Evaluation of Taste Masking of Ondansetron Using Insent Taste Sensing System (original) (raw)
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Ondansetron Hydrochloride is a potent antiemetic drug indicated for the treatment and/or prophylaxis of postoperative or chemotherapy-or radiotherapy-induced emesis. It is extremely bitter in taste. The purpose of this research was to mask the bitter taste of Ondansetron Hydrochloride with carbopol by neutralization method. The effect of variables like type of alkali, concentration of alkali, grades of carbopol and concentration of carbopol on bitterness level was studied. Results showed that neutralization of drug with equimolar sodium hydroxide and subsequent complexation with 0.6% carbopol 971G gave effective taste masking. The drug polymer complex was used to formulate orodispersible tablets by direct compression method using three different superdisintegrants like croscarmellose sodium, crospovidone and Kyron T-314. The prepared tablets were evaluated for the parameters like general appearance, thickness, hardness, weight variation, friability, wetting time, water absorption ra...
Taste Masking and Formulation of Ondansetron Hydrochloride Mouth Dissolving Tablets
International Journal of Drug Delivery Technology, 2015
This study was done to mask the bitter taste of ondansetron HCl using complexing agent, a polacrilex resin: Tulsion 335 and subsequently forming mouth dissolving tablet using superdisintegrants: Croscarmellose sodium and sodium starch glycollate. A preliminary screening was done. Batch process, a most preferential method for drug loading with ion exchange resins was selected. The process was optimized for drug: resin ratio to get maximum drug loading. A ratio of drug: resin at 1:3 was selected. Taste evaluation was carried out by selecting volunteers. Drug resin complex (DRC) was evaluated for drug release. The resultant DRC was formulated by direct compression into mouth dissolving tablet using microcrystalline cellulose PH 102, as diluent and croscarmalose sodium and sodium starch glycolate as superdisintegrants and aspartame was used as sweetening agent to enhance palatability. Thirteen formulations were developed by using superdisintegrants: croscarmellose sodium and sodium star...
INTERNATIONAL RESEARCH JOURNAL OF PHARMACY TASTE MASKING IN PHARMACEUTICAL: AN UPDATE
Taste is an important factor in the development of dosage form. Nevertheless it is that arena of product development that has been overlooked and undermined for its importance. The problem of bitter and obnoxious taste of is a challenge to the pharmacist in the present scenario. Taste is an important parameter governing compliance. Several oral pharmaceuticals and bulking agents have unpleasant, bitter-tasting components. In numerous cases, the bitter taste modality is an undesirable trait of the product or formulations and can considerably affect its acceptability by consumers. Bitter characteristics found in such systems have been eliminated or minimized by various known processes, but no universally applicable technology for bitterness inhibition has ever been recognized. The desire of improved palatability in these products has prompted the development of numerous formulations with improved performance and acceptability Taste masking technologies offer a great scope for invention and patents. Several approaches like adding flavors and sweeteners, use of coating polymers for inhibiting bitterness, microencapsulation, prodrug formation, formation of inclusion and molecular complexes, solid dispersion system, addition of effervescent agents and application of ion exchange resins have been tried by the formulators to mask the unpleasant taste of the bitter drugs. The present review attempts to give a brief account of different technologies of taste masking with respect to dosage form and novel methods of evaluation of taste masking effect.
AAPS PharmSciTech, 2007
The purpose of this research was to mask the intensely bitter taste of ondansetron HCl and to formulate a rapiddisintegrating tablet (RDT) of the taste-masked drug. Taste masking was done by complexing ondansetron HCl with aminoalkyl methacrylate copolymer (Eudragit EPO) in different ratios by the precipitation method. Drug-polymer complexes (DPCs) were tested for drug content, in vitro taste in simulated salivary fluid (SSF) of pH 6.2, and molecular property. Complex that did not release drug in SSF was considered taste-masked and selected for formulation RDTs. The complex with drug-polymer ratio of 8:2 did not show drug release in SSF; therefore, it was selected. The properties of tablets such as tensile strength, wetting time, water absorption ratio, in vitro disintegration time, and disintegration in the oral cavity were investigated to elucidate the wetting and disintegration characteristics of tablets. Polyplasdone XL-10 7% wt/wt gave the minimum disintegration time. Tablets of batch F4 containing spray-dried mannitol and microcrystalline cellulose in the ratio 1:1 and 7% wt/wt Polyplasdone XL-10 showed faster disintegration, within 12.5 seconds, than the marketed tablet (112 seconds). Good correlation between in vitro disintegration behavior and in the oral cavity was recognized. Taste evaluation of RDT in human volunteers revealed considerable taste masking with the degree of bitterness below threshold value (0.5) ultimately reaching to 0 within 15 minutes, whereas ondansetron HCl was rated intensely bitter with a score of 3 for 10 minutes. Tablets of batch F4 also revealed rapid drug release (t 90 , 60 seconds) in SGF compared with marketed formulation (t 90 , 240 seconds; P G .01). Thus, results conclusively demonstrated successful masking of taste and rapid disintegration of the formulated tablets in the oral cavity.
PHARMACEUTICAL TASTE MASKING TECHNOLOGIES OF BITTER DRUGS: A CONCISE REVIEW
Taste refers to a perception arising from the stimulation of taste buds present on the surface of the tongue. Humans can distinguish among five components of taste: sourness, saltiness, sweetness, bitterness, and umami (savory). Taste is an important parameter in case of drugs administering orally and is a critical factor to be considered while formulating orodispersible, melt in mouth, buccal tablet and other formulations which comes in contact with taste buds. Bitter and unpalatable taste is a major problem of certain drugs in formulations. Masking the bitter taste of drugs is a potential tool for the improvement of patient compliance which in turn decides the commercial success of the product. According to the year 2003 survey of pediatricians by the American Association of Pediatrics, unpleasant taste was the biggest barrier for completing treatment in pediatrics. The field of taste masking of active pharmaceutical ingredients (API) has been continuously evolving with varied technologies and new excipients. Two approaches are commonly utilized to overcome the bad taste of the drug. The first includes reduction of drug solubility in the saliva and second approach is to alter the ability of the drug to interact with taste receptor. Various methods are available to mask the undesirable taste of the drugs. Some of them are coating of drug particles, by formation of inclusion complexes, molecular complexes of drugs with other chemicals, solid dispersions, melting method, micro encapsulation, prodrugs, mass extrusion methods and ion exchange resins.
The purpose of this study was to evaluate the possibility of taste masking of Levocetirizine dihydrochloride (L-CTZ) by means of inclusion complexation and ion exchange resin. Initially an attempt was given to mask the bitter taste of the drug by inclusion complexation with β-Cyclodextrin using kneading method. But from gustatory evaluation, it was found that β-Cyclodextrin was not proven good for effective taste masking. So, another attempt was given to mask bitter taste of Levocetrizine diHCl by Kyron T-114 (weak cation exchange resin). It is a water-insoluble, high molecular weight, cross linked polymer of methacrylic acid. Kyron T-114 is inexpensive and this method is simple, rapid and cost-effective method for taste masking. Ion exchange resin complex was prepared by the batch technique and various parameters viz. resin activation, drug: resin ratio, pH, temperature, swelling time and stirring time were optimized to successfully formulate the tasteless Drug Resin Complex (DRC). Maximum drug loading was obtained when the resin was activated by acid treatment, with 1:3 drug: resin ratio, soaked in water for 90 min. and stirred with the drug for 240 minutes, pH maintained 5.5 and temperature maintained 30áµ’C. Complexation was confirmed by FT-IR and DSC study. The drug resin complex was evaluated for taste in-vitro and in-vivo evaluation. The volunteers rated the complexes as tasteless and agreeable. Drug release from DRC in salivary pH was insufficient to impart bitter taste. Complete drug release was observed at gastric 0.1 N HCl (pH 1.2). Formulation of drug resin complex was confirmed by FT-IR and DSC studies.
Acceptability of any dosage form are mainly depends over its taste i.e. mouth feel. Drug molecule interacts with taste receptor on the tongue to give bitter, sweet or salty taste sensation, when they dissolve in saliva. This sensation of the taste is the result of signal transduction from the receptor organs for taste, commonly known as taste buds. 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. To overcome this problem, many techniques have been developed to mask the bitter taste of drugs. These techniques are not only mask the bitter taste of drug but also enhance the bioavailability and performance of drug dosage form. It includes adding sugars, flavors, sweeteners, use of lipoproteins, numbing taste buds, granulation, use of adsorbates ,coating drug, microencapsulation, multiple emulsion, viscosity modifier, vesicles and liposomes, prodrug and salt formation, inclusion and molecular complexes, solid dispersion and Ion Exchange Resins (IERs) which have been tried by the formulators to mask the unpleasant taste of the bitter drugs. The present review article highlights different technologies of taste masking with respect to dosage form and novel methods of evaluation of taste masking effect.
2016
Taste drives appetite and protects us from poisons. Taste is a crucial factor that determines the palatability of pharmaceutical oral dosage form and patient compliance. It also gives a unique identity to a product and thereby provides a competitive advantage to a company, especially in the case of over-thecounter products. There are several taste masking methods available, which either involve modification of bitter active pharmaceutical ingredient itself or the formulation. Some of them are coating of drug particles, by formation of inclusion complexes, molecular complexes of drugs with other chemicals, solid dispersions, melting method, microencapsulation, prodrugs, mass extrusion methods and ion exchange resins. In past few years, Ion exchange resin and Formation of Inclusion Complexes with β-Cyclodextrin Derivative have been extensively used in the drug delivery technologies included; site specific drug delivery system, Modified release dosage form, Fast dissolving tablet, clin...
Most of the pharmaceuticals are administered by the popular route of drug delivery, the oral route. Taste is an important and critical parameter in administering formulations which comes in contact with the taste buds. Many drugs have bitter taste, thus this is one of the important formulation problem encountered. Bitter taste of drugs has posed a constant problem in the treatment of patients due to their inability or unwillingness to swallow such formulation especially in children and elderly. Thus masking of unpleasant taste characteristics of drug is an important factor in formulation of these agents. This lead to the development of taste masking technologies which improved the characteristics of the dosage form and good patient compliance is achieved. This review describes the trend in taste masking technologies by studying various methodologies for masking the obnoxious taste of drugs, some of which includes Taste-masking by Granulation, Ion Exchange Resins, Sweeteners and flavorants, Microencapsulation, Formulation of Inclusion Complexes, adsorption, Prodrug Approach, Gelation, Solid Dispersion System, Development of Liposome, Multiple Emulsions. The recent techniques which include the use of bitter taste blockers which specifically block the bitter taste but not the pleasant taste of any additive as well as taste masking nanotechnology using nanolipidic particles were also discussed. KEYWORDS: Taste masking, dosage form, palatability, and polymer.