I lupi artificiali e la panne del diritto (original) (raw)
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Tramadol is a centrally acting analgesic having amino cyclo hexanol group, which has a strong analgesic action .It is administered when non steroidal anti inflammatory drugs fail to mitigate pain. Conventional sustained release formulation of Tramadol hydrochloride is not adequate because of lack of initial bolus dose. This drawback can be overcome by combining immediate release and sustained release in a single bilayer tablet. Hence, the aim of the current work is to develop a bilayer dosage form which would release 30% of the drug within 30 minutes and the balance 70% would then release over a period of 12 to 24 hours. In order to optimize the various parameters six different formulations of IR layer and twelve different formulations of SR layer were prepared and compressed separately . The best formulation for both IR nd SR layer selected on the basis of their dissolution profiles. A tablet press had been specifically designed and developed for the production of bilayer tablets. From the study it was concluded that bilayer tablets of Tramadol Hydrochloride can be successfully formulated with 4% crosspovidone as superdisintegrant for immediate release layer and 25% HPMC K 100M and 25% PEO N80 as polymers for sustained release layer. The percentage drug release of the optimized batch was found to be 97.51% at 24 th hour. Thus bilayer tablets could be a potential dosage form for delivering Tramadol as immediate release and controlled release manner.
2013
Tramadol is a centrally acting analgesic having amino cyclo hexanol group, which has a strong analgesic action .It is administered when non steroidal anti inflammatory drugs fail to mitigate pain. Conventional sustained release formulation of Tramadol hydrochloride is not adequate because of lack of initial bolus dose. This drawback can be overcome by combining immediate release and sustained release in a single bilayer tablet. Hence, the aim of the current work is to develop a bilayer dosage form which would release 30% of the drug within 30 minutes and the balance 70% would then release over a period of 12 to 24 hours. In order to optimize the various parameters six different formulations of IR layer and twelve different formulations of SR layer were prepared and compressed separately . The best formulation for both IR nd SR layer selected on the basis of their dissolution profiles. A tablet press had been specifically designed and developed for the production of bilayer tablets. ...
Pakistan journal of pharmaceutical sciences, 2015
Bi-layer tablets of tramadol hydrochloride were prepared by direct compression technique. Each tablet contains an instant release layer with a sustained release layer. The instant release layer was found to release the initial dose immediately within minutes. The instant release layer was combined with sustained release matrix made of varying quantity of Methocel K4M, Methocel K15MCR and Carbomer 974P. Bi-layer tablets were evaluated for various physical tests including weight variation, thickness and diameter, hardness and percent friability. Drug release from bi-layer tablet was studied in acidic medium and buffer medium for two and six hours respectively. Sustained release of tramadol hydrochloride was observed with a controlled fashion that was characteristic to the type and extent of polymer used. % Drug release from eight-hour dissolution study was fitted with several kinetic models. Mean dissolution time (MDT) and fractional dissolution values (T25%, T50% and T80%) were also ...
The main objective of the present work was to develop sustained release bilayer tablets ofwater soluble drug tramadol using Guargum, HPMC, NaCMC and Xanthan gum, either alone or in combinations. Tablets were prepared by immediate release direct compression and sustained release wet granulation method and evaluated for various physical parameters. The drug release studies were performed using USP apparatus type І using 0.1N Hcl and pH 6.8 phosphate buffer as dissolution medium. The drug release was dependent on the type and concentration of the polymer. Drug release was faster from tablets prepared with Guargum, NaCMC and HPMC alone. However, in combination with HPMC, NaCMC, Guargum with Xanthan gum it sustained drug release effectively. The rate and mechanism of release of Tramadol Hcl analysed by fitting the dissolution data into the zero order, First order, Higuchi, Korsmeyer-Peppas and hexon crowel equations. All the Formulations (F1-F10) followed Zero order release Mechanism. Higuchi plots for all the formulations were linear indicating the drug release by diffusion controlled. Hixon-Crowell cube root model showed high r 2 value proportionality due to erosion of hydrophilic gel layer. To explore the release pattern, results of the in-vitro dissolution data were fitted to the Korsmeyer-Peppas equation, which characterizes the transport mechanism indicates the non fickian transport it refer to combination of both diffusion and erosion rate release. It can be concluded that the optimized batch F7 by adopting biphasic drug release pattern in a single dosage could improve patient compliance and give better disease management.
The main objective of this research work was formulation, develop and evaluation of sustained release matrix tablets of Tramadol Hydrochloride using various hydrophilic natural polymers like acacia, Xanthan gum and gum of tragacanth as non-toxic, easily available and suitable matrix system. Sustained release tablet of Tramadol Hydrochloride were prepared by direct granulation method using different concentrations of hydrophilic natural polymers. The prepare tablet were evaluated for pre-compression such as Bulk density, Tapped density, the angle of repose, Carr's compression index, Hausner ratio and post-compression parameter's such as weight variation, hardness, thickness, friability, drug content, uniformity of drug and in-vitro dissolution studies. FTIR studies shown there was no interaction between drug and polymer. In-vitro drug release using USP dissolution apparatus. The dissolution study revealed that formulations containing the tragacanth as a polymer showed the drug release up to 12 hours and found to be most promising polymer among three polymers used in the research work.
Formulation and Evaluation of Bi-layered Sustained Release Matrix Tablets of Tramadol Hydrochloride
Bi-layer tablets of tramadol hydrochloride were prepared by direct compression technique incorporating an immediate release layer and a sustained release layer. An immediate release layer was successfully designed to release the bolus dose instantaneously. Water soluble Xanthan gum, water insoluble Kollidon SR and Eudragit L 100 were used as carriers in the sustained release layer of the matrix tablet. All the tablets were evaluated for thickness, diameter, weight variation, hardness and friability. The in vitro drug release was studied for eight hour, first two hours dissolution in acidic medium followed by six hour dissolution in buffer medium. Matrix tablet showed a sustained release rate with a controlled fashion as a function of the quantity of polymer used. The in vitro drug release data were fitted with several mathematical models and mean dissolution time along with fractional dissolution time values (T 25% , T 50% and T 80%) were calculated. Xanthan gum was found to be the most effective rate retarding agent compared to Kollidon SR and Eudragit L 100, when used at same ratio in the formulations.
Chemical Industry and Chemical Engineering Quarterly, 2015
This study investigates using of high molecular weight hydrophilic polymers, hypromellose and hydroxypropylcellulose, for the preparation of sustained release matrix tablets containing high dose, highly soluble drug, tramadol HCl. Proportion of polymer, type of insoluble filler, proportion of tramadol HCl, amount of drug in the tablet and compression pressure were recognized as critical formulation and process parameters and their influence on drug release and tablet mechanical properties was evaluated. Tensile strength was used as indicator of mechanical properties of the tablets. Experiments were performed with utilization of compaction simulator as a device which simulates compaction profiles of large scale rotary tablet presses. In formulations with both polymers proportion of tramadol HCl was the most critical formulation parameter wherein increasing of the tramadol HCl proportion increased its release rate in early stages of drug release. Regarding the tablet mechanical charac...
International Journal of Applied Pharmaceutics, 2018
Objective: Experiments were performed to design, develop and characterize bilayer buoyant tablets having tramadol (TH), immediate release (IR) layer and gabapentin (GBP), sustained release (SR) layer. Methods: Natural hydrophilic polysaccharide disintegrants were modified by sequential processes to obtain treated xanthan gum (TXG) and treated gellan gum (TGG), utilized for IR layer whereas carbopol and sodium carboxymethylcellulose, as sustaining polymers for SR layer and gas producing substance sodium bicarbonate which librates carbon dioxide for adequate buoyancy, was used in formulated bilayer tablet. A full twolevel factorial experimental design was used for sustaining GBP release from buoyant SR layer. Results: Fourier transform infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC) studies conducted, explain overall drug and excipients compatibility. More than 90% of tramadol was released from IR layer within 30 min. Diffusion exponents (0.36-0.59) and T50% (2.4-4.4h) were determined for all SR tablet formulations. Optimised (S7) formulation exhibited 95.77% GBP released over 12h. Conclusion: Developed tablet can provide excellent therapeutic result by the sequential immediate release of TH and sustained release of GBP for effective combination pharmacotherapy of neuropathic pain with once a day administration.
Tramadol Hydrochloride is an opioid analgesic drug, which has a strong analgesic action. It acts as an opioid agonist through selective binding to µ-opioid receptors. It is administered when non-steroidal anti-inflammatory drugs (NSAIDs) fail to mitigate pain. It is available as three oral formulations: (i) Tramadol Hydrochloride immediate release (IR) [Tramacon®] administered three times daily; (ii) Tramadol Hydrochloride sustained-release (SR) [Tramacip SR®]. Administered twice daily, and (iii) Tramadol Hydrochloride control release (CR) [Tramazac®] administered once daily. All three formulations are bioequivalent in terms of systemic exposure to Tramadol. The objective of the present investigation is to design and evaluate sustained release dosage form of Tramadol Hydrochloride. Because of its shorter half-life and more adverse effect Tramadol was selected as the desired candidates for the formulation of sustain release preparation. Sustained-release tablets were prepared by direct compression method using HPMC K100M (hydrophilic polymer) and HEC (hydrophobic polymer) as matrixing agents. Total nine batches of sustained-release tablet of Tramadol Hydrochloride were formulated and evaluated with a variation in the quantities; among them, batch F8 showed the most satisfactory drug release pattern by sustaining the release of tramadol.
International research journal of pharmacy, 2015
The objective of this work was to develop sustained release tablets of highly water soluble Tramadol HCl using polymers (HPMC K100M, HPMC K15M, Sodium Carboxy Methyl Cellulose, Polyethyleneoxide-N-80) as cost effective, non toxic easily available and suitable hydrophilic matrix system. Tramadol is a centrally acting analgesic drug, Due to high frequency of drug administration (4-6 hourly), small dose (50-100 mg) and short biological half-life (6 h) rationally call for the development of its sustained release. Highly soluble and permeable, this drug can be safely regarded as a BCS class I therapeutic agent. In order to optimize the various parameters 9 different formulations of SR layer were prepared and compressed separately. Sustained release tablet of Tramadol HCl (dose 100mg) were produced by wet granulation method. The drug release studies were performed using USP apparatus type І using pH 1.2 buffer and pH 6.8 phosphate buffer as dissolution medium. The best fit release kinetics was achieved with the zero order plot followed by the Zero order, First order, Hixon Crowel, Higuchi and Korsmyer and Peppas equation. The data obtained proved that the formulations are useful for a sustained release of Tramadol HCl due to the percentage released after 24 hr. is nearly to 100%. The drug release was dependent on the type and concentration of the polymer.