Determination and tissue distribution studies of dantrolene sodium with hydroxypropyl-β-cyclodextrin in rat tissue by HPLC/MS/MS.

Published on Oct 1, 2019in Biomedical Chromatography1.728
· DOI :10.1002/BMC.4616
Ruixue Liu1
Estimated H-index: 1
,
Yu Chen1
Estimated H-index: 1
+ 3 AuthorsMiao Wang9
Estimated H-index: 9
Sources
Abstract
: The established analytical method for determining the concentration of dantrolene sodium (Da) in rat tissues by HPLC/MS/MS technique was successfully applied to tissue distribution studies of Da in rats. Tissue homogenate samples were pretreated by protein precipitation with pre-cooled methanol. Chromatographic separation was achieved on an Acquity HPLC column (Kromat Universil XB-C18 , 2.1 × 150 mm, 3 μm). Mass spectrometry was conducted with an electrospray ionization interface in negative ionization mode and multiple reaction monitoring was used for quantitative analysis. The results showed that Da was rapidly and widely distributed in tissues and reached the maximum concentration within 0.5 h in all tissues after oral administration of Da-hydroxypropyl-β-cyclodextrin (DHC). It was then metabolized by liver and finally excreted from kidney,which indicated that DHC inclusion complex has better absorption and higher oral bioavailability than Da. The results also provided evidence for the safety and effectiveness of drug clinical application.
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Aim: Differential pulse polarography was used for the concurrent analysis of the coadministered dantrolene (DAN) and indomethacin (IND) in plasma. Materials & methods: DAN and IND, Hanging mercury drop electrode and Britton–Robinson buffer at pH 5 were used. In plasma, cathodic reduction of DAN nitro group and its active metabolite at -0.2 V was done. IND was analyzed after carbonyl group reduction at -1.1 V. Results: Drugs determination in rat plasma with good recoveries and low limit of quanti...
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Abstract Dantrolene sodium (Da) is an effective skeletal muscle relaxant. However, its pharmacological effects are severely limited owing to its poor solubility and low oral bioavailability. In order to solve these problems, an inclusion complex using hydroxypropyl-β-cyclodextrin (HP-β-CD) to improve the oral bioavailability of Da was prepared successfully by freeze-drying. The prepared complex was characterized by Powder X-ray diffractometry (PXRD), Fourier transform infrared spectroscopy (FTIR...
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#1Yunhui Liao (Guangzhou Higher Education Mega Center)H-Index: 2
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Agomelatine (AGM), is efficacious in both the acute phase and the continuation phase of depression. However, its poor water-solubility, low bioavailability and polymorphism limit its pharmacological effects. To address these problems, agomelatine-hydroxypropyl-β-cyclodextrin inclusion complex (AGM/HPβ-CD) was prepared successfully by freeze-drying. The products was evaluated by structural characterization, solubilization test, in-situ absorption of rat intestinal tract and pharmacokinetic study....
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#1Jenica L. Haraschak (MSU: Mississippi State University)H-Index: 2
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The pharmacokinetics of dantrolene and its active metabolite, 5-hydroxydantrolene, after a single oral dose of either 5 mg/kg or 10 mg/kg of dantrolene were determined. The effects of exposure to dantrolene and 5-hydroxydantrolene on activated whole blood gene expression of the cytokines interleukin-2 (IL-2) and interferon-γ (IFN-γ) were also investigated. When dantrolene was administered at a 5 mg/kg dose, peak plasma concentration (Cmax) was 0.43 µg/ml, terminal half-life (t1/2) was 1.26 hrs, ...
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Abstract Over the last decades the poor solubility of new drugs has become an important issue, with one of the main challenges being to develop oral dosage forms with acceptable bioavailability for such compounds. The specific purpose of our study was to combine the advantages of cyclodextrins with those of solid dispersion approaches to improve the bioavailability of poorly soluble weak acids. Glyburide, an antidiabetic, was used as a model drug. First, binary drug inclusion complexes were prep...
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Abstract The interaction of 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) and a poorly water-soluble flavonoid, baicalein (Ba), chemically 5,6,7-trihydroxy flavone in solution and solid-state was studied. Ba/HP-β-CD solid systems were prepared by freeze-drying method. The formation of Ba/HP-β-CD complex in aqueous solution was demonstrated by UV spectroscopy, while Ba/HP-β-CD co-lyophilized product was characterized by differential scanning calorimetry (DSC) and X-ray diffractometry (XRD). Through co...
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#1T. Krause (UHH: University of Hamburg)H-Index: 2
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Summary Human malignant hyperthermia is a life-threatening genetic sensitivity of skeletal muscles to volatile anaesthetics and depolarizing neuromuscular blocking drugs occurring during or after anaesthesia. The skeletal muscle relaxant dantrolene is the only currently available drug for specific and effective therapy of this syndrome in man. After its introduction, the mortality of malignant hyperthermia decreased from 80% in the 1960s to < 10% today. It was soon discovered that dantrolene dep...
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#1Mehmet Emin Buyukokuroglu (Atatürk University)H-Index: 27
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Abstract In our study, we examined anti-ulcerogen and antioxidant effects of dantrolene sodium on ethanol-induced gastric lesions in rats. Dantrolene sodium was administered intraperitoneally (i.p.) in several doses, and famotidine was used at a dose of 20 mg kg −1 . It was found that pretreatment with dantrolene sodium at doses of 1, 5 and 10 mg kg −1 significantly reduced ethanol-induced gastric damage and malondialdehyde levels, and significantly increased antioxidant enzymes superoxide dismu...
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#1Mehmet Emin Buyukokuroglu (Atatürk University)H-Index: 27
#2İlhami GülçinH-Index: 98
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Dantrolene sodium is a skeletal muscle relaxant, which inhibits intracellular Ca 2+release from the sarcoplasmic reticulum. The aim of this study is to examine possible in vitroantioxidant effects of dantrolene sodium. For this reason, the in vitroantioxidant effects of dantrolene sodium were studied using thiocyanate methods. Additionally, the reducing power and free radical scavenging activity were determined. Dantrolene sodium showed strong antioxidant activity in the linoleic acid emulsion s...
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#1Mahmood Hassan Dalhat (KAU: King Abdulaziz University)
#2Hisham N. Altayb (KAU: King Abdulaziz University)H-Index: 5
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N-acetyltransferase 10 (NAT10), is an acetyltransferase that regulates RNA stability and translation processes. Association of NAT10 with several diseases including cancer, makes it a promising therapeutic target. Remodelin is the only known NAT10 inhibitor, but the structural information related to its binding with NAT10 is still obscure. Here, we predicted the human NAT10 structure using homology modeling that was not available previously and used human NAT10 to identify the novel binding site...
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