| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Dexpantol is soluble in water and alcohol, but insoluble in fats and oils. With a suitable carrier, dexpantol readily penetrates the skin. When administered in an oil/water formulation, the rate of penetration and absorption of dexpantol decreases. The breast milk of a lactating mother on a normal diet contains approximately 2 micrograms of pantothenic acid per milliliter. After oral administration of pantothenic acid, approximately 70% is excreted unchanged in the urine and approximately 30% in the feces. Dexpantol is readily converted to pantothenic acid, which is widely distributed throughout the body, primarily in the form of coenzyme A. The highest concentrations of pantothenic acid are found in the liver, adrenal glands, heart, and kidneys. The breast milk of a lactating woman on a normal diet contains approximately 2 micrograms of pantothenic acid per milliliter. After oral administration of pantothenic acid, approximately 70% is excreted unchanged in the urine and approximately 30% in the feces. Metabolism/Metabolites Dextantanol is readily converted to pantothenic acid, which is widely distributed throughout the body and mainly exists in the form of coenzyme A. Dextantanol is readily converted to pantothenic acid, which is widely distributed throughout the body and mainly exists in the form of coenzyme A. Dextantanol is converted to pantothenic acid...and then acetylcholine is produced. Biological Half-Life Half-life has not been reported. |
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| Toxicity/Toxicokinetics |
Protein Binding
No reports of plasma protein binding have been found. Interactions Dexpanthenol has been reported to prolong the muscle relaxant effect of succinylcholine; however, a controlled trial failed to confirm this effect. The manufacturer recommends that dexpanthenol should not be taken within 1 hour of taking succinylcholine. Panthenol enhances the toxicity and paralytic effects of D-tubocurarine but does not protect pigeons from lethal doses of curare. It does not stimulate respiration and muscle activity in rabbits already blocked by curare. Based on theoretical considerations, the dexpanthenol manufacturer recommends that this drug should not be taken concurrently with neostigmine or other parasympathomimetic drugs, or within 12 hours of administration. Although its clinical significance is undetermined, the miotic effect of anticholinesterase ophthalmic preparations (e.g., etorizine iodide (discontinued in the US), isoflurane) has been reported to be enhanced by pantothenic acid. The manufacturer also warns that rare, unexplained allergic reactions have occurred when dexpanthenol injection is used concurrently with antibiotics, opioids, and barbiturates. For more complete data on interactions of dexpanthenol (9 types in total), please visit the HSDB record page. Non-human toxicity values Oral LD50 in mice: 15,000 mg/kg Intraperitoneal LD50 in mice: 9,000 mg/kg Intravenous LD50 in mice: 7,000 mg/kg Intravenous LD50 in rabbits: 4,000 mg/kg |
| References |
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| Additional Infomation |
Therapeutic Uses
Dextropanthenol (topical use) relieves itching caused by mild eczema and skin diseases and aids in skin healing; suitable for skin irritation caused by itching, minor wounds, stings, bites, poison ivy, and poison oak (dried sage). Also used in infants and young children to treat diaper rash, abrasions, and mild skin irritation. Prophylactic use immediately after major abdominal surgery to minimize the risk of paralytic ileus. Can be used to treat abdominal distension caused by intestinal atony; postoperative or postpartum gas retention, or delayed recovery of postoperative intestinal motility; paralytic ileus. Veterinary Uses: ...Dextropanthenol...is commonly used as a source of vitamin B5. Only the D-isomer is biologically active, but the dl-isomer is also frequently used...Equivalent value: 1 gram of D-pantothenic acid = 936 mg of D-dextropanthenol. /Experimental Uses (Veterinary)/: The effects of B vitamins on experimental liver injury in rats were studied. Intraperitoneal injection of dexpanthenol inhibited initial lipid deposition in rats after resection of 2/3 of the regenerated fatty liver. For more complete data on the therapeutic uses of dexpanthenol (13 in total), please visit the HSDB record page. Drug Warnings Direct intravenous injection of dexpanthenol is not recommended. One case of heartburn and several cases of gastrointestinal spasms have been reported after administration of dexpanthenol. Occasionally, there have been reports of allergic reactions to dexpanthenol; however, these reactions have not been directly attributed to the drug. Although there have been sporadic reports of adverse reactions such as itching, tingling, dyspnea, erythema, generalized dermatitis, urticaria, transient dyspnea (after administration of dexpanthenol 5 minutes after discontinuation of succinylcholine), hypotension, persistent (up to 10 days) diarrhea, and agitation following the use of dexpanthenol injection, a causal relationship between these adverse reactions and the drug has not been established. It is currently unknown whether the use of dexpanthenol in pregnant women will harm the fetus. During pregnancy, dexpanthenol injection should only be used when clearly necessary. Dexpanthenol injection should not be used to treat mechanical intestinal obstruction; for such patients, treatment should primarily focus on correcting the obstruction. The manufacturer of dexpanthenol injection advises that treatment for non-motorized intestinal obstruction includes correcting fluid and electrolyte imbalances (especially hypokalemia), anemia, and hypoproteinemia; treating infections; avoiding medications that reduce gastrointestinal motility; and, in cases of significant gastrointestinal distension, using a nasogastric tube or long bowel tube for gastrointestinal decompression. For more complete data on dexpanthenol (9 of 9), please visit the HSDB record page. Pharmacodynamics Pantothenic acid is a precursor to coenzyme A, which is a cofactor in many enzymatic reactions involving acetyltransferase. The final step in acetylcholine synthesis is the transfer of acetyl groups from acetyl-CoA to choline by choline acetyltransferase. Acetylcholine is a neurohumoral neurotransmitter in the parasympathetic nervous system and thus maintains normal intestinal function. Decreased acetylcholine levels can lead to weakened intestinal motility and, in extreme cases, even paralytic ileus. |
| Molecular Formula |
C9H19NO4
|
|---|---|
| Molecular Weight |
205.254
|
| Exact Mass |
205.131
|
| CAS # |
81-13-0
|
| PubChem CID |
131204
|
| Appearance |
Colorless to light yellow ointment
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
483.6±45.0 °C at 760 mmHg
|
| Melting Point |
< 25 °C
|
| Flash Point |
246.3±28.7 °C
|
| Vapour Pressure |
0.0±2.8 mmHg at 25°C
|
| Index of Refraction |
1.502
|
| LogP |
-0.92
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
14
|
| Complexity |
182
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
[C@@H](O)(C(C)(C)CO)C(=O)NCCCO
|
| InChi Key |
SNPLKNRPJHDVJA-ZETCQYMHSA-N
|
| InChi Code |
InChI=1S/C9H19NO4/c1-9(2,6-12)7(13)8(14)10-4-3-5-11/h7,11-13H,3-6H2,1-2H3,(H,10,14)/t7-/m0/s1
|
| Chemical Name |
(2R)-2,4-dihydroxy-N-(3-hydroxypropyl)-3,3-dimethylbutanamide
|
| Synonyms |
D-Panthenol; EC 201-327-3; Dexpanthenol
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
Ethanol : ~110 mg/mL (~535.93 mM)
DMSO : ~33 mg/mL (~160.78 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (10.13 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (10.13 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (10.13 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.8721 mL | 24.3605 mL | 48.7211 mL | |
| 5 mM | 0.9744 mL | 4.8721 mL | 9.7442 mL | |
| 10 mM | 0.4872 mL | 2.4361 mL | 4.8721 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.