Easily sublimating medicament injection solution and intravenous injection thereof

Abstract

The invention relates to the technical field of medicines, in particular to an easily sublimating medicament injection solution and an intravenous injection thereof. Easily sublimating medicaments comprise borneol, camphor, menthol crystal and the like. The injection solution of easily sublimating medicaments mainly consists of the easily sublimating medicaments, a solvent for injection and a small amount of pH regulator. When in use, the easily sublimating medicament intravenous injection can be prepared by uniformly mixing the easily sublimating medicament injection solution with emulsion or a 5 percent glucose injection solution according to a volume ratio of 1:5 to 1:250. After the easily sublimating medicament injection solution is mixed with the emulsion or 5 percent glucose injection solution, a drug loading rate of the easily sublimating medicaments in the intravenous injection can reach 1.5mg / ml and the easily sublimating medicaments cannot be crystallized and separated out in 18 hours. The easily sublimating medicament injection solution has a simple and safe preparation method, high solution stability, is convenient to store and transport and has no toxic or side effects. The difficult problem on clinical application of the injection preparation prepared from the easily sublimating medicaments is solved.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to an easily sublimable drug injection solution and an intravenous injection thereof. Background technique [0002] Borneol, camphor and menthol are commonly used active ingredients in traditional Chinese medicine. Borneol has anti-inflammatory, anti-myocardial ischemia, antibacterial, pain-relieving and antiseptic effects; Efficacy such as pain relief; Menthol has effects such as cool and refreshing, fragrance, seasoning, and expelling wind and relieving pain. Their common characteristics are easy sublimation and insoluble in water, so it is difficult to make an injection form, so oral and external dosage forms are in the majority, but oral absorption is poor and bioavailability is low. Take borneol as an example, it is a colorless transparent or white translucent flaky crisp crystal; it is fragrant, pungent and cool; it is volatile and easy to sublimate, and it is easily soluble i...

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Problems solved by technology

[0003] 1. β-cyclodextrin inclusion compound, Wang Yizhen et al. (Preparation process of borneol β-cyclodextrin inclusion compound [J]. Guangxi Medicine, 2004, 26 (6): 820-821), the prepared borneol β- The encapsulation efficiency of cyclodextrin inclusion compound is relatively low. If water is used as solvent, the encapsulation efficiency is only 47.3%; if 20% ethanol is used as solvent, although the encapsulation efficiency can reach 56.9%, there are potential safety hazards in the preparation process. In addition, β-cyclodextrin has strong hemolysis and nephrotoxicity, so borneol β-cyclodextrin inclusion complex is difficult to apply clinically

[0004] 2. Liposomes, Ren Weiqiong etc. (research on the preparation technology of borneol liposomes optimized by orthogonal experiments [J]. Hunan Herald of Traditional Chinese Medicine, 2005, 11 (1): 67-68), the prepared borneol liposomes The encapsulation rate is about 20%, the highest can only reach 26.3%, and the drug-making property is poor; moreover, complex rotary steaming process is required, the operation is complicated, and it is difficult to realize industrial production; the most important thing is that borneol is volatile and needs to be emulsified with Tween-80 , while Tween-80 has a strong hemolytic property and has great toxic and side effects

[0005] 3. Tween-80 solubilization. At present, many insoluble components of traditional Chinese medicines need Tween-80 solubilization to make injections. For example, in order to increase the water solubility of borneol, Guo Lirong, etc. (polyoxyethylene sorbitan monooleate solubilization Research on Borneol [J], Chinese Journal of Experimental Formulas, 2010, 16 (12): 10-13) the research results show that when Tween-80: borneol mass ratio = 15: 1, the borneol aqueous solution is stable, that is, in order to borneol Dissolved in water, need to add a large amount of Tween-80, and the hemolytic property of Tween-80 and anaphylaxis (particularly Tween-80 class anaphylaxis causes the direct cause of the clinical death case that often occurs in traditional Chinese medicine injection) seriously affects borneol Clinical Application of Injection

[0006] Camphor and menthol are also because of characteristics such as easy sublimation and insoluble water, therefore, the above-mentioned method is often used to develop its injections, and there are also problems such as safety, stability, and industrialization, so no very safe, very stable, Clinical Application of Yishenghua Drug Injection with Significant Curative Effect

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