Coenzyme Q10 intramuscular injection liquid and preparation method thereof

Abstract

The present invention discloses a formula and a preparation method of a coenzyme Q10 subcutaneous infusion liquid, wherein the coenzyme Q10 subcutaneous infusion liquid comprises coenzyme Q10, a solvent (vegetable oil for injection), an anti-oxidant and a preservative, and the active ingredient is coenzyme Q10. The preparation method comprises: adding coenzyme Q10 and an anti-oxidant to a heated solvent, dissolving, adding a preservative, and then carrying out volume metering, filtration, packaging, and sterilization to prepare the preparation meeting the injection requirement and suitable for subcutaneous injections. According to the present invention, the disadvantages of low bioavailability, poor stability in aqueous solution, easy precipitation, and short shelf life of the coenzyme Q10 are solved, Tween80 and other surfactants with safety hidden dangers are not used, the stability under high light is improved, the first pass effect of the oral preparation during absorption is avoided, the infusion safety risk is reduced, the cross-infection of the powder injection and the water injection is avoided, the stable blood drug level can be maintained, the related side effects can be reduced, and the clinical application level and the safety of the coenzyme Q10 are improved to the new realm.

Description

technical field [0001] The invention relates to a formula, a dosage form and a preparation method of coenzyme Q10, in particular to an intramuscular injection of coenzyme Q10 and a preparation method thereof, and belongs to the field of biochemical medicine. Background technique [0002] Coenzyme Q10 is a fat-soluble quinone compound, which is composed of a p-benzoquinone ring and a side chain (the dominant configuration) containing 10 isoprenoid units (see the figure below for the structural formula), so the The drug has good stability and is not sensitive to high temperature, high humidity, acid, and oxidation, but is only unstable to light and alkali. [0003] Coenzyme Q10 has a vitamin K-like structure. Its structural formula I is shown below. It has many biological functions. It is an endogenous synthetic substance in organisms. It exists in mitochondria and participates in the aerobic respiration of cells in the form of electron transport chain to generate energy subst...

AI Technical Summary

Problems solved by technology

[0010] 1. Low bioavailability. Co Q10 is a fat-soluble quinone compound synthesized by endogenous organisms. The solubility in water is extremely small, and the solubility in water at 20°C is less than 1×10 ‐6 mg / ml, the oral bioavailability is less than 30%;

[0011] 2. Disadvantages of dosage forms. The drug is an adjuvant therapy drug for hemorrhagic heart failure, coronary heart disease, hypertension, arrhythmia, secondary aldosteronism, sequelae of neck trauma, cerebrovascular disorders, hemorrhagic shock, and hepatitis. Most of the cases admitted to the hospital cannot be administered orally;

[0012] 3. It takes a long time to enter the blood. According to reports, the oral absorption of coenzyme Q10 is mainly through the emulsification with bile salts, and then dissolves into the low specific gravity chyloprotein through the small intestine wall, and then enters the blood circulation through the lymphatic absorption of the chest tube.

Therefore, there are strict restrictions on the use of Tween 80. It is a potentially unsafe excipient, and improper use will have a great impact on human health.

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