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Asarone submicron emulsion and its preparation method

A technology of octina submicroemulsion and asarone, which is applied in the direction of antiviral agents, antibacterial drugs, and pharmaceutical formulations, can solve unsatisfactory results and cannot be directly made into nasal sprays or lung inhalants, nasal mucosa or problems such as lung irritation

Inactive Publication Date: 2007-08-08
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The effective dose of asarone injection is 16-24mg each time, but its solubility is only 0.148mg / ml, so it cannot be directly made into nasal spray or lung inhalant
The research group has discussed cyclodextrin inclusion or solid dispersion technology in order to improve solubility, but the result is not ideal, and the solubility is only increased by 2-5 times; by adding a large amount of organic solvents and non-ionic surfactants (such as Tween) , improves solubility but can produce significant nasal or pulmonary irritation

Method used

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  • Asarone submicron emulsion and its preparation method
  • Asarone submicron emulsion and its preparation method
  • Asarone submicron emulsion and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Asarone feeds at 40mg / ml

[0041] Soybean Oil 20% (ml / ml)

[0042] Lecithin 1.5% (g / ml)

[0043] Poloxamer 188 3% (g / ml)

[0044] Glycerin 2.5% (g / ml)

[0045] Oleic acid 0.6% (g / ml)

[0046] α-tocopherol (antioxidant) 0.05% (g / ml)

[0047] Water for injection 77% (ml / ml)

[0048] Take glycerin and water for injection, heat it to 40-60°C, add refined lecithin and poloxamer, put it in a tissue masher, stir at a high speed to form a uniform water phase, and keep it warm; take asarone and α-tocopherol, add Put it into soybean oil and heat it to 40-60°C to make an oil phase. Slowly add the water phase to the oil phase under the stirring condition, put it in a tissue masher and stir at a high speed to form uniform colostrum. Quickly transfer the colostrum to a high-pressure homogenizer for homogenization, control the particle size below 500nm, collect all the emulsion, adjust the pH of the emulsion to 7.0±0.5 with NaOH, and obtain the product.

Embodiment 2

[0050] [Prescription Composition]

[0051] Asarone feeds at 60mg / ml

[0052] Soybean Oil 25% (ml / ml)

[0053] Lecithin 1.5% (g / ml)

[0054] Poloxamer 188 3% (g / ml)

[0055] Glycerin 2.5% (g / ml)

[0056] Oleic acid 0.6% (g / ml)

[0057] α-tocopherol (antioxidant) 0.05% (g / ml)

[0058] Water for injection about 75% (ml / ml)

[0059] [Preparation method]: with embodiment 1.

Embodiment 3

[0061] [Prescription Composition]

[0062] Asarone fed at 30mg / ml

[0063] Soybean Oil 20% (ml / ml)

[0064] Lecithin 1.5% (g / ml)

[0065] Poloxamer 188 4% (g / ml)

[0066] Mannitol 6.0%

[0067] Oleic acid 0.6% (g / ml)

[0068] α-tocopherol (antioxidant) 0.05% (g / ml)

[0069] Water for injection about 80% (ml / ml)

[0070] [Preparation method]: with embodiment 1.

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Abstract

The invention relates to a method for preparing asaryl sub-micro-emulsion, which comprises that dissolving the insoluble drug asaryl into oil, adding emulsifier, auxiliary emulsifying agent and other additives, to prepare the water-coat-oil sub-micro-emulsion. The sub-micro-emulsion carrier can improve the solubility of asaryl, to obtain uniform liquid agent. And the diameter of sub-micro-emulsion is lower than 500nm, which will not accumulated and laminate at room temperature in two years, with stable quality. The invention can be made into injection, atomization agent or nasal feeding agent, with high effect than oral agent. And the invention can avoid organic solvent and towen dissolvent to improve safety. The inventive asaryl sub-micro-emulsion can be used to treat bronchial asthma, or the like.

Description

technical field [0001] The invention relates to an oil-in-water (O / W) type submicroemulsion preparation of asarum. Submicron emulsion is formed by oil phase, water phase, emulsifier, co-emulsifier and stabilizer. Asarone, as an active ingredient, is dissolved in the oil phase (internal phase). Using the submicron emulsion as the carrier can significantly improve the solubility of the non-polar drug asarone, and increase the drug loading capacity of the system by hundreds of times. The submicron emulsion is milky white homogeneous liquid preparation, which does not flocculate and stratify after two years of storage, and has stable quality. It can be made into nasal spray or lung inhalation, and can also be made into small infusion for intravenous drip. Background technique [0002] a-asarone, also known as a-asarone and asarone, mainly exists in the volatile oil of plants such as calamus calamus. Since the 1960s, extensive studies have been conducted on asarone at home and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/075A61K47/14A61K47/44A61P31/04A61P39/06
Inventor 刘玉玲陈伟夏学军王洪亮
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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