Itraconazole sustained-release drop pills and preparation method thereof

Abstract

The invention discloses a drug combination oral preparation having antifungal effect, that is, an Itraconazole sustained-release pill and a preparation method thereof; the invention aims at overcoming the defect of the present antifungal drug oral preparation and providing Itraconazole sustained-release pill which is characterized by high bioavailability, rapid effect, high drug content, less times of medicine taking, long acting time, stable blood concentration, convenient oral administration, low price and no pollution in the production, and the preparation method thereof. The Itraconazole sustained-release pill related by the invention uses Itraconazole as raw material and is prepared together with officinal carriers of hydrophilic framework material and hydrophobic framework material that are taken as substrate.

Description

technical field [0001] The invention relates to a pharmaceutical composition with antifungal effect, in particular to a sustained-release oral preparation of triazole antifungal drugs prepared from itraconazole. Background technique [0002] Itraconazole is a triazole oral antifungal drug. Its antibacterial spectrum is similar to that of ketoconazole. It has antibacterial effects on both deep fungi and superficial fungi. The mechanism of action is that it highly selectively acts on fungal cytochrome P-450 , to inactivate cytochrome P-450-dependent enzymes, resulting in the accumulation of 14 sterols, inhibiting the synthesis of ergosterol, thereby inhibiting and killing fungi. This product is more effective than ketoconazole at low concentrations, and is effective against some molds Infections (such as Aspergillus and Brachyphyllum sp.) are also effective, whereas ketoconazole is not effective against molds. This product is well absorbed after oral administration. It reache...

AI Technical Summary

Problems solved by technology

[0008] "Itraconazole Injection", "Itraconazole Tablets" and "Itraconazole Capsules" with itraconazole as the main active ingredient have been approved by the health administrative department for production, but the injections are carried and administered Inconvenient, easy to cause adverse reactions, etc.; tablets and capsules have defects such as slow dissolution of active ingredients, poor absorption, frequent medication by patients, short effective time, and inability to take effect in time

[0009] Due to reasons such as preparation technology, oral preparations of most drugs, especially oral preparations of traditional Chinese medicines, have long dissolution time, low dissolution rate, poor absorption, many times of daily medication by patients, and unstable blood drug concentration after taking them. Hepatic and intestinal first-pass effect and low bioavailability, which affect the efficacy of the drug and directly affect the therapeutic effect

In addition, conventional oral dosage forms, such as tablets, capsules, granules (infusions), etc., due to the granulation process in the preparation process, will generate relatively large dust pollution, which will cause health problems to the staff to a certain extent. harm, and also cause some pollution to the environment

Although injections overcome the shortcomings of low bioavailability of conventional oral preparations, they also have the disadvantages of prone to allergic reactions, inconvenient use, and great pain for patients

Furthermore, the production process of conventional oral preparations and injections is complicated and the production cost is high, so that the cost of medication for patients is also increased, which is not conducive to improving the ability of patients to seek medical treatment, and is also not conducive to improving the overall health level of society

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