DESIGN AND CHARACTERIZATION OF ACECLOFENAC FAST DISSOLVING TABLETS USING SUPER DISINTEGRATING AGENTS

INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (01) ◽  
pp. 34-40
Author(s):  
V.L Narasaiah ◽  
◽  
Ch. Praneetha ◽  
P Mallika ◽  
K. Pullamma ◽  
...  
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
Content Uniformity ◽  
Disintegration Time ◽  
First Order ◽  
Drug Content ◽  
Weight Variation

The aim of this project was to develop fast dissolving tablets (FDT) of aceclofenac by wet granulation using super disintegrating agents such as cross carmellose sodium (CCS), Crospovidone (CP) and sodium starch glycolate (SSG) were formulated and evaluated. The tablets evaluated for thickness, hardness, friability weight variation, drug content, water absorption ratio, wetting time, disintegration time and in vitro dissolution studies. The in vitro release studies were conducted in pH 7.4 phosphate buffer. Different release models like zero order, first order, Higuchi and Korsmeyer-Peppas were applied to in vitro drug release data in order to evaluate drug release mechanisms and kinetics. The formulation ‘F4’ showed satisfactory physico-chemical properties and drug content uniformity. The formulation ‘F4’ follows first order kinetics and the mechanism of drug release was governed by Higuchi. The ‘n’ value showed between <0.5, it was followed that Fickian transport. The FTIR studies were conducted and it shows that there is no interaction between drug and excipients.

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 Formulation design, optimization & in vitro evaluation of novel orodissolving tablets of efavirenz for hiv infections

2015 ◽  
Vol 49 (3) ◽  
pp. 173-180
Author(s):  
T Ayyappan ◽  
C Poojitha ◽  
T Vetrichelvan
Keyword(s):  
Drug Release ◽  
In Vitro Dissolution ◽  
Dissolution Time ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Sodium Starch Glycolate ◽  
Weight Variation ◽  
Wetting Time

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

scholarly journals DESIGN, DEVELOPMENT AND EVALUATION OF MOUTH DISSOLVING TABLETS OF TOFACITINIB CITRATE

2022 ◽  
pp. 238-245
Author(s):  
MEGHANA RAYKAR ◽  
MALARKODI VELRAJ
Keyword(s):  
Drug Release ◽  
Stability Study ◽  
In Vitro Dissolution ◽  
Design Development ◽  
Disintegration Time ◽  
Drug Content ◽  
Weight Variation ◽  
Wetting Time ◽  
Bulk Drug

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.

Design and Evaluation of Rectal Suppositories of Carvedilol

2009 ◽  
Vol 2 (3) ◽  
pp. 654-660
Author(s):  
P. V. Swamy ◽  
Laeeq Farhana ◽  
S. B. Shirsand ◽  
Md.Younus Ali ◽  
Ashokgoud Patil
Keyword(s):  
Drug Release ◽  
Significant Degree ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Physical Parameters ◽  
Content Uniformity ◽  
Drug Content ◽  
Weight Variation ◽  
Rectal Suppositories

Carvedilol (non-cardio selective b-blocker) is an antihypertensive used in management of hypertension, angina pectoris and heart failure.  But its oral bioavailability is about 25-35% only due to significant degree of first pass metabolism.  It has gastrointestinal side effects such as diarrhea, gastric pain and irritation.  Hence, rectal suppositories of carvedilol were developed by using different water-soluble polymeric bases like gelatin and agar-agar using propylene glycol as plasticizer. The gelatin suppositories were disintegrating/dissolving type while gelatin–agar based suppositories were non-disintegrating/non-melting. All the formulations were evaluated for various physical parameters like weight variation,  drug content uniformity, liquefaction time, micro-melting range, in vitro dissolution, short-term stability and drug-excipient interaction (FTIR).  The mechanism of drug release was diffusion controlled and follows first order kinetics in majority of cases. The results suggested that when gelatin is replaced up to 25% w/w with agar, liquefaction time and drug release were not appreciably affected; higher proportions of agar exhibited incomplete and slow release.  Stability studies conducted at 25±3º C and 60±5% relative humidity for three months indicated that the formulations were stable in the drug-content and in vitro drug release rate (p<0.05).

scholarly journals Use of hydrophilic and hydrophobic polymers for the development of controlled release tizanidine matrix tablets

2014 ◽  
Vol 50 (4) ◽  
pp. 799-818 ◽  
Author(s):  
Tariq Ali ◽  
Muhammad Harris Shoaib ◽  
Rabia Ismail Yousuf ◽  
Sabahat Jabeen ◽  
Iyad Naeem Muhammad ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
In Vitro Release ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Physical Parameters ◽  
Disintegration Time ◽  
Weight Variation ◽  
Vitro Release

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.

scholarly journals FORMULATION AND EVALUATION OF METOCLOPRAMIDE HCL RECTAL SUPPOSITORIES

2019 ◽  
Author(s):  
Deborah Ejiogu Chioma ◽  
Felix Sunday Yusuf
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Diffusion Mechanism ◽  
In Vitro Release ◽  
Content Uniformity ◽  
Disintegration Time ◽  
Weight Variation ◽  
Rectal Suppositories ◽  
Vitro Release

Metoclopramide hydrochloride is a dopamine receptor antagonist, used mostly for stomach and esophageal problems as it is a prokinetic agent. The aim of the present study was to design and evaluate the suppositories of Metoclopramide HCl.  Six different, rectal suppositories were developed by fusion (pour-moulding) method by employing various hydrophilic and hydrophobic polymeric bases like gelatin, PEG-400 and hydrogenated vegetable oil using propylene glycol as plasticizer and beeswax as hardening agent.  Metoclopramide HCl suppositories were evaluated for appearance, weight variation, drug content uniformity, liquefaction time and temperature, micro-melting range, disintegration and in-vitro release study.  The in-vitro release rate data was evaluated statistically and was found that from all the formulations the drug release is by diffusion mechanism. Optimum formulation of batch S1 has shown 83.427% Metoclopramide HCl in a study of 2 hrs. These drug release results are supported by the disintegration time of suppositories. Lesser the disintegration time faster the drug release. All formulations has shown zero, first and Higuchi release kinetics. The result suggests that the Metoclopramide HCl suppositories can be prepared by employing hydrophilic and hydrophobic polymers.

scholarly journals FORMULATION AND EVALUATION OF FAST DISSOLVING TABLETS OF LANSOPRAZOLE BY SOLUBILITY ENHANCEMENT TECHNIQUE

2021 ◽  
Vol 11 (2) ◽  
pp. 54-64
Author(s):  
ARTI CHOURSIYA ◽  
◽  
DEEPIKA PANDIT ◽  
Keyword(s):  
Gastric Ulcer ◽  
Solid Dispersion ◽  
In Vitro Release ◽  
Content Uniformity ◽  
Direct Compression ◽  
Compression Method ◽  
Disintegration Time ◽  
Drug Content ◽  
Weight Variation

The present study was focused on preparation and evaluation of Lanzoprazole fast dissolving tablets. Lansoprazole (LAN) is a proton pump inhibitor drug and used for the treatment of gastric ulcer. Lansoprazole is acid labile drug and to avoid the acidic pH of the stomach LAN is formulated as oral fast dissolving tablets. Lansoprazole is the class II drug of the BCS classification and has a low aqueous solubility. Hence, to improve the solubility of the drug we have prepared Lansoprazole solid dispersion with poly ethylene glycol and complex with β cyclodextrin. Fast Dissolving tablets of LAN were formulated using different superdisintegrants like Sodium Starch Glycolate, Cross Povidone, Cross Carmellose Sodium by direct compression method. The prepared fast dissolving tablets were evaluated for various parameters like weight variation, hardness, friability, disintegration time, drug content, wetting time, in-vitro drug release and short term stability studies. Percentage weight variation, hardness, friability and drug content uniformity were found to be within the approved range for all the formulations. The in-vitro release studies showed that 99.6% of LAN within 90 sec. Overall, in the formulations prepared by the direct compression method, F3, which contains 6% CCS as super disintegrants release 99% of (LAN) in 2 min was found to be the best formulation. The results concluded that fast dissolving tablets of LAN showing enhanced dissolution might lead to improved bioavailability and effective therapy for gastric ulcer. KEYWORDS: β cyclodextrin, Cross Povidone, Fast dissolving tablets, Gastric ulcer, Lanzoprazole, Solid dispersion

Formulation and Evaluation of Orodispersible Tablets Containing Taste Masked Mirabegron Resinate

2021 ◽  
pp. 4736-4742
Author(s):  
Sarika S. Malode ◽  
Milind P. Wagh
Keyword(s):  
Overactive Bladder ◽  
Bitter Taste ◽  
In Vitro Release ◽  
In Vitro Dissolution ◽  
Dissolution Time ◽  
Disintegration Time ◽  
Orodispersible Tablets ◽  
Weight Variation

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.

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, DEVELOPMENT AND IN VITRO EVALUATION OF TRAMADOL EXTENDED RELEASE TABLETS

2019 ◽  
pp. 63-73
Author(s):  
SANJAY KUMAR GUPTA ◽  
AFRAH HUNEZA ◽  
SRADHANJALI PATRA
Keyword(s):  
Drug Release ◽  
Polyethylene Oxide ◽  
Extended Release ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Wet Granulation ◽  
Matrix System ◽  
First Order ◽  
Vitro Release

Objective: The objective of the present study was to develop “once daily” extended release tablets of tramadol (100 mg) by wet granulation using hydrophilic polymer like hydroxy propyl methyl cellulose K100M,K15M and polyethylene oxide (PEO). Methods: The tramadol matrix tablets were prepared by using different polymers like hydroxy propyl methyl cellulose (HPMC K15M and K100M), polyethylene oxide (PEO) as the nontoxic and easily available suitable matrix system. The extended release tablets of tramadol (400 mg) were prepared wet granulation technique. Different pre compression and post compression were performed. In vitro dissolution tests were performed and percentage drug release was calculated. The fourier-transform infrared spectroscopy (FTIR) studies conducted on pure drug tramadol and the optimize formulation (T6). Different release models like zero order, first order, higuchi and Korsemeyer-Peppas were applied to in vitro drug release data in order to evaluate the drug release mechanisms and kinetics. Results: Pre compression and post compression parameters satisfied with pharmacopeia specifications. The In vitro release studies were performed using USP type II apparatus showed that optimized formulation T6 consisting of polyethylene oxide (PEO) with 25 mg of the polymer was found to extended release of tramadol over a period of 24h. The optimized formulation T6 followed the zero order kinetics as correlation coefficient (r2) values are higher than that of first-order release kinetics. In order to understand the complex mechanism of drug release from the optimized formulation T6 matrix system, the in vitro release rate were fitted to Korsemeyer-Peppas model and the release exponent value (n) obtained was 0.82105 exhibited anomalous (non fickian) diffusion mechanism. Conclusion: The present study shows that polyethylene oxide was found to play a great role in controlling release of tramadol from the matrix system. Accordingly it can be concluded that the formulation is robust in the performance is less likely to be affected by the various factors studied.

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