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Asarin lipid nanospheres and method for preparing same

A technology of octylenol lipid and nanospheres, which is applied in the field of asarum lipid nanospheres and their preparation, can solve the problems that are not specified, and achieve the effects of reducing drug concentration, reducing degradation, and improving targeting.

Active Publication Date: 2011-06-08
SHENYANG WANJIA INST OF BIOLOGICAL TECH RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Through the adjustment of the composition and process of the prescription, and through the investigation of the common combination of the drug asarone, oil for injection, phospholipid, HS15, glycerin, and sterile water for injection, we have prepared a microparticle with a small particle size (average particle size less than 100nm). Xinnao lipid nanosphere preparations, traditional submicron emulsions prepared by patent 200510020878.2, patent 200610021154.4, patent 200610092037.7, patent 200510130064.4, its particle size will be greater than 150nm, and patent 200510045827.5, although listed in the patent includes drug asarum brain, injection oil, soybean lecithin, HS15, pure water, and glycerin, but the purpose is to prepare dry milk, so a large amount of freeze-drying protective agent is added and the freeze-drying process is adopted, so that the particle size of the emulsion cannot be smaller than 100nm, and in this patent, it is not specifically pointed out that only this prescription combination of the present invention can achieve the effect of the small particle size of lipid nanoparticles

Method used

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  • Asarin lipid nanospheres and method for preparing same
  • Asarin lipid nanospheres and method for preparing same
  • Asarin lipid nanospheres and method for preparing same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Preparation of Asarum Lipid Nanospheres:

[0027] Raw materials used: Asarone 4g, egg yolk lecithin 12g, soybean oil 50g, medium chain oil 50g, glycerin 24g, polyethylene glycol-12 hydroxystearate 35g, take asarone and medium chain oil respectively according to the above weight ratio Put oil, soybean oil, phospholipid and polyethylene glycol-12 hydroxystearate (HS 15) into a high-speed homogenizer and mix at 60°C to form an oil phase; then take glycerin according to the above weight ratio, and take 60°C Water for injection, add 825g of water for injection that has dispersed glycerin to the oil phase, homogenize at 15000-20000rpm for 3-5 minutes to form colostrum; then, use a high-pressure homogenizer to pass N 2 After 4 to 6 cycles, a uniform emulsion is formed and the pH is adjusted to 7. The prepared emulsion is firstly filtered with a 0.45 μm microporous membrane under pressure, and then filtered with a 0.22 μm microporous membrane; or packed and sealed , autoclaved...

Embodiment 2

[0031] Preparation of Asarum Lipid Nanospheres:

[0032]Raw materials used: asarone 2g, soybean oil 30g, medium chain oil 70g, egg yolk lecithin 2g, soybean lecithin 3g, polyethylene glycol-12 hydroxystearate 20g, glycerin 24g, add sterile water for injection to 1000mL , prepared according to the process method of Example 1.

[0033] The Asarone lipid nanospheres particle size assay method prepared by the present embodiment is to get Asarone lipid nanospheres 0.1ml, add purified water (with a pore diameter of 0.22 μm membrane filter in advance) and dilute to 5000 times, Mix well, as the test solution, and use Malvern Nano-ZS 90 particle size analyzer to measure. The average particle size is 94nm, see the results figure 2 .

[0034] The medium-chain oil in this example is caprylic / capric glyceride (abbreviated as medium-chain triglyceride MCT)

Embodiment 3

[0036] Preparation of Asarum Lipid Nanospheres:

[0037] Raw materials used: Asarone 5g, medium chain oil 150g, egg yolk lecithin 50g, polyethylene glycol-12 hydroxystearate 300g, glycerin 22g, add sterilized water for injection to 1000mL, and prepare according to the process of Example 1.

[0038] The Asarone lipid nanospheres particle size assay method prepared by the present embodiment is to get Asarone lipid nanospheres 0.1ml, add purified water (with a pore diameter of 0.22 μm membrane filter in advance) and dilute to 5000 times, Mix well, as the test solution, and use Malvern Nano-ZS 90 particle size analyzer to measure. After measurement: the average particle size is 35nm, see the results image 3 .

[0039] The medium chain oil in this embodiment is caprylic / capric glyceride (abbreviated as medium chain triglyceride MCT).

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Abstract

The invention discloses asarin lipid nanospheres and a method for preparing the same, and belongs to the technical field of medicaments. The asarin lipid nanospheres are prepared by the homogenization of the following raw materials in part by weight: 0.2 to 1.0 part of asarin, 5 to 15 parts of medium chain oil, soybean oil or the mixture of the medium chain oil and the soybean oil, 0.5 to 5 parts of lecithin, 1 to 30 parts of polyethylene glycol-12-methyl hydroxystearate, 1 to 4 parts of glycerol and 40 to 100 parts of water for injection. The preparation method comprises the following steps of: adding the oil phase into the aqueous phase, stirring the mixed solution to obtain the coarse product, adjusting the pH value, and repeatedly homogenizing the coarse product by a homogenizer to obtain the finished product. The average grain size of the lipid nanospheres is less than 100nm; compared with asarin injections and big-grain size emulsions which are sold on markets, the asarin lipid nanospheres obviously improve the targeting property in the lung, obviously reduce the distribution in the hepatic tissue, lower the potential hepatic toxicity and improve the drug efficacy.

Description

technical field [0001] The invention relates to an injectable asarone lipid nanosphere and a preparation method thereof, belonging to the technical field of medicines. Background technique [0002] Asarone, also known as α-asarone and α-asarone, mainly exists in the volatile oil of plants such as Shichangpu. Since the 1960s, extensive research has been carried out on asarone at home and abroad, and it has been confirmed that it has strong pharmacological activity. The research results show that the drug can resist histamine and acetylcholine, relieve bronchospasm and play an antiasthmatic effect. The cough center also has a strong inhibitory effect; it can cause an increase in secretions and play an expectorant role; it has a similar effect to aminophylline and has a relaxing effect on isolated bronchial smooth muscle; it can inhibit the brain by increasing the electrical stimulation valve of the cerebral cortex. Synaptic transmission of point stimulation and diffusion of e...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/09A61K47/44A61P11/00A61P11/06A61P25/08A61K47/34A61K47/14
Inventor 董英杰艾莉李乐
Owner SHENYANG WANJIA INST OF BIOLOGICAL TECH RES
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