Taste Masking and Formulation of Ondansetron Hydrochloride Mouth Dissolving Tablets

2015 ◽  
Vol 5 (3) ◽  
Author(s):  
Subedi R. ◽  
Poudel K. ◽  
Budhathoki U ◽  
Thapa P.
Keyword(s):  
Bitter Taste ◽  
Drug Loading ◽  
Taste Masking ◽  
Complexing Agent ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
Sodium Starch Glycolate ◽  
Ondansetron Hydrochloride ◽  
Croscarmellose Sodium ◽  
Mouth Dissolving Tablet

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 starch glycolate. Concentration of superdisintegrants ranged from 0.75-9.24 %. The formulated tablet had satisfactory disintegration time and dissolution profile. Optimization was carried out using central composite design. The disintegration and dissolution times were tallied with marketed ondansetron HCl tablets. From the results, it was deduced that the most effective concentration for desired disintegration was of croscarmellose sodium and sodium starch glycollate respectively at concentration above 5%. Therefore, it can be concluded that the intensely bitter taste of ondansetron HCl can be masked by using tulsion 335 and mouth dissolving ondansetron HCl can be successfully prepared by adding aforementioned superdisintegrants. This sort of mouth dissolving ondansetron HCl can be used in controlling vomiting in paediatric and geriatric patients and also for pregnancy induced vomiting.

scholarly journals Formulation and Evaluation of Mouth Dissolving Tablet of Almotriptan Malate

2021 ◽  
Vol 11 (5) ◽  
Keyword(s):  
Hepatic Metabolism ◽  
Taste Masking ◽  
Content Uniformity ◽  
Disintegration Time ◽  
Drug Content ◽  
Sodium Starch Glycolate ◽  
Wetting Time ◽  
Croscarmellose Sodium ◽  
Mouth Dissolving Tablet

Mouth dissolving tablet disintegrates and dissolves rapidly in the saliva, within a few seconds without the need of drinking water or chewing. A mouth dissolving tablet usually dissolves in the oral cavity within 15 seconds to 3 minutes. Almotriptan malate is an anti migraine drug with bitter taste and shows hepatic metabolism. In the present work, Mouth dissolving tablets of almotriptan malate were prepared by direct compression method using sodium starch glycolate and croscarmellose sodium as superdisintegrant with a view to enhance patient compliance and to avoid gastric dysmotility which is common with migraine drugs and for fast action of drug. The prepared batches of tablets were evaluated for hardness, friability, drug content uniformity, wetting time, water-absorption ratio and in-vitro dispersion time. Short-term stability studies on the promising formulation indicated that there are no significant changes in drug content and disintegration time. Keywords: Almotriptan malate, Superdisintegrant, Sodium starch glycolate, Crosscarmellose sodium, Taste masking.

scholarly journals FORMULATION AND EVALUATION OF MOUTH DISSOLVING TABLET OF AMLODIPINE BESYLATE

2019 ◽  
pp. 132-139
Author(s):  
MEGHAWATI R. BADWAR ◽  
SANDHYA L. BORSE ◽  
MANISH S. JUNAGADE ◽  
ANIL G. JADHAV
Keyword(s):  
Drug Release ◽  
Research Work ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Sodium Starch Glycolate ◽  
Treatment Of Hypertension ◽  
Croscarmellose Sodium ◽  
Artery Disease ◽  
Mouth Dissolving Tablet

Objective: The main objective of this research work was to formulate and evaluate the mouth dissolving tablet of amlodipine besylate for the treatment of hypertension and coronary artery disease. Methods: In this study, mouth dissolving tablet were prepared by direct compression method by using croscarmellose sodium and sodium starch glycolate as superdisintegrants. The designed tablets were subjected to various assessment parameters like friability test, hardness test, disintegration test, wetting time, in vitro drug release and drug content. Results: All the prepared formulations were subjected to various assessment parameters, and the findings obtain within the prescribed limit. The calibration curve of pure drug using various solvents like phosphate buffer pH 6.8, methanol was plotted. F1-F9 containing croscarmellose sodium and sodium starch glycolate in various concentration demonstrate the minimum disintegration time. Among all these formulations F9 shows disintegration time up to 22±1.12 seconds due to the high concentration of superdisintegrants. In vitro drug release was tested in phosphate buffer pH 6.8 at a time interval of 0, 1, 2, 3, 4, 5 min. The F9 shows drug release 100.22±1.08%. Accelerated stability study of optimized formulation (F9) up to 2 mo showed there was no change in disintegration time and percentage drug release. Conclusion: The results obtained in the research work clearly showed a promising potential of mouth dissolving tablets containing a specific ratio of croscarmellose sodium and sodium starch glycolate as superdisintegrants for the effective treatment of hypertension and coronary artery disease.

Formulation and Evaluation of Taste Masked Oral Disintegrating Tablets of Aripiprazole

2015 ◽  
Vol 8 (1) ◽  
pp. 2723-2734
Author(s):  
Y. Shravan Kumar ◽  
Prashanthi Patel ◽  
Sravanthi Ch ◽  
Rashmi B
Keyword(s):  
Depressive Disorders ◽  
Partial Agonist ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
Sodium Starch Glycolate ◽  
Weight Variation ◽  
Croscarmellose Sodium

Aripiprazole is an atypical antipsychotic agent used for treatment of schizophrenia, bipolar disorder and major depressive disorders. In the present work, oral  disintegrating tablets of aripiprazole were developed to  enhance the patient compliance and provide rapid onset of  action. The efficacy of aripiprazole is mediated through a combination of partial agonist activity at dopamine D2 and serotonin 5HT-1A receptors and antagonist activity at 5HT-2A receptors. It has a bitter taste and poor-solubility in water. Thus, the main objective of the study is to formulate taste masked oral disintegrating tablets of aripiprazole by using inclusion complex beta-cyclodextrin to achieve a better dissolution rate and further improving the bioavailability of the drug. Oral disintegrating tablets were   prepared by direct compression method using  super disintegrant like crospovidone, croscarmellose sodium,  sodium starch glycolate and combinations of  cros-povidone with croscarmellose sodium, and crospovidone with sodium  starch glycolate in different concentrations. They were evaluated for the pre-compression parameters such as bulk density, compressibility, Hausner ratio and angle of repose. The prepared batches of tablets were evaluated for hardness, weight variation, thickness, friability, drug content, disintegration time, wetting time,    in vitro dispersion time, and in vitro dissolution profile. All these parameters were found to be satisfactory. Among all, the formulation F15 containing crospovidone 5% + cros-povidone with croscarmellose sodium 5% was considered to be the optimum formulation, which released nearly 99% of the drug in 20 minutes with a disintegration time of 10. 20 seconds. These studies indicate the viability and benefits of oral disintegrating tablets of aripiprazole. 

The Effect of Different Superdisintegrants and their Concentrations on the Dissolution of Topiramate Immediate Release Tablets

2009 ◽  
Vol 2 (2) ◽  
pp. 531-5366
Author(s):  
V A. Vamshi Priya ◽  
G. Chandra Sekhara Rao ◽  
D. Srinivas Reddy ◽  
V. Prabhakar Reddy
Keyword(s):  
Immediate Release ◽  
Drug Dissolution ◽  
Dissolution Profile ◽  
Dissolution Medium ◽  
Lactose Monohydrate ◽  
Sodium Starch Glycolate ◽  
Tablet Disintegration ◽  
Croscarmellose Sodium ◽  
Model Drug ◽  
Usp Apparatus

The purpose of this study was to investigate the efficiency of superdisintegrants: sodium starch glycolate, croscarmellose sodium and crospovidone in promoting tablet disintegration and drug dissolution of Topiramate immediate release tablets. The efficiency of superdisintegrants was tested, by considering four concentrations, viz., like 2%, 3%, 4% and 5% in the formulations. The dissolution was carried out in USP apparatus II at 50 rpm with distilled water as a dissolution medium. The dissolution rate of the model drug topiramate was found highly dependent on the tablet disintegration, on the particle size of the superdisintegrant, on the solubility of the drug and also on the type of superdisintegrant in the dissolution medium. There was no effect of the diluent (Lactose monohydrate) on the disintegration of different concentrations of superdisintegrants. These results suggest that, as determined by the f2 metric (similarity factor), the dissolution profile of the formulation containing 4% sodium starch glycolate and lactose monohydrate as a diluent was similar to that of a marketed product.

scholarly journals Formulation and evaluation of taste masked oral disintegrating tablets of lornoxicam

2021 ◽  
Vol 11 (5) ◽  
pp. 115-120
Author(s):  
Kritika Rai ◽  
Vivek Jain ◽  
Sunil Kumar Jain ◽  
Pushpendra Kumar Khangar
Keyword(s):  
Cation Exchange Resin ◽  
The Elderly ◽  
In Vitro Dissolution ◽  
Taste Masking ◽  
Direct Compression ◽  
Compression Technique ◽  
Disintegration Time ◽  
Weight Variation ◽  
Croscarmellose Sodium

Orally disintegrating tablets (ODT) disintegrate quickly with saliva when administered into the oral cavity and taken without water or chewed. ODT are easy to take for children and the elderly, who may experience difficultly in taking ordinary oral preparations such as tablets, capsules, and powders.  The ODT threes substantial benefits for the patient (or elder) who cannot swallow (Dysphagia), or who is not permitted water intake due to disease. The reason of the current research was to prepare taste masking oral disintegrating tablets of poorly soluble lornoxicam (LXM) by direct compression technique using Kyron T-114 (cation exchange resin) as a taste masking agent. With in various ratios the Drug-resin of 1:4 was established to present best taste masking. The superdisintegrants used in formulation are croscarmellose sodium and cross povidone. Among these croscarmellose sodium demonstrated superior drug release. The tablets were evaluated for friability, weight variation, wetting time, hardness, disintegration time and uniformity of content. Optimized formulations were evaluated for in vitro dissolution test. Amongst all the formulations F-6 was found to be most successful tablets prepared by this technique had disintegration time of 30sec and % CDR 94.78 within 30min. Hence, this advance can be utilized for taste masking of bitter pharmaceutical ingredients leading to superior patient compliance. Keywords: Oral disintegration tablets, Lornoxicam, Kyron T-114, Superdisintegrants, Direct Compression.

scholarly journals FORMULATION AND IN VITRO EVALUATION OF FAST DISSOLVING TABLET OF VERAPAMIL HYDROCHLORIDE

2018 ◽  
Vol 10 (10) ◽  
pp. 93 ◽  
Author(s):  
Dattatraya M. Shinkar ◽  
Pooja S. Aher ◽  
Parag D. Kothawade ◽  
Avish D. Maru
Keyword(s):  
Drug Release ◽  
Phosphate Buffer ◽  
Research Work ◽  
Time Interval ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Verapamil Hydrochloride ◽  
Sodium Starch Glycolate ◽  
Croscarmellose Sodium

Objective: The main objective of this research work was to formulate and evaluate fast dissolving tablet of verapamil hydrochloride for the treatment of hypertension.Methods: In this study, fast dissolving tablet were prepared by wet granulation method by using croscarmellose sodium and sodium starch glycolate as superdisintegrants in the concentration of 2%, 4%, and 6%. Polyvinyl pyrollidone K30 is used as a binder. The designed tablets were subjected to various assessment parameters like friability test, hardness test, disintegration test, wetting time, in vitro drug release and drug content.Results: All the prepared formulations were subjected to various assessment parameters, and the findings obtain within the prescribed limit. The calibration curve of pure drug using various solvents like distilled water, phosphate buffer pH 6.8 was plotted. F1-F9 containing croscarmellose sodium and sodium starch glycolate in various concentration demonstrate the minimum disintegration time. Among all these formulations F8 shows disintegration time upto 19±0.06 seconds due to the high concentration of superdisintegrants. In vitro drug release was tested in phosphate buffer pH 6.8 at a time interval of 0, 1, 3,6,9,12,15 min. The F8 shows drug release 98.5±0.567%. Accelerated stability study of optimized formulation (F8) up to 2 mo showed there was no change in disintegration time and percentage drug release.Conclusion: The results obtained in the research work clearly showed a promising potential of fast dissolving tablets containing a specific ratio of crosscarmellose sodium and sodium starch glycolate as superdisintegrants for the effective treatment of hypertension. 

scholarly journals DESIGN, OPTIMIZATION AND EVALUATION OF ACECLOFENAC FAST DISSOLVING TABLETS EMPLOYING STARCH VALERATE–A NOVEL SUPERDISINTEGRANT

2021 ◽  
pp. 168-176
Author(s):  
R. SANTOSH KUMAR ◽  
SHAMBHAVI KANDUKURI ◽  
M. RAMYA ◽  
B. KUSUMA LATHA
Keyword(s):  
Factorial Design ◽  
Immediate Release ◽  
Compression Method ◽  
Disintegration Time ◽  
23 Factorial Design ◽  
Sodium Starch Glycolate ◽  
Wetting Time ◽  
Croscarmellose Sodium ◽  
Dissolution Efficiency

Objective: To synthesize, characterize and evaluate starch valerate as a superdisintegrant in the formulation of aceclofenac fast dissolving tablets by employing 23 factorial design. Methods: Starch valerate was synthesized and its physical and micromeritic properties were performed to evaluate it. The fast dissolving tablet of aceclofenac was prepared by employing starch valerate as a superdisintegrant in different proportions in each case by direct compression method using 23 factorial design for evaluation of tablet parameters like disintegration and dissolution efficiency in 5 min. Results: The starch valerate prepared was found to be fine, amorphous and free flowing. Starch valerate exhibited good swelling in water with swelling index (125.2%). The study of starch valerate was shown by fourier transform infrared spectra (FTIR). The drug content (200±5%), hardness (3.5–4 kg/sq. cm), and friability (<0.15%) has been effective with regard to all the formulated fast dissolving tablets employing starch valerate. The disintegration time of all the formulated tablets was found to be in the range of 14±0.04 to 25.7±0.02 sec. The optimized formulation F4 had the least disintegration time i.e., 12.8±0.02 sec. The wetting time of the tablets was found to be in the range of 76±0.21 to 217±0.17s. The In vitro wetting time was less (i.e., 28±0.02s) in optimized formulation F4. The water absorption ratio of the formulated tablets was found to be in the range of 46±0.12 to 100±0.27%. The percent drug dissolved in the optimized formulation F8 was found to be 99.93% in 5 min. Conclusion: Starch valerate, when combined with sodium starch glycolate, croscarmellose sodium, with aceclofenac, was found to be an effective super disintegrant which improved the dissolution efficiency and could therefore be used in the formulation of quick dissolving tablets to provide immediate release of the contained drug within 5 min.

FORMULATION AND EVALUATION OF MOUTH DISSOLVING TABLETS OF RANITIDINE HYDROCHLORIDE

INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (09) ◽  
pp. 13-20
Author(s):  
V Arora ◽  
◽  
S Kumar ◽  
P. B Mishra ◽  
N. Vashisht
Keyword(s):  
Research Work ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Taste Masking ◽  
Dissolution Profile ◽  
Cyclodextrin Complex ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Ranitidine Hydrochloride ◽  
Weight Variation

In present research work, taste masked Mouth Dissolving Tablets (MDTs) of Ranitidine Hydrochloride were designed with a view to enhance the patient compliance and provide a quick onset of action. Taste masking of the drug was done by formation of complex with β cyclodextrin. Tablets were prepared by direct compression, using superdisintegrants like crosscarmellose sodium and crosspovidone in different proportion and evaluated for the pre-compression parameters such as bulk density, compressibility, angle of repose etc. In view of the better taste palatability of such a bitter API, taste masking was carried out via making the cyclodextrin complex and sucralose was used as the sweetener to impart a palatable taste to the formulation. The prepared batches of tablets were evaluated for hardness, weight variation, friability, drug content, disintegration time and in vitro dissolution profile and found satisfactory. Among all, the formulation F7 containing 5% w/w proportion of both crosscarmellose sodium and crosspovidone was considered to be best formulation, which disintegrated completely in 19 seconds and released up to 98.38% of the drug.

scholarly journals Formulation and Evaluation of Ketorolac Tromethamine Mouth Dissolving Tablets

2021 ◽  
Vol 11 (1) ◽  
pp. 60-64
Author(s):  
Rishabh Bindal ◽  
Arpna Indurkhya
Keyword(s):  
Ketorolac Tromethamine ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Solid Dosage ◽  
Sodium Starch Glycolate ◽  
Weight Variation ◽  
Croscarmellose Sodium ◽  
Fast Release

Due to more versatility and comfort, mouth dissolving tablets are the most advanced type of oral solid dosage forms. Compared to conventional tablets, it increases the effectiveness of APIs by dissolving within a minute in the oral cavity after contact with less saliva, without chewing and without the need for water for administration. Mouth Dissolving Tablets of Ketorolac tromethamine were prepared by direct compression method using various superdisintegrants like crospovidone, Croscarmellose sodium, and Sodium starch glycolate in different concentrations. Prepared tablets were evaluated for hardness, friability, weight variation, disintegration time, wetting time and in vitro drug release. Results of pre-compression and post-compression studies of all formulations were found within the standard limits. The tablets of all the batches were found to release more than 80% of drug in 5 minutes, which is the desired quality of mouth dissolving tablets that helps in faster absorption of the drug and quick onset of therapeutic effect. The the order of dissolution of various disintegrants was found to be Crospovidone˃ SSG˃ CCS. There was no significant variation in drug content of drug during stability studies for selected batch F3 in accelerated conditions over three months. It was concluded from the study that fast release of Ketorolac tromethamine from formulation F3 may reduce onset of drug action with better patient compliance. Keywords: Crospovidone, Croscarmellose sodium, Ketorolac tromethamine, Mouth dissolving tablets, Sodium starch glycolate, superdisintegrants.

scholarly journals OPTIMIZATION OF STARCH CROTONATE AS A NOVEL SUPERDISINTEGRANT IN THE FORMULATION OF FAST DISSOLVING TABLETS THROUGH 23 FACTORIAL DESIGN

2021 ◽  
pp. 247-256
Author(s):  
A. HARI OM PRAKASH RAO ◽  
SANTOSH KUMAR RADA ◽  
SHAMBHAVI KANDUKURI
Keyword(s):  
Factorial Design ◽  
Immediate Release ◽  
Compression Method ◽  
Disintegration Time ◽  
23 Factorial Design ◽  
Sodium Starch Glycolate ◽  
Wetting Time ◽  
Croscarmellose Sodium ◽  
Dissolution Efficiency

Objective: To synthesize, characterize and evaluate starch crotonate as a superdisintegrant in the formulation of Piroxicam fast dissolving tablets by employing 23 factorial design. Methods: Starch crotonate was synthesized and its physical and micromeritic properties were performed to evaluate it. The fast dissolving tablet of Piroxicam were prepared by employing starch crotonate as a superdisintegrant in different proportions in each case by direct compression method using 23 factorial design. Results: The starch chrotonate prepared was found to be fine, free flowing and amorphous. Starch crotonate exhibited good swelling in water with swelling index (50%). The study of starch crotonate was shown by fourier transform infrared spectra (FTIR). The drug content (100±5%), hardness (3.6–4 kg/sq. cm), and friability (<0.15%) have been effective with regard to all the formulated fast dissolving tablets employing starch crotonate. The disintegration time of all the formulated tablets was found to be in the range of 18±03 to 66±03 sec. The optimized formulation F8 had the least disintegration time i.e., 18±03 sec. The wetting time of the tablets was found to be in the range of 49.92±0.11 to 140±0.18s. The In vitro wetting time was less (i.e., 74±0.37s) in optimized formulation F8. The water absorption ratio of the formulated tablets was found to be in the range of 27.58±0.01 to 123.07±0.33%. The percent drug dissolved in the optimized formulation F8 was found to be 99.83% in 10 min. Conclusion: Starch crotonate, when combined with sodium starch glycolate, croscarmellose sodium, with Piroxicam was found to be an effective super disintegrant which improved the dissolution efficiency and could therefore be used in the formulation of quick dissolving tablets to provide immediate release of the contained drug within 10 min.

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