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A kind of gefitinib tablet and preparation method thereof

A technology of gefitinib and nigra tablets, applied in the field of pharmaceutical preparations, can solve the problems of non-compliance with green chemistry, damage to instruments and equipment, lactose intolerance, etc.

Active Publication Date: 2020-10-27
NANJING YOKO PHARMA +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because gefitinib is difficult to dissolve in water when the pH is above 5, it brings great difficulties to the preparation research of gefitinib
[0005] CN1638805 discloses a kind of IRESSA pharmaceutical preparation containing water-soluble cellulose derivatives, the patent improves the solubility of gefitinib in the intestinal tract by adding water-soluble cellulose ethers or esters, but the tablets prepared by this method cannot collapse into Fine particles, dissolution is not complete, and lactose monohydrate is used as a filler in the examples. For Asian populations with intestinal lactase deficiency, lactose intolerance may occur, and abdominal cramps, diarrhea, abdominal distension and flatulence may occur. Clinical symptoms
[0006] CN102631347, CN102266300 disclose the method for improving the solubility of gefitinib by adding acidic substances, hydrochloric acid, acetic acid or citric acid, etc., but these acids have pungent odor or corrosiveness, do not meet the requirements of green chemistry, long-term use is harmful to instruments and equipment cause damage

Method used

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  • A kind of gefitinib tablet and preparation method thereof
  • A kind of gefitinib tablet and preparation method thereof
  • A kind of gefitinib tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] In order to avoid lactose intolerance, pregelatinized starch and microcrystalline cellulose 101 were used as fillers, and the traditional wet granulation process was used to compress tablets. The basic prescription was designed as shown in Table 1. By selecting different disintegrants, Croscarmellose sodium, carboxymethyl starch sodium, carboxymethylcellulose sodium, crospovidone XL-10 and low-substituted hydroxypropyl cellulose were used to investigate the disintegration and dissolution of gefitinib tablets .

[0064] Table 1 Selection of disintegrants

[0065]

[0066]

[0067] According to "Chinese Pharmacopoeia" 2015 edition four general rules 0921 to determine the disintegration time limit. It can be seen from Table 1 that Rx4 uses crospovidone XL-10 as the disintegrant, which has the fastest disintegration and can be disintegrated into large particles, while Rx1~Rx3 and Rx5 use croscarmellose sodium , sodium carboxymethyl starch, sodium carboxymethylcellul...

Embodiment 2

[0073] On the basis of Rx4, different granulation methods were selected to prepare gefitinib tablets, and the suitable process was determined by tablet disintegration and dissolution.

[0074] Preparation Process:

[0075] Pretreatment: Gefitinib micronization treatment, D50<3μM, D90<5μM.

[0076] a. Fluidized bed: Weigh the raw and auxiliary materials of the prescription amount respectively, add the materials into the fluidized bed, set the inlet air temperature to 55°C, the atomization pressure to 1.5MPa, and the air inlet volume to 30m 3 / h, granulate with appropriate parameters, spray the binder with the top spray method for granulation, dry at the same time, granulate with 20 mesh, add external materials for total mixing, and press into 11mm shallow concave tablets.

[0077] b. Powder direct compression: Weigh the raw and auxiliary materials of the prescription amount, mix them in equal increments, and press them into tablets with a shallow concave of 11 mm.

[0078] c....

Embodiment 3

[0087] On the basis of Rx8, gefitinib tablets were obtained by dry granulation by adjusting the ratio of pregelatinized starch and microcrystalline cellulose, and the disintegration and dissolution of plain tablets were investigated. The results are shown in Tables 5 to 6 and attached image 3 .

[0088] Table 5 Investigation results of fillers with different proportions

[0089]

[0090]

[0091] It can be seen from Table 5 that the weight ratios of filler pregelatinized starch / microcrystalline cellulose in Rx9~Rx13 are 8:13, 10:11, 4:3, 2:1 and 16:5, respectively. The higher the ratio of pregelatinized starch / microcrystalline cellulose 101, the faster the disintegration of gefitinib tablets. It may be due to the high viscosity of microcrystalline cellulose, which affects the disintegration speed of plain tablets, so the amount of microcrystalline cellulose in the filler should be controlled. When the weight ratio of pregelatinized starch / micronised cellulose 101 is ...

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Abstract

The invention discloses a method for improving dissolution rate of gefitinib. By screening a disintegrating agent, a technology and filler, the dissolution rate of gefitinib tablets, prepared by using crospovidone XL-10 as the disintegrating agent and taking a mixture of pregelatinized starch and microcrystalline cellulose which have a weight ratio of (4 to 3)-(16 to 5) as the filter and using the dry granulation technology, is found to be consistent with that of commercially available gefitinib tablets; furthermore, the method is less in loss of production equipment, simple in technology and easy to operate, thus being suitable for industrial mass production.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a gefitinib tablet and a preparation method thereof. Background technique [0002] Gefitinib, the English name is gefitinib, and the trade name is Iressa. It is suitable for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) who have previously received chemotherapy or are not suitable for chemotherapy. The structure is shown in the following formula: [0003] [0004] Gefitinib is a weakly basic compound. As the pH increases, its solubility decreases sharply between pH 4 and pH 6, and it is almost insoluble above pH 7. According to the biopharmaceutical classification system, gefitinib belongs to BCS classification type II, that is, low solubility and high permeability drugs. Because gefitinib is insoluble in water when the pH is above 5, it has brought great difficulties to the preparation research of gefitinib. [0005] CN1638805 ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K47/38A61K47/36A61K47/32A61K31/5377A61P35/00
CPCA61K9/2027A61K9/2054A61K9/2059A61K9/2095A61K31/5377
Inventor 杨勇杨婷张峰朱素华薛峪泉
Owner NANJING YOKO PHARMA
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