Huperzine A derivative xipulin preparations

A technology of huperzine A and its derivatives, which is applied in the field of huperzine A derivative Xipulin preparations, can solve the problems of low selectivity of acetylcholinesterase, unsatisfactory curative effect and the like

Inactive Publication Date: 2008-06-04
YANGTZE RIVER PHARM GRP CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] The anti-senile dementia drugs currently on the market and clinically used are huperzine A, donepezil, etc., but the curative effect does not meet the ideal requirements, and because the selectivity to acetylcholinesterase is not high, it is easy to cause cardiovascular problems that are not related to the therapeutic effect. There is an urgent need to develop drugs with high selectivity to acetylcholinesterase in order to improve the curative effect and reduce side effects.

Method used

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  • Huperzine A derivative xipulin preparations
  • Huperzine A derivative xipulin preparations

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Make 1000 pieces of Xipulin tablets with the raw materials in the following weight ratio, and the weight of the tablet is 90mg

[0028] Shiplin 0.25g

[0029] Lactose 55g

[0030] Microcrystalline Cellulose 22g

[0031] Sodium Lauryl Sulfate Appropriate amount

[0032] Sodium carboxymethyl starch 10g

[0033] Magnesium Stearate 2g

[0034]

[0035] Made into 1000 pieces

[0036] Preparation Process:

[0037] 1. Grind and mix Shiplin raw material with sodium lauryl sulfate.

[0038] 2. Gradually sieve and mix Shipulin with lactose and microcrystalline cellulose according to the method of equal increase, and granulate by dry method.

[0039] 3. Add sodium carboxymethyl starch and magnesium stearate, mix well, and press into tablets.

Embodiment 2

[0041] Make 1000 Xipulin capsules with the raw materials in the following weight ratio, each weighing about 90mg

[0042] Shiplin 0.5g

[0043] 45g pregelatinized starch

[0044] Microcrystalline Cellulose 35g

[0045] Sodium Lauryl Sulfate 0.5g

[0046] Sodium carboxymethyl starch 6g

[0047] Micronized silica gel 1g

[0048] Magnesium Stearate 2g

[0049]

[0050] Make 1000 capsules

[0051] Preparation Process:

[0052] 1. Grind and mix Shiplin raw material with sodium lauryl sulfate.

[0053] 2. Gradually sieve and mix Shipulin with pregelatinized starch and microcrystalline cellulose according to the method of equal increment, and granulate by dry method.

[0054] 3. Add sodium carboxymethyl starch and magnesium stearate, mix well, pack into capsules, and get ready.

Embodiment 3

[0056] Make 1000 dispersible tablets of Shipulin with the raw materials in the following weight ratio, each weighing about 90mg

[0057] Shiplin 1g

[0058] Pregelatinized starch 42g

[0059] Microcrystalline Cellulose 25g

[0060] Polyvinylpyrrolidone 5g

[0061] Sodium Lauryl Sulfate 1g

[0062] Sodium carboxymethyl starch 15g

[0063] Magnesium Stearate 1g

[0064]

[0065] Made into 1000 pieces

[0066] Preparation Process:

[0067] 1. Grind and mix Shiplin raw material with sodium lauryl sulfate.

[0068] 2. Gradually sieve and mix Shipulin with pregelatinized starch, microcrystalline cellulose, and polyvinylpyrrolidone according to the method of equal increments, and granulate by dry method.

[0069] 3. Add sodium carboxymethyl starch and magnesium stearate, mix well, and press into tablets.

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Abstract

The invention discloses a huperzine-A derivant ZT1 preparation, having a chemistry-name: N-(2'-Hydroxyl-3'-methoxy-5'-chlorin-phenylmethylene) huperzine-A, which has the molecular formula of C23H23CIN2O and the molecular weight of 410.88. The invention comprises the ZT1 and ethanol content of the ZT1 that are shown by the structural formula. The invention adopts the huperzine-A derivant-ZT1 and subsidiary substances to be made into oral common tablets, dispersible tablets, enteric-coated tablets, hard capsules and granules by preparation techniques. As oral common tablets, dispersible tablets, enteric-coated tablets and granules, the invention mainly comprises ZT1, filling agents, bonds and disintegrants. The content of huperzine-A derivant-ZT1 is 50ug to 2.0mg in each tablet, each granule or each bag. The weights of filling agent and disintegrant respectively occupy 60 to 90 percent and 3 to 30 percent. The quality of the ZT1 preparation of the invention is stable, controllable, safe and effective.

Description

technical field [0001] The invention relates to a huperzine A derivative shiprin preparation. technical background [0002] The anti-senile dementia drugs currently on the market and clinically used are huperzine A, donepezil, etc., but the curative effect does not meet the ideal requirements, and because the selectivity to acetylcholinesterase is not high, it is easy to cause cardiovascular problems that are not related to the therapeutic effect. There is an urgent need to develop drugs with high selectivity to acetylcholinesterase in order to improve the curative effect and reduce side effects. Contents of the invention [0003] In order to improve the activity of medicines and reduce toxicity and side effects, the invention provides a huperzine A derivative shiprin preparation. [0004] In order to achieve the above object, the present invention adopts the following technical scheme: a huperzine A derivative shiprin preparation, the chemical name is: N-[2'-hydroxyl-3'-...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/439A61P25/28
Inventor 朱大元徐镜人唐希灿孙田江沈竞康蔡伟吴关松陈国俊蒋山好
Owner YANGTZE RIVER PHARM GRP CO LTD
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