Asarin lipid nanospheres and method for preparing same

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...

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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

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