  
Marion E. Frank ◽  
Thomas P. Hettinger ◽  
April E. Mott

The sense of taste is an oral chemical sense in mammals that is involved in the choice of foods. Initial transduction of taste stimuli occurs in taste buds, which are distributed in four discrete fields in the oral cavity. Medications can affect the taste buds and ion channels in taste-bud cell membranes involved in stimulus transduction. The sense of taste gradually declines with aging, with bitter taste most affected. Neural circuits that mediate taste in primates include cranial nerves VII, IX, and X, the solitary nucleus in the brain stem, the ventroposteromedial nucleus of the thalamus, and the insular-opercular cortex. The central taste pathways process taste information about sweet, salty, sour, and bitter stimuli serially and in parallel. Medications associated with "metallic" dysgeusia and taste losses affect the taste system via unknown mechanisms.


Author(s):  
Sunao Fujimoto ◽  
Raymond G. Murray ◽  
Assia Murray

Taste bud cells in circumvallate papillae of rabbit have been classified into three groups: dark cells; light cells; and type III cells. Unilateral section of the 9th nerve distal to the petrosal ganglion was performed in 18 animals, and changes of each cell type in the denervated buds were observed from 6 hours to 10 days after the operation.Degeneration of nerves is evident at 12 hours (Fig. 1) and by 2 days, nerves are completely lacking in the buds. Invasion by leucocytes into the buds is remarkable from 6 to 12 hours but then decreases. Their extrusion through the pore is seen. Shrinkage and disturbance in arrangement of cells in the buds can be seen at 2 days. Degenerated buds consisting of a few irregular cells and remnants of degenerated cells are present at 4 days, but buds apparently normal except for the loss of nerve elements are still present at 6 days.


2020 ◽  
pp. 25-32
Author(s):  
Mariya Anurova ◽  
Elena Bakhrushina ◽  
Anna Moiseyeva ◽  
Ivan Krasnyuk

Patient compliance of drug therapy is the key factor in achieving the pharmaceutical effect. Taste masking is particularly important in pediatrics and geriatrics because the unpleasant taste negatively affects drug uptake. Patient compliance can be improved through balanced organoleptic properties of medicines. It is particularly important to choose optimal correction method for medicines with high concentration of the active substance. Hopantenic acid has been chosen as a model drug due to its bitter taste. Taste masking technologies for creating a new dosage form with optimal organoleptic properties are proposed in the article. The objective is to achieve an experimentally justified choice of technological approach to masking bitter taste of a substance and to create a new dosage form on its basis. Materials and methods. Alternative technologies were considered to solve this problem: granulation, creation of complexes with ion-exchange resins, introduction of a gel composition and taste-masking using sweeteners. Organoleptic properties in dry compositions (pure substance of hopantenic acid, granulate and resinate based on it), and also after preparation of liquid dosage forms and incorporation them into gel, were evaluated by A. I. Tentsova method. Choice of sweetener and its concentration to achieve an optimally balanced taste took place at the final stage. Hopantenic acid was chosen as a model substance. Hopantenic acid is a nootropic drug stimulating cognitive functions, nervous system, enhancing intellectual functioning, decreasing nervous system activity, with anticonvulsant action. The main therapeutic indications are mental retardation, dementia, epilepsy. Results and discussion. The study has shown that optimal technology for masking unpleasant taste of hopantenic acid is its introduction into a gel composition, and a promising dosage form is an oral gel. Compri-Zucker G sweetener (Südzucker АG, Germany) in concentration of 5 % has been chosen to create pleasant taste due to its highest taste rating. Conclusion. It has been determined as a result of the study that oral gel with active drug concentration of 5 % and sweetener concentration of 5 % has optimal organoleptic properties. Thus, this combination of active and additional substances can be considered the most perspective for developing a new dosage form of a medicine.


2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Nur’ Adilah Abdul Nasir ◽  
Ameen Gabr Ahmed Alshaghdari ◽  
Mohd Usman Mohd Junaidi ◽  
Nur Awanis Hashim ◽  
Mohamad Fairus Rabuni ◽  
...  

Abstract Efficient purification technology is crucial to fully utilize hydrogen (H2) as the next generation fuel source. Polyimide (PI) membranes have been intensively applied for H2 purification but its current separation performance of neat PI membranes is insufficient to fulfill industrial demand. This study employs blending and crosslinking modification simultaneously to enhance the separation efficiency of a membrane. Polyethersulfone (PES) and Co-PI (P84) blend asymmetric membranes have been prepared via dry–wet phase inversion with three different ratios. Pure H2 and carbon dioxide (CO2) gas permeation are conducted on the polymer blends to find the best formulation for membrane composition for effective H2 purification. Next, the membrane with the best blending ratio is chemically modified using 1,3-diaminopropane (PDA) with variable reaction time. Physical and chemical characterization of all membranes was evaluated using field emission scanning electron microscope (FESEM), X-ray diffraction (XRD), and Fourier transform infrared (FTIR). Upon 15 min modification, the polymer membrane achieved an improvement on H2/CO2 selectivity by 88.9%. Moreover, similar membrane has demonstrated the best performance as it has surpassed Robeson’s upper bound curve for H2/CO2 gas pair performance. Therefore, this finding is significant towards the development of H2-selective membranes with improved performance.


Development ◽  
1997 ◽  
Vol 124 (7) ◽  
pp. 1333-1342 ◽  
Author(s):  
C.A. Nosrat ◽  
J. Blomlof ◽  
W.M. ElShamy ◽  
P. Ernfors ◽  
L. Olson

A combination of anatomical, histological and physiological data from wild-type and null-mutated mice have established crucial roles for BDNF and NT3 in gustatory and somatosensory innervation of the tongue, and indeed for proper development of the papillary surface of the tongue. BDNF is expressed in taste buds, NT3 in many surrounding epithelial structures. Absence of BDNF in mice leads to severely malformed taste bud-bearing papillae and severe reduction of taste buds, a loss of proper innervation of remaining taste buds and a loss of taste discrimination although not of the suckling reflex per se. In contrast, absence of NT3 leads to a massive loss of somatosensory innervation of lingual structures. These findings demonstrate distinct roles for BDNF and NT3 in the establishment of the complex innervation apparatus of the tongue with non-overlapping roles for the lingual gustatory and somatosensory systems. The distinction between different sensory modalities, being dependent on either BDNF or NT3 may also have clinical implications.


Author(s):  
Ichie Ojiro ◽  
Hiromi Nishio ◽  
Toyomi Yamazaki-Ito ◽  
Shogo Nakano ◽  
Sohei Ito ◽  
...  

Abstract Many functional food ingredients activate human bitter taste receptors (hTAS2Rs). In this study, A novel inhibitor, Trp-Trp, for hTAS2R14 was identified by searching for the agonist peptide's analogs. Trp-Trp also inhibited hTAS2R16, hTAS2R43, and hTAS2R46, which share the same agonists with hTAS2R14. The multi-functional characteristic of Trp-Trp is advantageous for use as bitterness-masking agents in functional foods.


Marine Drugs ◽  
2022 ◽  
Vol 20 (1) ◽  
pp. 45
Author(s):  
Magdalena Mititelu ◽  
Elena Moroșan ◽  
Anca Cecilia Nicoară ◽  
Ana Andreea Secăreanu ◽  
Adina Magdalena Musuc ◽  
...  

Nowadays, the use of marine by-products as precursor materials has gained great interest in the extraction and production of chemical compounds with suitable properties and possible pharmaceutical applications. The present paper presents the development of a new immediate release tablet containing calcium lactate obtained from Black Sea mussel shells. Compared with other calcium salts, calcium lactate has good solubility and bioavailability. In the pharmaceutical preparations, calcium lactate was extensively utilized as a calcium source for preventing and treating calcium deficiencies. The physical and chemical characteristics of synthesized calcium lactate were evaluated using Fourier Transform Infrared Spectroscopy, X-ray diffraction analysis and thermal analysis. Further, the various pharmacotechnical properties of the calcium lactate obtained from mussel shells were determined in comparison with an industrial used direct compressible Calcium lactate DC (PURACAL®). The obtained results suggest that mussel shell by-products are suitable for the development of chemical compounds with potential applications in the pharmaceutical domain.


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