Review of extended-release formulations of Tramadol (original) (raw)
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Formulation , development , and evaluation of tramadol Hcl sustained-release dosage form
2018
Due to its side effect profile in comparison with other analgesics, tramadol Hcl may have a role in patients who are intolerant of conventional opioid and other non-opioid analgesics, those who have preexisting cardiopulmonary disease, such as the elderly or obese, and those in whom codeine use is inappropriate. In the acute and post-operative settings, it may have a place in multimodal, analgesia, where opioid and non-opioid drugs are given in combination to achieve analgesia, with a reduction in the incidence and severity of side effects.[1]
Pain is defined by the International Association for the Study of Pain (IASP) as "an unpleasant sensory and emotional experience associated with actual or potential tissue damage, or described in terms of such damage". Pain has now been equated to a " fifth vital sign " highlighting the significance of pain management in patient care. Tramadol is a centrally acting analgesic, structurally related to codeine and morphine .It is effectively used to treat moderate-to-severe acute and chronic pain in diverse conditions. Tramadol is placed on the second step of WHO analgesic ladder and in contrast to traditional opioids, exerts its analgesic activity, a dual mechanism of action inhibiting transmission as well as perception of pain. Tramadol is more suitable than NSAIDs and coxibs for patient with GI, renal and cardiovascular problems. Combined with low dependence/abuse potential, it has proven to be of significant advantage over other agents, especially in the elderly.
Tramadol Safer and Effective Analgesic to Treat Chronic Pain: A Review
International Journal of Biomedical and Advance Research, 2012
Pain is defined by the International Association for the Study of Pain (IASP) as "an unpleasant sensory and emotional experience associated with actual or potential tissue damage, or described in terms of such damage". Pain has now been equated to a "fifth vital sign" highlighting the significance of pain management in patient care. Tramadol is a centrally acting analgesic, structurally related to codeine and morphine .It is effectively used to treat moderate-to-severe acute and chronic pain in diverse conditions. Tramadol is placed on the second step of WHO analgesic ladder and in contrast to traditional opioids, exerts its analgesic activity, a dual mechanism of action inhibiting transmission as well as perception of pain. Tramadol is more suitable than NSAIDs and coxibs for patient with GI, renal and cardiovascular problems. Combined with low dependence/abuse potential, it has proven to be of significant advantage over other agents, especially in the elderly.
Clinical Drug Investigation, 2005
Abstract have been introduced in pain treatment in order to prolong the dosage interval to improve convenience for the patient. The objective of this study was to compare tramadol pharmacokinetics and intra-and intersubject variability after replicate single-dose administrations of a multiple-units SR formulation (capsule) and a single-unit formulation (tablet). Methods: This was a randomised, single-dose, single-centre study with an open-label, four-period, two-sequence, two-formulation, replicate crossover design in healthy subjects under fed conditions. The main outcome measures were the intra-and intersubject variance of the area under the concentration-time curve from 0 to 12 hours (AUC12) and maximum concentration (Cmax), as well as the mean AUC12 and Cmax for tramadol. Study drugs were a tramadol SR multiple-units formulation (capsule) and a tramadol SR single-unit formulation (tablet), each containing tramadol hydrochloride 100mg. The time interval from 0 to 12 hours of AUC12 of the single-dose design corresponds to the recommended twice-daily dosage interval for both study drugs during long-term treatment.
Pharmacokinetic evaluation of a new oral sustained release dosage form of tramadol
British Journal of Clinical Pharmacology, 2003
To compare the pharmacokinetic profile of a new modified release formulation of tramadol (Tramadol LP 200 mg, SMB Technology, Marche-en-Famenne, Belgium) with that of an immediate release capsule (Topalgic® 50 mg, Grünenthal, Aachen, Germany) after single and multiple dosing and to assess the potential effect of food on its relative bioavailability.
International Journal of Pharmacy and Pharmaceutical Sciences, 2019
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 hydroxypropyl methylcellulose K100M, K15M and polyethylene oxide (PEO). Methods: The tramadol matrix tablets were prepared by using different polymers like hydroxypropyl 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 optimized 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 (r 2 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.) 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.
TRAMADOL AND IT'S THERAPEUTIC EFFECTIVENESS
Tramadol is a centrally acting analgesic structurally related to codeine and morphine containing two enantiomers both of which contribute to analgesic activity. [+]Tramadol and the metabolite (+)-O-desmethyl-tramadol (M1) are agonists of the μ. opioid receptor. [+]Tramadol inhibits serotonin reuptake and [−]tramadol inhibits norepinephrine reuptake, enhancing inhibitory effects on pain transmission in the spinal cord. Tramadol is available as drops, capsules and sustained released formulations for oral use and suppositories for rectal use and solution for IM, IV and subcutaneous injection. After oral administration it is rapidly and completely absorbed. Sustained released tablets releases the active ingredient over a period of 12 hours and have a bioavailability of 87–95% compared with capsules. It is rapidly distributed in the body and plasma protein binding is about 20% [3] Tramadol has two chemical names which includes (
Formulation and Evaluation of Extended Release Tablets of Tramadol Hydrochloride
INTERNATIONAL RESEARCH JOURNAL OF PHARMACY, 2013
Multi-particulate drug delivery systems are mainly oral dosage forms consisting of a multiplicity of small discrete units, each exhibiting some desired characteristics. The extended release products are formulated to make the contained medicament available over an extended period of time after administration within its therapeutic range and hence reduction in dosing frequency as compared to the conventional dosage forms. Indomethacin is a non-steroidal anti-inflammatory drug (NSAID) commonly used for the reduction of pain and inflammation caused by condition such as osteoarthritis, gout, ulcerative colitis, colon cancer. Aim of the present work is to formulate the Indomethacin pellets to present it in the form of capsules (Extended release pellets).To develop and over an extended period of time in the gastro intestinal track and compared the in-vitro dissolution profile with that of the marketed product.