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Novel preparation of neostigmine and derivatives thereof

A technology of neostigmine and its derivatives, which is applied in the field of new formulations of neostigmine and its derivatives, can solve unsolved clinical compliance problems and other problems, and achieve the effects of avoiding the first-pass effect, rapid dissolution, and precise dosage

Pending Publication Date: 2022-02-08
江苏谛奇医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the above-mentioned inventions all improve the current marketed preparations from the aspect of improving the stability of neostigmine and its analogs, and the prepared product administration route is injection administration, which can effectively avoid neostigmine and its analogs. Significant first-pass effect of drugs, but the clinical compliance problem caused by invasive drug administration has not yet been solved

Method used

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  • Novel preparation of neostigmine and derivatives thereof
  • Novel preparation of neostigmine and derivatives thereof
  • Novel preparation of neostigmine and derivatives thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-6

[0036] The component composition of embodiment 1-6 is as shown in table 1 below:

[0037] Table 1 is the composition table of embodiment 1-6

[0038]

[0039] The preparation steps of the preparation method of embodiment 1 to embodiment 6 are basically the same, and the main difference is that the prescription is different, specifically as follows:

[0040] S1, according to the proportion of the above components, add the prescribed amount of neostigmine bromide, mannitol, sodium carboxymethyl starch, pH regulator sodium carbonate, citric acid, and sodium bicarbonate to the three-dimensional motion mixer, and set the mixing frequency 10Hz, mixing for 20min;

[0041] S2, adding the prescribed amount of magnesium stearate to the mixed powder of S1, setting the mixing frequency to 10 Hz, and mixing for 5 minutes;

[0042] S3, compressing the mixed mixed powder into tablets with a high-speed rotary tablet press equipped with a 6mm circular mold to obtain sublingual bromostigmi...

Embodiment 7-9

[0060] The component composition of embodiment 7-9 is as shown in table 1 below:

[0061] Table 4 is the composition table of embodiment 7-9

[0062]

[0063] The preparation steps of the preparation method of embodiment 7 to embodiment 9 are basically the same, and the main difference is that the prescription is different, specifically as follows:

[0064] Disperse the prescribed amount of hypromellose in purified water at 90°C, stir and dissolve to obtain a colorless and transparent solution, then cool to room temperature and add the prescribed amount of bromoneostigmine, polyethylene glycol, and aspar Tan, edetate disodium, polysorbate, titanium dioxide, sodium carbonate, stirred for 5 minutes; then dispersed with a high-speed disperser for 7 minutes (rotating speed was set at 2000rpm); finally a white milky solution was obtained, and the above white milky solution was ultrasonically sterilized After soaking, it is added to a continuous coating machine for continuous fi...

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Abstract

The invention provides a novel preparation of neostigmine and derivatives thereof. The preparation comprises a sublingual mucosa preparation, a nasal mucosa preparation, a rectum mucosa preparation, a vagina and uterus mucosa preparation and an oral buccal mucosa preparation which take neostigmine or neostigmine derivatives as active ingredients. The preparation is administered through any mucosa pathway of oral buccal mucosa, sublingual mucosa, nasal mucosa, rectum mucosa or vagina and uterus mucosa. The preparation has a great clinical application value in preparation of drugs for treating myasthenia gravis, postoperative abdominal distension and urinary retention, supraventricular paroxysmal tachycardia and detoxification in the case of excessive tupistrine.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a new preparation of neostigmine and its derivatives and applications thereof. Background technique [0002] Neostigmine has a reversible cholinesterase inhibitory effect, so that acetylcholine will not be enzymatically hydrolyzed, and it exists in the cholinergic nerve endings for a long time, which has the effect of exciting smooth muscle; and can directly stimulate N2 on the motor end plate of skeletal muscle Choline receptors, so it has a strong effect on skeletal muscle and a small miotic effect; it is mostly used for myasthenia gravis, abdominal distension and urinary retention after surgery, and can also be used for supraventricular paroxysmal tachycardia and tube curare Detoxification in case of excess of alkali etc. The structural formula of neostigmine bromide is as follows: [0003] [0004] The clinical drug administration routes are mainly di...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/20A61K9/70A61K31/27A61P21/04A61P1/00A61P7/10A61P9/06A61P39/02
CPCA61K9/006A61K9/2018A61K9/2013A61K9/2009A61K9/2059A61K9/0043A61K9/0031A61K9/0034A61K9/7007A61K31/27A61P21/04A61P1/00A61P7/10A61P9/06A61P39/02
Inventor 张译芳江华胡华胜王蓉玲
Owner 江苏谛奇医药科技有限公司
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