Formulation, Optimization and In Vitro Evaluation of Fast Disintegrating Tablets of Salbutamol Sulphate using a Combination of Superdisintegrant and Subliming Agent

2021 ◽  
Vol 18 ◽  
Author(s):  
Fikadu Ejeta ◽  
Tesfaye Gabriel ◽  
Nisha Mary Joseph ◽  
Anteneh Belete
Keyword(s):  
Research Work ◽  
Ammonium Bicarbonate ◽  
Optimal Point ◽  
Disintegration Time ◽  
Salbutamol Sulphate ◽  
Wetting Time ◽  
Predicted Values ◽  
Optimized Conditions ◽  
Fast Disintegrating Tablets

Aim: The present research work was aimed to formulate fast disintegrating tablets (FDTs) of salbutamol sulphate (SBS) using a combination of superdisintegrant and subliming agent, optimize the formulation and evaluate the in vitro performance of the developed FDTs. Materials and Methods: A formulation of SBS FDT was developed using a combination of superdisintegrant – crospovidone and subliming agent – ammonium bicarbonate (AB) in which formulation variables, namely levels of crospovidone and microcrystalline cellulose (MCC):Mannitol (MNTL) ratio were evaluated for their effects on the response variables - disintegration time, hardness, friability and wetting time of the resulting FDTs. By employing a central composite design (CCD) methodology, the FDTs were optimized to achieve optimum levels of the formulation factors. Results: The desired optimum condition was obtained at 7.82% crospovidone and 70% of 1.56:1 MCC: MNTL ratio while maintaining AB at 5% level for aesthetic reasons. Under the optimized conditions, the disintegration time, hardness, friability and wetting time were 14.57±0.53 sec, 7.17±0.82 kg/cm2, 0.311% and 13.14±0.69 sec, respectively. The experimentally observed responses were found to be in close agreement with the predicted values for the optimized formulation. Moreover, the validity of the obtained optimal point was confirmed by the low magnitude of percent prediction error (<5%). Conclusion: FDTs of SBS were successfully formulated and optimized using CCD employing a combination of superdisintegrant and subliming agents.

Formulation and Evaluation of Fast Disintigrating Meloxicam Tablets and Its Comparison with Marketed Product

2010 ◽  
Vol 2 (2) ◽  
Author(s):  
Suresh Kulkarni ◽  
Ranjit P. ◽  
Nikunj Patel ◽  
Someshwara B. ◽  
Ramesh B. ◽  
...  
Keyword(s):  
Water Absorption ◽  
In Vitro Dissolution ◽  
Thickness Variation ◽  
Wet Granulation ◽  
Disintegration Time ◽  
Absorption Ratio ◽  
Wetting Time ◽  
Fast Disintegrating Tablets ◽  
Cox 1

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.

scholarly journals FORMULATION AND EVALUATION OF FLURBIPROFEN FAST DISINTEGRATING TABLETS USING NATURAL SUPERDISINTEGRANTS

2016 ◽  
Vol 9 (6) ◽  
pp. 247 ◽  
Author(s):  
Mohammed Sarfaraz ◽  
Surendra Kumar Sharma
Keyword(s):  
Drug Release ◽  
Angle Of Repose ◽  
Lepidium Sativum ◽  
Disintegration Time ◽  
Natural Sources ◽  
Weight Variation ◽  
Wetting Time ◽  
Tapped Density ◽  
Fast Disintegrating Tablets

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.

scholarly journals FORMULATION DEVELOPMENT AND EVALUATION OF FAST DISINTEGRATING TABLETS OF CINITAPRIDE HYDROGEN TARTARATE BY USING DIRECT COMPRESSION TECHNIQUE

2017 ◽  
Vol 9 (6) ◽  
pp. 98 ◽  
Author(s):  
Krishna Mohan Chinnala ◽  
Sirish Vodithala
Keyword(s):  
Drug Release ◽  
Water Absorption ◽  
Bulk Density ◽  
Direct Compression ◽  
Disintegration Time ◽  
Absorption Ratio ◽  
Wetting Time ◽  
Tapped Density ◽  
Fast Disintegrating Tablets

Objective: In the present study, efforts were taken to develop fast disintegrating tablets of Cinitapride hydrogen tartrate, is a gastro-prokinetic agent and antiulcer agent with an objective to achieve rapid disintegration, and further improving the bioavailability of the drug. Also, to resolve the swallowing problems (Dysphasia) in pediatric, geriatric patients by rapid disintegration in saliva and improve the patient compliance.Methods: Fast disintegrating tablets were prepared by direct compression method using superdisintegrants like crospovidone (CP), croscarmellose sodium (CCS), sodium starch glycolate (SSG) and combination of super-disintegrants in different concentrations. The prepared formulations were evaluated for the pre-compression parameters like bulk density, tapped density, Carr’s compressibility, Hausner’s ratio and angle of repose. The prepared batches of fast disintegrating tablets of Cinitapride hydrogen tartarate were evaluated for hardness, weight variation, thickness, friability, drug content, disintegration time, wetting time, water absorption ratio, and in vitro dissolution profile.Results: Bulk density and tapped density were found in the range of 0.412–0.432 g/cc and 0.507–0.528 g/cc respectively. In all formulations, tablet weight and thickness were within mean±9.5% and mean±5% respectively. Wetting time values lie between 19.76 to 39.53 sec. Water absorption ratio ranged from 57.30 to 78.82 %. The in vitro disintegration time for all the 12 formulations varied from 17.43 to 38.61 seconds. Formulation F8 which contained crosspovidone have recorded drug release 96.94±0.47% at the end of 30 min.Conclusion: The formulation containing crospovidone (F8) showed better performance in terms of disintegration time and drug release when compared to other formulations.

scholarly journals Designing fabrication and evaluation of Oral fast Disintegrating tablet of Ranitidine HCL

2019 ◽  
Vol 9 (1) ◽  
pp. 95-102
Author(s):  
Afroza Akbar Patel ◽  
Siraj N Shaikh ◽  
Huzaifa Patel ◽  
Afzal Band ◽  
Ahmed Shaoor
Keyword(s):  
Drug Release ◽  
Optimization Technique ◽  
Research Work ◽  
Stability Study ◽  
In Vitro Dissolution ◽  
Compression Technique ◽  
Disintegration Time ◽  
Fenugreek Gum ◽  
Fast Disintegrating Tablets

The aim of this research work was to design develop & evaluate oral fast disintegrating tablets of Ranitidine HCL. The Orodispersible tablets of Ranitidine HCl were prepared by using direct Compression technique with a Synthetic Superdisintegrant such as Crosspovidone and a natural Superdisintegrant Fenugreek gum in different concentration. 32 factorial designs was applied to study the effect of independent variables,  concentration of Crosspovidone & Fenugreek gum on dependent variables like Cumulative % Drug release and Disintegration time by using design expert software. Prepared oral fast disintegrating tablets evaluated for Pre and Post-compression parameters. The prepared tablets exhibited satisfactory physico-chemical characterise especially fast disintegration & dissolution property. Full factorial design and optimization technique successfully used in the development oral fast disintegrating tablets. Comparing the all the formulations, formulation F9 was considered as optimized formulation which shows excellent fast disintegration, in vitro dissolution, and faster drug release within 6 min in comparison to other batches also stable in stability study. Keywords:  Fast disintegrating, Ranitidine, Crosspovidone, Gum, Optimizations, Water absorption ratio

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

2010 ◽  
Vol 2 (2) ◽  
Author(s):  
N. G. Rao ◽  
Upendra Kulkarni ◽  
Hari Prassanna C. ◽  
Basawaraj Patil ◽  
Rabbani G.
Keyword(s):  
Dissolution Rate ◽  
Chemical Interaction ◽  
Ammonium Bicarbonate ◽  
In Vitro Dissolution ◽  
Vacuum Drying ◽  
Disintegration Time ◽  
Ftir Studies ◽  
Weight Variation ◽  
Fast Disintegrating Tablets

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.

scholarly journals Effect of superdisintegrants on formulation of taste masked fast disintegrating Ciprofloxacin tablets

1970 ◽  
Vol 1 (4) ◽  
pp. 62-67
Author(s):  
Nilesh Jain ◽  
Sumain Mandal ◽  
Jitendra Banweer ◽  
Surendra Jain
Keyword(s):  
Drug Class ◽  
Pharmaceutical Journal ◽  
In Vitro Dissolution ◽  
Thickness Variation ◽  
Disintegration Time ◽  
Sodium Starch Glycolate ◽  
Wetting Time ◽  
In Vitro Disintegration ◽  
Fast Disintegrating Tablets

The present investigation deals with the formulation of taste masked fast disintegrating tablets of Ciprofloxacin that disintegrate in the oral cavity upon contact with saliva and thereby improve therapeutic efficacy. Ciprofloxacin is a synthetic chemotherapeutic antibiotic of the fluoroquinolone drug class. It is a second-generation fluoroquinolone antibacterial that kills bacteria by interfering with the enzymes that cause DNA to rewind after being copied, which stops synthesis of DNA and protein. It may also be used to prevent or slow anthrax after exposure. The influence of superdisintegrants, crospovidone and sodium starch glycolate on disintegration time, wetting time and water absorp-tion ratio were studied. Tablets were evaluation 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 disinte-gration tablets was found to be within 36 seconds. Tablets containing crospovidone (40%) exhibits quick disintegration time than tablets containing sodium starch glycolate. The fast disintegrating tablets of ciprofloxacin with shorter disintegration time, acceptable taste and sufficient hardness could be prepared using crospovidone and other excipients at optimum concentration.Key Words: ciprofloxacin; sodium starch glycolate; crospovidone; superdisintegrants; taste mask; fast disintegrating tablet.DOI: http://dx.doi.org/10.3329/icpj.v1i4.10059International Current Pharmaceutical Journal 2012, 1(4): 62-67

scholarly journals Formulation Development and Optimization of Fast Dissolving Tablets of Aceclofenac Using Natural Superdisintegrant

2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Lovleen Kaur ◽  
Rajni Bala ◽  
Neha Kanojia ◽  
Manju Nagpal ◽  
Gitika Arora Dhingra
Keyword(s):  
Drug Release ◽  
Research Work ◽  
Angle Of Repose ◽  
Lepidium Sativum ◽  
Formulation Development ◽  
Disintegration Time ◽  
Weight Variation ◽  
Two Factors ◽  
Wetting Time

The current research work involves preparation of fast dissolving tablets of Aceclofenac by direct compression method using different concentrations of Lepidium sativum mucilage as natural superdisintegrant. A two-factor three-level (32) factorial design is being used to optimize the formulation. Nine formulation batches (D1–D9) were prepared accordingly. Two factors as independent variables (X1-amount of β-cyclodextrin and X2-amount of Lepidium sativum mucilage) were taken with three levels (+1,0,-1). The levels of two factors were selected on the basis of preliminary experiments conducted and their effect on three dependent variables (disintegration time, wetting time, and in vitro drug release) was studied along with their % prediction error. All the active blends were evaluated for postcompression parameters (angle of repose, Carr’s index, Hausner ratio, etc.) and the tablets were evaluated for postcompression parameters (weight variation, hardness, and friability, wetting time, disintegration time, water absorption ratio, and in vitro drug release studies). The optimum batch was further used for SEM and stability studies. Formulation D5 was selected by the Design-Expert software which exhibited DT (15.5 sec), WT (18.94 sec), and in vitro drug release (100%) within 15 minutes.

Formulation and Evaluation of Orally Disintegrating Tablets of Lamotrigine

2015 ◽  
Vol 8 (2) ◽  
pp. 2881-2888
Author(s):  
Sudarshan Singh ◽  
S S Shyale ◽  
P Karade
Keyword(s):  
Drug Release ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Disintegration Time ◽  
Orally Disintegrating Tablet ◽  
Drug Content ◽  
Weight Variation ◽  
Wetting Time ◽  
Croscarmellose Sodium

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.

scholarly journals QUALITY BY DESIGN (QBD) AS A TOOL FOR THE OPTIMIZATION OF INDOMETHACIN FREEZE-DRIED SUBLINGUAL TABLETS: IN VITRO AND IN VIVO EVALUATION

2021 ◽  
pp. 160-171
Author(s):  
MERVAT SHAFIK IBRAHIM ◽  
NIHAL MOHAMED ELMAHDY ELSAYYAD ◽  
ABEER SALAMA ◽  
SHEREEN H. NOSHI
Keyword(s):  
Response Surface ◽  
Quality By Design ◽  
Drug Dissolution ◽  
Disintegration Time ◽  
Optimization Study ◽  
Freeze Dried ◽  
Screening Study ◽  
Wetting Time

Objective: This study aims to prepare and optimize indomethacin freeze-dried sublingual tablets (IND-FDST) by utilizing a quality by design (QbD) approach to achieve rapid drug dissolution and simultaneously bypassing the GIT for better patient tolerability. Methods: A screening study was utilized to determine the most significant factors which the quality attributes, namely disintegration time and % friability. Then an optimization study was conducted using a full response surface design to determine the optimized formula by varying the amount of the matrix-forming polymer (gelatin) and super disintegrant (croscarmellose sodium (CCS)). The variables' effect on the % friability, disintegration time, wetting time, and amount of drug release after 10 min (%Q10) was studied. The optimized formula was tested for compatibility, morphology as well as stability studies under accelerated conditions in addition to the in vivo pharmacodynamics in rats. QbD was adopted by utilizing a screening study to identify the significant formulation factors followed by a response surface optimization study to determine the optimized IND-FDST formulation. Results: Optimized IND-FDST comprised of gelatin/CCS combination in a ratio of 1:1 possessed adequate %friability (0.73±0.03%), disintegration time (25.40±1.21 seconds), wetting time (3.49±0.68 seconds), and % Q10 (100.99±5.29%) as well as good stability under accelerated conditions. IND-FDST also showed significant inhibition of edema, tumour necrosis factor-alpha, and interleukin-6 release in vivo compared to the oral market product by 70%, 42%, and 65%, respectively. Conclusion: QbD presents a successful approach in the optimization of a successful IND-FDST formula that showed superior in vivo and in vitro characteristics.

Fabrication and Evaluation of Mouth Dissolving Strips of Metoclopramide Hydrochloride by Using Novel Film Former

2021 ◽  
pp. 5515-5520
Author(s):  
Hemant A. Deokule ◽  
Smita S. Pimple ◽  
Praveen D. Chaudhari ◽  
Ajit S. Kulkarni
Keyword(s):  
Drug Release ◽  
Research Work ◽  
Systemic Circulation ◽  
In Vitro Dissolution ◽  
Disintegration Time ◽  
Visual Appearance ◽  
Dsc Studies ◽  
Weight Variation ◽  
Metoclopramide Hydrochloride

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.

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