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At least 343 records · Page 19Linked to original sources

Flow-injection chemiluminescence determination of enalapril maleate in pharmaceuticals and biological fluids using tris(2,2'-bipyridyl)ruthenium(II).

A chemiluminescence (CL) method using flow injection (FI) has been investigated for the rapid and sensitive determination of enalapril maleate. The method is based on the CL reaction of the drug with tris(2,2'-bipyridyl)ruthenium(II), Ru(bipy)3(2+) and acidic potassium permanganate. After selecting the best operating parameters, calibration graphs were obtained over concentration ranges of 0.005-0.2 microg/ml and 0.7-100 microg/ml with a detection limit (S/N=2) of 1.0 ng/ml. The average % found was 99.9 +/- 0.7 and 100.2 +/- 0.3 for the two concentration ranges respectively. %RSD (n=10) for 5.0 microg/ml was 0.44. The method was successfully applied to the determination of enalapril maleate in dosage forms and biological fluids without interferences.

2,2'-Dipyridyl↗

Effect of topical administration of 2% dorzlamide hydrochloride or 2% dorzlamide hydrochloride-0.5% timolol maleate on intraocular pressure in clinically normal horses.

OBJECTIVE: To evaluate the effect of topical administration of 2% dorzolamide hydrochloride or 2% dorzolamide hydrochloride-0.5% timolol maleate on intraocular pressure (IOP) in clinically normal horses. ANIMALS: 18 healthy adult horses without ocular abnormalities. PROCEDURE: The IOP was measured at 5 time points (7 AM, 9 AM, 11 AM, 3 PM, 7 PM) over 11 days. On days 1 and 2, baseline values were established. On days 3 through 5, horses received 2% dorzolamide HCI (group D, n = 9) or 2% dorzolamide HCl-0.5% timolol maleate (group DT, 9) in 1 randomly assigned eye every 24 hours immediately following each daily 7 AM IOP measurement. On days 6 through 9, each drug was given every 12 hours (7 AM and 7 PM) in the treated eye. Measurements on days 10 and 11 assessed return to baseline. Mixed linear regression models compared mean IOP difference for each drug at each time period. RESULTS: Mean IOP decreased significantly in all eyes during the 2 dose/d period, compared with the baseline, 1 dose/d, and follow-up periods. CONCLUSIONS AND CLINICAL RELEVANCE: Administration of either drug every 24 hours for short-term treatment does not reduce IOP significantly. Administering either drug every 12 hours induced a significant reduction of IOP; however, controlling for all variables, the reduction was less than 2 mm Hg.

Administration, Topical↗

[Therapeutic effect of lisuride maleate on post-stroke depression].

Twenty post-stroke depressive patients who obtained more than 11 points on Self-Rating Questionnaire for Depression, were treated with 0.075 mg/day lisuride maleate for 12 weeks. The drug effect on depression was evaluated quantitatively by the Hamilton Rating Scale for Depression. The relationships between brain CT or MRI and SRQ-D score were investigated in 24 subjects. More than 80% of post-stroke depressive patients improved after lisuride maleate treatment for 8 or 12 weeks. In particular, depressed mood, hypobulia, sleep disturbance, anxiety, etc. were significantly improved compared to the baseline condition. As for the relationships with CT and/or MRI findings, the group with moderate to severe brain atrophy had a significantly higher grade of depressive state than those without.

Aged↗

A double-blind trial of perhexiline maleate in the prophylaxis of angina pectoris.

Perhexiline maleate, which has no beta adreno-receptor-blocking activity, has been suggested as an effective prophylactic agent for angina pectoris. The effects of perhexilline were compared with those of placebo by a double-blind crossover trial in seven patients with moderate to severe angina pectoris. Attack rates and glyceryl trinitrate consumption were significantly lower during the perhexilline phase than during the placebo phase of treatment. There was also a mild fall in resting heart rate. Three patients who had failed to respond to beta adrenoreceptor-blocking drugs, and one who had suffered reccurrence of symptoms after coronary artery surgery responded favourably to perhexiline. It thus appears that perhexiline maleate is an effective and potentially valuable agent in this condition.

Adult↗

[Analysis of paracetamol, caffeine and chlorphenamine maleate in suxiaoshangfeng capsules by capillary gas chromatography].

A simple and rapid method for simultaneous determination of paracetamol, caffeine and chlorphenamine maleate in Suxiaoshangfeng capsule by capillary gas chromatography with n-hexadecane as internal standard has been reported. In the capsule, the three components can be separated on a 5% Ph-Me-Silicone column (2.65 microns x 0.53 mm x 10 m), with programmed column temperature from 180 degrees C to 230 degrees C at 8 degrees C/min, hold 6 min and then 230 degrees C to 260 degrees C at 10 degrees C/min, hold 10 min. Both the injector and FID detetor temperatures were 280 degrees C. N2 flow rate was 3.5 mL/min and H2 35 mL/min. The injection volume was 1 uL with splitting ratio of 1/25. These components were identified by their retention times and quantitatively determined by their peak areas. The calibration curves were, r = 0.9996 for paracetamol, r = 0.9984 for caffeine and r = 0.9996 for chlorphenamine maleate. The linear ranges were 4.0-20 g/L, 0.15-0.75 g/L and 0.080-0.40 g/L, respectively. The average recoveries were 99.62% (RSD = 0.40%, n = 5), 96.46%. (RSD = 1.32%, n = 5) and 98.55% (RSD = 0.65%, n = 5), respectively.

Acetaminophen↗

A comparative evaluation of therapeutic effects of once a day dose of losartan potassium versus enalapril maleate in mild to moderate essential hypertension.

Hypertension is a major public health problem both in the developing and developed countries of the world and if untreated, can lead to various fatal complications like cerebral stroke, encephalopathy, ischaemic heart disease (IHD), renal failure and sudden cardiac death, etc. In the present study, a comparative evaluation was made between angiotensin-II receptor antagonists like losartan potassium (50 mg daily) and angiotensin converting enzyme (ACE) inhibitors like enalapril maleate (5 mg daily) in 100 patients (50 males and 50 females having 25-50 years of age) of mild to moderate essential hypertension with diastolic blood pressure (DBP) 90-109 mmHg. Both the drugs were tried as monotherapy for their clinical efficacy, safety, tolerability and adverse effect profile in this open trial. Losartan potassium lowered the DBP to <90 mmHg in 62% of the patients at the end of 8 weeks compared to 40% in the enalapril group. Percentage of side effects with losartan was 20 and 50 with enalapril. It is concluded that both the drugs are effective antihypertensive agents and cause significant and comparable fall in systolic blood pressure (SBP) and DBP in patients of mild to moderate essential hypertension. But losartan potassium has been found to be more effective with fewer side effects when compared to enalapril maleate.

Adult↗

Evaluation of the local anaesthetic activity of dimetindene maleate by means of laser algesimetry in healthy volunteers.

Dimetindene maleate (DMM, Fenistil, CAS 3614-69-5) a specific H1-receptor antagonist, is therapeutically used for the treatment of respiratory allergies, urticaria, itching dermatoses and generally pruritic sensations occurring with various diseases. As it exhibits local anaesthetic activity in the rabbit cornea and the local anaesthetic activity of a couple of H1-antagonists was found to be linearly correlated to the H1-potency represented by the pA2-values--and dimethindene maleate demonstrates a high pA2-value--it seemed worth investigating the local anaesthetic potency in man making use of an objective and well validated pain model, the Laser algesimetry. The study was carried out with 24 healthy volunteers in a double-blind placebo- and reference-controlled, randomized, cross-over design. Three different medications were applied with occlusive dressing: DMM, lidocaine, and placebo. Selective thermo-noxious stimulation of A-delta- and C-fibers was induced by a CO2-laser. Somato-sensory evoked vertex potentials (SEPs) were simultaneously recorded. Both verum treatments showed a remarkable analgesic potency compared to placebo. Effects were preferably concentrated on the peripheral N1-component of the SEPs. The overall means of the N1-amplitudes were suppressed compared to placebo by both active drugs, with the effects being more pronounced for DMM.

Adolescent↗

The effect of varying concentrations of ergometrine maleate on the pituitary prolactin of the lizard, Uromastix hardwickii.

Present study deals with the effect of ergometrine maleate on prolactin (PRL) of Uromastix pituitaries. Administration of 0.02, 0.04 and 0.06 mg/day/animal ergometrine maleate for 3 days to individuals of 3 respective groups resulted in decreased pigeon crop-sac diametric response. Intramuscularly treated pituitaries showed more PRL inhibition than the pituitaries of animals treated intravenously.

Journal Article↗

[Dimethindene maleate administered via intramuscular route in man: local and systemic tolerance].

Local and systemic tolerance of dimethindene maleate was studied in 10 healthy volunteers by the intramuscular route (4 mg in 4 ml solvent). Subjective perception of pain and other reported side effects were registered and objective signs at the injection site were assessed repeatedly. Hematologic and biochemical tests were performed before and after completion of the study. Two volunteers complained about local pain immediately and one hour after the injection. An other volunteer developed a small hematoma within 48 hours after injection. No other side effects or adverse reactions were noted. Good tolerance of dimethindene maleate after intramuscular application could thus be established.

Adult↗

Effect of two weeks of timolol maleate treatment on the normal retinal circulation.

The effect of 2 weeks of topical treatment with timolol maleate 0.5% ophthalmic solution on the retinal circulation was investigated using bidirectional laser Doppler velocimetry and monochromatic fundus photography. Fifteen normal healthy volunteers were included in this study. In a double-masked, randomized design one eye of each received one drop of timolol maleate 0.5% twice daily for 14 days, and the fellow eye received placebo. Vessel diameter (D), maximum erythrocyte velocity (Vmax), and volumetric blood flow rate (Q) were determined in one major retinal vein of each eye before treatment, and then, 2 hr after the instillation of drops on the morning of the 15th day of treatment. After treatment, the average change from baseline in D (+0.7%), Vmax (-8.2%) and Q (-7.7%) were not statistically significant in the placebo-treated eyes. In the timolol-treated eyes, the average increase from baseline in D (+0.1%) and Q (+10%) were not statistically significant. Average Vmax, on the other hand, increased significantly from baseline (P less than 0.05) by 9.6%. In comparison to the placebo-treated eyes, Vmax and Q were significantly increased in the timolol-treated eyes (P less than 0.0005 and P less than 0.01, respectively). These results are similar to those reported previously in a study of the effect of a one-time instillation of timolol and, therefore, suggest that the effect of timolol on the retinal circulation is maintained over a 2-week period.

Administration, Topical↗

Effects of topical administration of timolol maleate on intraocular pressure and pupil size in dogs.

Effects of topical administration of a single dose of timolol maleate on intraocular pressure (IOP) and pupil diameter were evaluated in normotensive eyes of 11 clinically normal dogs over 12 hours (7:00 AM to 7:00 PM). Mean (+/- SEM) normal IOP was 15.5 (+/- 1.1) mm of Hg and diurnal fluctuation was observed, with the highest IOP seen in the morning. Mean normal pupil diameter was 8.5 (+/- 0.3) mm. Topical treatment with 0.5% timolol resulted in reduction of IOP in the treated and nontreated eyes. Mean reduction of IOP in the treated eye was 2.5 mm of Hg, a reduction of 16.1%, with maximal reduction of 3.7 mm of Hg. Mean reduction of IOP in the nontreated eye was 1.4 mm of Hg, a reduction of 9.0%. The treated eye had reduced pupil diameter at 30 minutes after treatment, which persisted throughout the 12 hours of the study. Mean reduction of pupil diameter in the treated eye was 2.9 mm, a reduction of 34.1%. In addition, a contralateral effect on pupil diameter was seen in the nontreated eye, with mean reduction of 1.2 mm, a reduction of 14.1%. Topical administration of timolol maleate resulted in reduction of IOP and pupil diameter in treated and contralateral eyes, thus supporting the use of timolol for treatment of glaucoma in dogs. Miosis indicates possible beta-adrenergic inhibition or alpha-adrenergic activation of the sphincter muscle. beta-Adrenergic blockade would then result in miosis.

Administration, Topical↗

Effects of topical administration of timolol maleate on intraocular pressure and pupil size in cats.

Effects of topical administration of a single dose of timolol maleate, a nonselective beta-adrenergic blocking agent, on intraocular pressure (IOP) and pupil diameter were evaluated in the normotensive eyes of 10 clinically normal cats over 12 hours. Mean (+/- SEM) normal IOP was 17.1 (+/- 1.1) mm of Hg and diurnal fluctuation was observed, with the highest IOP seen in the evening. Mean (+/- SEM) normal pupil diameter was 10.1 (+/- 0.5) mm. Topical treatment with 0.5% timolol resulted in reduction of IOP in treated and nontreated eyes. This effect was time-dependent and was first observed at 6 hours after treatment. Mean reduction of IOP was 22.3% in the treated eye and 16.3% in the nontreated eye. The treated eye had reduced pupil diameter at 30 minutes after treatment, and miosis persisted throughout the 12 hours of the study. Mean reduction of pupil diameter was 38.7%. A contralateral effect on pupil diameter was not seen in the nontreated eye. Topical administration of timolol maleate results in a reduction of IOP in treated and contralateral eyes, which supports the use of timolol for treatment of glaucoma in cats. In addition, the treated eye becomes miotic. This effect may indicate beta-adrenergic inhibition or alpha-adrenergic activation of the iris sphincter muscle. beta-Adrenergic blockade would then result in miosis.

Administration, Topical↗

Effect of timolol maleate on the retinal circulation of human eyes with ocular hypertension.

We studied the effect of topical timolol maleate 0.5% on the retinal circulation of eyes with ocular hypertension using laser Doppler velocimetry and monochromatic fundus photography. Patients with ocular hypertension had normal eye examinations and had documented elevated intraocular pressures of 23 mmHg or higher on two or more separate occasions. In a double-masked randomized design, one eye of each subject received timolol maleate 0.5% and the fellow eye received placebo. Vessel diameter, maximum velocity of red blood cells, and volumetric blood flow rate were determined in a major retinal vein of each eye just prior to the instillation of drops, and then 2 hr later. In comparison to the baseline value, there was an increase of 12.0% in average red blood cell velocity (P less than 0.005, statistically significant) and of 8.4% in volumetric blood flow rate in the timolol-treated eyes (P less than 0.05, statistically significant). No significant changes in these quantities were observed in the placebo-treated eyes. Also, no significant change in venous diameter was detected in the placebo- and the timolol-treated eyes. In comparison to the baseline, a significantly larger increase in red blood cell velocity was observed in the timolol-treated eyes than in the placebo-treated eyes (P less than 0.05). The difference between the increase in blood flow observed in the timolol-treated eyes and the placebo-treated eyes achieved a probability value of P = 0.058. The increase in blood flow observed in the timolol-treated eyes may be related to the increase in perfusion pressure produced by this drug.

Administration, Topical↗

Determination of chlorpheniramine maleate, dihydrocodeine bitartrate and ephedrine hydrochloride in cough mixture by derivative and differential spectrometry.

A method is presented for the determination of chlorpheniramine maleate, dihydrocodeine bitartrate and ephedrine hydrochloride in a three-component mixture without prior separation. Chlorpheniramine maleate was determined by the first and second derivative-differential spectrophotometry, while dihydrocodeine bitartrate was directly determined using first and second derivative measurements. Ephedrine hydrochloride could be determined by first and second derivative spectrophotometry after its oxidation with sodium metaperiodate. The method was proved using synthetic mixtures of these drugs and was applied for their determination in syrup with a coefficient of variation less than 2%.

Antitussive Agents↗

Effect of topical timolol maleate on the ophthalmic artery blood pressure.

The effects of topical timolol maleate 0.5% on the ophthalmic artery diastolic (OABPd), systolic (OABPs) and mean blood pressure (OABPm) were investigated in 19 healthy subjects using compression ophthalmodynamometry. In a randomized, double-blind study, one eye of each subject received one drop of timolol maleate 0.5% and the fellow eye received a drop of placebo. Measurements of OABPd and OABPs were performed just prior to instillation of the drops, and then 2 hr later. OABPm was calculated as OABPm = OABPd + 1/3 (OABPs - OABPd). No significant changes in OABPd, OABPs or OABPm were observed following the drops in the timolol-treated eyes or in the placebo-treated eyes. A significant difference (P = 0.0198) was found, however, when the changes in OABPm occurring in the timolol-treated eyes were compared with the changes occurring in the placebo-treated eyes, suggesting that the drug may have an effect upon ophthalmic artery pressure and retinal artery pressure that is expressed differently in each eye.

Administration, Topical↗

Effect of chloropheniramine maleate on liver and kidney functions as well as blood count of guinea pigs.

The present study aimed at exploring the effect of antihistamine chloropheniramine maleate (H1-blocker) on liver and kidney functions as well as on blood count. 60 mature guinea pigs were used. Histamine or chloropheniramine maleate was given, either alone or together, intramuscularly for 7 successive days. At the end of the experimental period, blood samples were collected for determination of blood counts and of the levels of urea, creatinine, GOT, GPT, and alkaline phosphatase in the sera of different groups. The results showed significant groupwise variations in blood count, liver function as well as kidney function.

Animals↗

The influence of dimetindene maleate on the endogenous hydrocortisone synthesis suppressing potency of betamethasone.

Plasma hydrocortisone (cortisol) levels in 7 healthy volunteers were measured following administration of 0.25 mg betamethasone or 0.25 mg betamethasone and 1 mg dimetindene maleate. The H1-receptor antagonist dimetindene maleate did not influence the hydrocortisone suppressing activity of betamethasone, which was proved by comparison with the published plasma hydrocortisone levels of 162 young healthy untreated volunteers.

Adult↗