The effect of concentration of hydrophilic (hydroxypropyl methylcellulose [HPMC]) and hydrophobic polymers (hydrogenated castor oil [HCO], ethylcellulose) on the release rate of Tramadol ( Generic Ultram ). Hydrophilic matrix tablets were prepared by wet granulation technique, while hydrophobic (wax) matrix tablets were prepared by melt granulation technique and in vitro dissolution studies were performed using United States Pharmacopeia (USP) apparatus type II. Hydrophobic matrix tablets resulted in sustained in vitro drug release (>20 hours) as compared with hydrophilic matrix tablets (<14 hours). The presence of ethylcellulose in either of the matrix systems prolonged the release rate of the drug. Tablets prepared by combination of hydrophilic and hydrophobic polymers failed to prolong the drug release beyond 12 hours. The effect of ethylcellulose coating (Surelease) and the presence of lactose and HPMC in the coating composition on the drug release was also investigated. Hydrophobic matrix tablets prepared using HCO were found to be best suited for modulating the delivery of the highly water-soluble drug, Tramadol ( Generic Ultram ) hydrochloride.
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AIM: To compare the pharmacokinetics of the enantiomers of trans-Tramadol ( Generic Ultram ) (trans-T) and its active metabolite, trans-O-demethylTramadol ( Generic Ultram ) (M1), in male and female rats. METHODS: Following a single oral dose of 10 mg/kg trans-T hydrochloride to rats, (+)-trans-T, (-)-trans-T, (+)-M1, and (-)-M1 in plasma were determined by a high performance capillary electrophoresis method. RESULTS: The females showed higher plasma concentrations of (+)-trans-T, (-)-trans-T, and (+)-M1 than the males. The enantiomers of trans-T were absorbed and eliminated more slowly in the females than in the males. (+)-M1 was eliminated more slowly in the females than in the males. All pharmacokinetic parameters but Tmax of the two enantiomers of trans-T were significantly different in both sex rats. The (+)/(-)-enantiomeric ratios of the pharmacokinetic parameters for trans-T in the males were similar to those in the females. The values of Cmax, AUC(0-infinity) of the two enantiomers of M1 were significantly different in both sex rats. The (+)/(-)-enantiomeric ratios of Cmax, AUC(0-infinity) for M1 were lower than 1 in the males, larger than 1 in the females. CONCLUSIONS: Systemic exposure of (+)-trans-T, (-)-trans-T, and (+)-M1 was higher in female rats than in male rats. The stereoselectivity in pharmacokinetics of trans-T was similar, and that of M1 was different in male and female rats.

Double-blind clinical trial of Tramadol ( Generic Ultram ) capsules. First communication: Comparison with pentazocine and placebo (author's transl)

A new administration form of Tramadol ( Generic Ultram ) (50 mg) was compared in a multicenter double-blind trial with pentazocine (50 mg) and with placebo in patients with acute pains. Each patient received a test preparation once. The preparations were available in identical capsules. During the five-hour observation period the effect on the intensity of pain was recorded with reference to a scale and the undesirable side effects noted. Tramadol ( Generic Ultram ) was shown to have an analgesic effect about equal to that of the comparative preparation. Both analgesics were superior in effect to the placebo, as was expected. The incidence of side effects from Tramadol ( Generic Ultram ) was less than that with the comparative substance, even if both analgesics had a higher incidence of side effects than the placebo. The results confirm earlier experience obtained with parenteral application of Tramadol ( Generic Ultram ).

Tramadol ( Generic Ultram ) (zydol, Searle).

The account of Tramadol ( Generic Ultram ) (Zydol) in this month's issue is the first in a new series of articles reviewing new drugs and drugs which have recently become established in intensive and critical care nursing practice. It is intended through these articles to consider drugs from a nursing perspective and, in doing so, the key role of the nurse in evaluating the appropriateness, efficacy and safety of drug therapy is readily acknowledged. The format provides a brief description of dosage and available dosage forms together with pharmaceutical aspects including preparation, administration and storage. The actions and clinical uses of drugs are also discussed and summarised in a brief therapeutic comment. The Editor is anxious that 'Drug Therapy Review' serves a useful and practical function within the nursing process and the comments of our readers, including suggestions on topics for future review, will be gratefully received.

Determination of Tramadol ( Generic Ultram ) in human plasma by capillary gas chromatography-mass spectrometry using solid-phase extraction.

An analytical method using solid-phase extraction, capillary gas chromatography and mass selective detection in the electron-impact ionization (EI) mode was developed for the determination of Tramadol ( Generic Ultram ) (2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol) in human plasma. The advantages of this method are the high sensitivity and selectivity and the linearity over the concentration range 2-500 ng/ml. Quantification was made using nefopam as an internal standard, and the detection limit was found to be 1 ng/ml. The standard deviations of the intra-day precision test ranged from 4.5 to 6.0% with respect to the concentration. Accuracy ranged from 1.0 to 4.0% (inter-day). The method was used for the determination of Tramadol ( Generic Ultram ) in a bioequivalence study.


Metabolic assessment in liver microsomes by Co-activating cytochrome P450s and UDP-glycosyltransferases.

A "dual-activity" microsomal system in which both CYPs and UGTs were active was evaluated for studies of metabolic stability and in-vitro metabolite profiling. In this "dual-activity" system, alamethicin, a pore-forming peptide, was used to activate UGTs in human liver microsomes without affecting CYP activity. Interference studies indicated that CYP cofactors had little effect on UGT surrogate activity as measured by glucuronidation of acetaminophen and trifluoperazine. Further, UGT cofactor, UDPGA (< 2 mM), did not inhibit the marker activity of five major CYPs including 1A2, 2C9, 2C19, 2D6 and 3A4, suggesting that both oxidation and glucuronidation can be co-activated in microsomes. In a comparison study, compounds with significant glucuronidation showed distinct stability profiles in the "dual-activity" system, compared to the conventional microsomal incubation in which only CYPs were active. For compounds with minor or no glucuronidation, the metabolic stability remained similar between the "dual-activity" system and the conventional microsomal incubation. The feasibility of this "dual-activity" system utilized for metabolite profiling was also investigated using Tramadol ( Generic Ultram ) as a model drug. It was found that oxidative metabolites of Tramadol ( Generic Ultram ) generated in the "dual-activity" system matched those detected in the conventional microsomal incubation. However, Tramadol ( Generic Ultram ) glucuronide was observed in the "dual-activity" system but not in the conventional micromosal incubation. Results clearly suggest that the "dual-activity" system is a valuable in vitro model for metabolism studies in drug discovery.

Advanced fibre optical scanning in thin-layer chromatography for drug identification.

Two simple and sensitive kinetic methods for the determination of Tramadol ( Generic Ultram ) hydrochloride are described. The first method is based upon a kinetic investigation of the oxidation reaction of the drug with alkaline potassium permanganate at room temperature for a fixed time at 20 min. The absorbance of the colored manganate ions was measured at 610 nm. The second method is based on the reaction of Tramadol ( Generic Ultram ) hydrochloride with 4-chloro-7-nitrobenzofurazan (NBD-Cl) in presence of 0.1 M sodium bicarbonate. The spectrophotometric measurements were recorded by measuring the absorbance at 467 nm, at fixed time at 25 min on thermostated water bath at 90+/-1 degrees C. All variables affecting the development of the colour have been investigated and the conditions were optimised. The absorbance concentration plots in both methods were rectilinear over the range 5-25 and 50-250 microg ml(-1), for the first and second methods, respectively. The two methods have been applied successfully to commercial capsule and ampoule dosage form. The results obtained are compared statistically with those given by the reference spectrophotometric method. The determination of Tramadol ( Generic Ultram ) hydrochloride by the fixed concentration and rate constant methods is feasible with the calibration equations obtained, but the fixed time method proves to be more applicable.