Preparation and Evaluation of Taste Masked Famotidine Formulation Using Drug/β-cyclodextrin/Polymer Ternary Complexation Approach

Patel, Ashok R.; Vavia, Pradeep R.

doi:10.1208/s12249-008-9078-0

Cited by 94 publications

(40 citation statements)

References 21 publications

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“…CD and its derivatives were used as taste masking agents for the preparation of rapidly dissolving films of CTZ by using a solvent casting method. The optimized ratio of 1:3 CTZ:hydroxypropyl β-CD was appropriate for taste masking [9,10] . CTZ was coated by a fluidized bed coating using Eudragit ® RL30-D and taste-masking evaluation was performed by healthy human volunteers and their perceived levels were recorded on a numerical scale [11,12] .…”

Section: Research Papermentioning

confidence: 99%

Cetirizine Dihydrochloride, beta-Cyclodextrin Inclusion Complex by Ethanol Kneading for Taste Masking

Katewongsa¹,

Lertsuphotvanit²,

Phaechamud³

2017

pharmaceutical-sciences

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Katewongsa, et al.: Cetirizine Dihydrochloride and β-Cyclodextrin Complex by Ethanol KneadingCetirizine dihydrochloride has a very unpleasant bitter taste. To mask the bitter taste, complexation with β-cyclodextrin using ethanol as a kneading solvent was investigated and evaluated by Fourier transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffractometry, thermogravimetric analysis, simultaneous X-ray diffractometry-differential scanning calorimetry measurement and 1 H-nuclear magnetic resonance spectroscopy. Taste was evaluated by human volunteers using an unstructured line scale. The basic characterization of the prepared tablets including in vivo disintegration time and drug dissolution was studied. Fourier transform infrared spectroscopy, differential scanning calorimetry and powder X-ray diffractometry data confirmed the inclusion complex formation. Thermogravimetric analysis, simultaneous X-ray diffractometry-differential scanning calorimetry measurements revealed the reduction of crystalline β-cyclodextrin due to the displacement of water molecules from complex formation. Proton nuclear magnetic resonance spectroscopy indicated an intermolecular interaction between protons of cetirizine dihydrochloride with the cavity of β-cyclodextrin. The prepared complex showed an unstructured line scale with apparent low average rating of 1.70. The inclusion complex-loaded fast disintegrating tablet prepared with direct compression had short disintegration time and good taste with an unstructured line scale with average rating of 0.28. Cetirizine dihydrochloride, β-cyclodextrin inclusion complex was successfully prepared by kneading method using ethanol as solvent. The inclusion complex-loaded fast disintegrating tablet had good taste and good perception in the mouth.

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Section: Research Papermentioning

confidence: 99%

Cetirizine Dihydrochloride, beta-Cyclodextrin Inclusion Complex by Ethanol Kneading for Taste Masking

Katewongsa¹,

Lertsuphotvanit²,

Phaechamud³

2017

pharmaceutical-sciences

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“…LID exhibited a characteristic sharp endothermic peak at 83.24°C, which corresponds to its melting point. The thermogram of HP-β-CD showed a very broad endothermic peak between 70°C and 100°C due to the release of water molecules present in the HP-β-CD cavity (34). When HP-β-CD interacts with a guest molecule, their melting peaks, boiling peaks, or sublimation peaks in DSC thermograms usually shift or disappear (35).…”

Section: Differential Scanning Calorimetrymentioning

confidence: 99%

Masking the Bitter Taste of Injectable Lidocaine HCl Formulation for Dental Procedures

et al. 2014

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Abstract. Several attempts have been made to mask the bitter taste of oral formulations, but none have been made for injectable formulations. This study aims to mask the bitter taste of dental lidocaine HCl (LID) injection using hydroxypropyl-β-cyclodextrin (HP-β-CD) and sodium saccharin. Inclusion complexes of LID and HP-β-CD were prepared by the solution method in 1:1 and 1:2 M ratios. Inclusion complexes in solution were studied using phase solubility in phosphate buffer solutions (pH 8, 9, and 10). Freeze-dried inclusion complexes were characterized using differential scanning calorimetry (DSC), Xray, Fourier transform infrared (FT-IR), nuclear magnetic resonance (NMR), scanning electron microscopy (SEM), and in vitro release. Injectable formulations were prepared using inclusion complexes and characterized for stability and for taste using an Alpha MOS ASTREE electronic tongue (ETongue). The association constants of HP-β-CD with lidocaine-free base and its ionized form were found to be 26.23± 0.00025 and 0.8694±0.00045 M −1 , respectively. Characterization studies confirmed the formation of stable inclusion complexes of LID and HP-β-CD. Injectable formulations were found to be stable for up to 6 months at 4°C, 25°C, and 40°C. The taste evaluation study indicated that HP-β-CD (1:1 and 1:2 M ratios) significantly improved the bitter taste of LID injectable formulation. In conclusion, inclusion complex in the 1:1 M ratio with 0.09% sodium saccharin was considered to be optimum in masking the bitter taste of LID.

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“…(34)(35)(36) The mechanism of the taste-masking effect of β-CD is the inclusion principle. (37)(38)(39)(40) It can enclose a certain amount of bitter drugs into its cavity. Thus, the taste-masking effect is proportional to the amount of β-CD.…”

Section: Taste-masking Mechanism Of Sl and β-Cdmentioning

confidence: 99%

Traditional Human Taste Panel and Taste Sensors Methods for Bitter Taste Masking Research on Combined Bitterness Suppressants of Berberine Hydrochloride

2017

Sensors and Materials

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Bitterness suppressants (BSs) can improve the taste of bitter medicines and mask the taste of bitter foodstuffs. Our goal here was to establish a method of analyzing bitterness using both a traditional human taste panel method (THTPM) and a taste sensors method. Sucralose (SL), sodium ferulate (SF), and β-cyclodextrin (β-CD), and their combinations were tested for their abilities to mask the bitter taste of berberine hydrochloride (BBR). SF showed a weak effect in masking the bitter taste of BBR, whereas SL and β-CD showed stronger effects. The effect of SL on bitter taste masking was linear with the logarithm of concentration, while the effect of β-CD was linear with its concentration. When β-CD and SL were used in combination, β-CD played a major role in taste masking. For this combination, a good correlation was found between the indices of THTPM and the taste sensors method. The taste sensors method can accurately predict the intensity of bitterness of BBR. Thus, it can be an effective tool for the screening of BS of BBR and the study of the taste-masking characteristics of BS combinations.

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Preparation and Evaluation of Taste Masked Famotidine Formulation Using Drug/β-cyclodextrin/Polymer Ternary Complexation Approach

Cited by 94 publications

References 21 publications

Cetirizine Dihydrochloride, beta-Cyclodextrin Inclusion Complex by Ethanol Kneading for Taste Masking

Cetirizine Dihydrochloride, beta-Cyclodextrin Inclusion Complex by Ethanol Kneading for Taste Masking

Masking the Bitter Taste of Injectable Lidocaine HCl Formulation for Dental Procedures

Traditional Human Taste Panel and Taste Sensors Methods for Bitter Taste Masking Research on Combined Bitterness Suppressants of Berberine Hydrochloride

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