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A kind of erlotinib hydrochloride pharmaceutical composition without surfactant

A technology of erlotinib hydrochloride and surfactants, which is applied in the field of erlotinib hydrochloride pharmaceutical composition and its preparation, can solve problems such as easy damage to the stability of pharmaceutical crystal forms and affect product stability, and improve safety sexual effect

Active Publication Date: 2018-02-16
CHENGDU SINO STRONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This solution is easy to destroy the stability of the pharmaceutical crystal form and affect the stability of the product during the shelf life
[0007] As can be seen from the prior art analysis, its ultimate goal is to improve the dissolution rate of erlotinib hydrochloride in vitro, but each has its own limitations.

Method used

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  • A kind of erlotinib hydrochloride pharmaceutical composition without surfactant
  • A kind of erlotinib hydrochloride pharmaceutical composition without surfactant
  • A kind of erlotinib hydrochloride pharmaceutical composition without surfactant

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055]Weigh each component according to prescription 1, mix mannitol, lactose monohydrate and erlotinib hydrochloride evenly and pass through a 60-mesh sieve for micronization. The particle size distribution of the mixed material is required to be D10=0.1~5μm, D50=1~15μm , D90<30 μm. Take the mixture that meets the particle size distribution requirements to monitor the content of erlotinib hydrochloride, and convert the ratio in the material; take the mixture with known solid content, put it in the mixer, add microcrystalline cellulose PH101, sodium starch glycolate and mix for 10 minutes; collect material. Take the mixed material and put it on the dry granulator, adjust the rotation speed of the extrusion wheel (3.6~5.3rpm), the rotation speed of the feeding screw (12~24rpm), the pressure of the oil cylinder (the pressure of the oil cylinder is 1.0 MPa~3.0 MPa) to make it three Those who cooperate effectively, until the hardness of the pressed medicine block (1~3kg) is moder...

Embodiment 2~5

[0057] Each component is weighed according to prescription 2-5, and the preparation method is the same as in Example 1.

Embodiment 6

[0059] The dissolution rate measurement of embodiment 1~5 preparation

[0060] Dissolution method: paddle method, 75 rpm, solvent: 0.1mol / L hydrochloric acid solution (1%V / V~SDS) 1000ml.

[0061] At 5min, 10min, 15min, 30min, 45min, and 60min, take 10ml and filter it, dilute it with dissolution medium and measure it; the concentration of the reference solution is 10μg / ml. The drug concentration detection method is UV method; the detection wavelength is 352nm. The dissolution data are shown in Table 2.

[0062] Table 2

[0063] .

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Abstract

The invention discloses a surfactant-free erlotinib hydrochloride pharmaceutical composition, which comprises 150-300 parts by weight of erlotinib hydrochloride, 40-250 parts by weight of a diluent, and 80-190 parts by weight of a disintegrating agent. 5-10 parts by weight of lubricant. The invention also provides a preparation method of the pharmaceutical composition. The invention eliminates the use of special excipients of sodium lauryl sulfate in the formula, and at the same time solves the problem that the in vitro dissolution reaches the dissolution platform under the specified measurement conditions, which is consistent with the reference preparation, does not affect the bioavailability in the body, and improves the product safety in clinical use.

Description

technical field [0001] The invention relates to a surfactant-free erlotinib hydrochloride pharmaceutical composition and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] Erlotinib Hydrochloride (Erlotinib Hydrochloride, N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinolinamine hydrochloride, trade name: Tarceva, Tarceva) is a cancer treatment drug developed by OSI Pharmaceuticals in the United States, which belongs to the selective inhibitor of epidermal growth factor tyrosine kinase (EGFR-TK), which selectively blocks human epidermal growth factor receptor tyrosine kinase and reduces EGFR Its autophosphorylation, which leads to cell growth arrest and apoptosis, is mainly used for the treatment of non-small cell lung cancer. In 2005, the FDA approved the combination of erlotinib hydrochloride and gemcitabine for the treatment of advanced pancreatic cancer, becoming the first approved drug for the treatment...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K9/30A61K31/517A61K47/38A61P35/00
Inventor 蒲洪黄汉伟徐杰陈小宁许娟
Owner CHENGDU SINO STRONG PHARMA
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