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PubMed2005

Derivative ultraviolet spectrophotometric determination of dexchlorpheniramine maleate in tablets in presence of coloring agents.

Formulation excipients can frequently affect the drug analysis in pharmaceuticals yielding background interference by ultraviolet spectrophotometry. Sample separation procedures to diminish such interferences are usually recommended as sample pre-treatment, however it can be difficult to eliminate them and they can still persist. In addition, these procedures can be time consuming and laborious to perform. Excipients, like dyeing agents can also be present in a formulation and yield color to drug solution. This work reports the successful development of a derivative ultraviolet spectrophotometry for dexchlorpheniramine maleate (DPM) determination in solid dosage forms, in spite of the color imparted to tablets solution. Standard curves obtained by second order derivative ultraviolet spectrophotometry showed linearity with a correlation coefficient of 0.9999 in the concentration range of 9.75-32.5 microg ml(-1) DPM in 0.1 mol l(-1) sulfuric acid, using zero-peak (ZP) and peak-peak (PP) methods. The average relative standard deviation range was between 0.26% and 1.08% and 0.18% and 0.63% for ZP and PP methods, respectively. Application of the method in tablet samples resulted in coefficients of variation in the range of 0.83-1.40%, and 0.63-0.83% for ZP and PP methods, respectively. Recovery test percentage values obtained were between 96.95% and 105.61% for the tested tablet samples.

Calibration↗
PubMed2005

Identification and characterization of potential impurities of amlodipine maleate.

Six impurities ranging from 0.43 to 1.42% in amlodipine maleate were detected by a simple isocratic reverse-phase high performance liquid chromatography (HPLC). LC-MS was performed to identify the mass of the impurities. Based on the spectral data (IR, NMR and MS), the structures of these impurities were characterized as 3-ethyl 5-methyl 4-(2-chlorophenyl)-2-[2-(1,3-dioxo-2,3-dihydro-1H-2-isoindolyl)ethoxymethyl]-6-methyl-1,4-dihydro-3,5-pyridinedicarboxylate (impurity I); 5-ethyl 3-methyl 4-(2-chlorophenyl)-2-methyl-6-[2-(2-methylcarbamoylphenyl-carboxamido)ethoxymethyl]-1,4-dihydro-3,5-pyridinedicarboxylate (impurity II); besylate salt of 3-ethyl 5-methyl 2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-3,5-pyridinedicarboxylate (impurity III); dimethyl 2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydro-3,5-pyridinecarboxylate (impurity IV); 3-ethyl 5-methyl 2-(2-aminoethoxymethyl)-4-(4-chlorophenyl)-6-methyl-1,4-dihydro-3,5-pyridinedicarboxylate (impurity V); diethyl 2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydro-3,5-pyridinedicarboxylate (impurity VI).

Amlodipine↗
PubMed2000

Long-term intraocular pressure-lowering efficacy and safety of timolol maleate gel-forming solution 0.5% compared with Timoptic XE 0.5% in a 12-month study.

PURPOSE: To evaluate the long-term intraocular pressure-lowering efficacy and safety of timolol maleate gel-forming solution 0.5% (Timolol GFS 0.5%, Alcon Research Ltd, Fort Worth, Texas) compared with Timoptic XE 0.5% (Merck, Inc, West Point, Pennsylvania) in patients with open-angle glaucoma or ocular hypertension. METHODS: Two hundred forty-one patients with open-angle glaucoma or ocular hypertension, who had intraocular pressure between 22 and 36 mm Hg in at least one eye, were randomly assigned in a 2:1 ratio to receive either Timolol GFS 0.5% once daily or Timoptic XE 0.5% once daily, in a 12-month randomized, multicenter, double-masked, prospective study. The primary efficacy variable was mean trough intraocular pressure measured at 8:00 AM, approximately 24 hours after dosing. RESULTS: The Timolol GFS 0.5% group produced significant trough intraocular pressure reductions from a baseline of 4.5 to 5.2 mm Hg (P =.0001), compared with reductions of 4.1 to 5. 3 mm Hg (P =.0001) in the Timoptic XE 0.5% group. The difference in mean intraocular pressure between the two treatments was 0.9 mm Hg or less, and the upper 95% confidence limit between groups was 0.92 mm Hg or less at all time points, demonstrating both clinical and statistical equivalence. A similar percentage of patients in the Timolol GFS 0.5% group (71%) and Timoptic XE group (72%) had clinically relevant reductions in intraocular pressure. There was no significant difference in the safety profiles of the two treatments. CONCLUSION: Both treatments were clinically effective in lowering intraocular pressure and maintaining the reductions over long-term use. Timolol GFS 0.5% is a safe and effective therapy for open-angle glaucoma or ocular hypertension and is both clinically and statistically equivalent to Timoptic XE 0.5% in reducing intraocular pressure.

Adrenergic beta-Antagonists↗
PubMed1997

Cardiovascular effects of topical carteolol hydrochloride and timolol maleate in patients with ocular hypertension and primary open-angle glaucoma. Night Study Group.

PURPOSE: To compare the effects of topical timolol maleate 0.5% and carteolol hydrochloride 1% on pulse rate and blood pressure. METHODS: In a randomized, double-masked, parallel-design, multicenter clinical trial, we compared the effects of timolol and carteolol on pulse rate and blood pressure measured by 24-hour ambulatory blood pressure monitoring in 169 adult patients with either ocular hypertension or primary open-angle glaucoma. RESULTS: From noon to 8 PM, baseline mean pulse rate of 82 to 83 beats per minute (bpm) had decreased by 4 to 6 bpm in both groups after 4 weeks of therapy with timolol or carteolol. From midnight to 4 AM, the pulse rate in the carteolol group was significantly above baseline (P = .005), while the timolol group was significantly below baseline (P < .001). Four times as many patients became bradycardic (heart rate, < 60 bpm) on timolol (18.4%) as did patients on carteolol (4.5%) from midnight to 4 AM. More than twice as many patients exhibited a resolution of their bradycardia with carteolol (46.7%) as did patients treated with timolol (18.2%) from midnight to 4 AM. Overall cardiovascular adverse effects were reported significantly more frequently in the timolol than the carteolol group (P = .002). CONCLUSIONS: Timolol causes significantly lower mean heart rate during the nighttime and more nocturnal bradycardia than carteolol does in patients with ocular hypertension and primary open-angle glaucoma. These differences may be because of the intrinsic sympathomimetic activity of carteolol.

Administration, Topical↗
PubMed1981

Separate and combined effects of timolol maleate and acetazolamide in open-angle glaucoma.

We compared the intraocular pressure-decreasing effect of timolol maleate alone, acetazolamide alone, and combined timolol and acetazolamide therapy in nine patients with bilateral chronic open-angle glaucoma. Timolol decreased intraocular pressure at least as effectively as acetazolamide. The two medications together were more effective than either medication alone, but they did not have a fully additive effect. Episcleral venous pressures and outflow facilities did not vary significantly with any of the three treatment regimens.

Acetazolamide↗
PubMed1999

Comparison of 24-hour intraocular pressure reduction with two dosing regimens of latanoprost and timolol maleate in patients with primary open-angle glaucoma.

PURPOSE: To compare the 24-hour diurnal ocular hypotensive efficacy of two dosing regimens of latanoprost, once daily (8 AM or 10 PM), vs timolol maleate, twice daily. METHODS: We measured six diurnal intraocular pressure curves (6 AM, 10 AM, 2 PM, 6 PM, 10 PM, and 2 AM) in one randomly selected eye of 34 Greek patients newly diagnosed with primary open-angle glaucoma. The first diurnal curve was an untreated baseline. Patients began taking timolol 0.5%, twice daily, for 2 months. Patients were randomly assigned to latanoprost 0.005% given at 8 AM or 10 PM for 1 month and then changed to the other dosing regimen for 1 month. A diurnal curve was performed after each dosing period. RESULTS: The baseline diurnal pressure for all 34 subjects was 23.1 +/- 3.7 mm Hg. The average intraocular pressures at 6 AM for patients who were given latanoprost in the evening (17.9 +/- 2.9 mm Hg) was statistically lower than that in patients given timolol solution (20.1 +/- 2.5 mm Hg, P = .003); however, patients who were given timolol demonstrated a similar diurnal intraocular pressure (19.1 +/- 2.8 mm Hg) to both morning (18.8 +/- 3.7 mm Hg) and evening doses (18.8 +/- 3.6 mm Hg) of latanoprost (P =.329). When the two latanoprost dosages were compared directly, evening administration provided a statistically lower intraocular pressure at 10 AM (P = .0001) and morning administration at 10 PM (P = .0001). This study had an 80% power to exclude a 1.2-mm Hg difference between groups. CONCLUSIONS: This study indicates that in a small population, both latanoprost and timolol are effective in lowering intraocular pressure throughout a 24-hour period; however, latanoprost is most effective in the 12-hour to 24-hour period after administration.

Adrenergic beta-Antagonists↗
PubMed1998

Nonprescription chlorpheniramine maleate and submaximal exercise responses.

OBJECTIVE: To determine if a single, over-the-counter dose of the H1 antagonist chlorpheniramine maleate (CM) alters total peripheral resistance (TPR) and oxygen uptake (VO2) during submaximal exercise. DESIGN: The study was a prospective, longitudinal, double-blind, random crossover analysis of the cardiovascular and respiratory responses to a single bout of moderately intense exercise. SETTING: Exercise tests were conducted in an exercise laboratory equipped with expired gas analysis and bioelectrical impedance cardiographic monitoring capabilities. PARTICIPANTS: Subjects were 18 (9 men, 9 women) volunteers (age=29.5+/-3.6yrs; weight=70.7+/-1.1kg), free from exercise-limiting pathology and rhinitis. INTERVENTION: Each subject completed a maximal exercise tolerance test on the cycle ergometer followed by two randomly ordered submaximal exercise tests at a power output of 50% of the peak power attained on the maximal test: the first, 2 hours after ingesting 4mg of CM, the second, 2 hours after ingesting a placebo. The submaximal exercise tests lasted 20min and data were recorded at 5, 10, 15, and 20min of exercise during both the CM and placebo tests. Tests were completed approximately 48 hours apart. RESULTS: Average VO2 was 1,488+/-367mL/min for the CM test and 1,477+/-351mL/min for the placebo test. TPR was 12.3+/-7.4PRU for the CM and 11.3+/-4.5PRU for the placebo tests. Analysis of variance revealed that these scores were statistically similar. CONCLUSION: A single over-the-counter dose of CM does not alter TPR or VO2 during submaximal exercise.

Adult↗
PubMed2003

In vitro release studies of chlorpheniramine maleate from gels prepared by different cellulose derivatives.

The objective of this study was to evaluate the in vitro and ex vivo percutaneous absorption of chlorpheniramine maleate (CPM) from different hydrogel formulations. Various concentrations of polymers, including hydroxypropylmethylcellulose (HPMC), sodium carboxymethylcellulose (NaCMC) and methyl cellulose (MC) were used in the hydrogel formulations. All experiments were conducted using cellulose dialysis membrane. The passive permeation of CPM was affected by the polymer concentrations. The effect of each polymer on the release rate of CPM was found to be statistically different (P<0.05). The formulation which exhibited maximum drug release through cellulose membrane was then used with other membranes namely polyurethane membrane, rat skin and human skin. The release rate of CPM from different membranes was found to be statistically different (P<0.05). Within the different diffusional barriers rat skin was found to be best alternative to human skin. It seems suitable the use of cellulose derivatives for topical application of CPM to obtain high therapeutic concentration at the application site. The synthetic membranes can be used to assess product performance in quality assurance but give little indication of its performance ex vivo.

Animals↗
PubMed2000

Full and fractionated experimental designs for robustness testing in the high-performance liquid chromatographic analysis of codeine phosphate, pseudoephedrine hydrochloride and chlorpheniramine maleate in a pharmaceutical preparation.

This paper describes the testing of a saturated factorial design using a full factorial design. Saturated factorial designs are often used to test the robustness of high-performance liquid chromatography (HPLC) methods, however they are based on several assumptions. A full factorial design relies on fewer assumptions and hence could be used to evaluate the effectiveness of the saturated design. Both designs were used to test a gradient HPLC method for the assay of codeine phosphate, pseudoephedrine hydrochloride and chlorpheniramine maleate. Six HPLC conditions, including wavelength, mobile phase pH and ion pairing reagent concentration were tested using the saturated design. Three of these factors were selected for full evaluation using a full factorial design. The results showed that the main effects calculated by each design were comparable. However, the saturated design showed higher standard errors, probably due to the effects of changing several more factors. One interaction effect was indicated as a confounding effect by the saturated design and this was confirmed by the calculation of the same interaction effect using the full design. Overall the method was shown to be robust under the variety of HPLC conditions tested.

Chlorpheniramine↗
PubMed2001

Efficacy and tolerability of timolol maleate ophthalmic gel-forming solution versus timolol ophthalmic solution in adults with open-angle glaucoma or ocular hypertension: a six-month, double-masked, multicenter study.

BACKGROUND: Timolol has been formulated in a highly purified gellan gum to improve its duration of action. The efficacy of this formulation in short-term studies using once-daily dosing has been reported. OBJECTIVE: The purpose of this study was to evaluate the efficacy and tolerability of 0.5% timolol maleate ophthalmic gel-forming solution (timolol GS) given once daily versus 0.5% timolol solution given twice daily in a long-term trial. METHODS: This was a multicenter, double-masked, 6-month trial. After a washout of ocular hypotensive medication, 286 patients with open-angle glaucoma or ocular hypertension were randomly assigned in a 2:1 ratio to receive 0.5% timolol GS in both eyes once daily or 0.5% timolol solution in both eyes twice daily. All patients received a morning (9 AM) and evening (9 PM) dose. For patients in the timolol GS group, the evening dose consisted of a vehicle only, whereas for patients in the timolol solution group, both doses consisted of active drug. Intraocular pressure (IOP) was measured at trough (before morning instillation) and peak (2 hours after instillation) at follow-up examinations at weeks 2, 4, 8, 12, and 24. Adverse events were monitored using patient reports. RESULTS: Of the 286 patients randomized, 191 received timolol GS and 95 received timolol solution. Ninety-three percent of patients (265/286) completed the study. At the end of the treatment interval (week 24), the mean decrease in IOP at trough ranged from 5.6 to 5.9 mm Hg in the timolol GS group and from 6.3 to 6.6 mm Hg in the timolol solution group. Similar efficacy was observed at 11 AM (peak). At week 24, the difference in mean IOP between treatments was -0.61 mm Hg (95% CI -1.44 to 0.22) at trough and -0.79 mm Hg (95% CI -1.77 to 0.20) at peak, indicating no significant difference between the 2 timolol formulations. The number of reports of blurred vision and tearing was significantly higher in the timolol GS group than in the timolol solution group (P = 0.04), whereas burning/stinging was reported more frequently in the timolol solution group than in the timolol GS group (P = 0.04). At week 12, the decrease in mean heart rate at trough (hour 0) was significantly less for patients in the timolol GS group than for those in the timolol solution group (-1.1 vs -4.2 bpm; P = 0.024). At week 24 (hour 0), the decrease in mean heart rate was less for patients treated with timolol GS by 2.5 bpm (P = 0.051). The heart rate data at peak (hour 2) was similar to that observed at trough at week 12 (-2.7 vs -5.7 bpm; P = 0.006) and week 24 (-3.1 vs -4.7 bpm; P = 0.063). The mean change in blood pressure was not significantly different between treatments. There were no clinically significant differences between the groups in visual acuity, biomicroscopy and ophthalmoscopy results, or visual fields. CONCLUSIONS: Timolol 0.5% GS administered once daily was shown to be as effective in lowering IOP as the equivalent concentration of timolol 0.5% solution administered twice daily in patients with ocular hypertension or open-angle glaucoma.

Adult↗
PubMed2003

Effects of rosiglitazone maleate when added to a sulfonylurea regimen in patients with type 2 diabetes mellitus and mild to moderate renal impairment: a post hoc analysis.

BACKGROUND: Patients with type 2 diabetes mellitus (DM) and renal impairment whose disease is inadequately controlled on a sulfonylurea (SU) have limited oral combination treatment options. OBJECTIVE: This post hoc analysis assesses the efficacy and tolerability of the insulin sensitizer rosiglitazone maleate (RSG) when added to an SU treatment regimen in patients with type 2 DM with mild to moderate renal impairment that is inadequately controlled by SU monotherapy. METHODS: Data were pooled from 3 randomized, double-blind, placebo-controlled, parallel-group studies in which RSG or placebo was added to an SU (glibenclamide, gliclazide, or glipizide) treatment regimen for a period of 6 months. Patients were subcategorized as having mild to moderate renal impairment or normal renal function based on a baseline creatinine clearance rate of 30 to 80 mL/min or >80 mL/min, respectively, as estimated by the Cockcroft-Gault equation. RESULTS: The population studied comprised 824 patients, 62% men and 38% women, aged 32 to 81 years, of whom 301 had mild to moderate renal impairment and 523 had normal renal function. In patients with and without renal impairment, glycemia was improved in the SU + RSG-treated group compared with the SU + placebo-treated group. The observed treatment differences between the groups were -2.6 mmol/L for fasting plasma glucose and -1.1% for glycosylated hemoglobin (for both renally impaired and nonimpaired patients). For patients receiving SU + RSG, little difference in the safety profile was found between patients with and without renal impairment. CONCLUSION: RSG was effective and well tolerated when added to SU therapy in this population of patients with mild to moderate renal impairment.

Adult↗
PubMed1989

Adjunctive glaucoma therapy. A comparison of apraclonidine to dipivefrin when added to timolol maleate.

The authors compared the additive intraocular pressure (IOP)-lowering effects of two different topical medications, apraclonidine hydrochloride and dipivefrin hydrochloride, when used in conjunction with timolol maleate. Eighteen patients with elevated IOPs entered a randomized, double-masked, cross-over study. Each used apraclonidine 1.0%, dipivefrin 0.1%, or placebo, twice daily for 3 weeks each, in addition to timolol 0.5% twice daily. Only apraclonidine produced a significant additional IOP lowering over timolol treatment alone at all time intervals (P less than 0.001). Its additive effect was significantly greater than that seen with dipivefrin at all time intervals (P less than 0.01), with the exception of day 22 (P = 0.061). No significant change in pulse rate or blood pressure was seen during apraclonidine administration. Apraclonidine may be a useful adjunctive agent in patients with poorly controlled glaucoma.

Adult↗
PubMed2001

In vitro transdermal iontophoretic transport of timolol maleate: effect of age and species.

Transdermal iontophoresis would be a promising method for the systemic delivery of water soluble and ionic drugs of relatively high molecular size, including peptides. In the present study, the effect of biological parameters such as age of the animal and species variation (rat, rabbit, mouse, guinea pig and human) on the transdermal iontophoretic transport was studied using timolol maleate (TM) as a model drug. The iontophoretic transport of TM across the skins obtained from the rats of different age groups was found to be similar. The results of the present study suggest that the age of the animal (Wistar rats: 1-8 months) did not appear to influence the transdermal iontophoretic transport of TM significantly. The amount of TM transported during iontophoresis (2 h) was significantly different among the different skin species. But the total amount of TM transported up to 24 h (2 h iontophoresis+22 h post-iontophoretic passive diffusion) was not significantly different among the different species studied. The present study provides further evidence that iontophoresis technique reduces the interspecies differences in the transdermal permeation of drugs, which is normally observed in passive diffusion of drugs. However, it must be noted that excised skins have been used in the present study to investigate the role of age and species variation on the iontophoretic transport of TM. The influence of these parameters under in vivo conditions might be different considering the physiological differences in different species and in the animals of different age groups.

Administration, Cutaneous↗
PubMed2002

Controlled transport of timolol maleate through artificial membranes under passive and iontophoretic conditions.

The passive and iontophoretic permeability of timolol maleate (TM) through porous and dense artificial membranes was investigated in order to select the most optimal membrane for a transdermal drug delivery system. For the meso-porous membranes (pore diameter 2-50 nm), the TM permeability for passive diffusion and iontophoresis was practically the same. For the micro-porous membranes (pore diameter<2 nm), a significant transport contribution of iontophoresis was observed, which was more pronounced when higher current densities were applied. The electrical resistance of all the porous membranes was lower than the electrical resistance of human skin. For dense membranes, passive and iontophoretic TM permeability was significantly lower than for porous membranes and in most cases their electrical resistance was comparable or even higher than the resistance of human skin. For most of the membranes studied the average adsorption of TM at 37 degrees C was low (0.02-0.33 mg/cm(2)) and independent of the TM concentration. For the meso-porous mixed cellulose acetate-cellulose nitrate membrane the TM adsorption was significantly higher and increased with the TM concentration. Based on our results, the optimum membrane for an iontophoretic transdermal TM delivery system is the LFC 1 micro-porous membrane because it mainly controls the TM delivery (TM iontophoretic permeability: 0.86 x 10(-6) cm/s), has very low electrical resistance (0.9-1.5 komega cm(2)) and the TM adsorption to it is low (0.15 mg/cm(2)). The therapeutic plasma TM concentration is achievable by application of this membrane in realistic sizes (5-64 cm(2)) and by application of current densities between 0.13 and 0.5 mA/cm(2).

Adsorption↗
PubMed1996

Subacute toxicity of ergometrine maleate in rats.

Ergot alkaloids, produced by the fungus Claviceps purpurea, are found in small amounts in foodstuffs. The human disease ergotism, caused by high intake of ergot alkaloids, is well known; however, little is known about the toxicity of these compounds. The subacute toxicity of an ergot alkaloid, ergometrine maleate, was therefore studied. Sprague-Dawley rats were treated with 0, 2, 10, 50 and 250 mg ergometrine maleate/kg diet for 4 wk. Plasma glucose levels were decreased in females at 50 and 250 mg/kg. Thyroxin levels were decreased at 50 (males only) and 250 mg/kg. At the high dose level, organ weights of heart, liver, ovaries and kidneys were increased. In male rats a slight dose-related increase in the incidence of enlarged mediastinal lymph nodes and, to some extent, of enlarged parathymal lymph nodes, was seen. Histopathological examination revealed evidence of increased glycogen storage in the liver of animals treated with 250 mg/kg. The no-observed-effect level in this study was 10 mg/kg.

Analysis of Variance↗
PubMed2001

Suppressive effect of irsogladine maleate on N-methyl-N-nitro-N-nitrosoguanidine (MNNG)-initiated and glyoxal-promoted gastric carcinogenesis in rats.

The modifying effect of irsogladine maleate (IRG) on N-methyl-N-nitro-N-nitrosoguanidine (MNNG)-initiated and glyoxal-promoted gastric carcinogenesis was examined in male Wistar rats. Six-week-old rats were divided into ten groups. Groups 1 through 6 were given MNNG (100 mg/l in drinking water) for 25 weeks from the start of the experiment, whereas groups 7 through 10 received distilled water in the initiation phase as the vehicle treatment. Groups 1 and 8 were kept on the basal diet and distilled water throughout the experiment (55 weeks). Groups 2-8 were given 0.5% glyoxal in the drinking water for 30 weeks from 26th week of the experiment. Group 3 was fed the diet mixed with 100 ppm IRG for 25 weeks from the start of experiment. Groups 4 and 8 were fed the diet mixed with 100 ppm IRG for 30 weeks from 26th week of experiment. Groups 5 and 9 or 6 were given 100 or 25 ppm IRG containing diet, respectively throughout the experiment. Group 10 was given the basal diet and distilled water as the vehicle treated control. Tumors of upper digestive tracts (stomach and duodenum) were developed in groups: 1 (12/17 rats, 71%), 2 (11/12 rats, 92%), 3 (9/16 rats, 56%), 4 (5/12 rats, 42%), 5 (6/15 rats, 40%) and 6 (7/12 rats, 58%). High dose of IRG in initiation and/or promotion phase significantly reduced the incidence of tumors of the upper digestive tracts. The average numbers of the digestive tracts neoplasms in groups 3,5 and 6 given glyoxal and IRG were less than those in group 2 which received only glyoxal. These results suggest that IRG could be a preventive agent against the occurrence of neoplasms of the upper digestive tract.

Animals↗
PubMed1979

Gas-liquid chromatographic method for the measurement of plasma levels of d-7,8-dimethoxy-3-methyl-phenyl-2,3,4,5-tetrahydro-1h-3-benzazepine acid maleate (SCH-12679) and its major metabolites in aggressive mental retardites.

A sensitive gas-liquid chromatographic technique for the quantitative analysis of SCH-12679 (d-7,8-dimethoxy-3-methyl-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine acid maleate) and its major metabolites in plasma of aggressive mental retardates receiving therapeutic doses of the medicament has been developed. The lower limits of detection are 20 ng/ml for SCH-12679, 0.5 ng/ml for 3-desmethyl SCH-12679 and 0.4 ng/ml for 7-desmethyl plus 8-desmethyl SCH-12679. SCH-12679 is estimated with a flame ionization detector. Its metabolites are quantitated using an electron-capture detector after conversion of the compounds to their heptafluorobutyryl derivatives by reaction with the appropriate anhydride. Data on plasma levels of unchanged SCH-12679, 3-desmethyl SCH-12679 and a combination of 7-desmethyl and 8-desmethyl SCH-12679 in fifteen patients treated with the medicament are presented.

2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-ben↗
PubMed1997

Simultaneous determination of a novel calcium entry blocker, monatepil maleate, and its metabolites in rat plasma by means of solid-phase extraction and reversed-phase liquid chromatography with electrochemical detection.

A reversed-phase LC method with electrochemical detection is described for the simultaneous determination of monatepil maleate (AJ-2615, AJ), a novel calcium entry blocker, and its three S-oxidized metabolites in plasma. These compounds were extracted from plasma by solid-phase extraction and injected onto an ODS column. The determination limit in plasma (0.5 ml) was 10 ng/ml for AJ and 5 ng/ml for the three metabolites. The method was applied to the determination of AJ and the metabolites in rat plasma samples.

Animals↗