scholarly journals Formulation and Optimization of Zolmitriptan Orodispersible Tablets

2021 ◽  
Vol 11 (3) ◽  
pp. 50-57
Author(s):  
T.V. Hari Hara Nadh ◽  
P. Sivaram Kumar ◽  
M. Venkata Ramana ◽  
N. Rama Rao
Keyword(s):  
Drug Release ◽  
Microwave Irradiation ◽  
Solid Dispersion ◽  
Water Solubility ◽  
Migraine Treatment ◽  
Disintegration Time ◽  
Independent Variables ◽  
Dsc Studies ◽  
Orodispersible Tablets ◽  
Croscarmellose Sodium

Zolmitriptan is a selective 5-hydroxytryptamine receptor agonist reported for the acute migraine treatment, having poor water solubility leads to poor bioavailability. In the present study, attempt to improve the bioavailability of zolmitriptan with the help of PVP K-30 using the microwave irradiation method.  The zolmitriptan and PVP K- 30 in 1:1 ratio was subjected to microwave irradiation for different times such as 60,80,100,120 seconds at 650 watts. Characterization of solid dispersion was done by drug content, XRD, FTIR, DSC. FTIR analysis demonstrated there are no compatibility issues. XRD studies prove that the solid dispersion was in amorphous form. DSC studies prove that solid dispersion was amorphous based on the intensity of peaks. The prepared dispersion was made into orodispersible tablets by direct compression. The optimization of these formulations was carried out by using 32 factorial designs on Design Expert 10.0 software. In order to examine the effect of independent variables Crospovidone (X1), croscarmellose sodium (X2), and combined effect of independent variables 32 factorial design was selected. In this design, two responses such as disintegration time and % drug release were evaluated, and experimental trials are performed for all 9 formulations. For all formulations, the precompression and post-compression parameters were studied. Based upon the model optimized formulation (C1 and C2) was obtained having the disintegration time (34.4±0.84 and 39.8±0.91) and %drug release (98.7±0.42 and 93.2±0.46) respectively. Keywords: Zolmitriptan, Solid dispersion, Microwave irradiation, Crospovidone, Croscarmellose sodium.

scholarly journals Formulation and Optimization of Orodispersible Tablet of Loratadine Using Box Behnken Design

2019 ◽  
Vol 9 (4-A) ◽  
pp. 86-94
Author(s):  
Aliasgar Kundawala ◽  
Pratik Patel ◽  
Khushbu Chauhan ◽  
Anjali Desai ◽  
Dhwani Kapadia
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Angle Of Repose ◽  
Drug Dissolution ◽  
Taste Masking ◽  
Disintegration Time ◽  
Box Behnken Design ◽  
Orodispersible Tablets ◽  
Orodispersible Tablet ◽  
Wetting Time

In present study Orodispersible tablets (ORDT) of Loratadine were prepared and optimized. Solid dispersion of Loratadine- β cyclodextrin complex were prepared and used in preparation of Orodispersible tablets. Various super-disintegrating agent like Cross carmellose sodium, Cross povidone and Kyron T-314 were employed for faster disintegrating effect. The 24 factorial and Box-Behnken design were utilized to optimize the tablet formulation. The Orodispersible tablet of Loratadine was optimized by Box Behnken Design, where concentrations Kyron T-314, CRP and Pearlitol SD200 were employed and its effect on Disintegration time (DT), Wetting time (WT) and % drug release at 20 min (Q20) was evaluated. Precompression parameters like angle of repose, bulk density, % compressibility, Hausner’s ratio was studies. The different batches of Orodispersable tablets were prepared and evaluated for disintegration time, friability, wetting time and drug release studies. Different batches prepared showed disintegration time in the range of 23 ± 2.52 to 59 ± 2.64, wetting time in between 27± 0.57 to 66.3 ± 3.4, drug release (Q 20) in between 86.1 ± 0.6 to 96.7 ± 0.4 in 20 min., friability less than 1 % and hardness 3.4 to 4.2 Kg/cm2. The optimized formula when compared with marketed product it showed faster disintegration time and rapid drug dissolution in phosphate buffer 6.8. The solid dispersion of Loratadine not only helped improve in solubility but may also help in taste masking. Keywords: Orodispersible tablets, Loratadine, β cyclodextrin Solid dispersion

scholarly journals FORMULATION AND EVALUATION OF ORODISPERSIBLE TABLETS OF A MODEL ANTI-HYPERTENSIVE DRUG

2017 ◽  
Vol 9 (10) ◽  
pp. 34
Author(s):  
S. P. Hiremath ◽  
Chidambar Makanapur
Keyword(s):  
Drug Release ◽  
Dissolution Time ◽  
Direct Compression ◽  
Compression Technique ◽  
Disintegration Time ◽  
Drug Content ◽  
Orodispersible Tablets ◽  
Time Dispersion ◽  
Wetting Time ◽  
Croscarmellose Sodium

Objective: The rationale of the current work was to formulate and evaluate orodispersible tablets by direct compression technique with a vision to augment patient compliance and rapid onset of action.Methods: Nine orodispersible formulations of propranolol were formulated by direct compression method using sodium starch glycolate, crospovidone and croscarmellose sodium as the super disintegrants. The prepared formulations were evaluated for wetting time, drug content, in vitro disintegration time, dispersion time, dissolution time and also projected to kinetic treatment to know the pattern of drug release. Further, the discovered promising formulation was subjected to stability studies.Results: Based on the results obtained, formulation F9 containing6 mg of croscarmellose sodium exhibited good wetting time, dispersion time, and disintegration time and drug release compared to orodispersible tablets prepared with other super disintegrants. The stability studies piloted as per International Conference on Harmonisation guidelines on the promising formulationF9disclosedno significant changes in the colour (white), drug content (94.87±0.141 mg), hardness (2.93±0.18 kg/cm2), disintegration time (17.11±0.089 s), and drug release after 4 w. After 60 s, the percentage drug release of F9 was found to be 98.52 % and 96.30 % after 1 and 4 w, respectively.Conclusion: Orodispersible tablets of propranolol hydrochloride were formulated successfully by employing direct compression technique. From the investigation, it can be reasonably concluded that F9 batch orodispersible tablets of propranolol with 6 mg of crospovidone exhibited maximum cumulative drug release in 60 s.

scholarly journals Research Paper DESIGN, OPTIMIZATION AND EVALUATION OF EMPAGLIFLOZIN ORODISPERSIBLE TABLETS USING DIFFERENT SUPERDISINTEGRANTS

2019 ◽  
pp. 32-41
Author(s):  
AKANKSHA DWIVEDI ◽  
G. N. DARWHEKAR
Keyword(s):  
Drug Release ◽  
Rapid Onset ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Orodispersible Tablets ◽  
Dependent Variables ◽  
Tablet Properties ◽  
Croscarmellose Sodium ◽  
Experimental Trials ◽  
Different Levels

Objective: The objective of this study was to formulate orodispersible tablets containing empagliflozin by direct compression method with sufficient hardness and rapid disintegration time and to study the effect of functionality differences of super-disintegrants on the tablet properties. Methods: A two factor three level factorial design (32) was used for the formulation optimization of orodispersible tablets of Empagliflozin and experimental trials were performed on all possible formulations, in which the amount of β-cyclodextrin, crospovidone and croscarmellose sodium were selected as independent variables (factor) varied at three different levels: low (-1), medium (0), and high (+1) levels. The drug release and disintegration time were used as dependent variables (response). All formulations were characterized for parameters such as diameter, hardness, weight, thickness, friability, disintegration time, drug release. Results: Formulation FD6 having 30 sec disintegration time, 98.84% drug release after 30 min, 2.8 kg/cm2 hardness and 0.292% friability was found best among all formulations and selected as an optimized formulation with rapid onset of action and enhanced bioavailability (more than 98% drug release within 30 min.) as compared to the oral empagliflozin tablet. Conclusion: Empagliflozin orodispersible tablets with different superdisintegrants were successfully prepared and formulation containing highest percentage of crospovidone was found best among all other formulations in terms of bioavailability and rapid onset of action.

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.

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.

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 Development and Optimization of Osmotically Controlled Asymmetric Membrane Capsules for Delivery of Solid Dispersion of Lycopene

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Nitin Jain ◽  
Rashmi Sareen ◽  
Neeraj Mahindroo ◽  
K. L. Dhar
Keyword(s):  
Drug Release ◽  
Osmotic Pressure ◽  
Correlation Coefficient ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Dip Coating ◽  
Asymmetric Membrane ◽  
Independent Variables ◽  
Coating Method ◽  
Dip Coating Method

The aim of the present investigation is to develop and statistically optimize the osmotically controlled asymmetric membrane capsules of solid dispersion of lycopene. Solid dispersions of lycopene withβ-cyclodextrin in different ratios were prepared using solvent evaporation method. Solubility studies showed that the solid dispersion with 1 : 5 (lycopene : β-cyclodextrin) exhibited optimum solubility (56.25 mg/mL) for osmotic controlled delivery. Asymmetric membrane capsules (AMCs) were prepared on glass mold pins via dip coating method. Membrane characterization by scanning electron microscopy showed inner porous region and outer dense region. Central composite design response surface methodology was applied for the optimization of AMCs. The independent variables were ethyl cellulose (X1), glycerol (X2), and NaCl (X3) which were varied at different levels to analyze the effect on dependent variables (percentage of cumulative drug release (Y1) and correlation coefficient of drug release (Y2)). The effect of independent variables on the response was significantly influential. The F18was selected as optimized formulation based on percentage of CDR (cumulative drug release) of 85.63% and correlation coefficient of 0.9994. The optimized formulation was subjected to analyze the effect of osmotic pressure and agitational intensity on percentage of CDR. The drug release was independent of agitational intensity but was dependent on osmotic pressure of dissolution medium.

scholarly journals Application of optimization tools for preparation of nebivolol liquid solid composite compressed tablet

2021 ◽  
Vol 12 (3) ◽  
pp. 1967-1976
Author(s):  
Kumar Babu P ◽  
Venkatachalam A ◽  
Bhaskar Reddy K
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Factorial Design ◽  
Dissolution Rate ◽  
Disintegration Time ◽  
Independent Variables ◽  
23 Factorial Design ◽  
Sustained Release Tablet ◽  
Wetting Time ◽  
Solid Liquid

The purpose of this study is to make Nebivolol more efficient by converting it into a liquid solid composite compressed tablet. Blending cum sonication process was used to create the liquid solid composite. By altering the independent variables such as vehicle, carrier, and superdisintegrants, nearly 12 compositions were created in a 23 factorial design with four centre points. The influence on response, such as disintegration time in seconds and wetting time in seconds, was then determined. In addition, the liquid solid composite was compacted into a tablet and its percent invitro drug release was assessed. Based on disintegration time and wetting time, the optimal solid liquid compacts sustained release tablet formulation was identified to be LSC6 , which may be ideal candidates for boosting the solubility and dissolution rate of less soluble medications like Nebivolol.

scholarly journals FORMULATION, OPTIMIZATIONANDEVALUATION OF SUBLINGUAL FILM OF ENALAPRILMALEATE USING 32 FULL FACTORIAL DESIGN

2021 ◽  
pp. 178-186
Author(s):  
SATYAJIT SAHOO ◽  
KIRTI MALVIYA ◽  
AMI MAKWANA ◽  
PRASANTA KUMAR MOHAPATRA ◽  
ASITRANJAN SAHU
Keyword(s):  
Tensile Strength ◽  
Drug Release ◽  
Factorial Design ◽  
Full Factorial Design ◽  
Disintegration Time ◽  
Surface Ph ◽  
Independent Variables ◽  
Folding Endurance ◽  
Full Factorial ◽  
32 Full Factorial Design

Objective: The purpose of this investigation was to formulate, optimize and evaluate sublingual film of Enalapril maleate for rapid management of Hypertension. Methods: Sublingual films were prepared by solvent casting method. Present investigation were formulated by using HPMC E 15 (X1) as polymer and Polyethylene glycol (X2) as plasticizer were chosen as independent variables in 32 full factorial design while Tensile strength (TS), Disintegration time (DT) and % Cumulative drug release at 10 min. (% CDR) were taken as dependent variables. The various physical parameters were evaluated for sublingual films such as thickness, tensile strength, folding endurance, disintegration time, surface pH and % CDR. Results: From the experimental study, it was concluded that the optimized batch F8 showed 98.6 %, the highest release of the drug. Stability study was performed by taking an optimized formulation and it was observed stable. The sublingual films showed acceptable results in all studies such as thickness, tensile strength, folding endurance, disintegration time, surface pH and % CDR at 10 min. R2 values for Tensile Strength (Y1), Disintegration time (Y2) and % cumulative drug release at 10 min. of Enalaprilmaleate(Y3) found to be 0.9852, 0.9829 and 0.9641 respectively. Thus, a good correlation between dependent and independent variables was developed. Conclusion: 32 full factorial design was successfully applied during preparation, optimization and evaluation of sublingual films of Enalapril maleate. The present investigation showed quick disintegration and fast release of the drug for rapid management of Hypertension.

scholarly journals Formulation and in vitro evaluation of orodispersible tablets of fexofenadine hydrochloride

2020 ◽  
Vol 19 (5) ◽  
pp. 919-925
Author(s):  
Durgaramani Sivadasan ◽  
Muhammad Hadi Sultan ◽  
Osama Madkhali ◽  
Shamama Javed ◽  
Aamena Jabeen
Keyword(s):  
Guar Gum ◽  
Polymer Concentration ◽  
In Vitro Release ◽  
Direct Compression ◽  
Compression Technique ◽  
Disintegration Time ◽  
Weight Fluctuation ◽  
Orodispersible Tablets ◽  
Croscarmellose Sodium

Purpose: To develop orodispersible tablets (ODTs) of fexofenadine hydrochloride using three different superdisintegrants in various ratios and to compare their disintegration properties.Methods: Direct compression technique was used for the preparation of ODTs. Mannitol and Avicel CE-15 (microcrystalline cellulose and guar gum) were used as direct compression diluents. The disintegration time of tablets using each polymer (superdisintegrant) was evaluated as well as othertablet properties including weight fluctuation, hardness, friability, wetting time and water absorption ratio.Results: Satisfactory values were obtained for all the evaluated parameters. As the polymer concentration increased, there was a decrease in disintegration time. A comparison of the three different polymers used revealed that CCM3 formulated with 12 % croscarmellose sodium and 14.66 % lactose had the least disintegration time of 32.33 ± 3.23 s. In vitro release studies showed that the maximum drug release of 94.38 ± 0.12 % in 25 min was obtained for ODT tablets containing croscarmellose sodium (CCM3).Conclusion: The orodispersible tablets had quick disintegrating property which was achieved using superdisintegrants. Thus, superdisintegrants improve the disintegration efficiency of orodispersible fexofenadine tablets at low concentrations, when compared to traditional disintegrants. Keywords: Croscarmellose sodium, Direct compression, Fexofenadine, Orodispersible tablets

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