Maleate Group Research Articles

Effects of carteolol and timolol on plasma lipid profiles in older women with ocular hypertension or primary open-angle glaucoma

PURPOSE: To determine the effect on serum lipid levels of carteolol hydrochloride 1.0% or timolol maleate 0.5% given twice a day to women age 60 years and older with primary open-angle glaucoma or ocular hypertension.METHOD: We included 112 patients in this double-masked, randomized, multicenter trial. Fasting clinical laboratory studies were evaluated at baseline and at 12 weeks. Patients were instructed not to change their dietary, alcohol consumption, or exercise habits during the study.RESULTS: For the carteolol group, the high-density lipoprotein (HDL) and total cholesterol/high-density lipoprotein (TC/HDL) ratio at baseline of 50.1 ± 1.5 mg/dl and 4.7 ± 0.2 changed by the 12-week visit to 51.3 ± 1.9 mg/dl (P = .25) and 4.6 ± .02 (P = .47), respectively. For the timolol maleate group, the baseline HDL and TC/HDL ratio of 53.6 ± 2.2 mg/dl and 4.4 ± 0.2 changed to 50.2 ± 1.9 mg/dl (P < .001) and 4.7 ± 0.2 (P = .001), respectively, at the 12-week visit. Carteolol patients showed no significant change from baseline, whereas the HDL (P < .001) and TC/HDL ratio decreased (P = .001) significantly in the timolol maleate group. There also was a significant difference in the change from baseline at 12 weeks between carteolol and timolol maleate groups for the HDL and TC/HDL ratio (P = .01 and .012, respectively). No differences in TC, low-density lipoprotein (LDL), or triglycerides (TG) or in changes from baseline were observed between groups at 12 weeks (P > .05). At 12 weeks, no differences were observed between carteolol and timolol maleate groups in intraocular pressure or safety (P > .05), except that patients given carteolol demonstrated fewer solicited ocular symptoms (P = .007).CONCLUSIONS: Carteolol appears to be neutral in its effect on serum lipid levels, whereas timolol maleate adversely affects the HDL and TC/HDL ratio in women age 60 years and older with ocular hypertension or primary open-angle glaucoma.

Functionalization of poly(organophosphazenes), 10. Thermally induced grafting reactions of maleates containing oxazoline groups onto aryloxy-substituted poly(organophosphazenes)

The functionalization reaction of aryloxy-substituted poly(organophosphazenes) with variable amounts of oxazoline groups is described as a function of different experimental parameters, such as the reaction time and temperature, the concentration of the peroxide initiator and of the oxazoline-containing maleate group, the solvent used to run the process and the type of substituents attached to the polyphosphazene skeleton. The resulting phosphazene grafted copolymers were characterized by IR and NMR ( 1 H, 13 C and 31 P) spectroscopy and by thin layer chromatography. These materials are successively reacted with poly(methacrylic acid) due to the well known reactivity of the oxazoline residues with carboxylic functions, to form new materials in which the inorganic and the organic macromolecules are linked together through genuine covalent bonds formed by ester-amide structures.

Functionalization of poly(organophosphazenes), 10. Thermally induced grafting reactions of maleates containing oxazoline groups onto aryloxy-substituted poly(organophosphazenes)

The functionalization reaction of aryloxy-substituted poly(organophosphazenes) with variable amounts of oxazoline groups is described as a function of different experimental parameters, such as the reaction time and temperature, the concentration of the peroxide initiator and of the oxazoline-containing maleate group, the solvent used to run the process and the type of substituents attached to the polyphosphazene skeleton. The resulting phosphazene grafted copolymers were characterized by IR and NMR (1H, 13C and 31P) spectroscopy and by thin layer chromatography. These materials are successively reacted with poly(methacrylic acid) due to the well known reactivity of the oxazoline residues with carboxylic functions, to form new materials in which the inorganic and the organic macromolecules are linked together through genuine covalent bonds formed by ester-amide structures.

Efficacy of Carteolol Hydrochloride 1% vs Timolol Maleate 0.5% in Patients with Increased Intraocular Pressure

To evaluate the ocular hypotensive effect and safety of carteolol hydrochloride 1% vs timolol maleate 0.5%. One hundred seventy-six patients with ocular hypertension or primary open-angle glaucoma were randomly assigned to receive either carteolol 1% twice a day or timolol maleate 0.5% solution twice a day in a randomized, double-masked, multicenter, parallel-group, active-control comparison trial during a 3-month period. After 12 weeks, carteolol 1% reduced the mean +/- SE intraocular pressure from 25.0 +/- 0.3 to 19.5 +/- 0.3 mm Hg; timolol maleate 0.5% reduced the mean intraocular pressure from 25.2 +/- 0.3 to 19.6 +/- 0.3 mm Hg. The mean difference in trough intraocular pressure between carteolol and timolol maleate of -0.14 mm Hg was not significantly (P = .745) different (95% confidence limits, -0.97 to 0.70 mm Hg). Trough pulse and blood pressure also showed no consistent statistically significant differences between groups. The 2-hour postdose pulse, however, demonstrated a greater decrease in the timolol maleate than in the carteolol group (P < .001). Systemic and ocular signs and symptoms were similar between the groups except that the number of treatment-emergent reports of bradycardia was greater in the timolol maleate group (P = .039), and the carteolol group reported fewer ocular symptoms than the timolol maleate group did (P < .01). Both carteolol 1% and timolol maleate 0.5% are highly effective in lowering intraocular pressure when measured at the end of the dosing interval. Carteolol 1% demonstrates an ocular hypotensive effect and safety profile similar to those of timolol maleate 0.5% solution.

Structure and stability of carboxylate complexes. Part VIII. Crystal and molecular structures of copper(II) hydrogen maleate tetrahydrate and copper(II) maleate hydrate

The crystal and molecular structures of copper(II) hydrogen maleate tetrahydrate and copper(II) maleate hydrate have been determined by three-dimensional X-ray methods. In copper(II) hydrogen maleate (monoclinic, a= 3·594, b= 18·79, c= 9·69 A, γ= 93·25°, space group l2/m, diffractometer data, R= 0·039) the copper atoms are co-ordinated only by water molecules to form [Cu(H2O)4]n2n+ chain cations which are hydrogen bonded to the planar hydrogen maleate anions. In the hydrogen maleate anion the intra-molecular hydrogen bond is 2·409 A. The copper co-ordination octahedron is distorted, Cu–OH2(bridging) 1·959 and 2·682 A, and Cu–OH2(non-bridging) 1·933 A. In copper maleate tetrahydrate (monoclinic, twinned, a= 8·78, b= 7·88, c= 5·35, γ= 125·1°, P21, photographic data, R= 0·096) the copper atom is in a five-co-ordinate square-pyramidal environment. The ligands are a water molecule, Cu–OH2, 2·26 A, a chelating maleate group forming a seven-membered chelate ring, and two oxygen atoms of two other maleate groups. In the basal plane the average copper–oxygen bond length is 1·99 A. Each maleate group is bound to three copper atoms to form a polymeric sheet. The sheets are joined by hydrogen bonding.