Dry asarol emulsion and its prepn and application

The technology of brain stem emulsion and Asarum brain is applied in the field of pharmaceutical dosage forms in the field of medical technology, which can solve the problems of reducing and reducing the volume of pharmaceutical compositions, and achieve the effects of high curative effect, improved stability and curative effect, and controllable drug content.

Inactive Publication Date: 2007-12-19
陈云生 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It not only has the advantages of emulsions: increased drug stability, quick onset, accurate dosage, easy membrane penetration, long residence time in the body, easy accumulation to lesions such as inflammation and diffusion to the brain through the blood-brain barrier, etc.; At the same time, it makes up for the shortcomings of some emulsions: because this product is in a solid powder state, the emulsion droplets are not easy to aggregate, and the asarone in the emulsion droplets is not easy to diffuse to the outside during storage, which improves the stability of the auxiliary materials in the emulsion and further improves the main drug. stability, thereby improving the quality of the preparation and prolonging its shelf life; reducing the volume of the pharmaceutical composition, thereby reducing the requirements for production, transportation, storage, and clinical administration conditions; in clinical applications, you can optionally add Water or NaCl solution or glucose solution or fat emulsion and other solutions, one or more mixtures, after shaking and hydrating, revert to emulsion or further mix with fat emulsion or other aqueous solutions, which is conducive to flexible clinical drug use; Patients provided safer, stable and effective asarone preparations

Method used

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  • Dry asarol emulsion and its prepn and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] 1) Evenly disperse 0.2 g of asarone in 2 ml of soybean oil for injection;

[0046] 2) Mix 20g of soybean lecithin for injection with an appropriate amount of water for injection, and add 20g of lidocaine;

[0047] 3) Add 1) to the stirring 2), stir at 30°C at high speed to form colostrum, and use a high-pressure homogenizer to repeatedly homogenize the solution to obtain a uniform emulsion;

[0048] 4) Adjust the pH value of the emulsion between 5-9 and stir evenly;

[0049] 5) Add 8% sucrose solution as a protective agent, and add water for injection to 1000ml;

[0050] 6) obtain white block through freeze-drying process, fill with nitrogen, obtain dry asarum emulsion;

[0051] 7) Add water to the prepared dry emulsion according to the required amount, revert to emulsion after hydration and shaking.

Embodiment 2

[0053] 1) In the preparation equipment, 0.5 g of asarone is dissolved in 1 ml of soybean oil for injection;

[0054] 2) Mix 10 g of lecithin for injection with an appropriate amount of water;

[0055] 3) Add 2) into 1) under the condition of stirring, and after stirring at 30° C., pass through a homogenizer to homogenize the solution repeatedly to obtain a uniform solution. Prepare a total of 2000ml of liquid medicine;

[0056] 4) Add 5% mannitol as a protective agent, pass through a 0.22um microporous membrane to produce bacteria, aseptically repackage under 100-grade conditions, remove moisture through freeze-drying, and fill with nitrogen to obtain dry asarum stem emulsion;

[0057] 5) Add water to the prepared dry emulsion according to the required amount, revert to emulsion after hydration and shaking.

Embodiment 3

[0059] 1) Evenly disperse Asarone 0.1g in 60ml soybean oil for injection;

[0060] 2) Mix 12g of soybean lecithin for injection and TPGS with an appropriate amount of water for injection;

[0061] 3) Add 1) to the stirring 2), stir at 30°C at high speed to form colostrum, and use a high-pressure homogenizer to repeatedly homogenize the solution to obtain a uniform emulsion;

[0062] 4) Adjust the pH value of the emulsion between 3-5 and stir evenly;

[0063] 5) Add 8% sucrose solution as a protective agent, and add water for injection to 1000ml;

[0064] 6) obtain white block through freeze-drying process, fill with nitrogen, obtain dry asarum emulsion;

[0065] 7) The prepared dry emulsion is added to NaCl solution in required amount, hydrated and shaken, and then restored to emulsion.

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Abstract

The present invention discloses one kind of dry AAA emulsion and its preparation and application, and the dry AAA emulsion has asarol as effective component, emulsifier and other supplementary material. The dry AAA emulsion has mature technological process, easy industrial production, high stability, high curative effect and other advantages. It is applied mainly in clinical treatment of bronchitis, lung infection, asthma and other diseases.

Description

Technical field: [0001] The invention relates to pharmaceutical dosage forms in the technical field of medicine, in particular to an asarum brainstem emulsion and a preparation method and application thereof. Background technique: [0002] Asarone, molecular formula C 12 h 16 o 3 , molecular weight 208. It is white or off-white needle crystal or crystalline powder; odorless and tasteless. This product is soluble in ethyl acetate, chloroform or ether, soluble in ethanol or petroleum ether, insoluble in water. [0003] Oral administration of asarone is rapidly absorbed, and the blood concentration reaches the peak within 15 minutes, and is rapidly distributed in the liver, kidney, bile, heart, brain, lung, spleen and other organs. Part of it is excreted by bile, it is still reabsorbed through the intestine and liver, and finally it is mainly excreted with urine, and a small part is metabolized by the liver. The main metabolites are 2, 4, 5-trimethoxyacrylic acid (cinnami...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/085A61K47/44A61K9/107A61P11/00A61P11/06A61P25/08A61K47/14
Inventor 陈云生贾奕
Owner 陈云生
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