Quinine hydrochloride dihydrate
(Synonyms: 奎宁盐酸盐二水合物) 目录号 : GC61231
An antimalarial agent
Cas No.:6119-47-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Quinine is an alkaloid antimalarial agent that has MIC values ranging from 10 to 500 nM for 60 Thai isolates of P. falciparum.1 It inhibits hemozoin formation in purified trophozoites, leading to an increase in free heme, similar to the mechanism of action of chloroquine .2 In mice, quinine reduces P. berghei parasite load in the blood with a minimum effective dose (MED) of 150 mg/kg.3 Formulations containing quinine have been used in the treatment of uncomplicated malaria.
1.Thaithong, S., Beale, G.H., and Chutmongkonkul, M.Susceptibility of Plasmodium falciparum to five drugs: An in vitro study of isolates mainly from ThailandTrans. R. Soc. Trop. Med. Hyg.77(2)228-231(1983) 2.Combrinck, J.M., Mabotha, T.E., Ncokazi, K.K., et al.Insights into the role of heme in the mechanism of action of antimalarialsACS Chem Biol.8(1)133-137(2013) 3.Thurston, J.P.The action of antimalarial drugs in mice infected with Plasmodium bergheiBr. J. Pharmacol. Chemother.5(3)409-416(1950)
| Cas No. | 6119-47-7 | SDF | |
| 别名 | 奎宁盐酸盐二水合物 | ||
| Canonical SMILES | COC1=CC2=C(N=CC=C2[C@H]([C@@]3([H])[N@](C[C@@H]4C=C)CC[C@@]4([H])C3)O)C=C1.Cl.O.O | ||
| 分子式 | C20H29ClN2O4 | 分子量 | 396.91 |
| 溶解度 | DMSO: ≥ 100 mg/mL (251.95 mM); Water: 20 mg/mL (50.39 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5195 mL | 12.5973 mL | 25.1946 mL |
| 5 mM | 0.5039 mL | 2.5195 mL | 5.0389 mL |
| 10 mM | 0.2519 mL | 1.2597 mL | 2.5195 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Synthesis of Saponite Based Nanocomposites to Improve the Controlled Oral Drug Release of Model Drug Quinine hydrochloride dihydrate
Pharmaceuticals (Basel) 2019 Jul 10;12(3):105.PMID:31295860DOI:10.3390/ph12030105.
In the present research study, a 2:1 type of smectite clay minerals, namely natural saponite (NSAP) and synthetic saponite (SSAP), was demonstrated for the first time to be controlled drug release host materials for the model drug Quinine hydrochloride dihydrate (QU). The popular sol-gel hydrothermal technique was followed for the synthesis of saponite. The QU was ion exchanged and intercalated into an interlayered gallery of synthetic as well as natural saponite matrices. The developed QU-loaded hybrid composite materials along with the pristine materials were characterized by powder X-ray diffraction (PXRD), Fourier transformed infrared spectroscopy (FTIR), thermal gravimetric analysis (TGA), the Brunauer-Emmett-Teller method (BET) for surface area (SA), and scanning electron microscopy (SEM). The characterization of material results using DSC, FTIR and PXRD confirmed the presence of saponite clay mineral phases in the original and the synthesized saponite samples. Similarly, the drug-loaded composites confirmed the successful intercalation of QU drug on the natural and synthesized saponite matrices. The oral drug release performance of both nanocomposites along with pure quinine drug was monitored in sequential buffer environments at 37 ± 0.5 °C. These composite hybrid materials showed the superior controlled release of QU in gastric fluid (pH = 1.2) and intestinal fluid (pH = 7.4). QU release was best fitted in the Korsmeyer-Peppas kinetic model and demonstrated a diffusion-controlled release from nanocomposite layered materials. The observed controlled drug release results suggest that the applied natural/synthetic saponite matrices have the potential to provide critical design parameters for the development of bioengineered materials for controlled drug release.
Palatability of pediatric formulations: do rats predict aversiveness?
Drug Dev Ind Pharm 2021 Jul;47(7):1121-1126.PMID:34545750DOI:10.1080/03639045.2021.1984519.
Background: The brief-access taste aversion (BATA) model has been used as an alternative taste assessment tool to human taste panels and became an important element of pharmaceutical drug development, especially regarding pediatric patient's compliance. This model has been validated, demonstrating a concentration-dependent sensitivity to drug aversiveness, as well as the capacity to evaluate the taste-masking effects of cyclodextrins. In the BATA model, samples are presented randomly to rodents in numerous sipper tubes and a lickometer is used for the electronic record of licks in a sophisticated approach. Objectives: The aim of this study was to test possible drug taste-masking strategies. Additionally, we have used an alternative approach to measure the animal lick number in the presence of different compounds, non-simultaneously. Results: In the present work we show for the first time the licking profile of different compounds during the time course of the experiment, with each animal being exposed to only one bottle of testing product. To validate the experiments, Quinine hydrochloride dihydrate (QHD) was used as a bitter reference compound. Conclusion: The results obtained using this simple approach showed that aversiveness is dependent on the assay duration, and that it is possible to predict the aversiveness just by measuring the mass of the tested substance consumption. Moreover, some taste-masking strategies, such as those used in pediatric formulations and corresponding to the addition of sweeteners or flavors, cannot be predicted from rodents BATA model.
The development of basic taste sensitivity and preferences in children
Appetite 2018 Aug 1;127:130-137.PMID:29729324DOI:10.1016/j.appet.2018.04.027.
This study aims at understanding how preference and sensitivity to the basic tastes develop in the preschool years, and how the two relate to each other. To expand on the existing literature regarding taste preferences conducted in cross-sectional studies, a longitudinal design was applied with children from age four to six years old. During the springs of 2015, 2016, and 2017, 131 children born in 2011 were tested in their kindergartens. To investigate preferences for sweet, sour and bitter tastes, the children performed ranking-by-elimination procedures on fruit-flavored beverages and chocolates with three taste intensity levels. The beverages varied in either sucrose, citric acid, or the bitter component isolone. The chocolates varied in the bitter component theobromine from cocoa and sucrose content. Each year, the children also performed paired-comparison tasks opposing plain water to tastant dilutions at four concentrations. The stimuli consisted of the five basic tastes: sweet (sucrose) sour (citric acid monohydrate) umami (monosodium glutamate), salty (sodium chloride), and bitter (Quinine hydrochloride dihydrate). Preference for sweetness levels increased with age, while preference for bitterness and sourness levels were stable. Concerning taste sensitivity, the children showed an increase in sensitivity for sourness and saltiness, a decrease for sweetness, and stability for umami and bitterness. A negative association was found between sweetness sensitivity and preference for sweetness. The study highlights different trajectories of sensitivity and preferences across tastes. On average, a reduction in sweetness sensitivity combined with an increase in preference for higher sweetness was observed from the age of four to six. The weak relationship between taste sensitivity and taste preference in our data suggests that taste preference development is shaped by a multitude of factors in addition to taste sensitivity.
Rats can predict aversiveness of Active Pharmaceutical Ingredients
Eur J Pharm Biopharm 2018 Dec;133:77-84.PMID:30267837DOI:10.1016/j.ejpb.2018.09.027.
Taste is crucial for patient acceptability and compliance with prescribed medicines, in particular with pediatric patients. Evaluating the taste of new active pharmaceutical ingredients (APIs) is therefore essential to put in place adequate taste-masking techniques, if needed, which will lead to acceptable palatable formulations. Thus, there is an urgent need to develop and optimize taste assessment methods that could be used at different stages of the drug development process. The aim of this study was to investigate the suitability of the rat brief-access taste aversion (BATA) model as a screening tool for assessment of APIs aversiveness that could predict human taste responses. Presently, the taste intensity of nine marketed APIs known to have different levels of bitter intensity (Quinine hydrochloride dihydrate, 6-n-propylthiouracil, sildenafil citrate, diclofenac sodium, ranitidine hydrochloride, caffeine citrate, isoniazid, telbivudine and paracetamol) was investigated at different overlapping concentrations with two in vivo taste assessment methods: the rat BATA model and human taste panels with the intention of determining the drugs' concentrations to produce half of the maximal rating. Overall there was a strong correlation (R2 = 0.896) between rats IC50 and humans EC50 values. This correlation verifies the BATA model as a rapid and reliable tool for quantitative assessment of API aversiveness. A comparable ranking order was obtained mainly for high and medium aversive compounds, whereas it was less aligned for weakly aversive compounds. It was nonetheless possible to propose a classification of poor taste intensity determined in rats that would predict human taste tolerability.
Inhibition of Radiation and Temozolomide-Induced Glioblastoma Invadopodia Activity Using Ion Channel Drugs
Cancers (Basel) 2020 Oct 8;12(10):2888.PMID:33050088DOI:10.3390/cancers12102888.
Glioblastoma (GBM) is the most prevalent and malignant type of primary brain cancer. The rapid invasion and dissemination of tumor cells into the surrounding normal brain is a major driver of tumor recurrence, and long-term survival of GBM patients is extremely rare. Actin-rich cell membrane protrusions known as invadopodia can facilitate the highly invasive properties of GBM cells. Ion channels have been proposed to contribute to a pro-invasive phenotype in cancer cells and may also be involved in the invadopodia activity of GBM cells. GBM cell cytotoxicity screening of several ion channel drugs identified three drugs with potent cell killing efficacy: flunarizine dihydrochloride, econazole nitrate, and Quinine hydrochloride dihydrate. These drugs demonstrated a reduction in GBM cell invadopodia activity and matrix metalloproteinase-2 (MMP-2) secretion. Importantly, the treatment of GBM cells with these drugs led to a significant reduction in radiation/temozolomide-induced invadopodia activity. The dual cytotoxic and anti-invasive efficacy of these agents merits further research into targeting ion channels to reduce GBM malignancy, with a potential for future clinical translation in combination with the standard therapy.