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Pharmaceutical preparation for avoiding or reducing generation of N-nitrosamine genotoxic substances

A technology of genotoxicity and nitrosamines, applied in the field of medicine, can solve problems such as genotoxic impurities that cannot be solved, achieve the effect of reducing the production of genotoxic substances and improving drug safety

Inactive Publication Date: 2021-07-16
JIANGNAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These methods are not able to solve the problem of genotoxic impurities in existing drug products due to the existence of problems such as carryover and storage degradation

Method used

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  • Pharmaceutical preparation for avoiding or reducing generation of N-nitrosamine genotoxic substances
  • Pharmaceutical preparation for avoiding or reducing generation of N-nitrosamine genotoxic substances
  • Pharmaceutical preparation for avoiding or reducing generation of N-nitrosamine genotoxic substances

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Ranitidine 300 mg bilayer tablet in a 50:50 immediate release:sustained release ratio.

[0041] Group distribution ratio:

[0042]

[0043] Note: The "300 mg" tablet in the present invention refers to the weight of ranitidine free base in the tablet; the mass ratio of tert-butyl-p-hydroxyanisole to ranitidine free base is 1:30.

[0044] (1) Particle size control of raw and auxiliary materials:

[0045] The particle size of raw and auxiliary materials is controlled by standard sieve:

[0046]

[0047]

[0048] (2) Mixing of slow-release layer materials:

[0049] Add ranitidine hydrochloride, lactose (monohydrate), hydroxypropyl methylcellulose, tert-butyl-p-hydroxyanisole to a double wall blender and blend for 30 minutes, then add stearin to the above mixture magnesium acid, and the mixture was stirred again for 1 minute.

[0050] Immediate release layer material mixing

[0051] Add ranitidine hydrochloride, microcrystalline cellulose, croscarmellose sodium...

Embodiment 2

[0056] 75mg ranitidine calcium carbonate tablets:

[0057]

[0058] Note: The "75 mg" tablet in the present invention refers to the weight of ranitidine free base in the tablet; the mass ratio of ascorbyl palmitate to ranitidine free base is 15:1.

[0059] Tablet Compression: Combine, mix and compress the appropriate amounts of the ingredients above into small pieces. These small pieces are ground to form granules which can pass through a 14-16 mesh screen and can be compressed into tablets using a suitable compression die.

[0060] No antioxidant was added, and the bilayer tablet prepared by the same preparation method as in Example 2 was Comparative Example 2.

Embodiment 3

[0062] 51 grams of sodium carboxymethylcellulose (Blanose 7HF) was mixed with 500 grams of metformin hydrochloride and granulated with 95% ethanol in an asteroid mixer. The wet granules were passed through a 2 mm mesh screen and then dried in an oven at 55°C for 1 hour. The dried granules (530 grams) were mixed with 344 grams of hydroxypropyl methylcellulose 2208USP (grade 100,000cps), 9.5 grams of hydroxypropyl methylcellulose 2910USP (grade 5cps), 10 grams of ascorbic acid (vitamin C), and 100 grams of micro Crystalline cellulose (mass ratio of ascorbic acid to metformin hydrochloride is 1:50), mixed in a planetary mixer for 10 minutes. Finally, the mixture was mixed with 1% by weight of magnesium stearate and compressed into capsule-like tablets, each tablet containing 500 mg of metformin hydrochloride.

[0063] Without adding antioxidant, the bilayer tablet prepared by the same preparation method as Example 3 is Comparative Example 3.

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Abstract

The invention discloses a pharmaceutical preparation for avoiding or reducing generation of N-nitrosamine genotoxic substances, and belongs to the technical field of medicine. According to the invention, a suitable antioxidant is used in combination with effective components of a drug using or producing a substance or precursor substance that can degrade into N-nitrosamine genotoxic components during production and storage of active pharmaceutical ingredients or preparations, so that the generation of the N-nitrosamine genotoxic substances in the drug is effectively avoided or reduced; the drug safety is obviously improved.

Description

technical field [0001] The invention relates to a pharmaceutical preparation for avoiding or reducing the production of N-nitrosamine genotoxic substances, and belongs to the technical field of medicine. Background technique [0002] Genotoxic impurities refer to compounds that can directly or indirectly damage cellular DNA, resulting in mutagenic and carcinogenic changes; compounds with genotoxic impurity warning structures and unproven toxicity are called potential genotoxic impurities. It is generally believed that genotoxic impurities damage DNA by causing chromosomal breakage, DNA recombination, and covalent bonding or insertion during DNA replication. Therefore, genotoxic impurities have extremely strict control standards in pharmaceuticals. [0003] N-nitrosamines are a class of compounds formed by connecting the nitrogen atom of nitroso-NO to the nitrogen atom in the amino group and substituted on the amino group. It is stable in alkaline solution. Its formation me...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K47/22A61K47/10A61K47/12A61K47/14A61K47/18A61K47/42A61K47/46A61K47/20
CPCA61K45/00A61K47/22A61K47/10A61K47/12A61K47/14A61K47/183A61K47/42A61K47/46A61K47/20
Inventor 唐春雷杨子毅范为正
Owner JIANGNAN UNIV
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