Pharmaceutical composition for treating breast cancer and preparation method of pharmaceutical composition

Abstract

The invention relates to the field of pharmaceutical preparations and particularly discloses pharmaceutical composition for treating breast cancer and a preparation method of the pharmaceutical composition. The pharmaceutical composition is prepared from components in percentage by mass as follows: 26%-30% of palbociclib, 38%-40% of lactitol, 28%-32% of microcrystalline cellulose, 1%-3% of polacrilin potassium and 1%-3% of methylcellulose. The composition is suitable for wet granulation, and tablets prepared through wet granulation have high dissolution rate, low impurity content, good fluidity, small tablet weight difference and good stability.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a pharmaceutical composition for treating breast cancer and a preparation method thereof. Background technique [0002] Palbociclib, chemical name 6-acetyl-8-cyclopentyl-5-methyl-2-[5-(1-piperazinyl)pyridin-2-ylamino]-8H-pyridine And[2-3-d]pyrimidin-7-one, whose trade name is Ibrance, is a new oral drug developed by Pfizer for the treatment of metastatic breast cancer. Palbociclib is a cyclin-dependent kinase 4, 6 The inhibitory drugs mainly prevent cells from G1 phase to S phase by inhibiting CDK4 / 6 activity, thereby inhibiting DNA synthesis. Clinical trial studies have found that palbociclib combined with letrozole is very effective for postmenopausal patients with locally invasive breast cancer or newly diagnosed estrogen receptor (ER) positive, HER-2 negative patients. Palbociclib was approved for marketing by the US Food and Drug Administration (FDA) on February ...

AI Technical Summary

Problems solved by technology

According to the international patent application publication WO2014128588, it is necessary to use a bulk drug of palbociclib with a larger particle size in order to improve its physical and chemical properties and the production capacity of the preparation product, but if the particle size is large, its fluidity is not satisfactory, especially Using powder direct compression or dry granulation, it is necessary to control the smaller particle size to meet the dissolution requirements

[0007] CN106667952A discloses a preparation method of a palbociclib pharmaceutical composition, which is firstly mixing lactose, microcrystalline cellulose, palbociclib raw material, a part of sodium carboxymethyl starch and magnesium stearate, and drying granulation, and then mixed with silicon dioxide, the remaining sodium carboxymethyl starch, and magnesium stearate; the obtained pharmaceutical composition has good content uniformity, drug stability, and high drug dissolution; but the dry granulation yield It is too low, and the raw and auxiliary materials need to be added separately for many times, and automatic continuous production cannot be realized. It is not the best choice for modern industrial production. At the same time, the particle size D 90 3.2-2.8 microns, poor fluidity

[0008] CN105213322A discloses a pharmaceutical composition prepared by a dry granulation process, which adopts internal and external addition to improve the dissolution rate and stability of the product, but the dry granulation also has problems such as low yield and poor fluidity

It adopts wet granulation and tabletting, and cornstarch is added with water to make a binder. The obtained composition has low dissolution rate, high water content in the granules, large difference in tablet weight, poor stability, high content of related substances, and poor dissolution rate.

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