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Ciprofibrate is a phenoxyacetic acid lipid-lowering drug, which is a new type of lipid-lowering drug.
Ciprofibrate competitively inhibits HMG-CoA reductase, reducing cholesterol synthesis; Increase the number of LDL receptors on the surface of hepatocytes, so that hepatocytes clear LDL cholesterol increased; Increase protease activity and increase very low-density lipoprotein clearance; Reduce blood viscosity, anticoagulant, antiplatelet aggregation, increase plasmin action, improve microcirculation.
Items | Specifications | Results |
Appearance | Off-white crystalline power | |
Solubility | Practically insoluble in water, freely soluble in anhydrous ethanol, soluble in toluene. | Conform |
Infrared absorption | Conform | Conform |
Chlorides | ≤350 ppm | Conform |
Melting point | About 115℃ | 117.5~117.6℃ |
Sulphated ash | ≤0.1% | 0.08% |
Water | ≤0.5% | 0.11% |
Solvent residues | Toluene ≤800 ppm n-Hexane ≤290 ppm | 693.2ppm 86.6ppm |
Appearance of solution. | The solution is clear and not more intensely coloured than reference solution BY4 | Conform |
Related substances | - impurity A ≤0.10% | N.D |
- impurity B ≤0.20% | N.D | |
- impurity C ≤0.10% | N.D | |
- impurity D ≤0.10% | N.D | |
- impurity E ≤0.8% | N.D | |
- any other impurity ≤0.10% | 0.08% | |
- total impurities ≤0.5% | 0.19% | |
-disregard impurity ≤0.05% | N.D | |
Assay (anhydrous substance) | 99.0~101.0% | 100.55% |
Conclusion | The product Complies to EP9.0 standard. |
Product parameters | |
Cas number: | 52214-84-3 |
Appearance: | White or almost white crystalline powder |
Purity: | 99% min |
Package details: | 25kg/drum |
Brand: | Fortunachem |
It is known for being a very potent fibrate with a long duration of action, allowing for once-daily dosing.
Chemical Class: It is a fibric acid derivative, similar to other fibrates like fenofibrate and gemfibrozil, but with a distinct chemical structure that contributes to its high potency and long half-life.
Key Feature: Its structure includes a dichlorocyclopropyl group, which makes it highly lipid-soluble and contributes to its long-lasting effect in the body.
Ciprofibrate works through several mechanisms, primarily by activating a specific nuclear receptor:
Primary Target: PPAR-alpha: Ciprofibrate is an agonist for the Peroxisome Proliferator-Activated Receptor alpha (PPAR-α). Activating this receptor changes the expression of genes involved in lipid metabolism.
Key Effects on Lipids:
Lowers Triglycerides (Major Effect): It dramatically increases the breakdown and clearance of triglycerides from the blood by stimulating the enzyme lipoprotein lipase (LPL). It also reduces the liver's production of Very-Low-Density Lipoprotein (VLDL), which is the main carrier of triglycerides.
Lowers LDL Cholesterol: It can moderately lower Low-Density Lipoprotein (LDL - "bad") cholesterol.
Raises HDL Cholesterol: It typically increases High-Density Lipoprotein (HDL - "good") cholesterol by increasing its synthesis.
Ciprofibrate is used to treat specific types of dyslipidemia (abnormal blood lipid levels), particularly in patients who have not responded adequately to diet, exercise, and other first-line medications like statins.
Its main uses include:
Hypertriglyceridemia: Treatment of very high triglyceride levels (Type IV and V hyperlipidemia) to prevent pancreatitis.
Mixed Dyslipidemia: Treatment of combined high triglycerides and low HDL cholesterol, often found in metabolic syndrome.
Hypercholesterolemia: It can be used to treat high cholesterol, though statins are usually preferred first-line.
Potency and Dosing: It is one of the most potent fibrates available. Due to its long half-life (~80 hours), it is taken only once a day.
Common Side Effects:
Gastrointestinal issues (dyspepsia, nausea, diarrhea).
Skin rashes.
Muscle pain (myalgia) and weakness.
Serious Side Effects and Risks:
Muscle Toxicity (Myopathy/Rhabdomyolysis): The risk is significantly increased when ciprofibrate is taken together with a statin (e.g., atorvastatin, simvastatin). This combination requires extreme caution and close monitoring.
Liver Function Abnormalities: Can cause an increase in liver enzymes (transaminases).
Cholelithiasis: Increases the risk of developing gallstones because it increases the cholesterol content of bile.
Renal Impairment: Should be used with caution in patients with pre-existing kidney disease, as it can be excreted by the kidneys.
Contraindications:
Severe liver or kidney disease.
Pre-existing gallbladder disease.
Pregnancy and breastfeeding.
Feature | Ciprofibrate (a Fibrate) | Statins (e.g., Atorvastatin) |
---|---|---|
Primary Effect | Lowers Triglycerides dramatically, raises HDL | Lowers LDL Cholesterol dramatically |
Mechanism | Activates PPAR-alpha receptor | Inhibits HMG-CoA reductase enzyme |
Best For | Hypertriglyceridemia, low HDL | Hypercholesterolemia, high LDL |
Key Risk | Muscle toxicity, especially when combined with statins | Muscle toxicity (alone or in combination) |
In essence, Ciprofibrate is a potent, long-acting fibrate drug used to correct abnormal blood lipid levels, with a particularly strong effect on reducing high triglycerides. Its use is highly effective but requires careful medical supervision due to the risk of serious side effects, especially muscle damage, particularly if used in combination with statin medications.
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