FORMULATION AND EVALUATION OF EFAVIRENZ COMPACTS BY LIQUISOLID TECHNIQUE FOR SOLUBILITY ENHANCEMENT

INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (04) ◽  
pp. 21-27
Author(s):  
V Ramya ◽  
◽  
Z Abbas ◽  
NGN Swamy
Keyword(s):  
Chemical Interaction ◽  
Hydroxypropyl Methylcellulose ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
X Ray Diffraction ◽  
Coating Materials ◽  
Hydroxypropyl Guar ◽  
Ir Studies ◽  
Weight Variation

The aim of this study was to improve the bioavailability by enhancing the solubility of efavirenz, a poor water soluble, anti-viral drug by using liquisolid technique. Different liquisolid formulations were prepared by using various non-volatile hydrophilic solvents. Microcystalline cellulose (Avicel PH 102) and Aerosil 200 were used as carrier and coating materials respectively. Additives such as polyvinyl pyrrolidone, hydroxypropyl methylcellulose and hydroxypropyl guar were incorporated into the formulations, to improve dissolution characteristics. The prepared liquisolid compacts were evaluated for hardness, friability, weight variation, drug content and in vitro dissolution studies. FT-IR studies were carried out to rule out the drug-excipient interactions. It was observed that there was no chemical interaction between the drug and excipients. DSC and X-ray diffraction studies were performed to evaluate the physicochemical properties of the liquisolid tablets, which would enable us to confirm the conversion of the crystalline form of the drug to the amorphous form in the formulation. The dissolution profiles of the liquisolid tablets were compared with that of the directly compressed tablets. The results obtained showed the liquisolid tablets of efavirenz, to exhibit a higher percentage of drug release than the directly compressed tablets.

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 and evaluation of bi-layer floating tablets of ziprasidone HCl and trihexyphenidyl HCl

2011 ◽  
Vol 47 (3) ◽  
pp. 545-553 ◽  
Author(s):  
Sathis Kumar Dinakaran ◽  
Santhos Kumar ◽  
David Banji ◽  
Harani Avasarala ◽  
Venkateshwar Rao
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Chemical Properties ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Floating Tablets ◽  
Ir Studies ◽  
Weight Variation ◽  
The Matrix

The purpose of this research study was to establish ziprasidone HCl NR 40 mg and trihexyphenidyl HCl SR 4mg in the form of bi-layer sustained release floating tablets. The tablets were prepared using sodium HPMC K4M / HPMC K15M as bio-adhesive polymers and sodium bicarbonate acting as a floating layer. Tablets were evaluated based on different parameters such as thickness, hardness, friability, weight variation, in vitro dissolution studies, content of active ingredient and IR studies. The physico-chemical properties of the finished product complied with the specifications. In vitro release from the formulation was studied as per the USP XXIII dissolution procedure. The formulations gave a normal release effect followed by sustained release for 12 h which indicates bimodal release of ziprasidone HCl from the matrix tablets. The data obtained was fitted to Peppas models. Analysis of n values of the Korsmeyer equation indicated that the drug release involved non-diffusional mechanisms. By the present study, it can be concluded that bi-layer tablets of ziprasidone HCl and trihexyphenidyl HCl will be a useful strategy for extending the metabolism and improving the bioavailability of Ziprasidone HCl and Trihexyphenidyl HCl.

scholarly journals FORMULATION AND EVALUATION OF PROCHLORPERAZINE MALEATE SUSTAINED RELEASE FLOATING TABLET

2017 ◽  
Vol 9 (2) ◽  
pp. 89 ◽  
Author(s):  
Ahmed Abdulameer Albadry ◽  
Wedad K. Ali ◽  
Fouad A. Al-saady
Keyword(s):  
Chemical Interaction ◽  
Hydroxypropyl Methylcellulose ◽  
Angle Of Repose ◽  
Weight Variation ◽  
Compressibility Index ◽  
Floating Drug Delivery ◽  
Tap Density ◽  
Floating Tablet ◽  
Optimum Formula

<p><strong>Objective: </strong>The objective of this study was to formulate once daily sustained oral release floating tablet of prochlorperazine maleate, this floating tablet has many advantages like reduction in dosing frequency, increase bioavailability, enhance patient compliance, and improve drug solubility.</p><p><strong>Methods: </strong>The prochlorperazine maleate floating tablets were formulated by using hydrophilic swellable polymer and gas generating agent. In this study, 15 formulas were prepared with many variables in order to achieve an optimum dissolution and floating behaviour for the floating tablet. The all prepared formulas were tested for bulk density, tap density, angle of repose, Carr's Index, thickness, weight variation, hardness, friability, drug content, <em>in vitro</em> dissolution test, <em>in vitro </em>buoyancy, and swelling index.</p><p class="Default"><strong>Results: </strong>Formula (F2) that contain 55% (w/w) <a href="https://www.google.iq/url?sa=t&amp;rct=j&amp;q=&amp;esrc=s&amp;source=web&amp;cd=3&amp;ved=0ahUKEwjh383ow9LPAhWF6RQKHRChCVgQFggpMAI&amp;url=https%3A%2F%2Fwww.ulprospector.com%2Fen%2Fna%2FFood%2FDetail%2F895%2F563462%2FBenecel-Hydroxypropylmethylcellulose-HPMC-K4M&amp;usg=AFQjCNGgfyJECkumK5cpU_6luVwwJ2fKxA&amp;bvm=bv.135258522,d.d24">hydroxypropyl methylcellulose</a> k4M (HPMCK4M), 5 % (w/w) sodium bicarbonate (NaHCO<sub>3</sub>) have acceptable flow properties and compressibility index and good physical properties with floating lag time (16±0.57) seconds and total floating time (32±0.29) h with 100% release of prochlorperazine maleate at the end of 24 h. Fourier transform infrared spectroscopy (FTIR) study of optimum formula (F2) showed no chemical interaction between the drug and the excipients that used in the formula.<strong></strong></p><p><strong>Conclusion: </strong>It can be concluded that that the selected formula (F2) can be a promising formula for the preparation of gastro retentive floating drug delivery systems of prochlorperazine maleate.</p>

scholarly journals Design, Development and Evaluation of Instant Release Oral Thin Films of Flunarizine

2021 ◽  
Vol 71 (1) ◽  
Author(s):  
Asfiya Fatima ◽  
Mamatha Tirunagari ◽  
Divya Theja Chilekampalli
Keyword(s):  
Thin Films ◽  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Rapid Onset ◽  
In Vitro Dissolution ◽  
Design Development ◽  
Onset Of Action ◽  
Weight Variation ◽  
Accelerated Stability

The main objective of the present study was to prepare and evaluate the instant release oral thin films of Flunarizine, in order to enhance the bioavailability of the drug and to provide rapid onset of action thereby improving patient compliance. The instant release oral thin films of Flunarizine were prepared by solvent casting method using film forming polymer like Hydroxypropyl Methylcellulose E-15. The film was evaluated for various physicochemical parameters that include thickness, weight variation, folding endurance, tensile strength, drug content and in vitro drug release studies. No differences were observed in in vitro dissolution of drug from the formulated film F1-F9 as the film instantly gets wet by dissolution medium. The drug release for F5 formulations was about 98.1%. The accelerated stability studies for the optimized film formulations F5 were performed that indicates that the formulated instant release oral thin films were unaffected after initial and 3 months storage under accelerated conditions.

scholarly journals FORMULATION AND EVALUATION OF ORAL DISINTEGRATING FILM OF ATENOLOL

2018 ◽  
Vol 11 (8) ◽  
pp. 312
Author(s):  
Sanjay P ◽  
Vishal Gupta N ◽  
Gowda Dv ◽  
Praveen Sivadasu
Keyword(s):  
Hydroxypropyl Methylcellulose ◽  
In Vitro Dissolution ◽  
Surface Ph ◽  
Morphological Evaluation ◽  
Weight Variation ◽  
Film Forming ◽  
Folding Endurance ◽  
Drug Polymer Interaction ◽  
Oral Films

Objective: The main objective of the study was to formulate the oral disintegrating films loaded with atenolol by solvent-casting method and to carry out its evaluation studies.Methods: The films were prepared using the film-forming hydrophilic polymer like hydroxypropyl methylcellulose (E-5) and super disintegrant like pectin in various proportions.The formulated oral films were characterized for Fourier transform infrared (FTIR) and morphological evaluations. Various physicochemical parameters such as weight variation, folding endurance, surface pH, in vitro disintegration, and in vitro dissolution studies were carried out.Results: FTIR studies revealed that there was no drug-polymer interaction. The morphological evaluation of films showed that all the films were homogenous and transparent. The folding endurance test ensured that the films had sufficient brittleness and by weight variation test, it was inferred that all the films were within the deviation. The surface pH study showed the pH of the films was around neutral pH. The drug was well distributed in all the films. The films disintegrated within 120 s and the fastest being disintegrated in 30 s. Based on all the evaluation parameters, F6 had shown optimal performance and remarkable increase in drug release of 94.38% in 2 min.Conclusion: Thus, formulated oral disintegrating films can be termed as an alternative approach to deliver atenolol.

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).

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.

Pharmaceutical Development and Clinical Pharmacokinetic Evaluation of Gastroretentive Floating Matrix Tablets of Levofloxacin

2011 ◽  
Vol 4 (3) ◽  
pp. 1463-1470
Author(s):  
Y. Madhusudan Rao ◽  
N Doodipala ◽  
C R Palem ◽  
S Reddy
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Alkaline Media ◽  
In Vitro Dissolution ◽  
Sustained Drug Release ◽  
Compression Technique ◽  
Weight Variation ◽  
Floating Drug Delivery System

The most common approach for achieving sustained drug release is by the use of hydrophilic polymeric excipients directly compressed with active ingredients into tablets. Hydrophilic polymers swell in the presence of water to form hydrogel structures from which drugs are released by slow diffusion. The purpose of this study was to prepare a floating drug delivery system of levofloxacin, a fluoroquinolone antibiotic.  Levofloxacin is highly soluble in acidic media and precipitates in alkaline media, thereby losing its solubility. We designed a gastroretentive system of levofloxacin to enhance bioavailability by retaining them in the acidic environment of the stomach. Tablets were prepared by the direct compression technique using polymers such as hydroxypropyl- methylcellulose (HPMC K4M, HPMC K15M, and HPMC K100M). Sodium bicarbonate was utilized as a gas-generating agent. Tables were evaluated for their physical characteristics such as hardness, thickness, friability, weight variation, drug content, swelling studies, and floating properties. Tablet formulations were evaluated by in vitro dissolution studies. Formulations showed a floating lag time of 30 seconds and a floating time above 12 hours. Among these formulations F3, F7 and F11 exhibited controlled and prolonged drug release profiles while floating over the dissolution medium. The best formulation (F3) was selected based on in vitro characteristics and further tested in healthy volunteers by radiographic studies of tablets by incorporating BaSO4. These clinical studies revealed that the tablets remained in the stomach for 240 ± 30 minutes in fasting human volunteers, indicating gastric retention of the system.

scholarly journals Double-layer Tablets of Lornoxicam: Validation of Quantification Method, In vitro Dissolution and Kinetic Modelling

2015 ◽  
Vol 14 (9) ◽  
pp. 1659-1666
Author(s):  
Ü Gönüllü ◽  
P Gürpınar ◽  
M Üner
Keyword(s):  
Drug Release ◽  
Double Layer ◽  
Oral Delivery ◽  
Kinetic Modelling ◽  
Uv Spectroscopy ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Dissolution ◽  
Disintegration Time ◽  
Weight Variation

Purpose: To formulate double-layer tablets of lornoxicam (LRX) prepared by direct compression method and evaluate their physical and drug release  characteristics.Methods: The outer layer of tablets, composed of microcrystalline cellulose (MCC), starch and lactose, incorporated tan initial or prompt dose of the drug (4 mg) for immediate release. Hydroxypropyl methylcellulose (HPMC), polyvinylpyrrolidone (PVP K90) and carbomer, in varying concentrations, were used to prepare the tablet cores for sustained drug delivery. Weight variation, dimensions, hardness,  tensile strength, friability and disintegration time of the tablets were evaluated. Drug release from double-layer tablets as well as kinetic models of drug release were determined after validating the method used for the quantification of the drug. The analytical method for quantification of LRX by UV spectroscopy was validated and verified for linearity, intra-day and inter-day precision, accuracy, recovery and specifity.Results: Tablet cores based on HPMC and HPMC:PVP K90 mixture displayed better compression and flow properties (good and fair to passable) than those  formulated with PVP K90 and carbomer (poor). Satisfactory results were obtained from all the tablet formulations met compendial requirements. The slowest drug release rate was obtained with tablet cores based on PVP K90 (1.21 mg%.h-1). Drug release followed Higuchi kinetic model and the tablet cores released drug by diffusion/polymer relaxation or diffusion/erosion.Conclusion: Double-layer tablet formulation of lornoxicam based on HPMC or HPMC-PVP mixture is suitable for the treatment of inflammatory and painful conditions.Keywords: Lornoxicam, Controlled release, Double-layer tablets, Non-steroidal antiinflammatory drug, Oral delivery

scholarly journals Solubility enhancement, physicochemical characterization and formulation of fast-dissolving tablet of nifedipine-betacyclodextrin complexes

2012 ◽  
Vol 48 (1) ◽  
pp. 131-145 ◽  
Author(s):  
Swati Changdeo Jagdale ◽  
Vinayak Narhari Jadhav ◽  
Aniruddha Rajaram Chabukswar ◽  
Bhanudas Shankar Kuchekar
Keyword(s):  
Physicochemical Characterization ◽  
Inclusion Complexation ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Phase Solubility ◽  
Binary Complex ◽  
Stoichiometric Ratio ◽  
Dissolution Profile ◽  
Weight Variation

The main objective of the study was to enhance the dissolution of nifedipine, a poorly water soluble drug by betacyclodextrin complexation and to study the effect of the preparation method on the in vitro dissolution profile. The stoichiometric ratio determined by phase solubility analysis for inclusion complexation of nifedipine with β-cyclodextrin was 1:1. Binary complex was prepared by different methods and was further characterized using XRD, DSC and FT-IR. A saturation solubility study was carried out to evaluate the increase in solubility of nifedipine. The optimized complex was formulated into fast-dissolving tablets by using the superdisintegrants Doshion P544, pregelatinized starch, crospovidone, sodium starch glycolate and croscarmellose sodium by direct compression. Tablets were evaluated for friability, hardness, weight variation, disintegration and in vitro dissolution. Tablets showed an enhanced dissolution rate compared to pure nifedipine.

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