Gluconate Calcium   中文名称: 葡萄糖酸钙

Absorption, Distribution and Excretion
Approximately one-fifth to one-third of orally administered calcium is absorbed in the small intestine, depending on presence of vitamin D metabolites, pH in lumen, and on dietary factors, such as calcium binding to fiber or phytates. Calcium absorption is increased when a calcium deficiency is present or when a patient is on a low-calcium diet. In patients with achlorhydria or hypochlorhydria, calcium absorption, especially with the carbonate salt, may be reduced.
Renal (20%) - The amount excreted in the urine varies with degree of calcium absorption and whether there is excessive bone loss or failure of renal conservation. Fecal (80%) - Consists mainly of nonabsorbed calcium, with only a small amount of endogenous fecal calcium excreted.
Not available
Approximately one-fifth to one-third of orally administered calcium is absorbed in the small intestine, depending on presence of vitamin D metabolites, pH in lumen, and on dietary factors, such as calcium binding to fiber or phytates. Calcium absorption is increased when a calcium deficiency is present or when a patient is on a low-calcium diet. In patients with achlorhydria or hypochlorhydria, calcium absorption, especially with the carbonate salt, may be reduced. /Calcium supplements/
Elimination: Renal (20%) - The amount excreted in the urine varies with degree of calcium absorption and whether there is excessive bone loss or failure of renal conservation. Fecal (80%) - Consists mainly of nonabsorbed calcium, with only a small amount of endogenous fecal calcium excreted. /Calcium supplements/

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Metabolism / Metabolites
Calcium gluconate does not require hepatic metabolism for the release of Ca++ and is as effective as calcium chloride in treating ionic hypocalcemia in the absence of hepatic function.

Protein Binding
Moderate, approximately 45% in plasma.

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Interactions
Concurrent use of excessive amounts of /alcohol, caffeine (usually more than 8 cups of coffee a day), or tobacco/ has been reported to decrease calcium absorption.
Concurrent use /of estrogens/ with calcium supplements may increase calcium absorption, which is used to therapeutic advantage when estrogens are prescribed for the treatment of postmenopausal osteoporosis. /Calcium supplements/
Concurrent use with calcium supplements may decrease effectiveness of cellulose sodium phosphate in preventing hypercalciuria. /Calcium supplements/
Concurrent use /of other calcium-containing medications or oral magnesium-containing medications/ with calcium supplements may increase serum calcium or magnesium concentration in susceptible patients, mainly patients with impaired renal function, leading to hypercalcemia or hypermagnesemia, respectively. /Calcium supplements/
For more Interactions (Complete) data for CALCIUM GLUCONATE (21 total), please visit the HSDB record page.

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Non-Human Toxicity Values
LD50 Rat oral >5,000 mg/kg bw

Calcium gluconate is the calcium salt of D-gluconic acid. It has a role as a nutraceutical. It contains a D-gluconate.
Calcium gluconate is used as mineral supplement and medication when there is insufficient calcium in the diet. Supplementation may be done to treat or prevent osteoporosis or rickets, consequences of hypocalcemia. It can also be taken by mouth but is not recommended by injection into a muscle. Calcium Gluconate Injection, USP is a sterile, nonpyrogenic supersaturated solution of calcium gluconate for intravenous use only. Each mL contains: Calcium gluconate 94 mg; calcium saccharate (tetrahydrate) 4.5 mg; water for injection q.s. Hydrochloric acid and/or sodium hydroxide may have been added for pH adjustment (6.0 to 8.2). Calcium saccharate provides 6% of the total calcium and stabilizes the supersaturated solution of calcium gluconate. Each 10 mL of the injection provides 93 mg elemental calcium (Ca++) equivalent to 1 g of calcium gluconate.
Calcium Gluconate is the gluconate salt of calcium. An element or mineral necessary for normal nerve, muscle, and cardiac function, calcium as the gluconate salt helps to maintain calcium balance and prevent bone loss when taken orally. This agent may also be chemopreventive for colon and other cancers. (NCI04)
The calcium salt of gluconic acid. The compound has a variety of uses, including its use as a calcium replenisher in hypocalcemic states.
See also: Calcium Cation (has active moiety) ... View More ...

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Drug Indication
Oral calcium salts are used as dietary supplemental therapy for person who may not get enough calcium in their regular diet. Calcium gluconate is used as a cardioprotective agent in high blood potassium. Calcium gluconate is the antidote for magnesium sulfate toxicity.

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Mechanism of Action
Calcium is essential for the functional integrity of the nervous, muscular, and skeletal systems. It plays a role in normal cardiac function, renal function, respiration, blood coagulation, and cell membrane and capillary permeability. Also, calcium helps to regulate the release and storage of neurotransmitters and hormones, the uptake and binding of amino acids, absorption of vitamin B 12, and gastrin secretion. The major fraction (99%) of calcium is in the skeletal structure primarily as hydroxyapatite, Ca 10(PO 4) 6(OH) 2; small amounts of calcium carbonate and amorphous calcium phosphates are also present. The calcium of bone is in a constant exchange with the calcium of plasma. Since the metabolic functions of calcium are essential for life, when there is a disturbance in the calcium balance because of dietary deficiency or other causes, the stores of calcium in bone may be depleted to fill the body's more acute needs. Therefore, on a chronic basis, normal mineralization of bone depends on adequate amounts of total body calcium.

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Therapeutic Uses
Some studies have shown that calcium supplementation begun in the second trimester may be effective in lowering blood pressure in pregnancy women with pregnancy-induced hypertension or pre-eclampsia, both of which may possibly be associated with increased calcium demand of the fetus during the last trimester. /Calcium supplements/
Oral calcium salts are used as dietary supplemental therapy for person who may not get enough calcium in their regular diet. Due to increased needs, children and pregnancy women are at greatest risk. Pre- and postmenopausal women; adolescents, especially girls and the elderly may not receive adequate calcium in their diets. ... Calcium supplements are used as part of the prevention and treatment of osteoporosis in patients with an inadequate calcium intake. The use of calcium citrate may reduce the risk of kidney stones in susceptible patients. The use of water-soluble salts of calcium (ie, citrate, gluconate, and lactate) may be preferable to acid-soluble salts (ie, carbonate and phosphate) for patients with reduced stomach acid or patients taking acid-inhibiting medication, such as the histamine H2-receptor antagonists. /Calcium supplements; Included in US product labeling/
Oral calcium supplements provide a source of calcium ion for treating calcium depletion occurring in conditions such as chronic hypoparathyroidism, pseudohypoparathyroidism, osteomalacia, rickets, chronic renal failure, and hypocalcemia secondary to the administration of anticonvulsant medications. When chronic hypocalcemia is due to vitamin D deficiency oral calcium salts may be administered concomitantly with vitamin D analogs. /Calcium supplements; Included in US product labeling/
Calcium chloride and parenteral calcium gluconate are used to decrease or reverse the cardiac depressant effects of hyperkalemia on electrocardiographic (ECG) function. /Calcium supplements; Included in US product labeling/
For more Therapeutic Uses (Complete) data for CALCIUM GLUCONATE (27 total), please visit the HSDB record page.

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Drug Warnings
VET: ... Calcium gluconate ... if given by iv injection, should be admin slowly ... given rapidly ... may have toxic effect on heart.
Calcium gluconate ... not recommended for im use because dose must be large and danger of sterile abscess formation is too great.
Many physicians recommend that pregnant women receive multivitamin and mineral supplements, especially those pregnant women who do not consume an adequate diet and those in high-risk categories )ie, women carrying more than one fetus, heavy cigarette smokers, and alcohol and drug abusers). Taking excessive amounts of a multivitamin and mineral supplement may be harmful to the mother and/or fetus and should be avoided. /Calcium supplements/
Side/adverse effects may be more likely to occur if oral calcium supplements are taken in much larger doses than recommended (greater than 2000 to 2500 mg a day), if they are taken for a longer period of time, or if they are taken by patients with renal function impairment or milk-alkali syndrome. /Calcium supplements/
For more Drug Warnings (Complete) data for CALCIUM GLUCONATE (15 total), please visit the HSDB record page.

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Pharmacodynamics
Calcium Gluconate is the gluconate salt of calcium. An element or mineral necessary for normal nerve, muscle, and cardiac function, calcium as the gluconate salt helps to maintain calcium balance and prevent bone loss when taken orally. This agent may also be chemopreventive for colon and other cancers.

C12H22CAO14

430.3727

430.063

299-28-5

9290

White to off-white solid powder

673.6ºC at 760 mmHg

195°C

375.2ºC

254.9

10

14

8

27

165

8

C([C@H]([C@H]([C@@H]([C@H](C(=O)[O-])O)O)O)O)O.C([C@H]([C@H]([C@@H]([C@H](C(=O)[O-])O)O)O)O)O.[Ca+2]

NEEHYRZPVYRGPP-IYEMJOQQSA-L

InChI=1S/2C6H12O7.Ca/c2*7-1-2(8)3(9)4(10)5(11)6(12)13;/h2*2-5,7-11H,1H2,(H,12,13);/q;;+2/p-2/t2*2-,3-,4+,5-;/m11./s1

calcium;(2R,3S,4R,5R)-2,3,4,5,6-pentahydroxyhexanoate

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中，避免吸湿/受潮。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O : ~20 mg/mL (~92.51 mM)
DMSO : ~1 mg/mL (~4.63 mM)

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
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。