Formula of asarone for injection and preparation method thereof

A technology for prescription and injection of Xinnao, which is applied in the field of preparation of Asarum for injection, can solve problems such as hidden safety hazards, inability to achieve therapeutic effects, and incomplete freeze-drying of products.

Inactive Publication Date: 2011-11-09
双鹤药业(海南)有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Asarone is a compound with extremely strong lipophilicity and extremely poor hydrophilicity, its tablets and capsules are difficult to disperse and dissolve after oral administration, and the effective specific surface area is small when in contact with body fluids, so the therapeutic effect cannot be achieved
Now many technologies use various methods to prepare Asarone injections, but there are many defects. For example, water and organic solvents are used to dissolve Asaron...

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Asarum 8.0g

[0023] Mannitol 400.0

[0024] PEG-400 225.0

[0025] Tween-80 130.0

[0026] Citric acid 1.5g

[0027] Water for injection 2.0kg

[0028] 0.15% of the total amount of activated carbon solution

[0029]

[0030] A total of 1000 bottles were made after freeze-drying

[0031] Weigh the prescription amount of raw and auxiliary materials, completely dissolve asarone in PEG-400 and Tween-80, and make "A" liquid; dissolve the prescription amount of mannitol in an appropriate amount of water for injection, and set aside; Measure citric acid and add water for injection to make a citric acid solution; add 70ml of citric acid solution to the mannitol solution, and the pH value of the solution should be 4.6; add the prescribed amount of activated carbon to stir and absorb for 30 minutes, and filter with a 0.45um filter membrane Remove charcoal to make "B" liquid medicine; add "B" liquid medicine to "A" liquid medi...

Embodiment 2

[0033] Asarum 8.0g

[0034] Mannitol 452.0

[0035] PEG-400 225.0

[0036] Tween-80 125.0

[0037] Citric acid 1.5g

[0038] Water for injection 3.0kg

[0039] 0.15% of the total amount of activated carbon solution

[0040]

[0041] A total of 1000 bottles were made after freeze-drying

[0042] Weigh the prescription amount of raw and auxiliary materials, completely dissolve asarone in PEG-400 and Tween-80, and make "A" liquid; dissolve the prescription amount of mannitol in an appropriate amount of water for injection, and set aside; Add 1.5g of acid to water for injection to make 72ml of citric acid solution; add 70ml of citric acid solution to the mannitol solution, and the pH value of the solution should be 4.6; add the prescribed amount of activated carbon to stir and absorb for 30 minutes, and use a 0.45um filter membrane to filter Remove charcoal to make "B" liquid medicine; add "B" liquid medicine to "A" liquid...

Embodiment 3

[0044] Asarum 16.0g

[0045] Mannitol 500.0

[0046] PEG-400 225.0

[0047] Tween-80 120.0

[0048] Citric acid 1.50g

[0049] Water for injection 4.0kg

[0050] 0.15% of the total amount of activated carbon solution

[0051]

[0052] A total of 1000 bottles were made after freeze-drying

[0053] Weigh the prescription amount of raw and auxiliary materials, completely dissolve asarone in PEG-400 and Tween-80, and make "A" liquid; dissolve the prescription amount of mannitol in an appropriate amount of water for injection, and set aside; Add 1.5g of acid to water for injection to make 80ml of citric acid solution; add 70ml of citric acid solution to the mannitol solution, and the pH value of the solution should be 4.6; add the prescribed amount of activated carbon and stir for 30 minutes, then use a 0.45um filter membrane to filter Remove charcoal to make "B" liquid medicine; add "B" liquid medicine to "A" liquid medicin...

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PUM

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Abstract

The invention provides a formula of asarone for injection and a preparation method thereof. In the invention, an injection is prepared by using asarone as a main ingredient, Tween-80 and polyethylene glycol (PEG)-400 as solubilizer and mannitol as an excipient, and the solubility of the asarone is improved effectively; and thus, the medicine carrying capacity of the injection is increased. The injection prepared by the invention has high re-solubility and product stability, and the preparation process is simple.

Description

Technical field: [0001] The invention relates to a drug injection, in particular to a preparation method of asarone for injection. Background technique: [0002] Asarone, also known as a-asarone or a-asarone, is mainly found in the volatile oils of plants such as Araceae plant Shichangpu, which has sedative, anticonvulsant, antispasmodic, antiasthmatic, hypolipidemic, choleretic, Anti-cancer and other pharmacological effects. It also has different degrees of inhibitory effect on the growth of pneumococcus, staphylococcus aureus and Escherichia coli, and it is mainly used clinically for pneumonia, bronchial asthma, chronic obstructive pulmonary disease with acute inflammation of the lungs, etc. [0003] Asarum is rapidly absorbed after oral administration, and the peak blood concentration can be reached in 15 minutes. The plasma protein binding rate is 61%, and it is quickly distributed in the liver, kidney, bile, heart, brain, lung, spleen and other organs, and the concentr...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/09A61K47/34A61P11/00A61P11/06
Inventor 魏雪纹李强
Owner 双鹤药业(海南)有限责任公司
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