Leflunomide sustained-release dropping pills and preparation method thereof

Abstract

The invention discloses a medicine composition used for curing rheumatoid arthritis. The invention aims at making up the deficiency of the existing oral medicine (leflunomide troche) used for curing rheumatoid arthritis, and provides a leflunomide sustained-release pill that has the advantages of high bioavailability, rapid effect, high medication content, enough medicine release, controllable medicine release, few times needed by the patient to take the medicine, convenient medicine taking, low price and no pollution in the production. The leflunomide sustained-release pill related by the invention takes leflunomide as raw material and can be prepared together with medicated carrier that takes hydrophilic framework material and hydrophobic framework material as stroma.

Description

technical field [0001] The invention relates to a pharmaceutical composition for treating rheumatoid arthritis, in particular to an oral drop pill sustained-release preparation prepared from eflunomide as a raw material. Background technique [0002] Leflunomide is a kind of pyrimidine synthesis inhibitor, which has been widely used in the treatment of rheumatoid arthritis recently. At the same time, it inhibits tyrosine phosphorylation, inhibits the initiation of transcription of interleukin (IL)-2 gene, thereby inhibiting the production of (IL)-2, blocking the proliferation of activated lymphocytes and cell cycle progression, and reducing antibody production . Leflunomide is also an effective inhibitor of NF-kB activation induced by various inflammatory stimuli, which can inhibit inflammation and immune activity, and is produced by inhibiting the activation of Th1 effector cells and regulating the differentiation of Th1 lymphocytes to Th2 lymphocytes Inhibition of T lymp...

AI Technical Summary

Problems solved by technology

[0003] Due to the preparation technology and other reasons, leflunomide tablets have problems such as long dissolution time, low dissolution rate, poor absorption, many times of taking medicine, hepatic and intestinal first-pass effect and low bioavailability after taking it, which affect the quality of the drug. Efficacy also directly affects the therapeutic effect

In addition, due to the granulation process in the tablet preparation process, it will generate relatively large dust pollution, which will cause harm to the health of the staff to a certain extent, and will also cause certain pollution to the environment.

Furthermore, the production process of the tablet is complicated and the production cost is high, so that the patient's medication cost is also increased, which is not conducive to improving the ability of the majority of patients to seek medical treatment, and is not conducive to improving the overall health level of the society.