Changes in proton T1 in dog brains due to the administration of haloperidol

Changes in proton T1 in dog brains due to the administration of haloperidol were determined by the intravenous administration of a single dose of 20 mg of haloperidol to mongrel dogs. The MRI used was the Aberdeen type with the static magnetic field of 0.1 T. A coil made exclusively for these animals (bore diameter 120 mm) was used. There was a significant increase in the T1 value in the striate body 30 minutes and more (within two hours) after the administration of haloperidol. Subtraction images were also obtained by subtracting the image of the pre-treatment (control) T1 values from the image of the post-treatment values (2 hours after the injection). The subtraction images also revealed increases in the T1 values of the striate body.     

Structure and molecular properties of (1)-Centbutindole. Comparison with Haloperidol

The structure and conformation of (1)-Centbutindole, a newly marketed neuroleptic compound, has been investigated by X-ray crystallography. It crystallizes in the monoclinic system and the non-centrosymmetric space group P2₁ (Z=2) with cell dimensionsa=8.434(6),b=6.620(3),c=18.419(9)Å, and =95.07(6)°. The chain conformation istrans extended. The embedded ³ piperidine ring exists in ahalf-chair conformation whereas the embedded piperazine ring exists in achair conformation. The propylene side chain is equatorial relative to the piperazine. A systematic conformational analysis of centbutindole and of a related molecule, Haloperidol, followed by a Monte Carlo search and a stochastic dynamics simulation, have been performed. Electronic and lipophilic properties have been computed and, molecular electrostatic potential (MEP) maps and molecular lipophilicity potential (MLP) maps, have been displayed for two selected conformers satisfying a reported pharmacophore. The two molecules exhibit very similar molecular properties.     

Quantitative determination of haloperidol in tablets by high performance thin-layer chromatography

A densitometric high performance thin-layer chromatography (HPTLC) method was developed and validated for the quantitative analysis of haloperidol in tablets. Chromatographic separation was achieved on precoated silica gel F 254 HPTLC plates using a mixture of acetone/chloroform/n-butanol/acetic acid glacial/water (5:10:10:2.5:2.5 v/v/v/v/v) as the mobile phase. Quantitative analysis was carried out at a wavelength of 254 nm. The method was linear in the 10-100 ng/microL range, with a determination coefficient of 0.999. The coefficients of variation for precision were not higher than 2.35%. The detection limit was 0.89 ng/microL, and the quantification limit was 2.71 ng/microL. The accuracy ranged from 97.76 to 100.33%, with a CV not higher than 4.50%. This method was successfully applied to quantify haloperidol in real pharmaceutical samples, including the comparison with HPLC measurements. The method was fast, specific, with a good precision and accuracy for the quantitative determination of haloperidol in tablets.