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

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.

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):  
Dr. Dilip Agrawal ◽  
Dr. Rakesh Goyal ◽  
Dr. Mukesh Bansal ◽  
Ashok Kumar Sharma ◽  
Mohit Khandelwal

The demands for fast dissolving tablets have received ever increasing day by day during the last decade. In the present projected study, the effect of natural Super disintegrants was compared with synthetic Super disintegrants and conventional Super disintegrants in the of fast dissolving tablet formulation of Meclofenamate Sodium. Meclofenamate sodium NSAID is used for the treatment of mild to moderate pain in various conditions like (e.g., dental pain, osteoarthritis) and to decrease pain and blood loss during menstrual periods. It is also used for other treatments like reducing pain, swelling, and joint stiffness caused with rheumatoid arthritis. In the present work 9 formulations of FDT (Fast dissolving tablet) of Meclofenamate Sodium were prepared by using Super disintegrants was evaluated and compiles with the official parameters and specifications. Various formulations were prepared using four different super disintegrants namely natural super disintegrant Banana Powder, sodium starch glycolate, crosscarmelose 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 with various post-compression parameters like thickness, drug content, hardness, weight variation, wetting time, friability, disintegration time, dissolution time, drug release study. Formulation F2 showed the lowest disintegration time and in-vitro dissolution studies recorded that formulation F2 showed 98.55% drug release at the end of 3 minutes. The best formulations among these were also found to be stable and optimized formulations were subjected to the stability studies as per ICH guideline.


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):  
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


Author(s):  
MEGHANA RAYKAR ◽  
MALARKODI VELRAJ

Objective: This study aims to Formulate Mouth Dissolving Tablets (MDTs) of Tofacitinib Citrate with the increase in bioavailability and patient compliance. Methods: Mouth Dissolving Tablets (MDTs) of Tofacitinib Citrate were developed by full factorial design at 32levelsand prepared by direct compression method using super integrants like sodium starch glycolate, Ludiflash. The tablets were compressed into compacts on a 10 station tablet machine. The bulk drug was characterised by determining, MP, Solubility, pH and FTIR spectra. Results: The weight variation, hardness and diameter, thickness, friability, drug content, wetting time, in vitro disintegration time and in vitro dissolution studies, and stability study, tablet thickness, weight variation and drug content post compression parameters remained consistent and reproducible. All the formulations showed, almost 100 percent of drug release within 75 min. Formulations F1, F2 and F3 were prepared with 5 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F1<F2<F3. Formulations F4, F5 and F6 were prepared with 10 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F4<F5<F6. Formulations F7, F8 and F9 were prepared with 15 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F7<F8<F9. Conclusion: It is concluded that the amount of superdisintegrants decreases disintegration time of tablets, decreases wetting time, increases the cumulative % drug release causes better absorption.


2013 ◽  
Vol 2 (10) ◽  
pp. 165-169 ◽  
Author(s):  
Manivannan Rangasamy ◽  
Venkata Krishna Reddy Palnati ◽  
Lakshmi Narayana Rao Bandaru

The present study involves in the formulation and evaluation of sustained release tablets of Voriconazole (250mg). The objective of the present study was to formulate Voriconazole sustained release tablets by wet granulation method by using natural (Xanthan gum, Karaya gum) and semi synthetic polymers (HPMC K100M). Lactose was used as diluting agent, Magnesium stearate was used as a lubricant and Talc was used as a glident. These sustained release tablets can release the drug up to 12 hours in predetermined rate. The formulated powder blend was evaluated for bulk density, tapped density, compressibility index and angle of repose. The formulated tablets were evaluated for physical characteristics of sustained release tablets such as thickness, hardness, friability, weight variation and drug content. The results of the formulations found to be within the limits specified in official books. The tablets were evaluated for In-vitro drug release studies by using USP type I dissolution test apparatus. The dissolution test was performed in 0.1 N HCL for 2 hr and phosphate buffer pH 6.8 for 10hrs. The in-vitro cumulative drug release profile of all formulations F1-F10 at 12 hours showed 84.25% to 99.82% drug release, respectively. From the data it was clear that by increasing the amount of polymer in the formulation the amount of drug release was decreased. Hence, Formulation F9 was the most promising formulation as it gives satisfactory release (99.82%) for 12 hours and F9 found to be the best formulation.DOI: http://dx.doi.org/10.3329/icpj.v2i10.16410 International Current Pharmaceutical Journal, September 2013, 2(10): 165-169


1970 ◽  
Vol 2 (2) ◽  
pp. 59-65
Author(s):  
Abu Kalam Lutful Kabir ◽  
Shaikh Mukidur Rahman ◽  
Md Arshad Jahan ◽  
Abu Shara Shamsur Rouf

Difficulty in swallowing (dysphagia) is common among all age groups, especially in elderly and pediatrics. Mouth dissolving tablets constitute an innovative dosage forms that overcome the problems of swallowing and provides a quick onset of action. The purpose of this study was to formulate and evaluate mouth dissolving tablet of loratadine using a special preparation technology (pharmaburst Technology) with a super disintegrating agent (Croscarmellose sodium). Tablets were prepared by direct compression technique. The granules were evaluated for angle of repose, bulk density, tapped density, bulkiness, compressibility index and hausners ratio. The tablets were evaluated for hardness, thickness, uniformity of weight, friability, wetting time, water absorption ratio, disintegration time and drug content. In vitro release studies were performed using USP-II (paddle method) in 900ml of pH 1.2 at 50rpm. The physical properties of the prepared tablets did not show any significant variations and were found to have good physical integrity. Tablets prepared with pharmaburst B2 and Croscarmellose sodium showed a lesser disintegration time and wetting time of 27±0.10 and 38±0.13 seconds respectively. The best formulations were subjected to stability studies at 40ºC/75% RH for 60 days. Key words: Loratadine; pharmaburst B2; croscarmellose sodium; mouth dissolving tablets; direct compression.DOI: 10.3329/sjps.v2i2.5825Stamford Journal of Pharmaceutical Sciences Vol.2(2) 2009: 59-65


2014 ◽  
Vol 50 (4) ◽  
pp. 799-818 ◽  
Author(s):  
Tariq Ali ◽  
Muhammad Harris Shoaib ◽  
Rabia Ismail Yousuf ◽  
Sabahat Jabeen ◽  
Iyad Naeem Muhammad ◽  
...  

The aim of the present study was to develop tizanidine controlled release matrix. Formulations were designed using central composite method with the help of design expert version 7.0 software. Avicel pH 101 in the range of 14-50% was used as a filler, while HPMC K4M and K100M in the range of 25-55%, Ethylcellulose 10 ST and 10FP in the range of 15 - 45% and Kollidon SR in the range of 25-60% were used as controlled release agents in designing different formulations. Various physical parameters including powder flow for blends and weight variation, thickness, hardness, friability, disintegration time and in-vitro release were tested for tablets. Assay of tablets were also performed as specified in USP 35 NF 32. Physical parameters of both powder blend and compressed tablets such as compressibility index, angle of repose, weight variation, thickness, hardness, friability, disintegration time and assay were evaluated and found to be satisfactory for formulations K4M2, K4M3, K4M9, K100M2, K100M3, K100M9, E10FP2, E10FP9, KSR2, KSR3 & KSR9. In vitro dissolution study was conducted in 900 ml of 0.1N HCl, phosphate buffer pH 4.5 and 6.8 medium using USP Apparatus II. In vitro release profiles indicated that formulations prepared with Ethocel 10 standard were unable to control the release of drug while formulations K4M2, K100M9, E10FP2 & KSR2 having polymer content ranging from 40-55% showed a controlled drug release pattern in the above mentioned medium. Zero-order drug release kinetics was observed for formulations K4M2, K100M9, E10FP2 & KSR2. Similarity test (f2) results for K4M2, E10FP2 & KSR2 were found to be comparable with reference formulation K100M9. Response Surface plots were also prepared for evaluating the effect of independent variable on the responses. Stability study was performed as per ICH guidelines and the calculated shelf life was 24-30 months for formulation K4M2, K100M9 and E10FP2.


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