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Lu, Mou-Ying Fu; Borodkin, Saul; Woodward, Linda; Li, Ping; Diesner, Curt; Hernandez, Lisa E.; Vadnere, Madhu

doi:10.1023/a:1015889631314

Cited by 76 publications

(11 citation statements)

References 3 publications

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“…[7][8][9] The techniques most often employed for achieving effective taste-masking have been described in literature when the addition of flavors or sweeteners is limited and may not be efficient enough to mask the unpleasant taste of some drugs. [10][11][12] These approaches include the use of ion exchange resins, 13,14) the use of inclusion complexes with cyclodextrins, 15,16) and drug-polymer complexes. 17,18) In recent years, the entrapment of bitter drug substance into polymerbased microspheres or microcapsules has become an increasingly attractive strategy for taste masking by creating a physical barrier around the bitter drug to keep them from coming in contact with the patients' taste buds.…”

mentioning

confidence: 99%

Preparation and Evaluation of Taste-Masked Donepezil Hydrochloride Orally Disintegrating Tablets

Yan

Woo

Kang

et al. 2010

Biological & Pharmaceutical Bulletin

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confidence: 99%

Preparation and Evaluation of Taste-Masked Donepezil Hydrochloride Orally Disintegrating Tablets

Yan

Woo

Kang

et al. 2010

Biological & Pharmaceutical Bulletin

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“…Hydroxypropyl methylcellulose phthalate (HPMCP-55) provided the best combination of taste making, suspension stability and bioavailability. 15) In the present investigation, an attempt has been made to fabricate a non friable taste masked orally disintegrating tablets (ODT) of an intensely bitter tasting antipsychotic drug risperidone, using a simple, rapid and cost effective process with equivalent efficiency to that of the previously reported lyophilized product.…”

mentioning

confidence: 99%

Fabrication and Evaluation of Taste Masked Resinate of Risperidone and Its Orally Disintegrating Tablets

Shukla

Chakraborty

Singh

et al. 2009

CHEMICAL & PHARMACEUTICAL BULLETIN

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The production of a palatable dosage form is very important for patient compliance, which in turn decides the commercial success of the product. The masking of unpleasant taste in orally-disintegrating tablets and chewable tablets is therefore an important consideration in the formulation of many therapeutic agents and is achieved by minimizing direct contact between the active species and the taste receptors in the buccal cavity of the subject. In order to improve the palatability of a pharmaceutical product, many techniques have been developed, which have not only improved the taste, but also the stability of the drug in the formulation and performance of the product. Use of ion exchange is one of the methods for taste masking.Ion Exchange Resins (IERs) for Taste Masking Ion exchange (IE) involves the reversible interchange of ions (of like charge) between a liquid and a solid phase, with no radical change in the structure and properties of the solid. 1) IERs are high molecular weight polymers and most frequently employed polymeric network is a copolymer of styrene and divinylbenzene. They have wide applications in enhancing the stability of sensitive drugs, sustaining the release of drug, 2) as disintegrating agents and for masking the bitter taste of drug.3) Drug binding to the resin can be achieved by two processes. First approach is repeated elution of drug solution through a column of swollen activated resin bead where drug is allowed to interact with binding sites of resin and second is by prolonged contact of resin with the drug solution. 4-7)Drug molecules get adsorbed on the IER, resulting in the formation of an insoluble adsorbate or resinate by forming weak ionic bonds which does not dissociate under the salivary pH conditions, hence, masks the unpleasant taste of drugs.After administration of resinate, the release of drug from the resin depends on the properties of the resin and the ionic environment within the gastrointestinal tract (GIT). Drug molecules get released from resin by exchanging with appropriately charged ions in the GIT and free drug is available for absorption.8) The IER devoid of drug is eliminated or biodegraded from or at the site of delivery. 9)Depending on nature of monomer and their ionic strength, IER can be classified into four major classes: strong acid cation exchange (CE) resin, weak acid CE resin, strong base anion exchange (AE) resin and weak base AE resin. Strong acid CE resins constituted of sulfonated styrene divinylbenzene copolymer are functional throughout the entire pH range and weak acid CE resins function at pH values above 6.0. Both can be used for masking the taste of basic drugs. Similarly, strong base AE resins are functional throughout the entire pH range, while the weak base AE resins function well below pH 7.0. 10) These can be used for masking the taste of acidic drugs.Application of IER for masking the bitter taste of drugs has been explored in many investigations. Oral suspension of quinolones (orbifloxacin) and/or their derivatives are prepared by IE...

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“…Various masking techniques such as the addition of sweeteners and flavorings, coating with water-soluble polymers, water-insoluble polymers, 4) or pH-dependent water-soluble polymers, 5,6) filling in capsules, complexing with cyclodextrins, 7) adsorption on ion-exchange resin, 8) and microencapsulation 9) have been attempted. Masking the properties of triethyl citrate in the enteric layer was thought to improve the unpleasant bitter taste and stability of lansoprazole.…”

Section: Effects Of the Enteric Layer Containing Macrogol 6000mentioning

confidence: 99%

Formulation Study for Lansoprazole Fast-disintegrating Tablet. II. Effect of Triethyl Citrate on the Quality of the Products

et al. 2003

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The lansoprazole fast-disintegrating tablet (LFDT) is a new formulation developed as a rapidly disintegrating tablet containing enteric-coated microgranules. Three issues were considered in the development of LFDT. The first issue is damage to the enteric layer during the compression process, because the enteric-coated microgranules are compressed with a tablet press. In our previous study, 1) it was clarified that sufficient flexibility of the enteric layer was achieved by the optimized combined ratio of methacrylic acid copolymer dispersion to ethyl acrylate-methyl methacrylate copolymer dispersion and adding the optimized concentration of triethyl citrate to reduce the damage during the compression process. The second issue is the taste of LFDT. Since patients take LFDT after disintegration in the mouth, it was thought important to formulate LFDT with a pleasant taste. The third issue is the stability of lansoprazole in LFDT, because lansoprazole is incompatible with many excipients.The purpose of this study was to develop enteric-coated microgranules with an improved taste and the stabilization of lansoprazole. Since triethyl citrate has an unpleasant bitter taste and is an oily liquid, 2) it was anticipated that it would affect the taste of the enteric-coated microgranules and the stability of lansoprazole. Tabata et al. 3) reported that the degradation content of lansoprazole should be proportional to the product of the degradation rate constant and the total solubility of lansoprazole and suggested that lansoprazole in enteric dosage form would be unstable when it coexisted with a liquid and would be easy to dissolve. We studied the effects of triethyl citrate on the unpleasant bitter taste and stability of lansoprazole in enteric-coated microgranules and also attempted to formulate enteric-coated microgranules by masking the unpleasant bitter taste and improving the stability of lansoprazole. ExperimentalMaterials Lansoprazole was synthesized at Takeda Chemical Industries, Ltd. Commercial lansoprazole capsules were obtained in-house at Takeda Chemical Industries, Ltd.Lactose monohydrate-microcrystalline cellulose spheres (Nonpareil 105T, mean particle size 150-180 mm) and low-substituted hydroxypropyl cellulose (LH-33, hydroxypropoxy groups 5.0-6.9%) were kindly supplied by Freund Industrial Co., Ltd., and Shin-Etsu Chemical Co., Ltd., respectively. Methacrylic acid copolymer dispersion (Eudragit ® L30D-55) and ethyl acrylate-methyl methacrylate copolymer dispersion (Eudragit ® NE30D) were purchased from Rölm GmbH. Low-substituted hydroxypropyl cellulose (LH-32, hydroxypropoxy groups 7.0-9.9%) and hydroxypropyl methylcellulose 2910 (TC-5 EW) were purchased from Shin-Etsu Chemical Co., Ltd. Mannitol and polysorbate 80 were purchased from Merck Japan Ltd. Magnesium carbonate (Tomita Pharmaceutical Co., Ltd.), hydroxypropyl cellulose (HPC-SSL, Nippon Soda Co., Ltd.), talc (Matsumura Industrial Co., Ltd.), titanium dioxide (Freund Industrial Co., Ltd.), citric acid (A. D. M. Faryast, Ltd.), glyceryl monost...

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Cited by 76 publications

References 3 publications

Preparation and Evaluation of Taste-Masked Donepezil Hydrochloride Orally Disintegrating Tablets

Preparation and Evaluation of Taste-Masked Donepezil Hydrochloride Orally Disintegrating Tablets

Fabrication and Evaluation of Taste Masked Resinate of Risperidone and Its Orally Disintegrating Tablets

Formulation Study for Lansoprazole Fast-disintegrating Tablet. II. Effect of Triethyl Citrate on the Quality of the Products

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