EVALUATION OF TWO TRANQUILIZERS: ACETOPHENAZINE MALEATE (TINDAL MALEATE): CARPHENAZINE MALEATE (PROKETAZINE MALEATE).
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Humans↗
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Evidence for the degradation of maleate moiety in chlorpheniramine maleate solution using a stability-indicating HPLC method.
The degradation phenomenon of maleate moiety of chlorpheniramine maleate in solution has been demonstrated by means of a peculiar ion-pair HPLC method developed by the authors, which permits the simultaneous determination of chlorpheniramine and maleate. A commercial cough drug containing chlorpheniramine maleate was dissolved in water with m-hydroxybenzoic acid as an internal standard, and then kept for several days at room temperature. It was recognized that the maleate content in the drug solution had gradually decreased, whereas chlorpheniramine content had not decreased. A simple solution of maleic acid was also kept for several days at room temperature, and it was also recognized that the maleate content in the solution preserved at the same concentration as the solution of the commercial cough drug had gradually decreased, and the percent of remaining maleate reached zero. The degraded peaks on HPLC chromatogram were not detected at all by UV detector, and the disappearance of maleate was ascertained by GC-MS. No detectable example of maleate of chlorpheniramine maleate in a commercial cough syrup has suggested that maleate moiety of chlorpheniramine maleate decomposed to carbon dioxide.
Chlorpheniramine↗
Stimulation of the hydrolytic activity and decrease of the transpeptidase activity of gamma-glutamyl transpeptidase by maleate; identity of a rat kidney maleate-stimulated glutaminase and gamma-glutamyl transpeptidase.
gamma-Glutamyl transpeptidase catalyzes transfer of the gamma-glutamyl moiety of glutathione (and other gamma-glutamyl compounds) to amino acid and peptide acceptors; this reaction probably involves (a) formation of a gamma-glutamyl enzyme and (b) reaction of the gamma-glutamyl-enzyme with an acceptor. Maleate decreases the latter reaction and markedly increases hydrolysis of the gamma-glutamyl donor, apparently by affecting the enzyme so as to facilitate reaction of the gammaglutamyl enzyme with water. Transpeptidase catalyzes gamma-glutamyl hydroxamate formation from many gamma-glutamyl compounds and hydroxylamine; this reaction is stimulated 4- to 5-fold by maleate. Glutamine, a poor substrate for transpeptidation as compared to glutathione, is slowly hydrolyzed and converted to gamma-glutamyl-glutamine by the transpeptidase; in the presence of maleate, hydrolysis of glutamine is markedly (>10-fold) increased, as is also its conversion to gamma-glutamyl hydroxamate in the presence of hydroxylamine. The findings suggest that the previously described "maleate-stimulated phosphate-independent glutaminase" is a catalytic function of gamma-glutamyl transpeptidase. Transpeptidase-catalyzed glutaminase activity may play a role in renal ammoniagenesis. The ability of maleate to decrease transpeptidation of gamma-glutamyl compounds (and to increase their hydrolysis to glutamate), when considered in the light of earlier findings that treatment of animals with maleate produces aminoaciduria, is consistent with function of transpeptidase and the gamma-glutamyl cycle in amino-acid transport.
Ammonia↗
Quantitative determinations of codeine phosphate, guaifenesin, pheniramine maleate, phenylpropanolamine hydrochloride, and pyrilamine maleate in an expectorant by high-pressure liquid chromatography.
The quantitative determinations of codeine phosphate, guaifenesin, pheniramine maleate, phenylpropanolamine hydrochloride, and pyrilamine maleate in a liquid dosage form are described. All active and inactive ingredients (sodium benzoate and FD&C Yellow No. 5 dye) can be separated with high-pressure liquid chromatography except the two antihistamines, pheniramine maleate and pyrilamine maleate. Pheniramine maleate is determined colorimetrically, and pyrilamine maleate is determined either by difference or spectrophotometrically. The methods are simple short, accurate, and precise. The standard deviations are reported.
Chromatography, High Pressure Liquid↗
Tribasic lead maleate and lead maleate: synthesis and structural and spectroscopic characterizations.
We report on the synthesis and structure of tribasic lead maleate hemihydrate ([Pb4O3]C2H2(CO2)2.(1/2)H2O, TRIMAL) and lead maleate (PbC2H2(CO2)2, PBMAL). The structure of [Pb4O3]C2H2(CO2)2.(1/2)H2O, solved ab initio from X-ray powder diffraction data, consists of infinite slabs of edge-sharing OPb4 tetrahedra, of composition [Pb4O3], running along the c axis and linked together into a three-dimensional network by tetradentate maleate anionic ligands. The structure of PbC2H2(CO2)2, solved from single crystal diffraction data, is lamellar and contains double layers of heptacoordinated lead atoms, bonded only to the oxygen atoms of the maleate ligands. In both compounds, lead is in the oxidation state 2+ and the coordination polyhedra around the Pb2+ exhibit a hemidirected geometry and are strongly distorted as a result of the lone pair of electrons. The absence of protons on the acidic portion of the maleate moieties was confirmed by Raman spectroscopy and by 1H MAS and 1H-13C CP MAS NMR experiments. The two compounds were further characterized using chemical and thermogravimetric analyses.
Journal Article↗
Plasma timolol concentrations of timolol maleate: timolol gel-forming solution (TIMOPTIC-XE) once daily versus timolol maleate ophthalmic solution twice daily.
PURPOSE: The objective of this study was to compare plasma concentrations of timolol following multiple dosing of the therapeutic regimens of timolol maleate ophthalmic gel-forming solution (Timolol GS; TIMOPTIC-XE) and timolol maleate ophthalmic solution. Timolol maleate ophthalmic gel-forming solution is also referred to as Timolol GS, i.e. gel-forming solution. METHODS: This was a masked observer, two-period crossover study in six normal male subjects randomized to receive either Timolol GS, 0.5% (TIMOPTIC-XE,) once daily (0530 hours) or timolol maleate ophthalmic solution (0.5% TIMOPTIC) twice daily (0530 and 1730 hours) for 8 days, in both eyes. On Day 8, a blood sample was obtained prior to treatment, as well as 1, 2, 4, 8, 10, 12, 13, 14, 16, and 24 hours following the morning instillation. After a 7-day inter-period washout interval, subjects received the opposite treatment. RESULTS: Timolol GS (TIMOPTIC-XE): Plasma concentrations of timolol rarely exceeded 0.375 ng/ml (the lower limit of assay quantification). For all subjects, peak plasma concentrations of timolol averaged <0.3 ng/ml within 4 hours after the last dose. The highest single observation was 0.49 ng/ml in one subject (at hour 2). Timolol solution: For all subjects, peak plasma concentrations of timolol averaged about 0.5 ng/ml and 0.3 ng/ml within 4 hours following the first and second dose, respectively, on Day 8. The highest single observation was 0.95 ng/ml in one subject (at hour 2). CONCLUSIONS: The data suggest that there is less systemic exposure to timolol following once-daily therapy with Timolol GS 0.5% compared with twice daily therapy with timolol maleate ophthalmic solution 0.5%.
Absorption↗
Fluoremetric determination of methylergonovine maleate and ergonovine maleate in tablets and injections.
A column cleanup, followed by a shakeout and fluorometric determination, has been developed to determine methylergonovine maleate and ergonovine maleate in tablets and injections. The ether eluate is extracted with tartaric acid solution. An aliquot is diluted with sodium tartrate solution, and this solution is excited at 325 nm. The resulting fluorescence is measured at 432 nm. Results obtained using this method compare favorably with those from the official NF XIV procedure and a semiautomated procedure. Recoveries of 100 and 99% were obtained from one sample each of spiked excipient tablets of methylergonovine maleate and ergonovine maleate, respectively.
Ergonovine↗
Timolol maleate 0.5% versus timolol maleate in gel forming solution 0.5% (Timolol GFS) in open angle glaucoma in India. Preliminary safety and efficacy study.
PURPOSE: To compare the efficacy and safety profile of Timolol maleate 0.5% versus Timolol gel forming solution (GFS) 0.5% in open angle glaucoma in Indian eyes. METHODS: In a prospective crossover study 52 patients of open angle glaucoma, well controlled intraocular pressure (IOP) on 0.5% timolol maleate solution were switched over to timolol GFS once a day, after a washout period of one month. A diurnal IOP measurement was done after 6 weeks and compared with patients on timolol maleate 0.5% twice a day. In addition, side effects reported or observed were compared. RESULTS: Statistically significant difference was not observed in ocular hypotensive effect of the two treatment. The side-effects in both the treatment groups were similar except for higher incidence of blurring of vision in patients on timolol GFS. The compliance was better with timolol GFS, but was not statistically significant. CONCLUSION: The results of this study suggest that the more convenient 0.5% timolol in gel forming solution can be offered as an equally efficacious and well-tolerated alternative to twice daily 0.5% timolol solution in open angle glaucoma.
Adrenergic beta-Antagonists↗
[Quantitative analysis of chlorpheniramine maleate in cough and cold drugs by ion-pair high-performance liquid chromatography for the simultaneous determination of chlorpheniramine and maleate].
A simple, rapid and convenient chromatographic method, which permits the simultaneous determination of chlorpheniramine (CP) and maleate (MA), recently developed by the authors was applied to the analysis of chlorpheniramine maleate (CPM) in cough and cold drugs. In this method, a Capcell Pak C8 column and an isocratic mobile phase containing 15% methanol, 50 mM KH2PO4 and 5mM tetra-n-butylammonium phosphate as an ion-pair reagent were used. By using the mobile phase adjusted to pH 3.0 with orthophosphoric acid, fumaric acid, MA, CP, acetaminophen (paracetamol), caffeine, and m- and p-hydroxybenzoic acid as candidates for an internal standard were eluted separately within 17 min. Detection was carried out with UV detector at 215 nm. Under the same conditions, five other antihistamines analogous to CPM were also separated. The calibration graphs for CP and MA showed good linearity in the range of 0.5-10 nmol (0.195-3.9 micrograms) per 20 microliters injection, respectively. The proposed method was successfully applied to the simultaneous determination of CP and MA, i.e., CPM analysis, in commercial cough and cold drugs which pharmaceutical forms were tablet, granule and syrups.
Antitussive Agents↗
Simultaneous GLC analysis of salicylamide, phenylpropanolamine hydrochloride, caffeine, chlorpheniramine maleate, phenylephrine hydrochloride, and pyrilamine maleate in capsule preparations.
A GLC method is described for the quantitative determination of salicylamide, phenylpropanolamine hydrochloride, caffeine, chlorpheniramine maleate, phenylephrine hydrochloride, and pyrilamine maleate. The sample was dissolved in ethanol, and an aliquot of the solution was brought to dryness and treated with 0.1 ml of 4-(dimethyl-amino)pyridine in pyridine-acetic anhydride (1:1). The components were isolated and measured by applying 1 microliter of the reaction mixture to a chromatograph equipped with a flame-ionization detector and fitted with 8% OV-101 glass columns. The accuracy was good. Dicyclohexylphthalate was used as the internal standard.
Aminopyridines↗
Patient preference, efficacy, and compliance with timolol maleate ophthalmic gel-forming solution versus timolol maleate ophthalmic solution in patients with ocular hypertension or open-angle glaucoma.
This study was designed to compare timolol maleate ophthalmic gel-forming solution 0.5% (timolol gel) once daily with timolol maleate ophthalmic solution 0.5% (timolol solution) twice daily with respect to patient preference, intraocular pressure (IOP)-lowering effect, and tolerability. A total of 202 patients with ocular hypertension or open-angle glaucoma and an IOP > or = 22 mm Hg were enrolled in this 12-week, randomized, observer-masked, two-period crossover study. Significantly more patients preferred timolol gel to timolol solution (P < 0.001). Ninety-two percent of patients preferring timolol gel strongly agreed or agreed that once-daily dosing was a reason for their preference. Those who preferred timolol solution did so because of fewer side effects. The mean IOP-lowering effects of the 2 treatments were similar at both morning trough and peak time points. The incidence of drug-related adverse experiences was similar (timolol gel 11.4% vs timolol solution 10.9%). Because both treatments were well tolerated and effective in lowering IOP, timolol gel, with its once-daily dosing regimen, should be considered in patients who are candidates for therapy with an ophthalmic beta-blocking agent.
Adrenergic beta-Antagonists↗
Comparative effect of dimethindene maleate and chlorpheniramine maleate on histamine-induced weal and flare.
Antihistaminic activity of 3 or 6 mg dimethindene maleate was compared with that of placebo and 12 mg chlorpheniramine maleate in 60 healthy volunteers in a randomized, crossover study. Activity of each drug was assessed by measuring 2 micrograms histamine-induced weal and flare areas. Compared with placebo, both doses of dimethindene and chlorpheniramine significantly (P less than 0.001) reduced weal area. Both doses of dimethindene (P less than 0.001) and chlorpheniramine (P less than 0.05) also significantly reduced flare area. Dimethindene (6 mg) brought about the maximum reduction in weal area (28.8%) and flare area (39.1%). Dimethindene (6 mg) also reduced weal area significantly (P less than 0.01) compared with chlorpheniramine and reduced flare area significantly (P less than 0.05) compared with 3 mg dimethindene. Using a 100 mm visual analogue scale for assessment of weal and flare intensities, 6 mg dimethindene again produced the maximum response. The study confirmed that the antihistamine activity of dimethindene was better than that of chlorpheniramine.
Adult↗
Liver disease induced by perhexiline maleate.
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Chemical and Drug Induced Liver Injury↗
Rapid identification and quantification of chlorpheniramine maleate or pheniramine maleate in pharmaceutical preparations by thin-layer chromatography-densitometry.
Thin-layer chromatography (TLC)-densitometry was used to separate, identify, and quantitate chlorpheniramine maleate (CPM) and pheniramine maleate (PM) when present in combination with other drugs in pharmaceutical preparations of tablets, syrups, eye and ear drops, etc. CPM or PM was extracted (tablets, capsules, etc.) or diluted (liquid preparations, if needed) with 80% ethanol and isolated from other ingredients by TLC on silica gel G using cyclohexane-chloroform-methanol-diethylamine (4.5 + 4.0 + 0.5 + 1.0, v/v) as the mobile phase. Separated CPM and PM were detected under shortwave ultraviolet light and quantitated by scanning densitometry at 260 nm. Recoveries of CPM and PM were 100.09+/-0.77% and 100.09+/-0.87%, respectively.
Chlorpheniramine↗
Comparison of ranitidine, domperidone maleate and ranitidine + domperidone maleate in the short-term treatment of reflux oesophagitis.
In the treatment of reflux oesophagitis, either drugs preventing regurgitation of gastric juice in the lower oesophagus or pharmacological agents increasing the pH of the refluxing material are employed. In the present study 45 outpatients with reflux oesophagitis were randomly treated with either ranitidine (150 mg b.i.d.) or domperidone maleate (20 mg t.i.d.) or both drugs for six weeks. Before and after treatment the severity of dyspeptic symptoms and the grade of endoscopic and histological changes were assessed. The three therapeutic regimens were significantly and equally effective in inducing symptomatic relief and promoting endoscopic and histological disappearance or improvement of oesophagitis. The combined use of ranitidine and domperidone maleate failed to show any additional benefit compared with treatment with either drug alone.
Clinical Trials as Topic↗
Semiautomated method for the analysis of formulations of chlorpheniramine maleate and brompheniramine maleate.
The determination of chlorpheniramine maleate and brompheniramine maleate in tablets, capsules, injections, and elixirs has been automated. The active ingredient is dissolved in dilute HCl. The dilute acid solution is sampled, made basic with dilute NaOH, and extracted with isooctane. The isooctane phase is resampled and the drug is re-extracted into dilute HCl. The absorbance of the acidic aqueous layer is monitored at 265 nm. The method is an automated version of the general USP XIX assay for salts of organic nitrogenous bases. The results from the semiautomated procedure agree well with the USP XIX and NF XIV official methods. Recoveries were 100% from an authentic tablet material. The system is linear from 0 to 300% of declared potency. The procedure is free from common excipient and dye interferences. Precision data are included for both the automated and official methods.
Autoanalysis↗
Semiautomated analysis of ergonovine maleate or methylergonovine maleate tablets and injections by colorimetric or fluorometric systems.
Two semiautomated analytical systems have been developed to determine ergonovine and methylergonovine maleate in single tablets and injections. The active ingredient is dissolved in a tartrate buffer. In the fluorometric method the stream is automatically diluted with tartrate buffer and excited with ultraviolet light; the resulting fluorescence is measured and recorded. In the colorimetric method, the stream is automatically made basic with sodium hydroxide and extracted with n-butanol. The extract is mixed with p-dimethylaminobenzaldehyde reagent. After reaction, the solution is mixed with sodium nitrite solution, and the developed color is measured at 550 nm. Recoveries of 100% were obtained from spiked placebos. Standard deviations for powdered tablet and injection samples ranged from 0.63 to 1.24%. Comparisons with the USP XVIII methods are presented.
Autoanalysis↗
Evaluation of a new antipsychotic agent. Butaperazine maleate (repoise maleate).
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Animals↗