Itraconazole pharmaceutical composition, preparation method and application thereof

Abstract

The invention discloses an itraconazole pharmaceutical composition which can significantly improve bioavailability and effectively improve individual difference. The composition comprises: a, a round or spherical pill core composed of medicinal excipients; b, a drug-containing layer composed of itraconazole, hydrophilic polymer and a releasing promoter; c, a protective layer composed of polyethylene glycol; wherein the releasing promoter preferably comprises Tweens, saccharides, inorganic acids, and alcohols, and further preferably comprises Tween-80, cane sugar, citric acid and mannitol; the weight ratio of the releasing promoter to the active component of itraconazole is 1:5 to 1:15, and is further preferably 1:8 to 1:13. The invention also discloses a preparation method and an application of the pharmaceutical composition.

Description

technical field [0001] The invention relates to a pharmaceutical composition containing itraconazole and a preparation method thereof, in particular to a pharmaceutical composition of itraconazole added with a release accelerator and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Fungal infection is a class of commonly encountered diseases and frequently-occurring diseases. In recent years, due to the increase in the incidence of tumors, diabetes, AIDS and other diseases and the increase in organ transplantation operations, the extensive use of antineoplastic drugs, immunosuppressants, and broad-spectrum antibiotics in clinical practice has led to bacterial imbalance and the body's resistance to fungi. Reduced resistance increases the incidence of superficial and deep fungal diseases and increases the mortality rate. Itraconazole is a triazole derivative, a third-generation antifungal drug, which has antibacterial e...

AI Technical Summary

Problems solved by technology

Adopt described release enhancer and other pharmaceutically acceptable micropill preparation forming auxiliary materials, as ball core, coating material etc., just can obtain high-quality itraconazole micropill by fluidized bed coating process, and Compared with the existing technology, it has the following obvious advantages: ①Solve the technical problem of low dissolution rate due to low solubility of itraconazole: compared with existing commercial products, the dissolution rate is increased from 80% to >90%; ② It solves the problem of large individual differences in oral bioavailability of commercially available products: it has significantly improved solubility compared with commercially available products at different pH values, indicating that it has significantly improved solubility for individuals with different gastric acid secretion;③ Solve the problem of large dosage and poor compliance of patients: due to the large volume of existing commercially available products, capsules of size 0 are required. Clinically, capsules of size 0 are not easy to swallow. In order to increase patient compliance, through research, the It was successfully changed to No. 1 capsule. Compared with the existing commercially available products, the dosage is reduced and it is convenient for patients to swallow; ④The problem of large amount of organic solvents used in commercially available products is solved: due to the special physical and chemical properties of itraconazole, it needs to be Dichloromethane and absolute ethanol are used as solvents. According to the relevant preparation patent materials of commercially available products, the amount of organic solvents used in the preparation process is relatively large. The newly invented preparation process reduces the amount of organic solvents by 20-30%, which is beneficial to environmental protection. And it reduces the cost of the product, which is more in line with the environmental protection and cost requirements of today's process transformation; ⑤ It further reduces the residue of organic solvents in the product, especially methylene chloride. Significantly reduce, especially the dichloromethane solvent that is particularly harmful to the body, which is 10-15 times lower than commercially available products, and is more conducive to the health of patients; 6. Further, formula 1 to formula 4 in embodiment 1 add release accelerators The itraconazole pharmaceutical composition also showed satisfactory bioavailability in Beagle dogs (bioavailability was significantly higher than that of existing commercial products)

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