Metformin and fenofibric acid complex and preparation thereof

Abstract

The present invention discloses a metformin and fenofibric acid complex and a preparation thereof, wherein metformin and fenofibric acid are subjected to a direct salt forming reaction to obtain the complex. According to the present invention, the experiment results prove that the complex is the enteric sustained-release preparation prepared from the active components, and can release the two active components such as metformin and fenofibric acid in a simulated artificial intestinal juice, wherein the metformin and the fenofibric acid have good release consistency, such that the complex can be used for preparing pharmaceutical preparations for treatment of hyperlipoidemia, diabetes and other metabolic diseases; with the complex, the problem of the release inconsistency caused by the inconsistent pharmacokinetics between the two active components is solved, the significant sustained-release property is provided, the food effect and the early release condition do not exist, and the clinical use requirements of pharmaceutical preparations can be met; and the advantages of good compressibility, simple preparation process, easy scalization, low cost, stable quality and the like are provided.

Description

technical field [0001] The invention relates to a compound of metformin and fenofibric acid and its preparation, belonging to the technical field of medicine. Background technique [0002] Metformin is a biguanide known to have mainly antihypertensive activity and is widely used in the treatment of non-insulin-dependent diabetes mellitus. Metformin can also be administered to patients in combination with insulin; The refractory substance refers to a substance that does not bind to form a tablet when a compressive force is applied. [0003] Fenofibrate, a lipid regulator, can be used to reduce the level of triglycerides (fat-like substances) in the blood, specifically, fenofibrate can reduce high LDL-C, total-C, triglycerides esters and Apo-B and raises HDL-C, the drug has also been approved as an adjunctive therapy for the treatment of hypertriglyceridemia, a condition characterized by elevated plasma levels of very low-density lipoprotein (VLDL) , the compound is known to...

AI Technical Summary

Problems solved by technology

It is known that fenofibric acid has higher solubility in the small intestine area and higher bioavailability, however, the enhanced solubility will lead to related problems: C max Beyond the acceptable (recognized) range, for example: In US Patent Application 2005 / 0148594 an immediate release dosage form comprising amorphous fenofibric acid is described, as reported in the patent: when administered to a patient, comprising amorphous Formulations of fenofibric acid showed twice the bioavailability of capsules containing fenofibrate described in Example 6 of said published application

[0008] 1) lead to a significant increase in the dosage of the prescription, which is not conducive to clinical administration;

[0009] 2) The compressibility is poor, the friability is high, and cracks are prone to occur during tablet compression, and the quality of the obtained tablet core is not high, which directly affects the quality of the coating, resulting in a low qualification rate of the preparation and unqualified anti-acid performance;

[0010] 3) The key point is that the pharmacokinetic properties of the two are still inconsistent, the release and absorption in the body are still inconsistent, and there is a problem of early release, which is not conducive to industrial production and clinical application, and hinders the combination of metformin and fenofibric acid. The synergistic effect is not conducive to the development of preparations, especially the development of sustained-release preparations with consistent pharmacokinetics

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