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

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.

Author(s):  
Sudarshan Singh ◽  
S S Shyale ◽  
P Karade

The aim of this study was to design orally disintegrating tablet (ODT) of Lamotrigine. It is an Antiepileptic drug which is widely used in epilepsy. It is also used in simple and complex partial seizures and secondary generalized tonic-clonic seizures. It is poorly water soluble drug (0.46 mg/ml). Thus, an attempt was made to enhance the water solubility by complexation with β-cyclodextrin (1:1 molar ratios). The orally disintegrating tablet of lamotrigine was prepared by direct compression method using different concentration of superdisintegrants such as Sodium starch glycollate, croscarmellose sodium by sublimating agent such as camphor. The formulations were evaluated for weight variation, hardness, friability, drug content, wetting time, in vitro disintegration time and in vitro dissolution studies. The prepared tablets were characterized by Fourier transform infrared spectroscopy and differential scanning calorimetry. The disintegration time for the complexed tablets prepared by different concentration of superdisintegrants was found to be in range of 32.54 ± 0.50 to 55.12 ± 0.57 sec and wetting time of the formulations was found to be in range of 28.47 ± 0.67 to 52.19 ± 0.72 sec. All the formulation showed almost 100 percent of drug release within 15 min. Among all the formulation F6 and F7 prepared with 18% croscarmellose sodium and camphor shows faster drug release, respectively 10 min, F6 gives good result for disintegration time, drug release, wetting time and friability. Further formulations were subjected to stability testing for 30 days at temperature of 40 ± 5 ºC/75 ± 5 %RH. Tablets showed no appreciable changes with respect to physical appearance, drug content, disintegration time and dissolution profiles. Results were statistically analyzed by one-way ANOVA at a p < 0.05. It was found that, the data at any point of time are significant at p < 0.05.


Author(s):  
R. SANTOSH KUMAR ◽  
SHAMBHAVI KANDUKURI ◽  
M. RAMYA ◽  
B. KUSUMA LATHA

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.


2015 ◽  
Vol 49 (3) ◽  
pp. 173-180
Author(s):  
T Ayyappan ◽  
C Poojitha ◽  
T Vetrichelvan

In the present work, orodissolving tablets of Efavirenz were prepared by direct compression method with a view to enhance patient compliance. A 23 full factorial design was applied to investigate the combined effect of three formulation variables. Amount of crospovidone, croscarmellose sodium and sodium starch glycolate were used as superdisintegrant material along with direct compressible mannitol to enhance mouth feel. The prepared batches of tablets were evaluated for hardness, friability, weight variation, disintegration time, wetting time, drug content and in-vitro dissolution studies. Based on wetting time, disintegration time, the formulation containing crospovidone (5% w/v), carscarmellose sodium (5% w/v) and sodium starch glycolate (8% w/v) was found to be promising and tested for in-vitro drug release pattern (in 0.1 N HCl), short term stability and drug- superdisintegrants interaction. Surface response plots are presented to graphically represent the effect of independent variables (conc. of superdisintegrants) on the in-vitro dissolution time. The validity of the generated mathematical model was tested by preparing extra-design check point formulation. The formulation showed nearly faster drug release compared to the conventional commercial tablet formulation. Stability studies on the optimized formulation indicated that there was no significant change found in physical appearance, hardness, disintegration time, drug content and in-vitro drug release. DOI: http://dx.doi.org/10.3329/bjsir.v49i3.22131 Bangladesh J. Sci. Ind. Res. 49(3), 173-180, 2014


Author(s):  
MEGHAWATI R. BADWAR ◽  
SANDHYA L. BORSE ◽  
MANISH S. JUNAGADE ◽  
ANIL G. JADHAV

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.


Author(s):  
A. HARI OM PRAKASH RAO ◽  
SANTOSH KUMAR RADA ◽  
SHAMBHAVI KANDUKURI

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.


2016 ◽  
Vol 15 (1) ◽  
pp. 73-81
Author(s):  
Md Mizanur Rahman Moghal ◽  
Sujit Chandra Mazumder ◽  
Dilshad Noor Lira ◽  
Abu Shara Shamsur Rouf

The main objective of the study was to formulate fast dissolving tablets of allopurinol to achieve better dissolution rate and further improving the bioavailability to provide a quick onset of action. Nine formulations of fast dissolving tablets of allopurinol were prepared by direct compression technique using croscarmellose sodium (Group A), sodium starch glycolate (Group B) and crospovidone (Group C) as superdisintegrants in different concentrations. All formulations showed satisfactory mechanical strength, uniform weight & drug content, and lesser wetting time & dispersion time. In vitro disintegration time, dispersion time, wetting time of all nine formulations were obtained from 11.67±0.88 to 40.67±1.20 seconds, 32.67±0.88 to 65.33±1.45 seconds and 21.67±0.33 to 50.00±1.53 seconds respectively. Amongst all formulations, formulation F-9 prepared by 4.17% crospovidone showed least disintegrating time of 11.67±0.88 seconds along with rapid drug release (98.88% within 15 minutes).Dhaka Univ. J. Pharm. Sci. 15(1): 73-81, 2016 (June)


Author(s):  
ANTHOSH KUMAR RADA ◽  
RAMYA M ◽  
SHAMBHAVI KANDUKURI

Objective: The main aim is to design, optimize, and evaluate ibuprofen fast-dissolving tablets by employing starch valerate-A novel super disintegrant. Methods: The fast-dissolving tablet of ibuprofen was prepared by employing starch valerate as super disintegrant in different proportions in each case by direct compression method using 23 factorial design, sodium starch glycolate, and crospovidone used as super disintegrants. In the 23 factorial design, these super disintegrants were applied to investigate the interaction effects of three variables, that is, (a) starch valerate, (b) sodium starch glycolate, and (c) crospovidone. The drug content, hardness, friability, disintegration time, and other dissolution characteristics were determined. Results: The starch valerate prepared was found to be fine, free-flowing, slightly crystalline powder. Starch xanthate exhibited good swelling in water with 125.2%. All the fast-dissolving tablets formulated employing starch valerate were of good quality with regard to drug content (100±5%), hardness (3.6–3.8 kg/sq. cm), and friability (0.11-0.12%). The disintegration time of all the formulated tablets was found to be in the range of 12±0.02 to 30±0.02s. The optimized formulation FL8 has the least disintegration time, that is, 12±0. 02s. The in vitro wetting time of the formulated tablets was found to be in the range of 21±0.09 to 44±0.10s. The in-vitro wetting time was less (i.e., 90s) in optimized formulation FL8. The water absorption ratio of the formulated tablets was found to be in the range of 30±0.12 to 100±0.09%. Conclusion: Starch valerate was found to be a super disintegrant which enhanced the dissolution efficiency when combined with sodium starch glycolate, crospovidone, with the ibuprofen.


Author(s):  
SANTOSH KUMAR R ◽  
ANNU KUMARI

Objective: The objective of the present research was to prepare starch phthalate (a novel superdisintegrant) and to optimize and formulate acyclovir fast dissolving tablets employing 23 factorial design using starch phthalate as superdisintegrant. Materials and Methods: Drug excipient compatibility studies such as Fourier-transform infrared spectroscopy, differential scanning calorimetry, and thin-layer chromatography were carried out to check the drug interaction between acyclovir and starch phthalate. The direct compression method was used for tablet preparation. Prepared tablets were then evaluated for hardness, friability, drug content, disintegration time, water absorption, and wetting time, in vitro dissolution studies. Response surface plots and contour plots were also plotted to know the main effects and interaction effects of independent variables (starch phthalate [A], croscarmellose sodium [B], and crospovidone [C] on dependent variables [disintegration time and drug dissolution efficiency in 1 min]) and stability studies were also done. Results: Tablets of all formulations were of good quality concerning drug content (100±5%), hardness (3.6–4.0 kg/cm2), and friability (<0.16%). In all formulations, formulation F8 found to be optimized formulation with least disintegration time 9±3 s, less wetting time 10±0.17 s, and enhanced dissolution rate in 1 min, i.e., 99.92±0.11 as compared to other formulation. Conclusion: From the research, it was concluded that on combination with crospovidone (5%) and croscarmellose sodium (5%), starch phthalate (10%) enhanced the dissolution efficiency of the drug. Hence, starch phthalate can be used as a novel disintegrant in the manufacturing of fast dissolving tablets.


Author(s):  
Subedi R. ◽  
Poudel K. ◽  
Budhathoki U ◽  
Thapa P.

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.


2018 ◽  
Vol 10 (6) ◽  
pp. 249
Author(s):  
Santosh Kumar Rada ◽  
T. Naga

Objective: To synthesize, characterize and evaluate starch xanthate as a superdisintegrant in the formulation of fast dissolving tablets by employing 23 factorial design.Methods: Starch xanthate was synthesized by gelatinization process. The physical and micromeritic properties were performed to evaluate the synthesized starch xanthate. The fast dissolving tablet of ibuprofen was prepared by employing starch xanthate as a superdisintegrant in different proportions in each case by direct compression method using 23 factorial design. The drug content, hardness, friability, disintegration time and other dissolution characteristics like percent dissolved in 5 min (PD5), dissolution efficiency in 5 min (DE5%) and first order rate constant (K1) were used in the evaluation of prepared fast dissolving tablets.Results: The starch xanthate prepared was found to be fine, free flowing slightly crystalline powder. Starch xanthate exhibited good swelling in water. The study between ibuprofen and starch xanthate was shown the absence of interaction by fourier transform infrared spectra (FTIR) and differential scanning calorimetry (DSC). The drug content (100±5%), hardness (3.6–4 kg/sq. cm), and friability (0.12-0.15%) has been effective with regard to all the formulated fast dissolving tablets employing starch xanthate. The disintegration time of all the formulated tablets was found to be in the range of 12±0.01 to 312±0.02s. The optimized formulation F5 has the least disintegration time i.e., 12±0.01s. The In vitro wetting time of the formulated 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., 90s) in optimized formulation F5. The water absorption ratio of the formulated tablets was found to be in the range of 16±0.16 to 174±0.21%. The cumulative drug dissolved in the optimized formulation F5 was found to be 99.83±0.56% in 5 min.Conclusion: The dissolution efficiency of ibuprofen was enhanced when starch xanthate was found to be a superdisintegrant when combined with sodium starch glycolate, croscarmellose sodium and, hence it could be used in the formulation of fast dissolving tablets to provide immediate release of the contained drug within 5 min.


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