Properties and Analysis of Haloperidol and Its Dosage Forms

Demoen, Paul J. A.

doi:10.1002/jps.2600500417

Cited by 33 publications

(5 citation statements)

References 9 publications

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“…Postmortem time was not significantly related to mean haloperidol concentration (r=0.35, N=11, p= 0.29). Furthermore, there was no significant correlation between storage time of brain tissue at -80°C and mean haloperidol concentration (r=-0.37, N=11, p= 0.26), which is consistent with a high chemical stability of haloperidol during prolonged storage (15).…”

Section: Resultssupporting

confidence: 83%

Persistence of Haloperidol in Human Brain Tissue

Kornhuber¹,

Schultz²,

Wiltfang³

et al. 1999

AJP

131

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Objective: After discontinuation of neuroleptic drugs, their antipsychotic and antiparkinsonian effects are still present for a prolonged period. It is not known whether the extended effects of neuroleptic drugs in humans are due to the continued presence of drug in brain tissue or to long-lasting drug-induced physiologic changes. The aim of this study was to directly examine haloperidol concentrations in human brain tissue in relation to drug-free time. Method: Haloperidol concentrations were measured in five regions (temporal cortex, cingulate gyrus, caudate nucleus, dentate nucleus, corpus callosum) of the postmortem brains of 11 patients previously treated with haloperidol. Haloperidol was analyzed by means of high-performance liquid chromatography with ultraviolet detection. The half-life in brain tissue was estimated by a population kinetic analysis. Results: Haloperidol concentrations in the human brain tissue were 10-30 times higher than optimal serum concentrations used in the treatment of schizophrenia. Haloperidol concentrations appeared to be homogeneously distributed across different brain areas within a single patient. There was no apparent relation between duration of treatment and mean haloperidol concentration. Higher doses of haloperidol seemed to be related to higher concentrations in brain tissue. The elimination half-life from brain tissue was calculated to be 6.8 days. Conclusions: The results may have implications for clinical treatment decisions and the design of clinical research protocols. Patients exposed to haloperidol cannot be considered to be free of residual effects of the drug for a number of weeks after withdrawal.(Am J Psychiatry 1999; 156:885-890)

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Section: Resultssupporting

confidence: 83%

Persistence of Haloperidol in Human Brain Tissue

Kornhuber¹,

Schultz²,

Wiltfang³

et al. 1999

AJP

131

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“…Haloperidol is an antipsychotic drug used to treat schizophrenia, delirium, nausea and vomiting, and other neuropsychiatric disorders (Chaparro et al, 2013;Krause et al, 2018;Zayed et al, 2019). It is a poorly-soluble drug that is commonly formulated as solutions for oral administration or injections, and also as tablets (Demoen., 1961). Previously, solid dispersions with haloperidol were prepared using different weak organic acids (Lee et al, 2017;Singh et al, 2013), PVP (Saluja et al, 2016) and polyethylene glycol (Baird and Taylor, 2011) and dispersions have been made into free flowing tabletable powders by combining with mesoporous metalosilicate (Shah and Serajuddin, 2015).…”

Section: Introductionmentioning

confidence: 99%

Polymer structure and property effects on solid dispersions with haloperidol: Poly(N-vinyl pyrrolidone) and poly(2-oxazolines) studies

Shan

Williams

Khutoryanskiy

2020

International Journal of Pharmaceutics

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Poly(2-methyl-2-oxazoline) (PMOZ), poly(2-propyl-2-oxazoline) (PnPOZ) and poly(2-isopropyl-2-oxazoline) (PiPOZ) were synthesized by hydrolysis of 50 kDa poly(2-ethyl-2-oxazoline) (PEOZ) and subsequent reaction of the resulting poly(ethylene imine) with acetic, butyric and isobutyric anhydrides, respectively. These polymers were characterized by proton nuclear magnetic resonance, FTIR spectroscopy, powder X-ray diffraction, and differential scanning calorimetry. The poly(2-oxazolines) as well as poly(N-vinyl pyrrolidone) (PVP) were used to prepare solid dispersions with haloperidol, a model poorly soluble drug. Dispersions were investigated by powder X-ray diffractometry, differential scanning calorimetry and FTIR spectroscopy. Increasing the number of hydrophobic groups (-CH 2 -and -CH 3 ) in the polymer resulted in greater inhibition of crystallinity of haloperidol in the order: PVP > PnPOZ=PEOZ > PMOZ. Interestingly, drug crystallization inhibition by PiPOZ was lower than with its isomeric PnPOZ because of the semi-crystalline nature of the former polymer. Crystallization inhibition was consistent with drug dissolution studies using these solid dispersions, with exception of PnPOZ, which exhibited lower critical solution temperature that affected the release of haloperidol.

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“…Haloperidol is practically insoluble in water over all p H values. Its solubility in water is 1.4mg/100ml, but it can be dissolved in l"/o lactic acid or tartaric acid solutions (3,10). In this study, the solubility of haloperidol in 1°h lactic acid, tartaric acid, hydrochloric acid and polysorbate 80 was determined at 37°C.…”

Section: Solubility Of Haloperidolmentioning

confidence: 99%

“…Haloperidol is supplied in the form of tablets containing 0.5, 1.0, 2.0, 5.0, 10.0 and 20.0 mg of the drug, an oral solution containing 2 mg/ml and an injectable solution containing 5 mg/ml. Demoen ( 3 ) indicated that haloperidol is stable in its dosage forms over considerable periods of time. However, exposure of haloperidol solutions to sunlight causes a rapid loss of stability.…”

Section: Introductionmentioning

confidence: 99%

Investigations of Some Physicochemical Properties of Haloperidol Which May Affect Its Activity

Hakyemez

1988

J Clin Pharm Ther

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Since the clinical response to haloperidol varies from individual to individual, an investigation was carried out to investigate some of the physiochemical properties of haloperidol which may affect its pharmacological activity. The stability of haloperidol in aqueous solutions containing 1% lactic acid, with or without 0.1% methyl paraben, was investigated. A colorimetric method based on a reaction between methyl orange and haloperidol was used. The samples (0.5 mg/ml) were stored in glass and plastic containers at 25, 37, 50, 80 and 110 degrees C for 9 months. The resulting data were analysed using principles of chemical kinetics. The shelf-life of haloperidol solutions was estimated to be at least 4 years. Other physiochemical factors which can affect the pharmacological activity of haloperidol were investigated, namely its solubility and complex-forming properties.

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Properties and Analysis of Haloperidol and Its Dosage Forms

Cited by 33 publications

References 9 publications

Persistence of Haloperidol in Human Brain Tissue

Persistence of Haloperidol in Human Brain Tissue

Polymer structure and property effects on solid dispersions with haloperidol: Poly(N-vinyl pyrrolidone) and poly(2-oxazolines) studies

Investigations of Some Physicochemical Properties of Haloperidol Which May Affect Its Activity

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