Design And Development Of Fast Disintegrating Tablet Of Felodipine By Vacuum Drying Technique

Author(s):  
N. G. Rao ◽  
Upendra Kulkarni ◽  
Hari Prassanna C. ◽  
Basawaraj Patil ◽  
Rabbani G.

Felodipine which is used in the present study is a dihydropyridine derivative, that is chemically described as ethyl methyl-4-(2, 3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylate, widely accepted for its excellent antihypertensive and anti-anginal properties since it is calcium antagonist compound (calcium channel blocker). Felodipine is practically insoluble in water and its dissolution rate is limited by its physicochemical properties. In the present study fast disintegrating tablets of felodipine were prepared by adopting vacuum drying technique to study the effect of different subliming agents with various concentrations on disintegrating time. The powder blend was examined for the pre-compressional parameters. The prepared formulations were evaluated for post-compressional analysis for the parameters like hardness, friability, thickness, wetting time, water absorption ratio, weight variation, in-vitro disintegration time, in- vitro dispersion time, in-vitro dissolution study. Drug compatibility with excipients was checked by FTIR studies. The results obtained showed that quantity of ammonium bicarbonate, urea and menthol significantly affect the response variables (P> 0.05). No chemical interaction between drug and excipients was confirmed by FTIR studies. Stability studies carried out as per ICH guidelines for three months and results revealed that upon storage disintegration time of tablets decreased significantly (P> 0.05). The results concluded that fast disintegrating tablets of felodipine showing enhanced dissolution rate with increasing the concentrations of subliming agents. Among all the formulations A3 and M3 shows the improved dissolution rate which lead to improved bioavailability and effective therapy by using vacuum drying technique.

Author(s):  
SHEEBA F. R. ◽  
KUNDAN CHAUDHARY

Objective: In the present study, the effects of a natural superdisintegrant gellan gum, karya synthetic gum superdisintegrants like sodium starch glycolate, crospovidone and combination of natural and synthetic superdisintegrant were compared in the formulations of rizatriptan benzoate oral dispersible tablets. Methods: This oral dispersible tablets were prepared by direct compression method and evaluated for weight variation, hardness, disintegration time, drug content, friability and dissolution. Drug compatibility with excipients was checked by FTIR studies. Stability study of the prepared tablets was done at 40±2°/75%±5% RH for a period of 1 mo. Results: FTIR studies showed that no any chemical interaction between drugs and excipients. The in vitro drug release study revealed that formulation F9 combination of both crospovidone and karya gum was the most successful formulation and disintegrate time within 13 seconds and drug release within 10 min. The drug release from the best formulations followed first-order kinetics, which is concentration-dependent. Short terms stability studies of the tablet for three months showed non-significant drug loss. Conclusion: The formulation containing a combination of natural and synthetic superdisintegrant was found to be the best results. Apart from fulfilling all official and other specifications, the tablets exhibited a higher rate of drug release.


Author(s):  
Suresh Kulkarni ◽  
Ranjit P. ◽  
Nikunj Patel ◽  
Someshwara B. ◽  
Ramesh B. ◽  
...  

The present investigation deals with the formulation of fast disintegrating tablets of Meloxicam that disintegrate in the oral cavity upon contact with saliva and there by improve therapeutic efficacy. Meloxicam is a newer selective COX-1 inhibitor. The tablets were prepared by wet granulation procedure. The influence of superdisintegrants, crosspovidone, croscaremellose sodium on disintegration time, wetting time and water absorption ratio were studied. Tablets were evaluated for weight and thickness variation, disintegration time, drug content, in vitro dissolution, wetting time and water absorption ratio. The in vitro disintegration time of the best fast disintegrating tablets was found to be 18 sec. Tablets containing crospovidone exhibit quick disintegration time than tablets containing croscaremellose sodium. The fast disintegrating tablets of Meloxicam with shorter disintegration time, acceptable taste and sufficient hardness could be prepared using crospovidone and other excipients at optimum concentration.


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):  
Sarika S. Malode ◽  
Milind P. Wagh

The objective of present work was to develop taste masked orodispersible tablets of mirabegron. Mirabegron is beta 3 adrenoceptor agonist used to treat overactive bladder. Overactive bladder (OAB) is defined as a symptom syndrome showing feeling of urgency to urinate, typically accompanied by frequent daytime and nocturnal urination, in the absence of proven infection or other obvious pathology. Over active bladders are generally common in geriatrics. Moreover, this drug has a very strong bitter taste. Frequent dosing requires frequent water intake, which further aggregates the condition of over active bladder and bitter taste of drug affects patient compliance. Hence a need arises to mask the bitter taste for development of an ODT which does not require consuming water with every dosage. In this work, the bitter taste of mirabegron was masked by forming a complex with an ion exchange resin tulsion 344. The drug resin complexation process was optimized for resin activation, drug: resin ratio, soaking time and stirring time. In –vitro release studies revealed complete drug elution from the complex within 10 minutes in pH 1.2 buffer. The taste-masked complex was then formulated into palatable orodispersible tablets using a direct compression approach by use of superdisintegrants to achieve a rapid disintegration. The tablets were evaluated for weight variation, hardness, friability, drug content, wetting time, In- vivo disintegration time and in-vitro dissolution time.


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.


2017 ◽  
Vol 9 (6) ◽  
pp. 39
Author(s):  
Zainab E. Jassim

Objective: The purpose of this study was to enhance the dissolution pattern of the practically water-insoluble diuretic drug, furosemide through its formulation into liquisolid tablets.Methods: A mathematical model was used to formulate four liquisolid powder systems using polyethylene glycol 400 as a non-volatile water miscible liquid vehicle. The liquid loading factors of the vehicle were used to calculate the optimum quantities of carrier (Avicel PH 102) and coating materials (Aerosil 200) needed to prepare acceptably flowing and compactible powder mixtures and (R) ratio used was 25. The liquisolid tablets were evaluated for weight variation, percent friability, hardness, content uniformity, disintegration time and in vitro drug release profile. Drug and the prepared systems were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and powder x-ray diffraction (PXRD) studies.Results: The enhanced dissolution rate due to the increased wetting properties and the large available surface areas for dissolution were obtained in case of the liquisolid tablets. The selected optimal formulation (F2) of 50% drug concentration released 90% of its content during the first 10 min compared to 65% of DCT. FTIR studies revealed that there was no interaction between drug and polymers. DSC and PXRD indicated conversion of crystalline to amorphous form of furosemide. Conclusion: The dissolution rate of furosemide can be enhanced to a great extent by liquisolid technique.


2021 ◽  
Vol 11 (5) ◽  
pp. 115-120
Author(s):  
Kritika Rai ◽  
Vivek Jain ◽  
Sunil Kumar Jain ◽  
Pushpendra Kumar Khangar

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.


Author(s):  
Hemant A. Deokule ◽  
Smita S. Pimple ◽  
Praveen D. Chaudhari ◽  
Ajit S. Kulkarni

Fast dissolving strips are used as novel approaches, as it dissolves rapidly in mouth and directly reaches the systemic circulation. In present research work, an attempt has been made to prepare mouth dissolving strips of Metoclopramide hydrochloride by using a novel film former Pullulan by solvent casting method. A33 full factorial design was utilized for the optimization of the effect of independent variables such as the amount of Pullulan, amount of PEF 400, amount of SSG on mechanical properties, and % drug release of strips. The drug compatibility studies using FTIR and DSC studies formulated strips were characterized for their physicochemical parameter like weight variation, visual appearance, folding endurance, thickness, disintegration time, drug content, and in vitro dissolution studies. FTIR and DSC studies revealed that the polymer is compatible with the drug. It was found that the optimum levels of the responses for a fast release strip could be obtained at low levels of Pullulan, PEG400, and SSG. The prepared strip was clear transparent and had a smooth surface. The surface pH was found 4.8 to 5.2 be in the range of to which is close to salivary pH, which indicates that strips may have less potential to irritate the oral mucosa, thereby they are comfortable. The drug release was found to be between 90.94 to 100.5% in 2 min. The in-vitro disintegration time of strips prepared with Pullulan was in the range of 19 to 57 sec. As the concentration of SSG increases the decrease in the disintegration time of strips a decrease. The dissolution rate increased with an increase in the concentration of SSG. Hence, it can be inferred that the fast dissolving oral strips of Metoclopramide hydrochloride may produce rapid action thereby improving bioavailability and enhance the absorption by avoiding the first-pass effect.


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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