Tramadol SR Formulations (original) (raw)
Related papers
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.
Comparative bioequivalence studies of tramadol hydrochloride sustained-release 200 mg tablets
2010
Background: Tramadol hydrochloride is available as 50 mg immediate-release (IR) and 100 mg, 200 mg, and 300 mg sustained-release (SR) tablets. The recommended dose of tramadol is 50-100 mg IR tablets every 4-6 hours. The tramadol SR 200 mg tablet is a better therapeutic option, with a reduced frequency of dosing, and improved patient compliance and quality of life. The present study evaluated the bioequivalence of a generic tramadol SR 200 mg tablet. Methods: A comparative in vitro dissolution study was performed on the test and reference products, followed by two separate single-dose bioequivalence studies under fasting and fed conditions and one multiple-dose bioequivalence study under fasting conditions. These bioequivalence studies were conducted in healthy human subjects using an open-label, randomized, two-treatment, two-period, two-sequence, crossover design. The oral administration of the test and reference products was done on day 1 for both the single-dose studies and on days 1-5 for the multiple-dose study in each study period as per the randomization code. Serial blood samples were collected at predefined time points in all the studies. Analysis of plasma concentrations of tramadol and O-desmethyltramadol (the M 1 metabolite) was done by a validated liquid chromatography-mass spectrometry analytical method. The standard acceptance criterion of bioequivalence was applied on log-transformed pharmacokinetic parameters for tramadol and its M 1 metabolite. Results: The ratios for geometric least-square means and 90% confidence intervals were within the acceptance range of 80%-125% for log-transformed primary pharmacokinetic parameters for tramadol and its M 1 metabolite in all the three studies. Conclusion: The test product is bioequivalent to the reference product in terms of rate and extent of absorption, as evident from the single-dose and multiple-dose studies. Both the treatments were well tolerated.
Review of extended-release formulations of Tramadol
2014
Abstract: Patients with chronic non-malignant pain report impairments of physical, social, and psychological well-being. The goal of pain management should include reducing pain and improving quality of life. Read this review and sign up to receive Journal of Pain Research here: http://www.dovepress.com/articles.php?article\_id=16193
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]
The Veterinary Journal, 2009
The study evaluated the pharmacokinetics of tramadol and its major metabolites O-desmethyltramadol (M1), N-desmethyltramadol (M2) and N-O didesmethyltramadol (M5) following a single oral administration of a sustained release (SR) 100 mg tablet to dogs. Plasma tramadol concentration was greater than the limit of quantification (LOQ) in three dogs, M1 was quantified only in one dog while M2 and M5 were quantified in all of the dogs. The median values of C max (maximum plasma concentration), T max (time to maximum plasma concentration) and T 1/2 (half-life) for tramadol were 0.04 (0.17-0.02) lg mL À1 , 3 (4-2) and 1.88 (2.211-1.435) h, respectively. M5 showed median values of C max , T max and T 1/2 of 0.1 (0.19-0.09) lg mL À1 , 2 (3-1) and 4.230 (6.583-1.847) h, respectively. M2 showed median values of C max , T max and T 1/2 of 0.22 (0.330-0.080) lg mL À1 , 4 (7-3) and 4.487 (6.395-1.563) h, respectively. The findings suggest that the SR formulation of tramadol may not have suitable pharmacokinetic characteristics to be administered once-a-day as an effective and safe treatment for pain in the dog.
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 (
European Journal of Pharmaceutical Sciences, 2016
Tramadol hydrochloride is a centrally acting analgesic used for the treatment of moderate-to-severe pain. It has three main metabolites: O-desmethyltramadol (M1), N-desmethyltramadol (M2), and N,O-didesmethyltramadol (M5). Because of the frequent use of tramadol by patients and drug abusers, the ability to determine the parent drug and its metabolites in plasma and cerebrospinal fluid is of great importance. In the present study, a pharmacokinetic approach was applied using two groups of five male Wistar rats administered a 20 mg/kg dose of tramadol via intravenous (i.v.) or intraperitoneal (i.p.) routes. Plasma and CSF samples were collected at 5-360 min following tramadol administration. Our results demonstrate that the plasma values of C max (C 0 in i.v. group) and area under the curve (AUC) 0-t for tramadol were 23,314.40 ± 6944.85 vs. 3187.39 ± 760.25 ng/mL (C max) and 871.15 ± 165.98 vs. 414.04 ± 149.25 μg•min/mL in the i.v. and i.p. groups, respectively (p b 0.05). However, there were no significant differences between i.v. and i.p. plasma values for tramadol metabolites (p N 0.05). Tramadol rapidly penetrated the blood-brain barrier (BBB) and blood-cerebrospinal fluid barrier (BCSFB) (5.00 ± 0.00 vs. 10.00 ± 5.77 min in i.v. and i.p. groups, respectively). Tramadol and its metabolites (M1 and M2) were present to a lesser extent in the cerebrospinal fluid (CSF) than in the plasma. M5 hardly penetrated the CSF, owing to its high polarity. There was no significant difference between the AUC 0-t of tramadol in plasma (414.04 ± 149.25 μg•min/mL) and CSF (221.81 ± 83.02 μg•min/mL) in the i.p. group. In addition, the amounts of metabolites (M1 and M2) in the CSF showed no significant differences following both routes of administration. There were also no significant differences among the K p,uu,CSF(0-360) (0.51 ± 0.12 vs. 0.63 ± 0.04) and K p,uu,CSF(0-∞) (0.61 ± 0.10 vs. 0.62 ± 0.02) for i.v. and i.p. pathways, respectively (p N 0.05). Drug targeting efficiency (DTE) values of tramadol after i.p. injection were more than unity for all scheduled time points. Considering the main analgesic effect of M1, it is hypothesized that both routes of administration may produce the same amount of analgesia.