Generic name: fenofibrate capsules

constitutional formula

Former name: trade name: English name: fenofibrate capsules Chinese pinyin: fenofibrate Jiɑonɑnɡ The main ingredient of this product is fenofibrate. Its chemical name is 2- methyl -2-[4(4- chlorobenzoyl) phenoxy] isopropyl propionate. Structural formula: (see Lobaye Sustained-release Capsule) Molecular formula: C20H2 1ClO4 Molecular weight: 360.84 Edit this paragraph.

This product is a capsule, and its contents are white or white-like crystalline powder. Edit this laboratory analysis method

Method Name: Fenofibrate Capsules-Determination of Fenofibrate-Scope of Application: This method uses spectrophotometry to determine the content of Fenofibrate in Fenofibrate Capsules. This method is suitable for fenofibrate capsules. Method principle: absolute alcohol was added to the sample to make the test solution, and the absorbance was measured at 286nm wavelength by ultraviolet-visible spectrophotometer to calculate its content. Reagent: anhydrous ethanol equipment: ultraviolet-visible spectrophotometer sample preparation: 1. Preparation of test solution Take the contents of the difference between the contents of the test sample, mix well, accurately weigh an appropriate amount (about 50mg of fenofibrate), put it in a 100mL volumetric flask, add 75mL anhydrous ethanol, shake well to dissolve fenofibrate, add anhydrous ethanol to the scale, and shake well. Note: "Accurate weighing" means that the weighing should be accurate to one thousandth of the weighing. "Precise measurement" means that the accuracy of measuring volume should meet the accuracy requirements of volume pipette in national standards. Operation steps: Take the test solution, measure the absorbance at the wavelength of 286nm by ultraviolet spectrophotometry, and calculate the absorption coefficient (E 1m) of c20h 2 1cl 4 to be 484, thus obtaining the product. Note: A timely absorption cell of 65438±0cm should be used as a reference for spectrophotometry. Taking the wavelength with the largest absorbance as the determination wavelength, the absorbance reading of general samples has a small error between 0.3 and 0.7. The slit band width of the instrument should be less than half the absorption band width of the sample, otherwise the measured absorbance is low. The choice of slit width should be based on the fact that the absorbance of the sample will not increase when the slit width decreases. Because there may be blank absorption in the absorption pool and the solvent itself, the blank reading should be subtracted after the absorbance of the test sample is determined, and then the content should be calculated. References: Pharmacopoeia of China, editor-in-chief of National Pharmacopoeia Committee, Chemical Industry Press, 2005, part II, page 332. Pharmacology and toxicology of this paragraph.

This product is a blood lipid regulator derived from clofibric acid, which can reduce blood low density lipoprotein, cholesterol and triglyceride by inhibiting the production of very low density lipoprotein and triglyceride and increasing their catabolism. It also increases the production of apolipoprotein A 1 and A 1 1, thus increasing high density lipoprotein. This product can also reduce the blood uric acid of normal people and patients with hyperuricemia. Animal experiments show that fenofibrate has teratogenic and carcinogenic effects. Edit the pharmacokinetics of this paragraph

After oral administration, this product is well absorbed in gastrointestinal tract, and taking it with food can increase the absorption of fenofibrate. After oral administration

Fenofibrate capsules

The plasma concentration reached its peak in about 4 ~ 7 hours. The absorption half-life and elimination half-life after a single oral administration were 4.9 hours and 26.6 hours respectively, and the apparent distribution volume was 0.9 liter/kg. After continuous treatment, the half-life b is 2 1.7 hours. The binding rate of plasma protein was about 99%, and no accumulation was found after multi-dose administration. After absorption, it is mainly distributed in liver, kidney and intestine, followed by lung, heart and adrenal gland, and a small amount is distributed in testis, spleen and skin. Metabolism in liver and kidney tissues, after carboxyl reduction and glucuronidation, most metabolites are glucuronic acid products. After radioactive labeling, about 60% of metabolites are excreted by kidney and 25% by feces. The elimination half-life of this product is 20 hours, so it can be administered once a day. Studies have shown that the clearance rate of this product is obviously decreased in patients with severe renal insufficiency, and long-term medication can cause accumulation. Edit this clinical study

Efficacy is mainly used to treat hypercholesterolemia and/or hypertriglyceridemia which are not ideal for adult diet control therapy. Pharmacological effects of fenofibrate This product is a clofibric acid derivative blood lipid regulator, which can reduce blood low density lipoprotein, cholesterol and triglyceride by inhibiting the production of very low density lipoprotein and triglyceride and increasing its catabolism. It also increases the production of apolipoprotein A 1 and A 1 1, thus increasing high density lipoprotein. This product can also reduce the blood uric acid of normal people and patients with hyperuricemia. Animal experiments show that fenofibrate has teratogenic and carcinogenic effects. Drug interaction HMG-CoA reductase inhibitors, such as pravastatin, fluvastatin and simvastatin, should be used with caution, which may cause myalgia, rhabdomyolysis and serum creatine phosphokinase elevation. In severe cases, the drug should be stopped. When this product is combined with bile acid-binding resin (such as sphingosine), fenofibrate should be taken at least 1 hour or 4-6 hours before taking these drugs. Because bile acids can also be combined with other drugs taken at the same time, it will affect the absorption of other drugs. This product can enhance the curative effect of coumarin anticoagulants and prolong prothrombin time, so the dosage of oral anticoagulants should be reduced when combined, and then adjusted according to the test results. This product is mainly excreted through the kidney. When combined with immunosuppressants such as cyclosporine or other drugs with nephrotoxicity, it may lead to deterioration of renal function and should be reduced or stopped. When this product is combined with other drugs with high protein binding rate, it can increase its free form and enhance its curative effect, such as sulfonylurea hypoglycemic drugs such as tolbutamide, phenytoin and furosemide. The dosage of hypoglycemic drugs and other drugs should be adjusted when taking the above drugs during hypolipidemic treatment. The incidence of adverse reactions was about 2%- 15%. Gastrointestinal reactions including abdominal discomfort, diarrhea and constipation are the most common (about 5%); Rash (2%); Adverse reactions of nervous system include fatigue, headache, loss of libido, impotence, dizziness and insomnia (about 3%-4%); This product is a derivative of clofibric acid, which may cause myositis, myopathy and rhabdomyolysis syndrome, leading to the increase of serum creatine phosphokinase; Rhabdomyolysis occurs, mainly manifested as myalgia complicated with increased blood creatine phosphokinase, myoglobinuria and renal failure, but rare; Patients with nephrotic syndrome and other renal damage who lead to decreased serum albumin or hyperthyroidism have an increased risk of myopathy. (about1%); There is a tendency to increase gallstones, which can cause gallbladder diseases and even require surgery; At the initial stage of treatment, it can cause mild to moderate hematological changes, such as hemoglobin, hematocrit and leukopenia, and occasionally increase blood transaminase, including alanine and aspartate transaminase. Contraindications are prohibited in patients with fenofibrate allergy; Patients with gallbladder disease and cholelithiasis are prohibited. This product can increase the excretion of cholesterol to bile, thus causing gallstones. Patients with severe renal insufficiency, hepatic insufficiency, primary biliary cirrhosis or unexplained persistent liver dysfunction are prohibited. Edit this instruction

This product is used to treat hyperlipidemia with unsatisfactory effect of adult diet control therapy, and its effect of reducing triglyceride and mixed hyperlipidemia is more obvious than that of lowering cholesterol. However, this product can not completely replace diet control therapy, and can only be used as an auxiliary therapy on the basis of diet control. Edit the usage and dosage of this paragraph.

Adults generally take 0. 1g capsules once, three times a day, and the maintenance dose is 0. 1g each time, 1 ~ 2 times a day. In order to reduce stomach discomfort, it can be taken with diet; Patients with renal insufficiency and elderly patients should reduce medication; After 2 months of treatment, no effect was observed. Edit this adverse reaction

The incidence rate is about 2% ~ 15%.

Fenofibrate capsules

Gastrointestinal reactions including abdominal discomfort, diarrhea and constipation are the most common (about 5%); Rash (2%); Adverse reactions of nervous system include fatigue, headache, loss of libido, impotence, dizziness and insomnia (about 3% ~ 4%); This product is a derivative of clofibric acid, which may cause myositis, myopathy and rhabdomyolysis syndrome, leading to the increase of serum creatine phosphokinase; Rhabdomyolysis occurs, mainly manifested as myalgia complicated with increased blood creatine phosphokinase, myoglobinuria and renal failure, but rare; Patients with nephrotic syndrome and other renal damage who lead to decreased serum albumin or hyperthyroidism have an increased risk of myopathy. (about1%); There is a tendency to increase gallstones, which can cause gallbladder diseases and even require surgery; At the initial stage of treatment, it can cause mild to moderate hematological changes, such as hemoglobin, hematocrit and leukopenia. Occasionally, blood transaminase is elevated, including alanine and aspartate transaminase. Edit this taboo

Fenofibrate allergy is prohibited; Patients with gallbladder disease and cholelithiasis are prohibited. This product can increase the excretion of cholesterol to bile, thus causing gallstones. Patients with severe renal insufficiency, hepatic insufficiency, primary biliary cirrhosis or unexplained persistent liver dysfunction are prohibited. Notes for editing this paragraph

This product will interfere with diagnosis. Platelet count, blood urea nitrogen, transaminase and blood calcium may increase when taking this product. Serum alkaline phosphatase, G- glutamyltranspeptidase and bilirubin may decrease. Regular examination should be carried out during medication: whole blood picture and platelet count; Liver function examination; Blood cholesterol, triglyceride or low density lipoprotein; Blood creatine phosphokinase. If you have suspicious symptoms of myopathy (such as myalgia, tenderness, fatigue, etc. ) or serum creatine phosphokinase increased significantly, should stop taking drugs. While treating hyperlipidemia, we should also pay attention to and treat various primary diseases that can cause hyperlipidemia, such as hypothyroidism and diabetes. Some drugs can also cause hyperlipidemia, such as estrogen, thiazide diuretics, B receptor blockers and so on. After drug withdrawal, there is no need for corresponding anti-hyperlipidemia treatment. Dietotherapy is always the primary method to treat hyperlipidemia, and exercise and weight loss will be superior to any form of drug treatment. Edit this paragraph for pregnant and lactating women.

Pregnant and lactating women are prohibited. This product has no human experimental data. Edit this paragraph of children's medication

At present, the efficacy and safety of this product for children have not been confirmed by experimental studies, so this product cannot be used for children. Edit this medication for elderly patients

The clearance rate of single dose of this product in the elderly is similar to that of adults, but if there is renal insufficiency, the dose of this product should be reduced appropriately. Edit this paragraph about drug interaction.

HMG-CoA reductase inhibitors, such as pravastatin, fluvastatin and simvastatin, should be used with caution, which may cause myalgia, rhabdomyolysis, serum creatine phosphokinase elevation and other myopathy, and should be stopped in severe cases. When this product is combined with bile acid-binding resin (such as sphingosine), fenofibrate should be taken at least 65438 0 hours or 4 ~ 6 hours before taking these drugs. Because bile acids can also be combined with other drugs taken at the same time, it will affect the absorption of other drugs. This product can enhance the curative effect of coumarin anticoagulants and prolong prothrombin time, so the dosage of oral anticoagulants should be reduced when combined, and then adjusted according to the test results. This product is mainly excreted through the kidney. When combined with immunosuppressants such as cyclosporine or other drugs with nephrotoxicity, it may lead to deterioration of renal function and should be reduced or stopped. When this product is combined with other drugs with high protein binding rate, it can increase its free form and enhance its curative effect, such as sulfonylurea hypoglycemic drugs such as tolbutamide, phenytoin and furosemide. The dosage of hypoglycemic drugs and other drugs should be adjusted when taking the above drugs during hypolipidemic treatment. Edit this paragraph of overdose

Fenofibrate is highly bound to plasma protein, so when the drug is overdosed, systemic support treatment should be taken instead of hemodialysis. Edit this paragraph specification

0. 1g Edit this section for storage.

Shading, sealing and storage. This paragraph edits the revised and updated contents of China Pharmacopoeia (version 20 10).

Fenofibrate Capsule Fenofibrate Capsule The fenofibrate (C20H2 1ClO4) in this product should be 90.0% ~ 1 10.0% of the labeled amount. Identification (1) Take an appropriate amount of the contents of this product, add an appropriate amount of anhydrous ethanol, shake it well, dissolve fenofibrate, filter it, dilute it with anhydrous ethanol into a solution containing about 10μg per 1ml, and determine it by UV-Vis spectrophotometry (Appendix Ⅳ a), with the maximum absorption at the wavelength of 286nm. (2) In the chromatogram recorded under the content determination, the retention time of the main peak of the test solution should be consistent with that of the reference solution. Check the content of related substances under the difference of sample amount, mix them evenly, accurately weigh an appropriate amount, add mobile phase and shake them evenly, dissolve fenofibrate to make a solution containing 0.4mg per 65438±0ml, filter, and take the filtrate as the test solution; Accurately measure 1ml, put it in a 100ml volumetric flask, add mobile phase and dilute it to scale as a control solution. According to the chromatographic conditions of related substances of fenofibrate, inject 10μl reference solution into the liquid chromatograph, and adjust the detection sensitivity to make the peak height of the main component chromatographic peak about 20% of the full scale; Then accurately measure 10μl of the test solution and the reference solution, and inject them into the liquid chromatograph respectively, and record the chromatogram until the retention time of the principal component peak is twice. If there are impurity peaks in the chromatogram of the test sample, the sum of the areas of each impurity peak shall not be greater than the main peak area of the reference solution (1.0%). Peaks smaller than 0. 1 times the peak area of the control solution can be ignored. Dissolution take this product, according to the dissolution determination method (Appendix X C Second Method), take 1.0% sodium dodecyl sulfate solution 1000ml as the solvent, rotate at 120 rpm, operate according to the law, and after 60min, take 10ml solution, filter it. In addition, accurately weigh 10mg fenofibrate reference substance, put it in 100ml volumetric flask, add anhydrous ethanol to dissolve and dilute it to scale, shake it evenly, accurately measure 5ml, put it in 50ml volumetric flask, add 5ml 1.0% sodium dodecyl sulfate solution, add water to dilute it to scale, and shake it evenly as reference substance solution. Take the above two solutions, and measure the absorbance at the wavelength of 289nm according to the ultraviolet-visible spectrophotometry (Appendix 4A), and calculate the dissolution amount of each tablet. The limit is 60% of the marked quantity, which should meet the requirements. Others shall comply with the relevant regulations in the capsule (Appendix I E). The content was determined by HPLC (Appendix V D). The chromatographic conditions and system applicability tests used octadecylsilane bonded silica gel as filler (4.6mm×250mm, 5? m)； Using water (pH adjusted to 2.5 with phosphoric acid)-acetonitrile (30∶70) as mobile phase; The detection wavelength is 286nm, and the theoretical plate number is not less than 3000 according to the fenofibrate peak. Determination method: Take the contents of different volumes, mix them evenly, accurately weigh an appropriate amount (about equivalent to 10mg fenofibrate), put them in a 100ml volumetric flask, add an appropriate amount of mobile phase, fully shake them to dissolve fenofibrate, dilute them with mobile phase to scale, shake them evenly, filter them, and accurately measure the continuous filtrate1. Take an appropriate amount of fenofibrate reference substance, determine it by the same method, and calculate the peak area according to the external standard method. The category is the same as fenofibrate. Specification 0. 1g Storage shading, sealed preservation.