Name | 2-Propylvaleric acid sodium salt |
Synonyms | valerin sodium valproate Valproate Sodium SODIUM DIPROPYLACETATE sodiumbispropylacetate sodiumn-dipropylacetate 2-PROPYLPENTANOIC ACID NA sodium 2-propylpentanoate 2-propyl-pentanoicacisodiumsalt 2-Propylvaleric acid sodium salt sodiumalpha,alpha-dipropylacetate 2-PROPYLPENTANOIC ACID SODIUM SALT |
CAS | 1069-66-5 |
EINECS | 213-961-8 |
InChI | InChI=1/C8H16O2.Na/c1-3-5-7(6-4-2)8(9)10;/h7H,3-6H2,1-2H3,(H,9,10);/q;+1/p-1 |
InChIKey | AEQFSUDEHCCHBT-UHFFFAOYSA-M |
Molecular Formula | C8H15NaO2 |
Molar Mass | 166.19 |
Density | 1.0803 g/cm3 |
Melting Point | 300 °C |
Boling Point | 220°C at 760 mmHg |
Flash Point | 116.6°C |
Water Solubility | soluble |
Solubility | Easily soluble in water, ethanol, hot ethyl acetate, almost insoluble in ether, petroleum ether, acetone |
Vapor Presure | 0.0435mmHg at 25°C |
Appearance | White powder |
Color | White |
Merck | 14,9913 |
pKa | 4.8(at 25℃) |
PH | 6.0~9.0 (50g/l, 25℃) |
Storage Condition | 2-8°C |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in distilled water may be stored at -20°C for up to 3 months |
Sensitive | moisture absorption |
MDL | MFCD00078604 |
Physical and Chemical Properties | Melting point 300°C water-soluble soluble |
Use | A nitrogen-free broad-spectrum antiepileptic drug, used for the treatment and prevention of various types of epilepsy, the absence of small seizures, epileptic action disorders and other better efficacy |
Risk Codes | R22 - Harmful if swallowed R61 - May cause harm to the unborn child R36/38 - Irritating to eyes and skin. R36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S36/37 - Wear suitable protective clothing and gloves. S53 - Avoid exposure - obtain special instructions before use. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) S37/39 - Wear suitable gloves and eye/face protection S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. |
UN IDs | 2811 |
WGK Germany | 3 |
RTECS | YV7876000 |
HS Code | 29159000 |
Hazard Class | 6.1(b) |
Packing Group | III |
Toxicity | LD50 orally in mice: 1700 mg/kg (Meunier) |
Reference Show more | 1. Liu Jianjun, Li Junfeng, Dai Wenting, et al. Study on the Value of HPLC Method for Determination of Blood Concentration of Sodium Valproate in Epilepsy Patients [J]. Journal of Clinical Rational Drug Use 2018 v.11(26):26-27. 2. Jiang Jiaomei, Lu Xiaomei, Zhang Ming, et al. Protective Effect of Vitamin U on Renal Toxicity Caused by Sodium Valproate in Rats [J]. Journal of Epilepsy, 2018, v.4(06):20-25. 3. Lu Haimei, Xie Meijuan, Li Shan, et al. Improvement of 6Hz corneal kindling drug-resistant epilepsy mouse model and effects of three traditional Chinese medicine prescriptions [J]. Journal of Pharmacy 2018 053(007):1048-1053. 4. Zhang Xiaoxu, Chen Ziyi, Ren Ruina, Li Ruitong, Wang Xuedin, Ni Guanzhong, Zhou Yafang, Dai Qilin, Zhou Liemin, Huang Min. Pharmacokinetic interaction between valproic acid and lamotrigine in epileptic patients [J]. Chinese Journal of Clinical Pharmacology, 2021,37(01):66-69. |
This product is sodium 2-propylvalerate. Calculated as dried product, C8H15Na02 shall not be less than 99.0%.
take L. 0g of this product, add 20ml of water to dissolve, and then measure it according to law (General rule 0631). The pH value should be 7.5~9.0.
take this product l.Og, add new boiling cold water 10ml to dissolve, the solution should be clear and colorless. In case of color development, it shall not be deeper than the yellow No. 1 Standard Colorimetric solution (General rule 0901 first method); In case of turbidity, it shall not be deeper than the No. 1 turbidity standard solution (General rule 0902 first method).
take 1.25g of this product, place it in a separatory funnel, add 20ml of water, shake to dissolve it, add 5ml of dilute nitric acid, shake it, place it for 12 hours, and take the lower solution for testing. Take 5ml of test solution, add 10ml of water, and check according to law (General rule 0801). Compared with the control solution made of 5.0ml of standard sodium chloride solution, it should not be more concentrated (0.02%).
Take 10ml of the test solution under the chloride check item and check it according to law (General rule 0802). Compared with the control solution made of 0.02% of the standard potassium sulfate solution, it should not be more concentrated ().
take about lg of this product, add 10ml of anhydrous ethanol, should be completely dissolved.
new system for clinical use. Take about 0.5g of this product, put it in a separatory funnel, add 10ml of water, add 5ml of dilute sulfuric acid, shake to dissolve, extract with dichloromethane for 3 times, 20ml each time, combine dichloromethane solution, add appropriate amount of anhydrous sodium sulfate, shake, filter, and the filtrate is evaporated to dryness on a rotary evaporator (temperature not exceeding 30°C). Add an appropriate amount of dichloromethane, shake to dissolve the residue, and quantitatively transfer it to a 100ml measuring flask, dilute with dichloromethane to the scale, shake, as a test solution; Take 1ml precision, 100ml flask, dilute to the scale with two gas methane, shake, as a control solution; take 2-phenylethanol 20mg, put it in a 10ml measuring flask, add dichloromethane to dissolve and dilute to the scale, shake well, take lml, Put in a 25ml measuring flask, add 1ml of test solution, dilute to the scale with dichloromethane, and shake to be used as the system applicable solution. According to the gas chromatography (General 0521) test, with polyethylene glycol (PEG ~ 20m) as stationary liquid capillary column; Starting temperature is 130 deg C, maintain 20 minutes, the temperature was then increased to 200°C at a rate of 5°C per minute for 15 minutes; The inlet temperature was 220°C; And the detector temperature was 220°C. Take 1ul of the applicable solution of the system, inject human gas chromatography, record the chromatogram, and the separation degree of 2-phenylethanol peak and valproic acid peak should be greater than 3.0. The sample solution and the control solution were respectively injected with 1ul of each sample, and the gas chromatograph was recorded to 3 times of the retention time of the main component peak. If there are impurity peaks in the chromatogram of the test solution, the sum of each impurity peak area shall not be greater than the main peak area of the control solution (1.0%). The chromatogram of the test solution is 0.05 times smaller than the main peak area of the control solution.
take this product, dry to constant weight at 105°C, weight loss shall not exceed 3.0% (General rule 0831).
This product l.Og, inspection according to law (General Principles 0821 third law), containing heavy metals shall not exceed 20 parts per million.
take about 0.5g of this product, precision weighing, add 30ml of water to dissolve, add 30ml of ether as potentiometric titration method (General rule 0701), use glass-saturated calomel electrode, with hydrochloric acid titration solution (0.1 mol/L) titrated to pH 4.50 per 1 ml of hydrochloric acid titrant (O. 1 mol/L) corresponds to 16.62mg of C8H15Na02.
antiepileptic drugs.
sealed and stored in a dry place.
This product contains sodium valproate (C8H15Na02) should be labeled the amount of 90.0% to 110.0%.
This product is sugar-coated tablet or film-coated tablet, white or almost White after removing the coating.
Take 10 tablets (0.2g specification) or 20 tablets (0.lg), put it in a 100ml measuring flask, add about 50ml of water, shake to dissolve sodium valproate, dilute to the scale with water, shake well, filter, take 25ml of continuous filtrate with precision, according to the method under the determination of sodium valproate content, from the "add ether 30ml", according to the law. Each l of hydrochloric acid titration solution (0.1 mol/L) corresponds to 16.62mg of C8H15Na02.
Same as sodium valproate.
(l)0.lg (2)0.2g
sealed and stored in a dry place.
This product is a sterile lyophilized product of sodium valproate. Based on the average loading, the content of sodium valproate (C8H15Na02) shall be between 95.0% and 105.0% of the label loading.
This product is white or off-white loose lumps or powder.
Same as sodium valproate.
0.4g
light shielding, closed storage.
antiepileptic drug | sodium valproate is a broad-spectrum antiepileptic drug without nitrogen, which has good therapeutic effect on various types of epilepsy. it occupies a dominant position in China's antiepileptic drug market and has a broad market prospect. Sodium valproate belongs to branched-chain fatty drugs and is a classic broad-spectrum antiepileptic drug that is more active in the world. Although with the rapid development of the pharmaceutical industry in recent years, new drugs continue to emerge, but in the domestic anti-epileptic drug market, traditional drugs still occupy a dominant position in the prescription drug market. Among them, sodium valproate, topiramate and lamotrigine are in the leading position, accounting for 80-90% of the market share over the years. These three drugs are also classic drugs used by clinicians at present, which are directly related to the excellent effects of drugs, the vigorous academic promotion of manufacturers and the medication habits of doctors. the main dosage forms of sodium valproate are tablet 200mg/granule and sustained-release tablet 500mg/granule. Syrup 300ml/bottle (40mg/ml) and injection (each bottle contains 400mg of nearly white sterile sodium valproate lyophilized powder, with 1 4ml water for injection). In addition to the easier syrup for children to take sodium valproate, older children can also use sustained-release tablets. Sustained-release tablets are convenient and effective, and the effect of treating epilepsy is better than that of sodium valproate in conventional dosage forms. In addition, the patient has high compliance and can take it for a long time, and the incidence of adverse reactions is lower than that of combined drugs. |
traits | this product is a white oval film coat with a score on each side. after removing the film coat, it appears white. |
pharmacological action | the antiepileptic effect of sodium valproate is related to GABA. it is an inhibitor of GABA transaminase in the brain and can slow down the catabolism of GABA. At the same time, the activity of glutamate decarboxylase is increased to increase the production of GABA, thus increasing the GABA content of inhibitory synapses in the brain and improving the reactivity of postsynaptic membrane to GABA, so as to enhance GABAergic postsynaptic inhibition. It does not inhibit the discharge of epileptic foci, but can prevent the spread of abnormal discharge of the foci. In addition, sodium valproate can also inhibit Na and L-type Ca2 + channels. Sodium valproate is suitable for almost all types of epilepsy and seizures. It is one of the most effective broad-spectrum antiepileptic drugs, especially for various comprehensive seizures. Due to its broad-spectrum antiepileptic effect, sodium valproate has ushered in a new era of antiepileptic drug sales since its launch. |
pharmacokinetics | oral gastrointestinal absorption is rapid and complete, the blood drug concentration peaks in about 1-4 hours, the bioavailability is nearly 100%, and the effective blood drug concentration is 50-100 ug/ml. When the blood drug concentration is about 50ug/ml, the plasma protein binding rate is about 94%. When the blood drug concentration is about 100ug/ml, the plasma protein binding rate is about 80-85%. When the blood concentration exceeds 120 ug/ml, obvious adverse reactions may occur. With the increase of blood drug concentration, the free part increases, thus increasing the gradient into brain tissue (the concentration in brain fluid is 10-200% of the concentration in plasma, T1/2 is 7-10 hours, mainly distributed in extracellular fluid and liver, kidney, intestine and brain tissue, etc. Most of it is metabolized by the liver, including combination with glucuronic acid and certain oxidation processes. It is mainly excreted by the kidney, and a small amount is excreted and exhaled with feces. Can pass through the placenta and secrete into milk. |
Indications | Sodium valproate can be used for various types of epilepsy. Epilepsy can be used as a single drug treatment or as an additive treatment: used to treat generalized Epilepsy: including absence seizures, myoclonic seizures, tonic-clonic seizures, atonic seizures and mixed seizures, special types of syndromes (West,Lennox-Gastaut syndrome), etc. For the treatment of partial epilepsy; local seizures, with or without generalized seizures. Mania: used to treat manic episodes associated with bipolar disorder. Sodium valproate sustained-release tablet is a film-coated tablet with obvious nicks on both sides. After removing the coating, it will show white. It is used to treat generalized or partial seizures. It can also be used to treat special types of syndromes. For myoclonic seizures, absence seizures, tonic-clonic seizures, etc., they can have satisfactory therapeutic effects, control the condition of patients with epilepsy, and reduce the number of patients, the efficacy of the drug is very accurate. |
adverse reactions and side effects | sodium valproate, as a traditional antiepileptic drug, has been recognized by long-term practice worldwide. Its main adverse reactions are tremor, anorexia, nausea, vomiting and drowsiness. Long-term use may lead to weight gain, hair loss, menstrual disorders or amenorrhea, polycystic ovary syndrome. Concerns about the side effects of sodium valproate have focused on two groups: women and children. The hormonal changes, weight gain and teratogenic effects caused by sodium valproate make most doctors unwilling to prescribe sodium valproate for young female patients; children use sodium valproate to pay more attention to whether there is liver function Abnormalities, especially children younger than 3 years old, children with multi-drug combination therapy or organic brain diseases are more likely to have fatal liver failure. The incidence of adverse reactions was classified by CIOMS frequency: very common ≥ 10%; Common ≥ 1 and <10%; Rare 20.1 and <1%; Rare 20.01 and <0.1%; Very rare <0.01%, unknown (cannot be estimated from existing data). Congenital and familial/hereditary abnormalities. (See [Medications for Pregnant and Lactating Women]) Blood and lymphatic system abnormalities are common: anemia and thrombocytopenia (see [Precautions]). Rare: pancytopenia, leukopenia. Rarely: bone marrow failure, including pure erythrocyte aplasia, agranulocytosis, large cell anemia, and macrocytosis. |
drug interaction | taking attack-inducing drugs or drugs that reduce the attack threshold while taking this product should be carefully considered. it can be determined not to use or disabled according to the severity of the potential risk. These drugs mainly include most antidepressants (imipramine, SSRI), sedative drugs (phenothiazine and phenbutanone drugs), melquinine, butanospirone, tramadol, etc. Prohibited combination application: Combination with Melquinine: When taken in combination with epilepsy patients, because Melquinine may increase valproic acid metabolism and its own induction of seizures, it can be at risk of seizures and St. John's wort Combination: has the risk of reduced blood concentration and reduced anticonvulsant efficacy. |
medication for children | monotherapy is recommended when sodium valproate is used in children, but the possible benefits of Debakin should be weighed against the risk of liver damage or pancreatitis before starting treatment in such patients (see [Precautions]). Due to the risk of liver toxicity and bleeding, children should avoid taking this product in combination with acetylsalicylic acid. Children with liver and digestive tract dysfunction of unknown etiology (such as anorexia, vomiting, cytolysis), depression or coma, mental retardation, or children with newborn or infant death in the family, must be tested for metabolic indicators before receiving any valproate treatment, especially fasting and postprandial blood ammonia levels. For children and young people under 18 years of age, the safety and effectiveness of Debakin in the treatment of mania associated with bipolar disorder have not been studied. |
medication for pregnant and lactating women | it is not suitable for women of childbearing age unless it is clearly needed (I. e. under the condition that other treatments are ineffective or intolerable). This assessment should be conducted before the first prescription of this product is prescribed or when a woman of childbearing age who is treated with this product plans to become pregnant. Women of childbearing age must use effective contraceptive methods during treatment. Pregnancy · Risk Related to Epilepsy and Antiepileptic Drugs Studies show that the incidence of malformations in the offspring of mothers receiving any antiepileptic drugs is 2-3 times higher than reported in the general population (about 3%). The number of deformities reported during multiple drug treatments has increased, with the most common deformities being cleft lip and cardiovascular malformations. Very few children born to epileptic mothers have reported delayed development. It is impossible to distinguish the causes of the above conditions from genetic, social, environmental factors, the mother's epilepsy or antiepileptic drug treatment. Despite the above potential risks, antiepileptic treatment cannot be terminated suddenly, because it may lead to epilepsy, and the latter will cause serious consequences for both the mother and the fetus. During pregnancy, maternal tonic-clonic seizures and hypoxia caused by status epilepticus may increase the risk of death for mothers and unborn babies. |
precautions | special tips: in rare cases, the use of an antiepileptic drug treatment may lead to an increase in the number of seizures, or the type of seizures that appear, and It is different from the phenomenon observed in some types of epilepsy. When valproate is used, the reasons for the above phenomenon are mainly related to the combination of antiepileptic drug treatment or pharmacokinetic interaction (see [Drug Interaction]), toxic reactions (liver disease or encephalopathy) (see [Precautions] and [Adverse Reactions]) or drug overdose. Since the drug is converted into valproic acid in the body after taking this product, other drugs containing active ingredients that can be converted into the same compound should not be taken together while taking this product to prevent excessive valproic acid in the body (such as divalproate, valproamide, etc.). * For women of childbearing age, in some cases, if the patient and her treating physician make an informed choice after careful evaluation of all relevant factors, then this product is the appropriate choice for women of childbearing age (see [Precautions] and [Drugs for Pregnant and Lactating Women]). |
use | a nitrogen-free broad-spectrum antiepileptic drug, used to treat and prevent various types of epilepsy, and has better curative effect on absence minor seizures and epileptic malmobility |
production method | made from diethyl malonate. |