Analytical and semi-preparative high-performance liquid chromatographic separation and assay of hydroxychloroquine enantiomers

Brocks, Dion R.; Pasutto, Franco M.; Jamali, Fakhreddin

doi:10.1016/0378-4347(92)80450-5

Cited by 48 publications

(27 citation statements)

References 15 publications

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“…enantiomers (see Fig. 1) (Witiak et al 1981;Craig et al 1988;Titus 1989;Brocks et al 1992;Brocks and Mehvar 2003) with variable stereo-selective elimination (Iredale et al 1993;McLachlan et al 1993McLachlan et al , 1994Tett et al 1994;Ducharme et al 1995;Midha et al 1998;Munster et al 2002;Brocks and Mehvar 2003;de Oliveira et al 2007); (c) wide variability in the concentration profiles from sampling of blood or plasma which is possibly due to differences in the sensitivity of analytical methods and calculations of kinetic parameters, especially the terminal elimination plasma half-life (T 1/2 ) Titus 1989); (d) marked variations of plasma concentrations in relation to dosage as well as Fig. 1 The stereochemistry is important for determining the pharmacokinetics of the drug which exists as a racemic mixture of R-(-) and S(?)…”

Section: Pharmacokineticsmentioning

confidence: 99%

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Therapy and pharmacological properties of hydroxychloroquine and chloroquine in treatment of systemic lupus erythematosus, rheumatoid arthritis and related diseases

et al. 2015

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HCQ and CQ have a good reputation for being effective and relatively safe treatments in SLE, mild-moderate RA and Sjøgren's syndrome. There is need for (a) more information on their mode of action in relation to the control of these diseases, (b) scope for developing formulations that have improved pharmacokinetic and therapeutic properties and safety, and (c) further exploring their use in drug combinations not only with other disease modifying agents but also with biologics.

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Section: Pharmacokineticsmentioning

confidence: 99%

“…HCQ and CQ exist as diastereoisomers and their pharmacokinetics in humans has been investigated in several studies (Titus 1989;Brocks et al 1992;Brocks and Mehvar 2003) (Fig. 7).…”

Section: Pharmacokineticsmentioning

confidence: 99%

Therapy and pharmacological properties of hydroxychloroquine and chloroquine in treatment of systemic lupus erythematosus, rheumatoid arthritis and related diseases

et al. 2015

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“…Concentrations of HCQ enantiomers in blood were measured by using a previously described high-performance liquid chromatography method (Brocks et al 1992). Briefly, after addition of chloroquine (internal standard), blood samples (0.2 mL) were alkalinized and extracted with 5 mL of diethyl ether.…”

Section: Hydroxychloroquine Assaymentioning

confidence: 99%

Insulin-sparing effect of hydroxychloroquine in diabetic rats is concentration dependent

Emami

Gerstein²,

Pasutto³

et al. 1999

Can. J. Physiol. Pharmacol.

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To study the effect of hydroxychloroquine (HCQ) on glucose and insulin homeostasis, healthy rats were dosed with 160 mg x kg (-1) x day(-1) of HCQ orally, and streptozocin-induced diabetic rats received 80, 120, and 160 mg x kg(-1) x day(-1) of HCQ, while controls received normal saline. Ten days after treatment with HCQ, healthy animals were challenged intravenously with insulin or glucose, while diabetic rats were given only an i.v. injection of insulin. In healthy rats, the areas within and under the glucose concentration - time curve following insulin and glucose challenge were estimated. In diabetic animals, the areas under the curve for both the percent change in serum glucose from baseline (AUG) and the percent change in serum insulin from baseline (AUI) were used as pharmacodynamic end points. In healthy rats, HCQ did not influence fasting serum glucose concentrations or glycemic profiles following i.v. administration of glucose or insulin. In diabetic rats, AUG and AUI were increased dependent on blood HCQ concentrations. The normal homeostatic mechanisms responsible for insulin-glucose regulation may compensate for possible HCQ-induced reduction of insulin metabolism in healthy rats. The HCQ dose- or concentration-effect relationships for glucose and insulin were linear over the range of HCQ concentrations tested. It is concluded that HCQ significantly elevated insulin blood concentration resulting in reduced glucose levels in a concentration-dependent fashion in diabetic rats. HCQ may have therapeutic potential in the treatment of type I and type II diabetes.

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“…The derivatization reagent DATAN is not expensive, has great separation potential, and is a good leaving group in the collision cell, allowing the use of low collision energy and thereby increasing the selectivity of the measurement. In spite of these unique characteristics, the reagent has rarely been mentioned in the literature (12)(13)(14)(15). Other biochemically important hydroxyacids, i.e., d/l-lactate, d/l-glycerate, and d/l-3hydroxybutyrate, can also be separated enantiomerically by use of DATAN as the derivatizing reagent, without the need to change chromatographic conditions (data not shown).…”

Section: Discussionmentioning

confidence: 99%

Measurement of Urinary d- and l-2-Hydroxyglutarate Enantiomers by Stable-Isotope-Dilution Liquid Chromatography–Tandem Mass Spectrometry after Derivatization with Diacetyl-l-Tartaric Anhydride

et al. 2004

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Analytical and semi-preparative high-performance liquid chromatographic separation and assay of hydroxychloroquine enantiomers

Cited by 48 publications

References 15 publications

Therapy and pharmacological properties of hydroxychloroquine and chloroquine in treatment of systemic lupus erythematosus, rheumatoid arthritis and related diseases

Therapy and pharmacological properties of hydroxychloroquine and chloroquine in treatment of systemic lupus erythematosus, rheumatoid arthritis and related diseases

Insulin-sparing effect of hydroxychloroquine in diabetic rats is concentration dependent

Measurement of Urinary d- and l-2-Hydroxyglutarate Enantiomers by Stable-Isotope-Dilution Liquid Chromatography–Tandem Mass Spectrometry after Derivatization with Diacetyl-l-Tartaric Anhydride

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