规格 | 价格 | 库存 | 数量 |
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100mg |
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500mg |
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Other Sizes |
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体外研究 (In Vitro) |
在化学上,硝酮或糖的高温氢化可产生 D-山梨醇(山梨醇)。通过酶促机制,运动发酵单胞菌和博伊尼念珠菌等细菌也可以产生 D-山梨醇(山梨醇)[1]。 (山梨醇)是片剂薄膜包衣中的增塑剂和胶囊的快速崩解剂。 D-山梨醇,通常称为山梨醇,在口服溶液中用作药物稳定剂和糖替代品。此外,D-山梨醇(山梨醇)经常用于溶解吲哚美辛等药物。山梨醇,也称为D-山梨醇,经常在冻干肠胃外蛋白质制剂中用作等渗剂和/或稳定赋形剂。 -在某些制剂中,山梨醇起到保湿剂的作用[1]。
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药代性质 (ADME/PK) |
Absorption, Distribution and Excretion
Sorbitol will either be excreted in the urine by the kidneys, or metabolized to carbon dioxide and dextrose. The amounts of sorbitol (SOR) excreted in 24-hr urine were determined on two groups, ie, diabetic and nondiabetic patients, using an improved method in which ion exchange resin column processing was applied, and these levels were compared with SOR levels in whole blood. Urinary SOR concentration was also determined in diabetic and normal rats in the same manner and its relationship to aldose reductase (AR) activity in whole blood was investigated. Changes in SOR levels in urine and whole blood were compared in diabetic rats after administration of an AR inhibitor (ARI). Whole blood SOR levels and urinary SOR excretion were significantly higher in diabetic patients than in nondiabetic patients. The same results were obtained in the animal models. In diabetic rats, the urinary SOR excretion was about five times higher than that in control rats, and the AR activity in whole blood was also significantly higher. The increase in urinary SOR excretion and whole blood SOR levels, as well as AR activity, in blood in the diabetic state was inhibited by ARI administration. The influence of the diabetic state and the efficacy of the ARI were more marked in urinary SOR excretion than in whole blood SOR levels. These data indicate that determinations of urinary SOR excretion and AR activity are easily measurable and of benefit to assessing the diabetic condition. An accelerated polyol pathway in diabetes contributes to the development of diabetic complications. To elucidate diabetic nephropathy involving also renal tubular damage, ...urinary sorbitol concentrations /were measured/ concomitantly with urinary N-acetyl-D-glucosaminidase (NAG) excretion in WBN-kob diabetic rats.Twenty-four-hour urinary sorbitol concentrations increased in the diabetic rats in parallel with whole blood sorbitol concentrations. An increase in 24-h urinary NAG excretion coincided with the elevated urinary sorbitol levels in the diabetic rats. The administration of epalrestat, an aldose reductase inhibitor, reduced the increased whole blood and urinary sorbitol concentrations and urinary NAG excretion concomitantly with renal aldose reductase inhibition in the diabetic rats. These results indicate that diabetic nephropathy involves distorted cell function of renal tubules, and that treatment with epalrestat may prevent at least the progress of the nephropathy. The purpose of this study was to determine whether sorbitol concentration is elevated in the cerebrospinal fluid (CSF) of non-medically ill patients with mood disorders. Lumbar punctures were performed on 30 subjects - 10 with bipolar mood disorder, 10 with unipolar mood disorder, and 10 age-matched normal controls, and CSF sorbitol concentrations were measured, using a gas chromatographic-mass spectroscopic technique. The mean+/-standard deviation of CSF sorbitol concentrations differed among the three groups as follows: bipolar (22.9+/-4.6 umoles/L) > unipolar (19.0+/-2.8 umoles/L)>normal control (15. 6+/-1.9 umoles/L). One-way ANOVA showed significant (P=0.0002) differences among the three groups. Post-hoc tests indicated a significant (P<0.05) difference between bipolars and normal controls, bipolars and unipolars, and unipolars and normal controls... Streptozocin (Str) diabetic rats were obtained by Str iv (35 mg/kg). Glycemia and sorbitol levels from sciatic nerve and lens were measured after 1 d, 2, 5, and 8 months of diabetes. Sorbitol concentrations in serum, heart, diaphragm, small intestine, and kidney after 8 months of diabetes were measured. RESULTS: Diabetic rats after Str injection showed hyperglycemia (> 1.7 g.L-1), hyperphagia, polyuria, polydipsia, and loss of body weight. Sorbitol levels in lens and sciatic nerve increased in normal and diabetic rats; the increase was higher in diabetic rats. No relationship was shown between glycemia and sorbitol levels. An increased sorbitol level after 8 months of diabetes was found in small intestine and kidney... For more Absorption, Distribution and Excretion (Complete) data for D-Sorbitol (8 total), please visit the HSDB record page. Metabolism / Metabolites Sorbitol is widely used in a number of pharmaceutical products and occurs naturally in many edible fruits and berries. It is absorbed more slowly from the gastrointestinal tract than sucrose and is metabolized in the liver to fructose and glucose ... Sorbitol is better tolerated by diabetics than sucrose and is widely used in many sugar-free liquid vehicles ... 70% of orally ingested sorbitol is converted to carbon dioxide without appearing as glucose in the blood ... |
毒性/毒理 (Toxicokinetics/TK) |
Interactions
PURPOSE: To examine the effect of common excipients such as sugars (sorbitol versus sucrose) on bioequivalence between pharmaceutical formulations, using ranitidine and metoprolol as model drugs. METHODS: Two single-dose, replicated, crossover studies were first conducted in healthy volunteers (N=20 each) to compare the effect of 5 Gm of sorbitol and sucrose on bioequivalence of 150 mg ranitidine or 50 mg metoprolol in aqueous solution, followed by a single-dose, nonreplicated, crossover study (N=24) to determine the threshold of sorbitol effect on bioequivalence of 150 mg ranitidine in solution. RESULTS: Ranitidine Cmax and AUC0-infinity were decreased by approximately 50% and 45%, respectively, in the presence of sorbitol versus sucrose. Similarly, sorbitol reduced metoprolol Cmax by 23% but had no significant effect on AUC0-infinity. An appreciable subject-by-formulation interaction was found for ranitidine Cmax and AUC0-infinity, as well as metoprolol Cmax. Sorbitol decreased the systemic exposure of ranitidine in a dose-dependent manner and affected bioequivalence at a level of 1.25 Gm or greater. CONCLUSIONS: As exemplified by sorbitol, some common excipients have unexpected effect on bioavailability/bioequivalence, depending on the pharmacokinetic characteristics of the drug, as well as the type and amount of the excipient present in the formulation. More research is warranted to examine other common excipients that may have unintended influence on bioavailability/bioequivalence. Non-Human Toxicity Values LD50 Rat sc 29,600 mg/kg LD50 Rat iv 7100 mg/kg LD50 Rat oral 15,900 mg/kg LD50 Mouse oral 17,800 mg/kg LD50 Mouse iv 9480 mg/kg |
参考文献 | |
其他信息 |
Therapeutic Uses
Cathartics; Diuretics, Osmotic; Indicators and Reagents; Pharmaceutic Aids A polyhydric alcohol with about half the sweetness of sucrose. Sorbitol occurs naturally and is also produced synthetically from glucose. It was formerly used as a diuretic and may still be used as a laxative and in irrigating solutions for some surgical procedures. It is also used in many manufacturing processes, as a pharmaceutical aid, and in several research applications. The objective of this report is to describe a cost-effective strategy for management of constipation in nursing home residents with dementia. ... A prospective observational quality improvement study of 41 residents with chronic constipation and receiving an osmotic laxative /was conducted/. Sorbitol was substituted for lactulose. ... The number and amount of laxative use over a period of 4 weeks that were required to maintain regular bowel function was measured. . RESULTS: There was no difference in efficacy of lactulose and sorbitol. Use of additional laxatives was infrequent ... . Osmotic diuretic given iv in 50% (wt/vol) solution to diminish edema, to lower cerebrospinal pressure, or to reduce intraocular pressure in glaucoma ... Dose: 50 to 100 mL of 50% solution; as laxative, oral, 30-50 g. /Former use/ For more Therapeutic Uses (Complete) data for D-Sorbitol (8 total), please visit the HSDB record page. Drug Warnings It is not to be injected. /Sorbitol solution USP/ The administration of a cathartic alone has no role in the management of the poisoned patient and is not recommended as a method of gut decontamination. Experimental data are conflicting regarding the use of cathartics in combination with activated charcoal. No clinical studies have been published to investigate the ability of a cathartic, with or without activated charcoal, to reduce the bioavailability of drugs or to improve the outcome of poisoned patients. Based on available data, the routine use of a cathartic in combination with activated charcoal is not endorsed. If a cathartic is used, it should be limited to a single dose in order to minimize adverse effects. Side effects occur rarely following rectal administration of glycerin or sorbitol ... Rectal discomfort, irritation, burning or griping, cramping pain, and tenesmus /(straining)/. Hyperemia of rectal mucosa with minimal amounts of hemorrhage and mucus discharge ... occur less frequently following rectal administration of sorbitol. Diarrhea frequently occurs with dosages of sorbitol used as adjuncts to sodium polystyrene sulfonate therapy. For more Drug Warnings (Complete) data for D-Sorbitol (15 total), please visit the HSDB record page. |
分子式 |
C6H14O6
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分子量 |
182.17
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精确质量 |
182.079
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CAS号 |
50-70-4
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相关CAS号 |
D-Sorbitol-d8;287962-59-8;D-Sorbitol-13C;287100-73-6;L-Sorbitol;6706-59-8;D-Sorbitol-d4;2714472-87-2;D-Sorbitol-18O-1;D-Sorbitol-13C6;121067-66-1;D-Sorbitol-13C-1;D-Sorbitol-13C-2;D-Sorbitol-d2;1931877-15-4;D-Sorbitol-d-2;1931877-16-5;D-Sorbitol-d2-1;2714432-33-2;D-Sorbitol-d2-2;1931877-14-3
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PubChem CID |
5780
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外观&性状 |
White to off-white solid powder
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密度 |
1.6±0.1 g/cm3
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沸点 |
494.9±0.0 °C at 760 mmHg
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熔点 |
98-100 °C (lit.)
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闪点 |
>100°C
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蒸汽压 |
<0.1 mm Hg ( 25 °C)
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折射率 |
1.597
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LogP |
-4.67
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tPSA |
121.38
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氢键供体(HBD)数目 |
6
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氢键受体(HBA)数目 |
6
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可旋转键数目(RBC) |
5
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重原子数目 |
12
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分子复杂度/Complexity |
105
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定义原子立体中心数目 |
4
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SMILES |
C([C@H]([C@H]([C@@H]([C@H](CO)O)O)O)O)O
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InChi Key |
FBPFZTCFMRRESA-JGWLITMVSA-N
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InChi Code |
InChI=1S/C6H14O6/c7-1-3(9)5(11)6(12)4(10)2-8/h3-12H,1-2H2/t3-,4+,5-,6-/m1/s1
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化学名 |
(2R,3R,4R,5S)-hexane-1,2,3,4,5,6-hexol
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别名 |
Glucitol; D-Sorbitol
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HS Tariff Code |
2934.99.9001
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外实验) |
H2O : ~100 mg/mL (~548.94 mM)
DMSO : ~100 mg/mL (~548.94 mM) |
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溶解度 (体内实验) |
配方 1 中的溶解度: ≥ 2.5 mg/mL (13.72 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。
例如,若需制备1 mL的工作液,可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中,混匀;然后向上述溶液中加入50 μL Tween-80,混匀;加入450 μL生理盐水定容至1 mL。 *生理盐水的制备:将 0.9 g 氯化钠溶解在 100 mL ddH₂O中,得到澄清溶液。 配方 2 中的溶解度: ≥ 2.5 mg/mL (13.72 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 例如,若需制备1 mL的工作液,可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中,混匀。 *20% SBE-β-CD 生理盐水溶液的制备(4°C,1 周):将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中,得到澄清溶液。 View More
配方 3 中的溶解度: ≥ 2.5 mg/mL (13.72 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 配方 4 中的溶解度: 110 mg/mL (603.83 mM) in PBS (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液; 超声助溶. 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 5.4894 mL | 27.4469 mL | 54.8938 mL | |
5 mM | 1.0979 mL | 5.4894 mL | 10.9788 mL | |
10 mM | 0.5489 mL | 2.7447 mL | 5.4894 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
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)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
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 ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。