Palbociclib pharmaceutical composition and preparation method thereof

Abstract

The invention discloses a palbociclib pharmaceutical composition, comprising palbociclib or its medicinal salt and a pharmaceutically acceptable auxiliary material, wherein the palbociclib or its medicinal salt is 50-150 Mum, and the medicinal salt includes isethionates, hydrochlorides, sulfates or benzene sulfonates.Direct mixing and capsuling process of raw and auxiliary materials is used for the pharmaceutical composition provided herein, the biological availability is high, product quality stability is good, the technical process is easy to control, inter-batch reproducibility is good, and the composition is easy to industrialize.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a pharmaceutical composition of palbociclib, in particular to a pharmaceutical composition of palbociclib prepared by a direct mixing process and a preparation method thereof. Background technique [0002] Breast cancer is one of the most common malignant tumors in women. The incidence rate accounts for 7% to 10% of all kinds of malignant tumors in the whole body. It is second only to uterine cancer and has become the main cause of threat to women's health. Its incidence is often related to heredity, and the incidence rate is higher in women around the age of 40 to 60 before and after menopause. It is one of the malignant tumors that usually occurs in the glandular epithelial tissue of the breast, seriously affecting the physical and mental health of women and even threatening their lives. The incidence rate has been higher than the world average. [0003] Aro...

AI Technical Summary

Problems solved by technology

However, there are many shortcomings in the current dry granulation process: First, there are many dry granulation machine manufacturers in my country, but the stability of the equipment is relatively poor, and the failure rate is high. The main problems include roll damage, water leakage, roll misalignment, and dust production. Large, low yield, difficult to clean, unstable pressure, etc.; secondly, the equipment is expensive; the important thing is that the production volume is small, the first-pass rate is low, and the obtained particles are irregular, and their particle fluidity is not as good as wet granulation.

In addition, the key to the success or failure of gastric floating preparation design lies in whether it can achieve the expected floating effect in the stomach and whether it can prolong the residence time in the stomach. If it cannot be in a floating state, it can only be equivalent to an ordinary sustained-release matrix tablet. When the pH value of buciclib is greater than 4.0, the solubility is significantly reduced, which will cause the drug to not be fully absorbed and reduce the efficacy

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