35results about How to "Less irritating to blood vessels" patented technology

The invention discloses a taxol submicroemulsion. The submicroemulsion comprises taxol-cholesterol complex, injection oil, injection water, emulsifier, assistant emulsifier and isosmotic agent, wherein the weight ratio of taxol to cholesterol in the taxol-cholesterol complex is (1: 0.09) to (1: 0.90). The invention also discloses a preparation method and application of the taxol submicroemulsion. The oil-in-water taxol submicroemulsion, the pH value of which is 4 to 6 and the average particle size of which is less than 600nm, is prepared by taking the cholesterol complex as an intermediate carrier through the step of dissolving the cholesterol complex into an oil phase by using the improvement of the drug oil solubility by the cholesterol complex. The taxol submicroemulsion is used for treating malignant tumors and has higher safety and efficiency.

The invention discloses an alprostadil medium-and-long-chain lipid emulsion for injection and a preparation method thereof, belonging to the technical field of biological medicines. The lipid emulsion is composed of the following components in parts by weight: 0.01-0.1 part of alprostadil, 10-100 parts of long-chain triglycerides, 10-100 parts of medium-chain triglycerides, 1-20 parts of phospholipids, 0.01-1 part of oleic acid, 5-20 parts of glycerol and 300-2500 parts of water for injection. The particle size of the lipid emulsion is 50-200 nm, the lipid emulsion has good stability while the pH value is 5.0-8.0, and the contents of degradation products including prostaglandin A1 and prostaglandin B1 of alprostadil measured by using an HPLC (High Performance Liquid Chromatography) method are respectively below 1%. Compared with traditional alprostadil long-chain lipid emulsions, aqueous-phase alprostadil is significantly decreased, so that the vascular stimulation is reduced, and the liver load is reduced, therefore, the lipid metabolism can be accelerated, and the triglyceride level of plasma can be reduced.

The invention provides PGE1 (prostaglandin E1) freeze-dried microemulsion composition. The composition is prepared from PGE1, a non-ionic emulsifier, chondroitin sulfate, anionic phospholipid and a freeze-drying protective agent, and raw materials and components comprise, in percentage by mass, 0.001%-0.04% of PGE1, 1%-55% of the non-ionic emulsifier, 0.1%-20% of anionic phospholipid, 0.6%-28% of an oil phase and 5%-98% of the freeze-drying protective agent. The encapsulation efficiency and the stability of the composition are significantly improved, reduction of free drug concentration is facilitated, vascular irritation of a preparation is reduced, and the composition is safer and more stable.

The invention relates to a method for preparing clarithromycin ion-pair lipid microsphere injection by using cholesterol succinate monoester (CHEMS). Based on 100ml injection, it contains: clarithromycin 0.05g-0.5g; cholesterol succinate monoester 0.3g-0.6g; medium-chain fatty acid triglyceride 10g-20g; soybean oil for injection 0-10g; egg yolk lecithin 0.2g~4g; soybean lecithin 0g~4g; Pluronic F‑68 0.2g~1g; glycerin 2g~5g; water for injection 70g~90g. The physical and chemical properties of the clarithromycin ion-pair lipid microsphere injection of the present invention meet the requirements for intravenous administration, and can withstand high-pressure steam sterilization at 121° C. for 10 minutes. At the same time, this study is the first in the world to apply ion-pairing technology to the preparation of nano-preparations, which improves the transmembrane ability of clarithromycin, reduces bacterial drug resistance, and improves drug efficacy. The samples prepared in this study have good physical and chemical stability in long-term storage, and have little vascular irritation, which can improve patient compliance and curative effect.

The invention relates to norcantharidin derivative lipid microsphere injection and a preparation method thereof. The injection contains norcantharidin imide derivative, oil phase, water and surfactant; and the formula of the injection contains the following components by mass: 5 to 30 percent of oil phase, 0.001 to 1 percent of norcantharidin imide N-alkyl derivative, 0.5 to 7 percent of surfactant, 1 to 5 percent of osmotic pressure regulator, and the balance of injection water. Norcantharidin is connected with a long-chain saturated alkane group through amino, so that the lipid solubility of the injection is greatly improved, and the lipid solubility of the injection is improved together with increase of the chain length of the saturated alkane group. Lipid microspheres can carry medicaments with the granularity of more than 90 percent into lipid cores and (or) an interfacial film, so that the medicament loading capacity and the encapsulation efficiency are greatly improved, the vascular stimulation during injection is reduced, the physical and chemical stability of the medicaments and the lipid microsphere injection is improved, the in-vivo acting time of the medicaments is prolonged, the treatment effect is improved, and the toxic or side effect is reduced.

The invention provides an artemether liposome for injection, and the artemether liposome is prepared by an ethanol injection method. The preparation process of the method is simple and can be applied to industrial production. With a suitable preparation process, the prepared artemether liposome has a small particle size (150-200nm), uniform particle size distribution, and an encapsulation efficiency greater than 90%. Artemether liposomes are released slowly in the body to avoid adverse reactions caused by excessive drug concentration at the initial stage of injection. At the same time, the inventors found that the artemether liposome prepared by this method has high stability, high bioavailability, good resolubility, and long storage time, which meets its medication requirements.

The invention discloses a lipid microsphere injection containing sodium demethyl cantharidate-phosphatide complex and preparation method thereof. The injection comprises the sodium demethyl cantharidate-phosphatide complex, fat-soluble medium, surfactant and other ingredients. In the sodium demethyl cantharidate-phosphatide complex, the molar ratio of sodium demethyl cantharidate to phosphatide is 1-1:10. The prepared sodium demethyl cantharidate-phosphatide complex improves the distribution of sodium demethyl cantharidate in oil-water 2-phase interfacial film and oil phase greatly, increasesthe entrapment efficiency of the medicine in preparation, realizes the interfacial film loading medicine, reduces the toxicity, and can carry out targeting drug release in vivo. The prepared lipid microsphere injection reduces the vascular stimulation of sodium demethyl cantharidate, improves the curative effect, and reduces toxic and side effect.

The invention discloses an antihypertensive drug fat milk injection and a preparation method thereof. The antihypertensive drug fat milk injection is a clevidipine butyrate fat milk injection and contains clevidipine butyrate and a pharmacologically acceptable medical excipient; the medical excipient comprises an oil-phase medium, an emulsifier, an osmotic pressure regulator, a stabilizer, a metalcheating agent, a pH value regulator and injection water. The antihypertensive drug fat milk injection has stable quality and high safety and is not irritant to blood vessels.