Trends in Pharmaceutical Taste Masking Technologies: A Patent Review

Ayenew, Zelalem; Puri, Vibha; Kumar, Lokesh; Bansal, Arvind K.

doi:10.2174/187221109787158364

Cited by 116 publications

(60 citation statements)

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“…Most often cited are formulations of a solid dispersion with a water-soluble, rate-enhancing polymer such as polyethylene glycol (5), microencapsulation with hydrophilic polymers (6), and formation of inclusion complexes with a water-soluble material such as β-cyclodextrin (7). Another possible strategy is the incorporation of pH modifiers in the dosage form.…”

Section: Introductionmentioning

confidence: 99%

Modulation of pH-Independent Release of a Class ΙΙ Drug (Domperidone) from a Polymeric Matrix Using Acidic Excipients

Khan¹,

Iqbal²,

Khan³

et al. 2016

Dissolution Technol.

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Drug release from polymeric matrix systems is the rate-limiting step for drug bioavailability and is determined by drug solubility; most drugs show pH-dependent solubility. Polymeric matrices remain in the gastrointestinal tract for a longer period of time and are exposed to environments of varying pH, which can adversely affect drug release. In the present study, the pH-independent drug release of domperidone was achieved by modifying the microenvironmental pH of a swollen polymeric matrix using acidic excipients (citric acid and tartaric acid). Matrices were prepared by a water-based, wet-granulation technique and evaluated for various official and unofficial parameters. In vitro drug release was studied using USP dissolution apparatus and pH 6.80 phosphate buffer as dissolution medium. Release kinetics was evaluated according to various mathematical models.Results show that domperidone release can be effectively modified by inclusion of acidic excipients in the formulations. Acidic excipients modulated microenvironmental pH and avoided the effect of dissolution medium pH on drug release. The resultant formulations are easy to prepare and scale up for commercial manufacturing. Better pH-independent release, following zero-order kinetics, was achieved with tartaric acid.

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Section: Introductionmentioning

confidence: 99%

Modulation of pH-Independent Release of a Class ΙΙ Drug (Domperidone) from a Polymeric Matrix Using Acidic Excipients

Khan¹,

Iqbal²,

Khan³

et al. 2016

Dissolution Technol.

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“…One of the major barriers that prevents patient from adhering to a prescribed medication regimen has been identified as the unacceptable taste of active pharmaceutical ingredients (APIs) in these dosage forms [5]. Taste has an important role in the development of oral pharmaceuticals, with respect to patient acceptability and compliance, and is one of the prime factors 2 Advances in Pharmaceutics determining the market penetration and commercial success of oral formulations, especially in pediatric medicine [6].…”

Section: Introductionmentioning

confidence: 99%

Formulation Development of Mouth Dissolving Film of Etoricoxib for Pain Management

Senthilkumar¹,

Vijaya²

2015

Advances in Pharmaceutics

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Etoricoxib is a potent, orally active, and highly selective COX-2 inhibitor that exhibits anti-inflammatory, analgesic, and antipyretic activities. The present research was undertaken to develop mouth dissolving films of etoricoxib to have rapid onset of action. Mouth dissolving film (MDF) is a better alternate to oral disintegrating tablets due to its novelty, ease of use, and the consequent patient compliance. Solubility enhancement and taste masking of etoricoxib were the two challenges solved by formulating druginclusion complex with beta-cyclodextrin (BCD). MDF prepared by solvent casting etoricoxib-BCD complex along with HPMC as film forming polymer was found to possess desirable physicomechanical properties. In vitro release of etoricoxib from MDF in simulated salivary fluid and 0.1 N HCl was more than 95% within 2 minutes. Taste masking and in vivo disintegration were in acceptable range as assessed by human volunteers. Etoricoxib MDF was further characterized by differential scanning calorimetry, powder X-ray diffraction, and scanning electron microscopy. The index of analgesia shown by etoricoxib MDF was comparable to that of immediate release tablets (100% activity within 40 minutes) in animal studies. Conclusively, the present study documents the development of a commercially viable formula for an MDF of etoricoxib with rapidity in pain management.

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“…One of the major barriers that prevent patients from following a prescribed medication regimen has been identified as the unpleasant taste of active pharmaceutical ingredients (APIs) in these dosage forms (1).…”

Section: Introductionmentioning

confidence: 99%

An Electronic Tongue: Evaluation of the Masking Efficacy of Sweetening and/or Flavoring Agents on the Bitter Taste of Epinephrine

et al. 2010

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Abstract. An epinephrine (E) tablet is under development for sublingual (SL) administration for the first-aid treatment of anaphylaxis; however, the inherent bitterness of E may hinder acceptability by patients, especially children. To assess the degree of E bitterness and to predict the masking effects of sweetening and/or flavoring non-medicinal ingredients (NMIs), the potential usefulness of an electronic tongue (e-Tongue) was evaluated. The e-Tongue sensors were conditioned, calibrated, and tested for taste discrimination. Six standard active pharmaceutical ingredients were used to build and validate a bitterness model which was then used to assess E bitartrate (EB) solutions from 0.3-9 mM. Tastemasking efficiency of aspartame (ASP), acesulfame potassium (ASK), and citric acid (CA) each at 0.5 mM was evaluated. Using EB 9 mM, the bitterness score was 20 on a scale of 20 (unacceptable) down to 1 (not detected). When NMIs 0.5 mM were added, neither ASK (17.2, unacceptable) nor was ASP (14.0, limit acceptable) effective in masking the bitter taste. When the combination of ASK and ASP was used, the bitterness score was reduced to 9.2 (acceptable). However, the addition of CA alone resulted in the best reduction of the bitterness score to 3.3 (not detected). Using the e-Tongue, the incorporation of a variety of sweetening and/or flavoring NMIs into a SL tablet of E could be shown to mask its bitter taste by up to 80%. These results should be confirmed by in vivo studies.

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Trends in Pharmaceutical Taste Masking Technologies: A Patent Review

Cited by 116 publications

References 0 publications

Modulation of pH-Independent Release of a Class ΙΙ Drug (Domperidone) from a Polymeric Matrix Using Acidic Excipients

Modulation of pH-Independent Release of a Class ΙΙ Drug (Domperidone) from a Polymeric Matrix Using Acidic Excipients

Formulation Development of Mouth Dissolving Film of Etoricoxib for Pain Management

An Electronic Tongue: Evaluation of the Masking Efficacy of Sweetening and/or Flavoring Agents on the Bitter Taste of Epinephrine

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