Coenzyme Q_ (10) Intravenous Emulsion
|School||Shenyang Pharmaceutical University|
|Keywords||Coenzyme Q10 Intravenous emulsion Preparation Process Physical and Chemical Properties Pharmacokinetic visits|
The coenzyme Q 10 (the CoQ 10 ) widely present in the body in a variety of higher animals, mainly distributed in the body to the heart, liver. Kidney, muscle, thyroid and pancreas, adult total body content of about 0.5 ~ 1.5g. Epidemiological studies consistently show that the human body after the age of 20, the body of coenzyme Q 10 levels decreased gradually, the the coenzyme within patients and lesions organizations Q 10 level will reduce the variety of due Coenzyme Q 10 deficiency disease is serious harm to human health. As fat-soluble endogenous highly active anti-oxidant, hydrogen delivery body of the mitochondrial respiratory chain and cell metabolism activator coenzyme Q 10 is widely used in the treatment of diseases such as cardiovascular disease and adjuvant therapy. Currently, the coenzyme Q of domestic commercially 10 injections, tablets, capsules, oil balls forms, since the coenzyme Q 10 highly lipophilic, poorly water-soluble, in the choice of dosage form and appropriate route of administration, the need for deeper exploration. Therefore, this article examines the basic physical and chemical properties of coenzyme Q 10 measured solubility, apparent oil / water partition coefficient (P), in the light, high temperature oxidation and strong acid, alkali environment of stability , based on the data obtained to determine the feasibility of coenzyme Q 10 prepared as intravenous emulsions. HPLC detection coenzyme Q 40 content. Drugs, oil phase carrier, mixed emulsifier system is drawn on the basis of the investigation in the basic physical and chemical properties of coenzyme Q 10 pseudo ternary phase diagrams screened soy lecithin and PluronicF-68 as mixed emulsifiers, and to determine the the mixed emulsifier best ratio and the total amount of, by orthogonal design experiments to determine the the intravenous emulsion prescription concentration (2.0mg/ml). Through the single factor experiment ultimately determine a reasonable process. Coenzyme Q 10 intravenous emulsion stability study is divided into physical and chemical stability study two aspects: the physical stability of the effects of the osmotic pressure of the emulsion and saline and 5% dextrose injection two kinds dilutions of with emulsion mixed after the particle size distribution changes, should be used before use injection diluent diluted 1:4, to better ensure Coenzyme Q 10 intravenous emulsion clinical application security. Description of the intravenous emulsion long-term storage of the physical parameters of change by accelerated experimental results; chemical stability study including heat, light and acceleration experiments, described by high-performance liquid test results in the homemade coenzyme Q 10 intravenous emulsion drug content changes. In vivo experimental part, the HPLC assay of the method of the plasma samples coenzyme Q 10 content, good linear relationship, recovery compliance, accuracy, high precision. By the method of the diluted sample to eliminate the rat blank plasma endogenous coenzyme Q 10 drugs Determination and credibility so as to improve the detection results. Fit pharmacokinetic study data to BAPP2.0 common procedures, the results showed: Coenzyme Q 10 intravenous emulsion belong to the two-compartment model pharmacokinetics in rats, and the solution agent is a single-compartment model. Both compared the coenzyme Q ( 10 intravenous emulsions significantly prolong the average retention time in the body, the drug area under the curve increases. On coenzyme Q 10 intravenous emulsions stability and pharmacokinetic evaluation. coenzyme Q 10 intravenous emulsion prescription, process, physical and chemical properties, pharmacokinetics evaluation results show that: Coenzyme Q 10 sub > intravenous emulsion prescription viable, mature technology, stable physical and chemical properties, body safe and effective, with good prospects for application development.