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At least 217 records · Page 12Linked to original sources
PubMed1993

Topical timolol maleate might adversely affect serum lipoproteins.

Conflicting observations have been reported about the effects of topically administered timolol maleate on serum lipoproteins. We therefore considered this issue in a series of eight glaucoma patients receiving timolol maleate. Cholesterol and triglycerides were measured in plasma and in low-density lipoproteins (LDL), and high-density lipoproteins (HDL), both before and following three months of treatment. Following the treatment, the mean atherogenic index was increased from 2.72 to 3.38 (p = 0.012). This suggests that the atherogenic index should be determined before and during timolol maleate treatment in high-risk cardiovascular patients.

Administration, Topical↗
PubMed1993

Effect of trimebutine maleate on emptying of stomach and gallbladder and release of gut peptide following a solid meal in man.

We investigated the effect of orally administered trimebutine maleate on gastric and gallbladder emptying and on the release of gut peptide, pancreatic polypeptide (PP), and gastrin in humans for 120 min after ingestion of a solid meal. Gastric emptying was measured by a radionuclide technique. Gallbladder emptying was estimated by real-time ultrasonography. The oral administration of 200 mg of trimebutine maleate significantly shortened the lag time in starting gastric emptying (P < 0.05). Considering gallbladder emptying, trimebutine significantly inhibited the fasting emptying induced by neural reflex. Postprandially, there was a tendency toward an accelerated gallbladder emptying in the early phase. Neither the maximal percentage of gallbladder emptying nor the time of peak gallbladder emptying were affected. Trimebutine significantly blunted the post-prandial PP response in the cephalic and gastric phases, reflecting a vagal-cholinergic activity (P < 0.05). The PP response in the intestinal phase was also blunted. Gastrin release was significantly augmented only during the period of fasting after drug administration (P < 0.05). The major effect of trimebutine maleate appears to be a shortening of the lag time at the start of gastric emptying probably via its anticholinergic activity.

Administration, Oral↗
PubMed1978

Pharmacokinetics of perhexiline maleate in anginal patients with and without peripheral neuropathy.

Perhexiline maleate (Pexid) which has been in general use in France with good results for the treatment of angina pectoris since 1973, may be associated with severe side effects including peripheral neuropathy. The present study is a comparison of the pharmacokinetics of perhexiline maleate in anginal patients with and without signs of peripheral neuropathy. Compared to the latter, those with neuropathy had higher plasma levels of perhexiline, slower hepatic metabolism and a longer plasma half-life. Thus, peripheral neuropathy associated with perhexiline maleate treatment appears to be a direct toxic effect due to accumulation of the drug. The accumulation might result either from a decreased volume of distribution secondary to a loss of body weight, possibly drug-induced, or to slow hepatic metabolism of perhexiline of genetic origin or due to hepatic disease, possibly drug-induced. The neuropathy is rarely an isolated event, as it is often associated with one or more adverse effects of perhexiline.

Aged↗
PubMed1988

Teratological and cytogenetical evaluation of two antihistamines (pipethiadene and pizotifen maleate) in mice.

The teratogenic and cytogenetic effects of two drugs with antihistamine properties, Pipethiadene and Pizotifen maleate, were investigated. Three groups of pregnant mice were treated daily with oral doses (0.24, 0.6 and 1.2 mg/kg) of these drugs from day 4 to day 16 of gestation. The following parameters were investigated: reproductive health of the dams, external, skeletal and visceral malformations of fetuses and frequencies of micronuclei and chromosome aberrations in bone marrow cells of dams. Oral administration of Pipethiadene or Pizotifen maleate produced no teratogenic effects. No elevation was observed in the frequencies of micronuclei and chromosome aberrations. However, the significant reduction of fetal weight after all doses of Pipethiadene or Pizotifen maleate was found to correlate well with the decreased values of the mitotic indices of bone marrow cells of mice, suggesting a potential embryotoxic effect of the tested substances.

Animals↗
PubMed1991

Effects of irsoglandine maleate in an experimentally-induced acute hepatic failure model using mice.

When heat-killed Propionibacterium acnes was intravenously injected into mice followed by an intravenous injection of a small amount of Gram-negative lipopolysaccharide seven days later, most of the mice died of massive hepatic cell necrosis within 24 hours. However, when irsoglandine maleate, an anti-ulcer agent, was administered to mice during the period of experimental induction of acute hepatic failure, the survival rate, serum transaminase levels and histological changes of the liver remarkably improved. These results suggested that irsoglandine maleate may have protective effects on the liver in our experimentally-induced acute hepatic failure model using mice. Therefore, in the absence of a definitive therapy for fulminant hepatitis, irsoglandine maleate may be a promising therapeutic agent.

Animals↗
PubMed1999

The dopamine D3 antagonist U-99194A maleate increases social behaviors of isolation-induced aggressive male mice.

RATIONALE: Blockade of D1/D2 dopamine receptors produce an antiaggressive action commonly associated with an impairment of other motor behaviors. The D3 receptor seems to present opposite actions to the D1 and D2, since the blockade of this receptor produces stimulation of motor activity which has been associated with an increase in dopamine neurotransmission. OBJECTIVE: In this work, the action of the dopamine D3 antagonist U-99194a maleate on locomotor activity and in a social interaction test in male mice was evaluated. METHODS: Animals isolated during 30 days were treated with U-99194a maleate (20-40 mg/kg) or saline and locomotor activity was measured 20 min after drug administration. The behavioral interaction test was performed afterwards, between the experimental isolated animal and a standard opponent. RESULTS: The higher dose used produces a significant decrease in spontaneous motor activity and presents an antiaggressive action without impairment of other behaviors, such as nonsocial exploration or immobility. At all doses tested, U-99194a maleate significantly increases social investigation. CONCLUSIONS: Our results give support to the hypothesis that the D3 receptor could play a role in emotional behaviors.

Aggression↗
PubMed1979

Evaluation of timolol maleate combination therapy in chronic open-angle glaucoma.

In an eight-week study, timolol maleate ophthalmic solution 0.25% was administered twice daily with either pilocarpine 2% four times a day, epinephrine 2% twice a day, carbachol 1.5% four times a day, or 250 mg of acetazolamide twice a day to 44 patients with chronic open-angle glaucoma. Compared to baseline readings on standard therapy alone, mean intraocular pressure was significantly reduced after addition of timolol maleate to each of the regimens. Mean facility of outflow was unaffected. No clinically significant ocular irritation or changes in visual acuity, pupil size, or vital signs were observed in any patient. Timolol maleate appears to be effective and well tolerated when administered with other antiglaucoma medications in patients with open-angle glaucoma.

Acetazolamide↗
PubMed1981

Safety and effectiveness of concomitant administration of dipivefrin and timolol maleate.

Dipivefrin, an epinephrine prodromal drug, was used in conjunction with timolol maleate to evaluate the safety and effectiveness of combined therapy. Seventeen patients who had used timolol maleate for at least six months added dipivefrin (Group 1) and seven patients who had used dipivefrin for at least six months added timolol maleate (Group 2). Intraocular pressure decreased further in both groups. Side effects were most prominent in Group 1.

Adult↗
PubMed1986

Interactions of perhexiline maleate and arylalkylamine derivatives with cytochrome P-450 and in-vitro hydroxylation.

In order to find a substitute for perhexiline maleate, an antiangina drug, for which several side effects due to poor hydroxylation have been reported, an arylalkylamine series with antianginal properties has been synthesized. The aim of the present work was to select a more rapidly hydroxylated compound than perhexiline maleate in this series. Two criteria have been retained. The binding of the molecules to liver microsomal cytochrome P-450 and their rate of hydroxylation were both studied in vitro using phenobarbital induced rat liver microsomes. Incubation with cofactors and extraction procedures have been tested on one of the molecules of the series taken as example: N-2-dicyclohexyl-2-phenethylamine. All of the molecules tested in the series substrates were type I substrates; nevertheless, no correlation was found between binding on cytochrome P-450 and oxidative metabolism of the drugs. Two of the studied molecules were more easily hydroxylated than the others and than perhexiline maleate: (N-2-dicyclohexyl-2-phenethylamine) and (II) (N-cyclohexyl-2-diphenylethylamine) with the following respective kinetics: Apparent Vmax: 0.073 and 0.32 units, apparent Km: 6.9 X 10(-5) M and 22.2 X 10(-5) M.

Animals↗
PubMed1984

Prolactin and luteinizing hormone levels of prelaying, laying and postlaying turkey hens following central administration of serotonin and peripheral administration of quipazine maleate.

The influence of serotonin (5-HT) on plasma prolactin and LH levels in female turkeys was studied by systemic injection of quipazine maleate, at 5-HT agonist, or by cerebroventricular injection of 5-HT itself. Within 30 min after injection, quipazine maleate (20 mg administered i.p.) elicited a significant increase in plasma prolactin in hens approaching sexual maturity as well as in laying hens. A 5-mg dose. had no effect on prolactin levels of either prelaying or laying hens. Intraventricular injection of 5 and 25 micrograms of 5-HT caused an increase in plasma prolactin of prelaying hens. A 5-micrograms dose of 5-HT was also effective in increasing prolactin levels in laying hens and in hens that had stopped laying due to ventricular cannula implantation. Neither quipazine maleate nor intraventricularly injected 5-HT had an effect on LH levels in any experiment.

Animals↗
PubMed1984

The mammalian spot test and its use for testing of mutagenic and carcinogenic potential: experience with the pesticide chlordimeform, its principal metabolites and the drug lisuride hydrogen maleate.

The mammalian spot test has recently been demonstrated to be a promising method for the detection of somatic mutations induced by chemicals and is at present under validation as an in vivo screening test for carcinogenic potential. The pesticide chlordimeform, its principal metabolites N-formyl-4-chloro-o-toluidine and 4-chloro-o-toluidine, and the drug lisuride hydrogen maleate, as well as the known mutagens ethyl methanesulfonate (EMS) and N-ethyl-N-nitrosourea (ENU) were tested in the mammalian spot test. Female C57BL/6J mice were mated to T-stock males and treated by gavage with maximal tolerated doses of the test compounds, or by intraperitoneal injection with EMS and ENU at days 8, 9 and 10 of pregnancy. Mutation induction was monitored post-natally by checking the fur of the offspring for color spots that result from expression of a recessive gene involved in coat-color determination. Of the environmental chemicals tested, only 4-chloro-o-toluidine was mutagenic in the spot test. This positive result was in agreement with in vitro experiments and its carcinogenic potential in the mouse. However, the mouse carcinogens chlordimeform and N-formyl-4-chloro-o-toluidine were negative, as was the non-carcinogen lisuride hydrogen maleate. N-Formyl-4-chloro-o-toluidine and lisuride hydrogen maleate have been reported to be weakly positive in the Ames test. The positive controls EMS and ENU showed a clear mutagenic response.

Amidines↗
PubMed2006

Spectrophotometric determination of carbinoxamine maleate in pharmaceutical formulations by ternary complex formation with Cu(II) and eosin.

A simple and sensitive spectrophotometric method was developed for the determination of carbinoxamine maleate in pharmaceutical formulations. The method is based on the formation of a ternary complex, extractable with chloroform, between copper(II), eosin, and carbinoxamine maleate. The absorption spectra of the ternary complexes shows, under optimum conditions, a maxima at 538 nm, with apparent molar absorptive 6.1690 x 10(4) mol(-1) cm(-1), Sandell's sensitives 6.75 x 10(-3) microg cm(-2), and linearity in the concentration range 0.75-10.0 microg ml(-1). The method can be achieved with high accuracy (recovery values, 100 +/- 2%) and precision (with standard deviation 0.029-0.155 and relative standard deviation 3.87-1.55%). The method was again successfully applied, with high accuracy and good precision, for the determination of carbinoxamine maleate in various pharmaceutical formulations (syrup, drops, and tablets).

Chemistry, Pharmaceutical↗
PubMed2005

Improved pharmacodynamics of timolol maleate from a mucoadhesive niosomal ophthalmic drug delivery system.

In the present study chitosan (REVTMbio1) or Carbopol (REVTMbio2 and 3) coated niosomal timolol maleate (0.25%) formulations were prepared by reverse phase evaporation (REV) and compared to timolol solution (TMS; 0.25%) in terms of in vitro release and IOP lowering pharmacodynamic effect. The in vitro release phase of timolol (91% release in 2 h) was extended significantly by its incorporation into niosomes and further by the polymer coating (40-43% release upto 10 h). The developed formulations were evaluated for their pharmacodynamics in albino rabbits, by measuring intraocular pressure (IOP) using a non-contact pneumatonometer, and were compared to a marketed in situ gel forming solution of timolol (Timolet GFS, 0.5%; Sun Pharma). REVTMbio1 formulation showed a more sustained effect of upto 8h (vis a vis 6 h for carbopol-coated niosomes). TMS in comparison showed effect for only 2 h though the peak effect was slightly more (14%). Lowering of IOP in the contralateral eye (20-40% as compared to 100% in case of TMS), considerably reduces with REV and REVbio formulations indicating lesser systemic side effects. Moreover, the results of REVTMbio1formulation containing 0.25% of timolol maleate compared well with the 0.5% marketed gel formulation, indicating our formulation to be significantly better considering that similar effect is obtained at half the concentration. The later becomes especially important in context to the cardiovascular side effects associated with ocular timolol maleate therapy.

Adhesives↗
PubMedDate not supplied

Clinical evaluation of a new formula of timolol maleate (WP-934 ophthalmic solution). WP-934 Study Group.

We investigated the ocular hypotensive effect and possible adverse reactions of a new timolol maleate formula, WP-934 ophthalmic solution, which is timolol maleate solution dissolved in a reversible thermo-setting gel. Once-daily instillation of 0.25 or 0.5% WP-934 ophthalmic solution was administered in a prospective, randomized manner at 29 institutions for 8 weeks to patients with primary open-angle glaucoma or ocular hypertension, and for another 16 weeks in a limited number of these patients. Patients were closely monitored throughout the study by ophthalmic and systemic examinations, and by continuous evaluation of symptoms. The new timolol formula demonstrated a significant ocular hypotensive effect throughout the study period. Adverse effects were minor. WP-934 ophthalmic solution, timolol maleate dissolved in a reversible thermo-setting gel, has a significant ocular hypotensive effect in eyes with primary open-angle glaucoma and ocular hypertension.

Administration, Topical↗
PubMed2000

Quantitative analysis of chlorpheniramine maleate and phenylephrine hydrochloride in nasal drops by differential-derivative spectrophotometric, zero-crossing first derivative UV spectrophotometric and absorbance ratio methods.

Three simple, rapid and accurate methods are described for the simultaneous determination of chlorpheniramine maleate and phenylephrine hydrochloride in two component mixtures. The first method comprised of measurement of difference absorptivities derivatized in first order of a nasal drops in 0.1 N NaOH relative to that of an equimolar solution in methanol at wavelengths of 271.6 and 250.2 nm, respectively. The second method, zero-crossing derivative spectrophotometry, is based on recording the first derivative curves and determining each component using the zero-crossing technique. Using first derivative spectrophotometry, the amplitudes in the first derivative spectra at 246.5 and 238.6 nm were selected to simultaneously determine chlorpheniramine maleate and phenylephrine hydrochloride in the mixture. The presence of identical zero-crossing points for pure drugs and nasal drop solutions established the non-interference of the excipients in the absorption at these wavelengths. Absorbance ratio method was also developed for a comparison method. The proposed procedures were successfully applied to the determination of chlorpheniramine maleate and phenylephrine hydrochloride in nasal drops, with a high percentage of recovery, good accuracy and precision.

Anti-Allergic Agents↗
PubMed2002

Simple and sensitive method for the determination of chlorpheniramine maleate in human plasma using liquid chromatography-mass spectrometry.

A convenient liquid chromatographic-single quadrupole mass spectrometric (LC-MS) method was developed and validated for the determination of chlorpheniramine maleate (INN name: chlorphenamine) in human plasma. The method had advantages of a single liquid-liquid extraction with diethylether and high sensitivity. The linearity was also excellent over the concentration range of 0.52-20.8 ng/ml of chlorpheniramine maleate. The intra- and inter-day precision and accuracy ranged between 0.0 and 13.9%, showing a good reproducibility. This developed method was successfully applied to analysis of chlorpheniramine maleate in clinical studies.

Chlorpheniramine↗
PubMedDate not supplied

Production of starch foams by twin-screw extrusion: effect of maleated poly(butylene adipate-co-terephthalate) as a compatibilizer.

Free-radical-initiated grafting of maleic anhydride (MA) onto poly(butylene adipate-co-terephthalate) (PBAT), a biodegradable aliphatic-aromatic copolyester, was performed by reactive extrusion. 2,5-Dimethyl-2,5-di(tert-butylperoxy)hexane was used as the free-radical initiator. The peroxide concentration was varied between 0.0 and 0.5 wt % at 3.0 wt % MA concentration; the MA concentration was varied between 1.0 and 5.0 wt % at 0.5 wt % peroxide concentration. The reaction temperature was maintained at 185 degrees C for all experiments. Under these conditions, between 0.194% and 0.691% MA was grafted onto the polyester backbone. Size-exclusion chromatography, melt flow index, intrinsic viscosity measurements, thermal gravimetric analysis, and differential scanning calorimetry were used to characterize the maleated copolyester. Increasing the initiator concentration at a constant MA concentration of 3% resulted in an increase in the grafting of MA while decreasing the molecular weight of the resulting polymer. Increasing the feed MA concentration also increased the grafting percentage. The maleation of the polyester proved to be very efficient in promoting strong interfacial adhesion with high amylose cornstarch in starch foams as prepared by melt blending. Thus, the use of maleated copolyester as a compatibilizer between starch and PBAT allowed the reduction of the density of resulting starch foams to approximately 21 kg/m3 and improved the resilience from 84% to as high as 95%. Also, the resulting starch foams exhibited improved hydrophobic properties in terms of lower weight gain and higher dimensional stability on moisture sorption.

Biodegradation, Environmental↗
PubMed1992

Correlation of in vitro release rate and in vivo absorption characteristics of four chlorpheniramine maleate extended-release formulations.

An in vitro/in vivo correlation was established for four formulations of chlorpheniramine maleate (histamine, H1-blocker) extended-release tablets exhibiting different in vitro release rate characteristics. In vitro release rate data were obtained for 12 individual tablets of each formulation using the USP Apparatus 2, paddle stirrer at 50 rpm in 1000 ml of distilled water at 37.0 +/- 0.5 degrees C. Inspection of the individual and mean release rate data indicated that the in vitro release rate of chlorpheniramine maleate was consistent with the intended design of the four extended-release formulations. The in vivo bioavailability and pharmacokinetics of these formulations were evaluated in 24 healthy subjects under fasting conditions. Wagner Nelson analyses of the in vivo data revealed extended release absorption profiles for all four formulations. Linear regression analyses of the mean percentage of dose absorbed versus the mean in vitro release resulted in a statistically significant correlation (r2 greater than 0.98, P less than 0.001) for each formulation. Qualitative rank-order correlations were observed among all combinations of in vitro and in vivo parameters. These data support a Level A correlation between the in vitro release rate profiles and the in vivo absorption for chlorpheniramine maleate determined under fasting conditions.

Adult↗