Erlotinib hydrochloride tablet and preparation method thereof

A technology for erlotinib hydrochloride tablets and erlotinib hydrochloride, which is applied in pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc., and can solve the risk of biological inequivalence. problem, to achieve the effect of easy sieving, not easy to stick and punch, and the particle size of raw materials increases

Inactive Publication Date: 2016-06-01
SICHUAN KELUN PHARMA RES INST CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Application number: 201310051789.9, name of invention: erlotinib hydrochloride tablet and its preparation method, the present invention discloses an erlotinib hydrochloride tablet, which contains a surfactant with an HLB value between 10 and 20 as a solubilizer, which can Effectively promote drug dissolution, but the invention selected a surfactant inconsistent with the HLB value of the original research, resulting in an increased risk of in vivo bioinequivalence of the preparation

Method used

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  • Erlotinib hydrochloride tablet and preparation method thereof
  • Erlotinib hydrochloride tablet and preparation method thereof
  • Erlotinib hydrochloride tablet and preparation method thereof

Examples

Experimental program
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preparation example Construction

[0035] The preparation process of the pharmaceutical composition of the present invention is as follows: the raw materials and auxiliary materials are all passed through a 60-mesh sieve, mixed uniformly in an equal-volume incremental manner, then wet-granulated with an aqueous solution of sodium lauryl sulfate, dried, and added with magnesium stearate. Blending, tableting, coating. The dosage range is as follows:

[0036] Process steps

final parameter

Parameter control recommended range

preferred range range

Raw material sieve mesh

60 mesh

60~100 mesh

60~80 mesh

Concentration of sodium lauryl sulfate aqueous solution (w / w)

0.5％

0.4％～0.6％

0.4％～0.5％

moisture after drying

1～2％

1～5％

1～3％

Tablet hardness

50～70N

40～100N

50～80N

[0037] The process flow diagram of the present invention is as figure 1 Shown:

[0038] Process flow of the present invention is described as follows: ...

experiment example 1

[0050] Experimental Example 1: Erlotinib Hydrochloride Tablets Containing Raw Materials of Different Particle Sizes

[0051]

[0052] Preparation method: mix erlotinib hydrochloride (passed through a corresponding mesh sieve) and silicon dioxide, lactose, microcrystalline cellulose, sodium carboxymethyl starch (internal addition), and mix with sodium lauryl sulfate aqueous solution Wet granulation, drying, adding sodium carboxymethyl starch (additional), mixing evenly, adding magnesium stearate, mixing evenly and pressing into tablets.

[0053] The results are shown in Table-1 and figure 2 .

[0054] Table-1. Particle size screening results of raw materials

[0055]

[0056] From the above results, it can be seen that the change of the particle size of the raw material has no obvious impact on the disintegration time of the tablet core, but has a significant impact on the particle properties after disintegration. With the decrease of the particle size of the raw mater...

Embodiment 2

[0058] Embodiment 2: sodium carboxymethyl starch dosage screening

[0059]

[0060] Preparation method: with embodiment 1. The results are shown in Table-2 and image 3 .

[0061] Table-2 Screening Results of Sodium Carboxymethyl Starch Dosage (n=3)

[0062]

[0063] From the above results, it can be seen that on the basis of prescription A, the dosage of disintegrant sodium carboxymethyl starch increased from 10mg / tablet to 30mg / tablet, the disintegration time of the tablet increased, and the disintegration behavior also changed significantly. It shows the phenomenon of swelling first and then disintegrating; within this range, the dissolution curve in 0.1mol / L hydrochloric acid has no significant change, but the dissolution curve in pH6.8 phosphate buffer solution decreases (prescription F: 30mg / tablet). When the internal disintegrant was increased to 40mg / tablet, the disintegration time of the tablet did not slow down further, and the dissolution in both media was ...

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Abstract

The invention provides an erlotinib hydrochloride tablet. The erlotinib hydrochloride tablet is prepared from 109-164 parts by weight of erlotinib hydrochloride, 69-104 parts by weight of lactose, 120-180 parts by weight of microcrystalline cellulose, 5-50 parts by weight of sodium carboxymethyl starch, 0.1-1 part by weight of sodium dodecyl sulfate, 10-30 parts by weight of silica, 0.5-10 parts by weight of magnesium stearate and 0-25 parts by weight of a coating agent. The invention also provides a preparation method of the erlotinib hydrochloride tablet. The preparation method solves the problem that the fine raw materials can easily form airborne dust and has high adhesion and a slow dissolution rate. The preparation method utilizes a wet granulation process, improves raw material granularity and utilizes a wetting agent so that material airborne dust is greatly reduced and sticking possibility is reduced. Through wet granulation, the raw materials and accessory materials are uniformly dispersed and bonded with each other and layering possibility is reduced. Through prescription adjustment of silica addition, a raw material dissolution rate is improved. The erlotinib hydrochloride tablet provides a novel choice for clinical application.

Description

technical field [0001] The invention relates to an erlotinib hydrochloride tablet. Background technique [0002] Erlotinib Hydrochloride Tablets, English name: Tarceva (Erlotinib Hydrochloride Tablets) trade name: Tarceva; chemical name: N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4 -Quinolinamine hydrochloride [0003] [0004] This product is a new type of oral epidermal growth factor receptor tyrosine kinase inhibitor. It specifically binds to the adenosine triphosphate (ATP) binding pocket located in the tyrosine kinase domain of the HER1 / EGFR molecule in the cytoplasm. By inhibiting the combination of adenosine triphosphate and HER1 / EGFR, it effectively inhibits tyrosine kinase activity and downstream signal transduction, thereby inhibiting tumor cell proliferation, invasion, and metastasis, reducing tumor cell adhesion, promoting tumor cell apoptosis, and enhancing sensitivity to chemotherapy. , thereby prolonging the survival of cancer patients. For the third-...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K31/517A61K47/38A61K47/36A61K47/04A61P35/00
Inventor 周丹胡祥琳梁玉峰林保全沈利赵栋胡思玉王利春王晶翼
Owner SICHUAN KELUN PHARMA RES INST CO LTD
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