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Asarone injection emulsion and its preparing method

A technology of asarum and emulsion, applied in the field of asarum emulsion and preparation thereof, can solve the problems of low absolute bioavailability, difficulty, low melting point and the like of tablets and capsules

Inactive Publication Date: 2006-08-09
曾列丹
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] For tablets and capsules, Wu Chuang reported in α-asarone research progress, Chinese Journal of Pharmaceutical Sciences, 1997, 3 (32): 129~132, because asarone is a very strong fat-soluble compound, the melting point is low (58 ~59.5°C), it is difficult to make solid preparations with high bioavailability, so the absolute bioavailability of tablets and capsules is extremely low. To reach the blood concentration, the dosage can only be increased, so that the side effects will be corresponding increase, the toxicity and side effects are strengthened, and bring safety hazards to clinical medication
[0004] For injection, because asarone is insoluble in water, to make an aqueous solution, co-solvent or solubilizer must be added, such as patent number: CN200510073418.6, a kind of asarone preparation and preparation method for injection; patent number: CN200410021105. As described in 1 asarone injection and its preparation method, a large amount of hydroxypropyl-β-cyclodextrin was added for inclusion or Tween 80 (polysorbate 80) and propylene glycol or Tween 80 (polysorbate 80) Solubilization, so as to solve its solubility problem, so in the clinical application of the injection, due to the addition of hydroxypropyl-β-cyclodextrin or Tween 80 (polysorbate 80), such as anaphylaxis, hemolysis Sexual and irritating reports occur from time to time, which also bring unsafe factors

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0072] Dissolve 0.04g of asarone and 22.5g of glycerin in water for injection, dissolve 12.0g of refined soybean lecithin in refined soybean oil, heat to 45°C respectively, mix well, first disperse and emulsify in a tissue masher, and then The high-speed homogenizer emulsifies to meet the particle size of the preparation. Add water for injection to 1000ml, cool, fill, and sterilize to obtain asarone injection emulsion. This process is a 1000ml prescription, and the production can be expanded, and nitrogen protection is required during the production process.

Embodiment 2

[0074] Dissolve 0.08g of asarone and 25.0g of sorbitol in water for injection, dissolve 10g of refined lecithin in refined corn oil, heat to 40°C respectively, mix well, first disperse and emulsify in a tissue masher, and then pass through a high-speed The homogenizer emulsifies to meet the particle size of the preparation. Add water for injection to 1000ml, cool, fill, and sterilize to obtain asarone injection emulsion.

Embodiment 3

[0076] Dissolve 2.0 g of asarone and 55.0 g of xylitol in water for injection, dissolve 15.0 g of refined lecithin in refined sesame oil, respectively heat to 80°C, mix well, first disperse and emulsify in a tissue masher, and then The high-speed homogenizer emulsifies to meet the particle size of the preparation. Add water for injection to 1000ml, cool, fill, and sterilize to obtain asarone injection emulsion.

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PUM

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Abstract

The present invention relates to an asarone injection emulsion and its preparation method. Its composition includes active component asarone and medicinal auxiliary material which can be selected from injection vegetable oil, emulsifying agent and isoosmotic regulating agent. Said asarone injection emulsion can be used for resisting bacteria, relieving inflammation, stopping cough, expelling phlegm, relieving asthma, relieving convulsion and resisting epilepsy, etc.

Description

technical field [0001] The present invention relates to an asarone emulsion for injection and a preparation method thereof, in particular to an asarone which is used for antibacterial and anti-inflammatory, cough relieving, expectorant, asthma relieving, sedative, antispasmodic, anticonvulsant and antiepileptic Injectable emulsion and its preparation method. Background technique [0002] Asarone, also known as asarone, is the main component of the volatile oil contained in the rhizome of the traditional Chinese medicine Shichangpu. Since the 1960s, extensive research has been done on it at home and abroad, and it has been confirmed that it has strong pharmacological activity, antibacterial and anti-inflammatory properties. , cough, expectorant, asthma, sedative, antispasmodic, anticonvulsant, antiepileptic effect. It also has different degrees of inhibitory effect on the growth of pneumococcus, staphylococcus aureus and Escherichia coli. Among them, tablets, capsules and i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/09A61K36/882A61K9/107A61P11/00A61P25/08
Inventor 曾列丹
Owner 曾列丹
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