scholarly journals Formulation and Evaluation of Mouth Dissolving Tablets Containing Losartan Potassium Using Natural Superdisinigrants

Author(s):  
Bhimi Kumari ◽  
Abhishek Soni ◽  
Shivali Singla ◽  
Sachin Goyal ◽  
Samriti Thakur ◽  
...  

Losartan potassium is used as an antihypertensive drug but it goes under first pass metabolism due do which it has low bioavailability. Fast onset of action is major concern in the management of hypertension. Therefore the aim of this study is to formulate mouth dissolving tablet of losartan potassium to improve its bioavailability, to achieve fast onset of action and increase patient compliance. Mouth dissolving tablets were prepared by direct compression method using natural super disintegrating agents (banana powder and apple pectin) and evaluated for pre-compression parameters and post compression parameters such as appearance, dimensions, hardness, weight variation, friability, wetting time, dispersion time, water absorption ratio, disintegration and dissolution study. According to results of optimized batches it has been concluded that formulation batch F9 was an ideal batch which contain banana powder (2.5%) and cross povidone (2.5%) showed least disintegration time that is 26 seconds and maximum drug release of (99.68%) within 12 minutes and was best among all the formulations.

Author(s):  
RezaSunidhi Mahant ◽  
Shivali Singla ◽  
Sachin Goyal ◽  
Bhimi Kumari ◽  
Abhishek Soni

Mouth dissolving tablet is an innovative solid unit dosage form that overcome the problem of swallowing and provide rapid disintegration and dissolution to release the drug as soon as they come in contact with saliva, hence provide quick onset action. The aim of this study was to formulate and evaluate mouth dissolving tablets of Ondansetron hydrochloride using natural super disintegrating agent. Ondansetron hydrochloride is a serotonin receptor (5-HT3) antagonist used to treat nausea and vomiting arises during chemotherapy and radiation therapy. Mouth dissolving tablets were prepared by direct compression method using natural super disintegrating agent (Plantago ovata mucilage). Prepared tablet were evaluated for Hardness, weight variation, friability, thickness, wetting time, dispersion time, water absorption ratio, disintegration and dissolution study. According to results of optimized batches it has been concluded that Formulation batch F6 was an ideal batch which contain 12% w/v concentration of Plantago ovata mucilage showed least disintegration time that is 7 seconds and maximum drug release of (98.57%) within 15 minutes and was best among all the formulations.


2015 ◽  
Vol 1 (1) ◽  
pp. 51
Author(s):  
Prasanna Kumar Desu ◽  
Brahmaiah Bonthagarala ◽  
Pasam Venkateswara Rao

The study was carried to formulate and evaluate dispersible tablet dosage form obtaining Nateglinide.Nateglinideis adrugfor the treatment oftype 2 diabetes. The present study is an attempt to select best possible combination of diluents and disintegrates to formulate dispersible tablet of Nateglinide which disintegrates within few minutes thereby reducing the time of onset of action. Mannitol is selected as diluents, Sodium starch glycol ate, Cross-povidone, cross-carmellose sodium were selected as super disintegrates, citric acid and sodium bi carbonate is effervescent active ingredient in different concentrations. Aspartame as a sweetening agent, Magnesiumstearate as a Lubricant and glidant.Direct Compression method was used to formulate the tablets.All the formulations were showed the acceptable flow properties and the pre-compression parameters like Bulk density, Tapped density and Hausner ratio. The post compression parameters like Hardness, Friability, Disintegration time, Weight variation, wetting time, Dispersion time values were found to be within the IP limits.The percentage Drug content of all tablets was found to be between 99% - 100 % of Nateglinide, which is within the limit.As the concentrations of the Citric acid (preservative) & sodium bicarbonate (active ingredient respectively taking increases in the formulations F7 F9 the disintegration time found to be decreased and the disintegration time for these formulations were 33, 31, 30 seconds respectively and the percentage drug release was also found to be increased for these formulations as 94 ,96, and 99 % respectively. From the above results it was found that as the concentration of citric acid decreased and sodium bi carbonate increases the disintegration and dissolution time was found to be improved, so considering the above results it was found that the F9 batch was found to be optimized batch and it pass all the pre-formulation parameters and evaluation results as per the IP limits.


Author(s):  
RAJNI BALA ◽  
SHAILESH SHARMA ◽  
IKGPTU

Objective: The present study was aimed to formulate fast dissolving tablets (FDTs) of Aprepitant (APT) using natural and synthetic superdisintegrants with the desired onset of action, increased bioavailability by reducing the frequency of dosage and also reduce the first-pass metabolism of the drug. Methods: In this research, the gum isolated from cordia dichotoma was investigated as super disintegrants in fast dissolving tablets (FDTs). The aprepitant tablets were prepared separately using cordia dichotoma (natural), sodium starch glycolate and croscarmellose sodium (synthetic) as superdisintegrants by direct compression method. The tablets were evaluated for various precompression and post-compression parameters. Results: The optimized formulation (APT F3) of cordia dichotoma (8%) showed satisfactory physicochemical properties, minimum disintegration time (34 seconds) and highest dissolution rate (86.52%) in 10 min than the other synthetic superdisintegrants. Also, the pharmacokinetic study of the optimized formulation showed effective results as compared with marketed product of aprepitant. Conclusion: The developed formulation can improve the onset of action as well as improve patient compliance.


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):  
Puttaswamy Nirmala

Ramipril being ACE inhibitor belongs to BCS class II drug with low solubility and undergoes first-pass metabolism that leads to reduced bioavailability of 28%. The current research is aimed at formulating and evaluating ramipril fast dissolving oral films (FDOF). Solubility enhancement of ramipril was done by formation of   inclusion complex with β-cyclodextrin in 3 ratios (1:0.5, 1:1, 1:2). Based on higher drug content and dissolution values the physical mixture of ramipril with β-cyclodextrin in 1:1 ratio (IC2) was chosen for further studies. Total 12 formulations of ramipril FDOF containing IC2 prepared with various polymers and evaluated for physicochemical properties. The optimized formulation F9 shown better tensile strength (11.6 g/cm2), significant % elongation (9.8) and maximum % drug content of 99.98 %. The formulation F9 exhibited minimum disintegration time of 9 sec that is desirable for immediate onset of action and maximum drug release. The FTIR data of F9 assured the compatibility of drug and formulation excipients, found to be stable for 180 days at accelerated conditions. The study confirmed that ramipril FDOF lead to quicker onset of action and enhanced therapeutic efficiency in comparison to marketed product.


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):  
Mohammed Sarfaraz ◽  
Surendra Kumar Sharma

ABSTRACTObjective: The main objective of this research was to formulate Fast disintegrating tablets of Flurbiprofen incorporating superdisintegrants, isolated from natural sources like Plantago ovata (PO) seeds, Lepidium sativum (LS) seeds and agar-agar.Methods: Superdisintegrants were isolated from their natural sources using reported methods. Swelling index and hydration capacity was determined for the natural superdisintegrants to know their disintegration capacity. The tablet formulations were designed using isolated natural superdisintegrants. The powder blends were evaluated for pre-compressional parameters like angle of repose, bulk density, tapped density, carr’s index, and hausner’s ratio. Fast disintegrating tablets were prepared by direct compression method. The compressed tablets were characterized for post compression parameters.Results: All formulations had hardness, friability, weight variation and drug content within the pharmacopoeial limits. The wetting time was 84 to 254 sec, in vitro disintegration time was between 59.2 to 221 sec, and in-vitro drug release was as low as 11.80% (LS1) to a maximum of 98.99% (PO4) after 4 min of study. Among all, optimized formulation was PO4, as it showed good wetting time (84 sec), fastest disintegration time (59.2 sec), dispersion time (135 sec) and drug release of 98.99.% within 4 min.Conclusion: Flurbiprofen FDT’s were successfully developed using isolated natural disintegrants. The natural disintegrants isolated showed promising results and can prove as effective alternative for synthetic disintegrants.


Author(s):  
Rupalben K. Jani ◽  
Gohil Krupa ◽  
Aanal Gandhi ◽  
Vijay Upadhye ◽  
Roshani Pragnesh Amin

The foremost objective of this research was to compare and evaluate natural super disintegrants with synthetic super disintegrants for the preparation of the orodispersible tablet. Tropisetron hydrochloride is widely used as an antiemetic drug, which is a potential drug candidate for developing an orodispersible tablet for quick onset of action. Various formulations were prepared using different concentrations (5%, 7.5%, and 10%) by direct compression method of natural super disintegrants (Banana power and Cassia tora powder) and synthetic super disintegrants (Croscarmellose sodium, Crospovidone, and Sodium starch glycolate). The compatibility studies between the drug and excipients were carried out using FTIR spectroscopy before tablet formulation. The pre-compression parameters were evaluated for additive properties. Standardization of banana powder was done by various parameters like extractive value, ash value, loss on drying, TLC identification test, etc. Post-compression parameters like hardness, weight variation, friability, thickness, the time required for disintegration, wetting time, the release of drug in-vitro, and in-vitro dispersion time of the tablets were evaluated. The disintegration time and in-vitro drug release of optimized formulation (F2) were found to be 4.66±1.15 secs and 99.25±0.15%. The optimized formulation (F2) was subjected to stability studies (40 C& 75 % RH) for one month. The results were shown that natural super disintegrants require less disintegration time as compared to synthetic super disintegrants. Hence present study reveals that the orodispersible tablets prepared using Banana powder and Cassia tora powder is super disintegrants that shown better appearance and rapid disintegration time.


2021 ◽  
Vol 10 (1) ◽  
pp. 59-67
Author(s):  
Mahipal Shakkarwal ◽  
Dr. Mukesh Sharma ◽  
Dr. Ram Garg ◽  
Shankar Lal Soni ◽  
Gopal Kumar Paswan ◽  
...  

The demands for fast dissolving tablets have received ever increasing day by day during the last 10-15 years for the onset of action. In the present study, the effect of superdisintegrant was compared with synthetic super disintegrants and other conventional super disintegrants in the of fast dissolving tablet formulation of Meclofenamate. Meclofenamate is an antihypertensive drug and in case of hypertension immediate treatment is required so the proposed investigation is totally based to provide the suitable treatment for hypertension. In the present work 9 formulations of Fast dissolving tablets of Cilnidipine were prepared by using Synthesized Co-proceed was evaluated and compiles with the official standards, parameters and specifications. Various formulations were prepared using four different superdisintegrant namely- kyron T-304, sodium starch glycolate, cross carmelose sodium with three concentrations (2%, 4%, 6%) by direct compression method. The blend was evaluated for pre-compression parameters like Angle of repose , bulk density , tapped density , and then tablet  evaluated post-compression parameters like thickness , drug content , hardness , weight variation  , wetting time , friability , disintegration time , dissolution time, drug release study. Formulation A8 showed the lowest disintegration time and in-vitro dissolution studies recorded that formulation A8 showed 98.64% drug release at the end of 3 minutes. The best formulations were also found to be stable and optimized formulations were subjected to the stability studies as per ICH guideline and standards.


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


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