Preparation and Evaluation of Taste Masked Orally Disintegrating Tablets with Granules Made by the Wet Granulation Method (original) (raw)
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Preparation and evaluation of taste-masked orally disintegrating tablets of prednisolone
2007
Using furosemide (FU) as a model drug, we examined the wet granulation method as a way to improve the taste masking and physical characteristics of orally disintegrating tablets (ODTs). In the wet granulation method, yogurt powder (YO) was used as a corrective and maltitol (MA) was used as a binding agent. The taste masked FU tablets were prepared using the direct compression method. Microcrystalline cellulose (AvicelPH-302) and mannitol were added as excipients at a mixing ratio of 1/1 by weight. Based on the results of sensory test on taste, the prepared granules markedly improved the taste of FU, and a su‹cient masking eŠect was obtained at the YO/FU ratio of 1 or more. Furthermore, it was found that the masking eŠect achieved by YO granules made with the wet granulation method was similar to or better than that produced by the granules made with dry granulation method. All types of tablets displayed su‹cient hardness (over 3.5×10-2 kN), and rapidly disintegrating tablets were obtained with YO granules produced at a mixing ratio of FU/YO＝1/1, which disintegrated within 20 s. Disintegration time lengthened as the mixing ratio of YO to FU increased. In the mixing ratio of FU/YO＝1/1, the hardness of tablets with granules made by the wet granulation method exceeded that of tablets with granules made by the dry granulation method, with minimal diŠerences in disintegration time. The hardness and disintegration time of the tablets with granules made by the wet granulation method could be controlled by varying the compression force. In conclusion, YO was found to be a useful additive for masking unpleasant tastes. FU ODTs with improved taste, rapid disintegration and greater hardness could be prepared with YOcontaining granules made by the wet granulation method using MA as a binding agent.
Optimized furosemide taste masked orally disintegrating tablets
Saudi Pharmaceutical Journal, 2017
Optimized orally disintegrating tablets (ODTs) containing furosemide (FUR) were prepared by direct compression method. Two factors, three levels (3 2) full factorial design was used to optimize the effect of taste masking agent (Eudragit E100; X1) and superdisintegarant; croscarmellose sodium (CCS; X2) on tablet properties. A composite was prepared by mixing ethanolic solution of FUR and Eudragit E100 with mannitol prior to mixing with other tablet ingredients. The prepared ODTs were characterized for their FUR content, hardness, friability and wetting time. The optimized ODT formulation (F1) was evaluated in term of palatability parameters and the in vivo disintegration. The manufactured ODTs were complying with the pharmacopeia guidelines regarding hardness, friability, weight variation and content. Eudragit E100 had a very slightly enhancing effect on tablets disintegration. However, the effects of both Eudragit E100 (X1) and CCS (X2) on ODTs disintegration time (Y1) were insignificant (p > 0.05). Moreover, X1 exhibited antagonistic effect on the dissolution after 5 and 30 min (D5 and D30, respectively), but only its effect on D30 is significant (p = 0.0004). Furthermore, the optimized ODTs formula showed good to acceptable taste in term of palatability, and in vivo disintegration time of this formula was about 10 s.
New Technologies in the Formulation of Oral Dispersible Tablets and Taste Masking: A Review
Indian Research Journal of Pharmacy and Science, 2018
In oral drug delivery system (ODDS), drug is administered through the oral route. Oral route is the most preferred and safe route for the delivery of dosage form. Enzymatic degradation of drug and first pass metabolism are the main drawback for this route. One of the tablet taken through this route is Oral dispersible tablet (ODT) is also known as Fast melting, Fast-dispersing, Fast dissolving, Mouth dissolving and Quick disintegrating tablet. These are the tablets which are intended to be placed in the mouth where before swallowing they are get to disperse rapidly. These tablets are made for the fast action basically due to their fast dispersion. ODTs having many merits such as water is not required for swallowing these tablets, having no difficulties for administration to geriatric, paediatric, mentally disabled, and bedridden patients these are having rapid onset of therapeutic action, give good mouth feels, particularly for paediatric patients. Some techniques to prepare ODT are Freeze-drying (Lyophilisation), spray drying, melt granulation, cotton candy process, Phase transition process and direct compression etc. But for these tablets the main challenge is the taste of drug. If the drug having bitter taste it becomes very difficult to take the tablet in this dosage form. However there are many taste masking techniques have been come in focus today to solve this problem. Some of taste masking techniques are such as flavouring and sweetening agents addition, Ion exchange resin,
Drug Development and Industrial Pharmacy, 2016
Context: Considering that bitter taste of drugs incorporated in orally disintegrating tablets (ODTs) can be the main reason for avoiding drug therapy, it is of the utmost importance to achieve successful taste-masking. The evaluation of taste-masking effectiveness is still a major challenge. Objective: The objective of this study was to mask bitter taste of the selected model drugs by drug particle coating with Eudragit ® E PO, as well as to evaluate taste-masking effectiveness of prepared ODTs using compendial dissolution testing, dissolution in the small-volume shakeflask assembly and trained human taste panel. Materials and methods: Model drugs were coated in fluidized bed. Disintequik™ ODT was used as a novel co-processed excipient for ODT preparation. Selected formulations were investigated in vitro and in vivo using techniques for taste-masking assessment. Results and discussion: Significantly slower drug dissolution was observed from tablets with coated drug particles during the first three minutes of investigation. Results of in vivo tastemasking assessment demonstrated significant improvement in drug bitterness suppression in formulations with coated drug. Strong correlation between the results of drug dissolution in the small-volume shake-flask assembly and in vivo evaluation data was established (R ≥ 0.970). Conclusion: Drug particle coating with Eudragit ® E PO can be a suitable approach for bitter taste-masking. Strong correlation between in vivo and in vitro results implicate that smallvolume dissolution method may be used as surrogate for human panel taste-masking assessment, in the case of physical taste-masking approach application.
CHEMICAL & PHARMACEUTICAL BULLETIN, 2010
The purpose of this study was to mask the intensely bitter taste of metoclopramide HCl and to formulate a rapid disintegrating tablet (RDT) of the taste-masked drug. Taste masking was done by complexing metoclopramide HCl with aminoalkyl methacrylate copolymer (Eudragit ® EPO) in different ratio by the extrusion-precipitation method. Drug-polymer complexes (DPCs) were tested for drug content, in vitro taste in simulated salivary fluid (SSF) of pH 6.8, taste evaluation in oral cavity and molecular property. The complex having drug-polymer ratio of 1 : 2 shows significant taste masking, confirmed by drug release in SSF and in-vivo taste evaluation; therefore, it was selected for further study. Taste evaluation of DPCs in human volunteers revealed considerable taste masking with the degree of bitterness below threshold value (0.5) within 10 s, whereas, metoclopramide HCl was rated intensely bitter with a score of ؉3 for 10 s. Tablets were evaluated for various parameters like tensile strength, wetting time, water absorption ratio, in-vitro disintegration time, and disintegration in oral cavity. The effect of diluents, lubricants and sweetening agent (Xylisorb) on the disintegration time was also evaluated. Tablets of batch F3 containing mannitol and microcrystalline cellulose in the ratio 1 : 1 and 8% w/w crosspovidone showed faster disintegration (within 20 s) than the marketed formulation (180 s). Good correlation between in vitro disintegration behavior and in the oral cavity was recognized. Tablets of batch F3 also revealed rapid drug release (t 90 , 90 s) in SGF compared with marketed formulation (t 90 , 600 s).
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.
Evaluation of preparation methods for orally disintegrating tablets
Medicine Science | International Medical Journal
Oral disintegrating tablets (ODT) are orally administered solid dosage forms commonly used in pediatric and geriatric patients with difficulty in swallowing. The lack of need for water during the use of ODTs is another advantage that increases patient compliance. Many methods are used for the production of ODTs such as direct compression (DC), freeze-drying (FD), spray drying, 3-D printing, melt granulation, phase transition process, molding, sublimation, mass extrusion, cotton candy process. Since the ODTs produced are aimed to disintegrate and dissolve rapidly, and consequently act quickly, the production method parameters need to be optimized in line with the critical product parameters. In this study, the most widely used manufacturing methods (especially DC and FD) for ODT and in vitro quality control tests of ODT are evaluated.
Formulation and optimization of orodispersible tablets of flutamide
2014
The present study aimed to formulate orodispersible tablets of flutamide (FTM) to increase its bioavailability. Orodispersible tablets were prepared by direct compression technique using three different approaches namely; super-disintegration, effervescence and sublimation. Different combined approaches were proposed and evaluated to optimize tablet characteristics. Sodium starch glycolate (SSG) was used as the superdisintegrant. The prepared powder mixtures were subjected to both pre and post compression evaluation parameters including; IR spectroscopy, micromeritics properties, tablet hardness, friability, wetting time, disintegration time and in-vitro drug release. IR studies indicated that there was no interaction between the drug and the excipients used except Ludipress. The results of micromeritics studies revealed that all formulations were of acceptable to good flowability. Tablet hardness and friability indicated good mechanical strength. Wetting and dispersion times decrea...
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...