35results about How to "Stable drug loading" patented technology

The invention relates to drug slow-release microparticles, in particular to triptorelin sustained-release microparticles and a preparation method thereof. The composition includes the following components by weight percentage: 0.5%-20% of triptorelin, 79%-99% of PLGA, and 0.1%-1% of poloxamer. The preparation method of the above-mentioned triptorelin sustained-release microparticles of the present invention comprises mixing each component and sending it into a hot-melt extruder, where heating and melting, extrusion and low-temperature pulverization are carried out. The praline sustained-release microparticles of the present invention have good shape, high encapsulation efficiency of the microparticles, good drug loading capacity and stable release. The synthesis process is simple, the product itself is non-toxic, and the product after degradation is non-toxic and stable in quality.

The invention relates to 2-methoxyl estradiol lipidosome freeze-dried powder injection and a preparation method thereof. The invention can effectively solve the problems of poor water solubility of 2-methoxyl estradiol, short half-life and low oral administration bioavailability, and adopts the technical proposal that the 2-methoxyl estradiol lipidosome freeze-dried powder injection comprises the following raw materials in weight portion: 1 portion of the 2-methoxyl estradiol, 3 to 100 portions of phospholipid, 1 to 30 portions of cholesterol, surfactant and freeze-dried preservative, wherein according to the weight ratio of the phospholipid, 0.1 to 10 portions of the freeze-dried preservative is added into 1 portion of the phospholipid, and the adding quantity of the surfactant is 0.2 to 3 percent of the total amount of the freeze-dried powder injection. The freeze-dried powder injection using the components as raw materials can be realized by three preparation methods, namely, a film dispersion method, a reverse phase evaporation method and an injection method, has high medicament content, is suitable for intravenous administration, has the advantages of slow release capability, in vivo targeting property and the like, can overcome the defects of oral preparations, is safe and reliable, and has large economic benefit and social benefit.

The invention discloses a solid preparation of atorvastatin calcium liposome. The preparation is prepared from the atorvastatin calcium liposome and other pharmaceutically common auxiliary materials, wherein the atorvastatin liposome is prepared from the following components in parts by weight: 1 part of atorvastatin calcium, 2-5 parts of phospholipid and 0.8-3 parts of additive. The atorvastatinsolid preparation prepared from the liposome has the advantages that the dissolution rate is increased, the stability and bioavailability are greatly improved, the product quality of the preparation is improved and the toxic and side effect is reduced.

The invention discloses a medicine slow-release composition and a preparation method. The drug sustained-release composition of the present invention is a granular composition obtained by foaming and jet milling techniques, which comprises 60-80 parts by weight of a fat-soluble polymer, 1-10 parts by weight of a hydrophilic polypeptide drug and 25-35 parts by weight. parts by weight of mannitol. Wherein, the fat-soluble high molecular polymer is a porous solid particle, the hydrophilic polypeptide drug is embedded in the inside of the fat-soluble high molecular polymer, and the mannitol is in powder form and mixed with the fat-soluble high molecular polymer to form a composition.

A kind of pH-sensitive nano-medicine based on calcium carbonate coordination chelation drug and its preparation method and application, calcium chloride is dissolved in absolute ethanol, then add additive solution, stir evenly, obtain solution A; Ethanol of antineoplastic drug The solution was added dropwise to solution A, and left to stand after dropping to obtain a mixed solution B; the mixed solution B and ammonium bicarbonate were placed in a vacuum oven for reaction, then dissolved in dichloromethane, and then added carboxyl-containing high Molecular substances, after stirring evenly, add 4-dimethylaminopyridine and dicyclohexylcarbodiimide, rise to room temperature, and continue to react in the dark to obtain pH-sensitive nano-medicines based on calcium carbonate coordination and chelation drugs. The preparation method of the present invention has mild conditions, easy operation, controllable size of nano medicine and good stability. The drug carrier prepared by the invention can selectively release anti-tumor drugs according to the difference in pH environment of tumor tissues and can be applied in the preparation of anti-tumor drugs.

The invention relates to a pectin-5-fluorouracil colon cancer two-targeting prodrug and the preparation method thereof, and mainly synthesizes a two-targeting prodrug for colon cancer by utilizing an anti-cancer drug, 5-fluorouracil (5-FU), and pectin. The two-targeting prodrug for colon cancer is used for treating colon cancer and is characterized in that the 6-digit carboxyl is utilized to be combined with 5-FU directly or through different bridging groups to synthesize a series of two-targeting prodrugs for colon cancer. The prodrug first targets 5-FU to the colon by utilizing pectin to realize colon positioned release, and then 5-FU-galactose is identified through high expression of colon cancer galactin-3, and then 5-Fu is targeted to the colon cancer cells to realize two-targeting of colon cancer to treat colon cancer. The prodrug improves the selectivity of 5-FU greatly, enhances the curative effect and reduces adverse reactions. In addition, the hydrolysis fragments of pectin play a role in resisting tumor metastasis and can have a synergic action with 5-FU. The pectin-5-fluorouracil two-targeting prodrug for colon cancer focuses on the drug design ideas of drug delivery, targeting and coordination; therefore, the prodrug achieves the goal of high selectivity, high efficiency and low toxicity.

The invention relates to a preparation method of baicalein drug-loaded nanorods, which belongs to the field of pharmacy. The method comprises the following steps: firstly weigh baicalein and pectin respectively and add them to a glass container, then add a phosphate buffer solution, and put the glass container Immerse in a constant temperature water bath at 50°C, stir and mix evenly with a magnetic force to obtain a mixed solution I; then add a Ca(OH)₂ aqueous solution to the mixed solution I dropwise, and heat at 50°C for 1 hour; then add a NaHCO₃ aqueous solution dropwise, Heating at 50°C for another 3 hours to obtain the mixed solution II; finally, add baicalein to the mixed solution II, continue magnetic stirring at 50°C for 24 hours, put it into a dialysis bag after cooling, and in the phosphate buffer solution at 20°C The baicalein-loaded nanorods were obtained by dialysis for 24 hours. The baicalein drug-loaded nanorods prepared by the preparation method exhibit good targeting, tissue compatibility, low toxicity and side effects and sustained release function.

The invention relates to an antineoplastic vinorelbine bitartrate liposome, its freeze-dried powder injection and preparing process, wherein the preparation comprises liposome of vinorelbine bitartrate and pharmaceutically acceptable carrying agent, the liposome of vinorelbine bitartrate contains the following constituents: vinorelbine bitartrate, phosphatide, cholesterin and vitamin E, their weight ratio being 1 : 1-100 : 1-15 : 0.01-0.05.

The invention relates to a liposome freeze-dried powder preparation containing chuanhuning and a preparation method thereof. The preparation is composed of penhuning as active ingredient, phospholipid as lipid component, emulsifier, freeze-drying protectant and auxiliary materials. Among them, the weight ratio of Chuanhuning to phospholipids is 1:1 to 200 parts, 0.0001 to 50 parts of emulsifier; 1 part of phospholipid is added with 0.1 to 30 parts of freeze-drying protective agent and appropriate amount of auxiliary materials to make a freeze-dried preparation, both The storage stability of the drug can be significantly improved, and the Chuanhuning liposome freeze-dried powder can be diluted with water for injection in any proportion and administered without precipitation and degradation products after being redispersed by adding water for injection. The encapsulation efficiency of the freeze-dried preparation is 50%-100%, and the particle size is 40nm-1000nm. The invention can be made into injections, oral preparations and pharmaceutically acceptable dosage forms, is suitable for industrial production, and has the advantages of low cost, good curative effect, few side effects, simple manufacturing process and the like.

The invention discloses a method for preparing a multifunctional sodium alginate scaffold embedded with drug-loaded microspheres by using a 3D printing technology based on in-situ emulsification, and aims to provide a preparation method for a multifunctional bone defect repair scaffold material. It is characterized in that: using the biologically active substance lecithin as an emulsifier, the aminated modified polylactic acid solution dissolved in antibacterial or anti-inflammatory drugs is dispersed in a sodium alginate solution to form a stable emulsion, and then the low temperature 3D printing technology is used to in situ Sodium alginate scaffolds embedded with drug-loaded microspheres were constructed, and divalent strontium ions (Sr 2+ ) as a cross-linking agent to improve the mechanical properties and osteogenic activity of the scaffold. The feature of the present invention is that the prepared scaffold can be individually designed according to the characteristics of the patient's bone defect, and the prepared scaffold has multiple functions such as good biological activity, osteogenic ability, mechanical properties, antibacterial and anti-inflammatory, and has potential in the field of bone tissue engineering. application prospects.