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Drug composition containing gefitinib

A gefitinib and composition technology, which is applied in the field of tablets containing gefitinib, can solve the problems such as changes in the dissolution profile, unsatisfactory stability, and inability to achieve therapeutically effective concentrations.

Active Publication Date: 2013-04-03
江苏万高药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Gefitinib is a poorly soluble drug, and its solubility in aqueous solution is pH-dependent, that is, the lower the pH, the greater the solubility in aqueous solution, and it is almost insoluble in water with a pH value of about 7. For the in vitro dissolution assay, 5% Tween-80 aqueous solution is selected as the dissolution medium. Under this condition, the gefitinib tablet of India NATCO Pharma Company only dissolves about 30% in 60 minutes, and the dissolution rate does not increase significantly in 90 minutes, indicating that A large amount of gefitinib is not released at all, and therapeutically effective concentrations cannot be reached
And how Iressa achieves the sustained and stable release of insoluble gefitinib, so far there is no literature or book to study and reveal it.
[0007] In addition, in the experimental research on Iressa on the market, it was found that its stability is not ideal, and the dissolution curve of products close to the expiration date has changed significantly. 99% has dropped to about 75%, which can no longer meet the quality standard requirements of the drug
That is to say, the release of the drug in the body can no longer reach the speed required for treatment, which will undoubtedly lead to a decline in the curative effect, ranging from prolonging the healing period, to delaying the best period of treatment, and causing the patient to lose the chance of recovery

Method used

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  • Drug composition containing gefitinib
  • Drug composition containing gefitinib
  • Drug composition containing gefitinib

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] Prescription (1000 tablets):

[0080] Gefitinib: 250.0g Lactose: 163.5g

[0081] Microcrystalline Cellulose: 50.0g Croscarmellose Sodium: 20.0g

[0082] Povidone K 30 : 10.0g Sodium lauryl sulfate: 1.5g

[0083] Magnesium stearate: 5.0g Gastric film coating premix: 12.5g

[0084] The particle size distribution of gefitinib is: D(0.1)=3μm, D(0.5)=13μm, D(0.9)=40μm.

Embodiment 2

[0086] The preparation process of embodiment 1: tablet core: earlier auxiliary material (that is, the material other than gefitinib) is passed through 80 mesh sieves respectively, standby; Get the gefitinib of prescription quantity, lactose, microcrystalline cellulose, twelve Sodium alkyl sulfate and croscarmellose sodium, mixed for about 15 minutes to make it uniform; Povidone K 30 Dissolve in water to make a binder solution with a concentration of 8%, add it to the above mixed powder, stir, and prepare soft materials; make granules with 14 mesh sieves; dry the wet granules at 60°C±5°C until the moisture content is lower than 2 %; The dry granules are sieved through a 20-mesh sieve, added with the prescribed amount of magnesium stearate, mixed evenly, and compressed into tablets.

[0087] Coating: adding water to the stomach-soluble film coating premix to make a coating solution with a concentration of 18%, the coating solution passes through a 100-mesh sieve to coat the tabl...

Embodiment 3

[0089] The types and dosages of raw and auxiliary materials for the prescription (1000 tablets) are the same as in Example 1, except that the particle size distribution of gefitinib is: D(0.1)=2μm, D(0.5)=18μm, D(0.9)=35μm.

[0090] Technology: with embodiment 2.

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Abstract

The invention relates to a drug composition containing gefitinib, in particular to a tablet comprising the gefitinib. The tablet containing the gefitinib is made of the gefitinib with the particle size distribution as follows: D(0.1) is equal to 2-6mm, D(0.5) is equal to 11-20mm, and D(0.9) is equal to 35-50mm. According to the drug composition, active ingredients can be released continuously and stably, and the drug composition has a good treatment effect on the local advanced lung cancer or metastatic non-small cell lung cancer subjected to the chemotherapy in the past.

Description

technical field [0001] The invention relates to a pharmaceutical composition containing gefitinib. The pharmaceutical composition is specifically a tablet containing gefitinib. The gefitinib tablet can continuously and steadily release active ingredients to exert medicinal effects, and belongs to field of pharmaceutical preparations. Background technique [0002] Gefitinib (chemical name: N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholinepropoxy)quinazolin-4-amine), is a A selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, suitable for locally advanced or metastatic non-small cell lung cancer (NSCLC) with sensitive mutations in the epidermal growth factor receptor tyrosine kinase (EGFR TK) gene Third-line, second-line or even first-line treatment for patients. [0003] Gefitinib tablets (trade name "Iressa", Iressa) were first developed by British AstraZeneca Pharmaceuticals Co., Ltd. (often referred to as original research), and were approved ...

Claims

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Application Information

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IPC IPC(8): A61K9/28A61K31/5377A61P11/00A61P35/00
Inventor 姚俊华
Owner 江苏万高药业股份有限公司
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