Molecular Formula | C15H22O3 |
Molar Mass | 250.33 |
Density | 1.1109 (rough estimate) |
Melting Point | 61-63°C |
Boling Point | 158-159 C |
Flash Point | 141.6°C |
Water Solubility | >0.5g/L(temperature not stated) |
Solubility | Soluble in DMSO (50 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), ethanol (50 mg/ml a |
Vapor Presure | 6.13E-07mmHg at 25°C |
Appearance | powder |
Color | White to Off-White |
Merck | 14,4388 |
pKa | 4.75±0.45(Predicted) |
Storage Condition | 2-8°C |
Refractive Index | 1.5020 (estimate) |
MDL | MFCD00079335 |
Physical and Chemical Properties | Crystallized from hexane, melting point 61-63 ℃, boiling point 158~159 ℃/2.67Pa. Acute toxic LD50 mice, rats (mg/kg):3162,4786 oral. |
Use | Blood Lipid regulating drug, can reduce blood cholesterol and triglyceride content |
Risk Codes | R22 - Harmful if swallowed R63 - Possible risk of harm to the unborn child R62 - Possible risk of impaired fertility R46 - May cause heritable genetic damage R36/38 - Irritating to eyes and skin. R21 - Harmful in contact with skin |
Safety Description | S36 - Wear suitable protective clothing. S53 - Avoid exposure - obtain special instructions before use. S36/37 - Wear suitable protective clothing and gloves. S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S25 - Avoid contact with eyes. |
WGK Germany | 3 |
RTECS | YV7120000 |
HS Code | 2918992090 |
Hazard Class | IRRITANT |
Toxicity | LD50 in mice, rats (mg/kg): 3162, 4786 orally (Kurtz) |
white crystalline powder, odorless, tasteless. Melting Point 61~63 ℃; bpo. 02 158~159 ℃, very soluble in chloroform, soluble in methanol, ethanol, acetone or hexane, insoluble in water; Soluble in sodium hydroxide solution.
2, 5-methylphenol is reacted with 1,3 dibromopropane to form 3-(2,5 dimethylphenoxy) propyl bromide. Isobutyric acid, magnesium oxide and toluene are mixed and stirred, and heated to reflux to obtain a concentrated solution containing magnesium isobutyrate. A tetrahydrofuran solution of diisopropylamine and a pentane solution of n-butyl lithium are added thereto, and appropriate conditions are controlled, the resulting 3-(2.5-dimethylphenoxy) propyl bromide was added, and the reaction was stirred at room temperature and treated to give gemfibrozil. Alternatively, isobutyl isobutyrate reacts with 1 monochloro-3-bromopropane under the action of lithium diisopropylamide to form 5 monochloro-2, 2-methylpentanoate isobutyl Ester, and then reacts with 2,5-= methylphenol, gemfibrozil was obtained by hydrolysis.
This product is 2, 2-dimethyl-5-(2, 5-xylyloxy)-pentanoic acid. The content of C15H2203 shall be between 98.0% and 102.0% based on the anhydrous content.
The melting point of this product (General 0612) is 58~61°C.
It was first launched in the United States in February 1982. It is a kind of lipid regulator, which can significantly reduce the content of triglyceride and cholesterol in blood, and can significantly reduce the very low density lipoprotein (VLDL). Increased high-density lipoprotein (HDL), but had little effect on low-density lipoprotein. For hyperlipidemia. Suitable for severe Type IV or V type hyperlipoproteinemia, coronary heart disease risk and diet control, weight loss and other treatment ineffective. It is also suitable for patients with type Ⅱ B Hyperlipoproteinemia, high risk of coronary heart disease and diet control, weight loss, and ineffective treatment with other blood lipid regulating drugs.
mouse, rat oral LDso (mg]kg): 3162,4786.
take this product, add the mobile phase to dissolve and dilute to make a solution containing about 10mg per 1ml, as a test solution; Take an appropriate amount of precision, A solution containing about 20ug per 1ml was prepared as a control solution by quantitative dilution with mobile phase. According to the chromatographic conditions under the content determination item, take 10ul of the test solution and the control solution respectively, inject the human liquid chromatograph, record the chromatogram to 2 times of the retention time of the main component peak. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak shall not be greater than the area of the main peak of the control solution (0.2%), the sum of each impurity peak area shall not be greater than 5 times (1.0%) of the main peak area of the control solution.
take about 0.2g of this product, weigh it accurately, put it in a 20ml headspace bottle, add 5ml of dimethyl sulfoxide with precision, shake to dissolve it, seal it, and use it as a test solution; in addition, ethyl formate, n-hexane, Tetrahydrofuran, methylcyclohexane and toluene were appropriately weighed and diluted quantitatively with dimethyl sulfoxide to make 200ug, 11.6ug, 28.8ug and, the mixed solution of 47.2UG and 35.5UG, 5ml is accurately measured, placed in a 20ml headspace bottle, sealed, and used as a reference solution. Test as residual solvent assay (General 0861 second method). With 100% dimethyl polysiloxane (or polar similar) as the fixing liquid; The initial temperature is 40°C, maintained for 7 minutes, and the temperature is raised to 200°C at a rate of 15°C per minute for 5 minutes; the inlet temperature was 200°C; The detector temperature was 250°C; The headspace bottle equilibrium temperature was 80°C and the equilibrium time was 30 minutes. Take the reference solution into the headspace, the separation degree between the peaks of each component shall meet the requirements. Then the sample solution and the reference solution were injected with headspace, and the chromatogram was recorded. According to the external standard method, the residual amount of ethyl formate, n-hexane, Tetrahydrofuran, methylcyclohexane and toluene shall be in accordance with the regulations.
take this product, according to the determination of moisture (General 0832 first method 1), the water content shall not exceed 0.25%.
take l.Og of this product and check it according to law (General rule 0841). The residue left shall not exceed 0.1%.
The residue left under the item of taking the ignition residue shall not contain more than 20 parts per million of heavy metal when examined by law (General rule 0821, Law II).
measured by high performance liquid chromatography (General 0512).
silica gel bonded with eighteen alkyl silane was used as the filler; Methanol-water-glacial acetic acid (75:24:1) was used as the mobile phase; The detection wavelength was 276nm. Appropriate amount of gemfibrozil reference substance and 2, 5-dimethylphenol (impurity I) were dissolved and diluted with mobile phase to prepare solutions containing about 0.2mg and 0.05mg respectively per 1 ml, and 10 u1 was taken, injected into the liquid chromatograph, the separation degree of gemfibrozil peak and impurity I peak shall meet the requirements, and the number of theoretical plates shall not be less than 1500 based on gemfibrozil peak.
take an appropriate amount of this product, precision weigh, add mobile phase to dissolve and quantitatively dilute to make a solution containing about 0.2mg per lml, as a test solution, take 10 u1 for precision measurement, injection liquid chromatograph, record chromatogram. Another gemfibrozil reference substance was used for precision weighing and determination by the same method. According to the external standard method to calculate the peak area, that is.
hypolipidemic drugs.
sealed storage.
This product contains gemfibrozil (C15H2203) should be 90.0% to 110.0% of the label amount.
The content of this product is white powder.
take the contents under the difference of loading amount, mix well, accurately weigh an appropriate amount (about 50mg equivalent to gemfibrozil), put it in a 50ml measuring flask, and add an appropriate amount of mobile phase under the determination of gemfibrozil content, shake to dissolve gemfibrozil, dilute to scale with mobile phase, shake well, filter, Take 5ml of continuous filtrate precisely, put it in a 25ml measuring flask, dilute to scale with mobile phase, shake well, as the test solution, according to the method under the item of gemfibrozil content determination, that is obtained.
Same as gemfibrozil.
(1)0.15g (2)0.3g
sealed and stored in a cool and dry place.