30results about How to "Meet the requirements of clinical medication" patented technology

The invention discloses a 7-ethyl-10-hydroxycamptothecine drug precursor, a preparation method and an application thereof. A structure formula of the drug precursor is represented as the formula I or II. The drug precursor is prepared through an esterification reaction between a C-10 hydroxyl group or a C-20 hydroxyl group of 7-ethyl-10-hydroxycamptothecine and a hydrophobic molecule. The drug precursor has excellent anti-tumor activity and can directly release active components in vivo in a hydrolysis manner without catalytic hydrolysis of carboxylesterase, thereby achieving a high bioavailability. The drug precursor not only has excellent solubility in water but also has great solubility in amphipathic surfactants, such as tween-80 and the like, wherein the solubility can reach more than 30 mg / ml, and a high stability is achieved even that the drug precursor is diluted in water. The drug precursor can be prepared just through a one-step esterification method, is high in yield and low in preparation cost, is high in stability and good in safety, satisfies requirements in clinical medication and in large-scale industrial production, and has excellent market prospect and clinical application value.

The invention discloses a cis-dammine dichloroplatinum (CDDP) prodrug, a preparation method and application. The structural formula of the CDDP prodrug is shown as formula (I), and is generated by theesterification reaction of activated dihydroxy cisplatin with hydrophobic molecules. Characterization of the nano-preparation by dynamic light scattering and transmission electron microscopy indicates that the nanoparticles involved in the invention are uniformly distributed and are at about 30nm. In vitro cytotoxicity experiments show that the nano-drug can significantly inhibit the proliferation of tumor cells (A549 and LoVo). In vivo experiments show that compared with CDDP injections, on the basis of reducing the systemic toxicity, the nano-drug has the effect of inhibiting the non-smallcell lung cancer A549 subcutaneous tumor, and has good market prospects and clinical application value.

The invention relates to a preparation process of a galangal and rhizoma cyperi liquid capsule, which comprises the following processing steps: (1) respectively pulverizing galangal and rhizoma cyperi based on the weight ratio of 1:1 into coarse powder; (2) extracting the galangal by a carbon dioxide supercritical extraction method to obtain the extract of the galangal; (3) extracting the rhizomacyperi by a carbon dioxide supercritical extraction method to obtain the extract of the rhizoma cyperi; (4) mixing the galangal extract and the rhizoma cyperi extract and dehydrating to obtain the galangal and rhizoma cyperi extract; (5) adding vegetable oil and tween 80 to the galangal and rhizoma cyperi extract and mixing evenly to obtain galangal and rhizoma cyperi liquid; and (6) filling the galangal and rhizoma cyperi liquid and sealing to obtain the galangal and rhizoma cyperi liquid capsule. The invention respectively adopts different extraction conditions for carrying out carbon dioxide supercritical extraction on the effective components of the galangal and the rhizoma cyperi, reserves the effective components in the raw materials and improves the extraction rate, and the prepared galangal and rhizoma cyperi liquid capsule has the characteristics of safety, reliability, convenient taking, small dose, convenient carrying and the like.

The invention discloses a compound sustained-release preparation containing apixaban and a preparation method thereof. The preparation is composed of apixaban granules, edoxaban sustained-release pellets and other pharmaceutically acceptable auxiliary materials. The edoxaban sustained-release pellets are, from the inside to the outside, successively a blank core, an isolation coat layer, and a drug-containing layer, and the drug-containing layer is composed of edoxaban, hydroxypropyl cellulose, and a filler. It is obtained by spraying the drug-containing dispersion solution onto the coated pellet core by the bottom spray coating method to obtain the drug-loaded immediate-release pellets, and then outsourcing the sustained-release coating layer; It is obtained by granulating with microcrystalline cellulose, hydroxypropyl cellulose and croscarmellose sodium. The compound sustained-release preparation of the invention can take effect quickly, release medicine stably for a long time, reduce the number of times patients take medicine, improve compliance, and improve the safety of patient medicine, thereby meeting the needs of treatment and meeting the requirements of clinical medicine.

The invention relates to a cholesterol-poloxamer-cholesterol triblock copolymer, a preparation method and application thereof. The triblock copolymer is obtained by taking poloxamer as the basic framework, and connecting cholesterol to both ends by carbonic ester bonds. The preparation method includes: placing poloxamer in a sealed container, adding an alkaline catalyst and an acid binding agent under a nitrogen condition, slowly adding a dichloromethane solution containing cholesteryl chloroformate dropwise, conducting stirring mixing in ice-water bath for 5-30min, then placing the mixture at room temperature to react for 1-72h, after the reaction, at the end of the reaction, reducing the pressure and removing the solvent so as to obtain a crude product; adding a proper amount of distilled water to the crude product, performing extraction with dichloromethane three times, then conducting washing three times with ice water, saturated sodium chloride and 100mM hydrochloric acid in order, and carrying out precipitation by ice ether to obtain a white wax matter; and subjecting the white wax matter to repeated precipitation refining by ice ether, thus obtaining the triblock copolymer. And the triblock copolymer has the advantages of low critical micelle concentration, large drug loading capacity, good dilution stability, simple synthetic process, low cost, and wide application range, etc. (structural formula).

The invention discloses a preparation method and application of an amphiphilic copolymer-maytansinoid covalently coupled drug. The amphiphilic copolymer-maytansinoid covalently coupled drug structure is: R-X-may; wherein, X is a connecting segment; R is from an amphiphilic polymer; may is a maytansinoid group. The present invention can obtain the drug precursor through a simple chemical reaction, and obtain nano-micelles loaded with anti-tumor drugs, which can significantly reduce the release of maytansine drugs in the blood, thereby greatly reducing the effect on normal tissues and organs. damage. The preparation cost of the conjugated drug is low, the stability is high, and the safety is good, which meets the requirements of clinical medication and large-scale industrial production, and has good market prospects and clinical application value.

The invention discloses a tetravalent platinum drug preparation, a preparation method and application thereof, including a drug precursor and an amphiphilic polymer material, and the structural formula of the drug precursor is as formula (I). Dynamic light scattering and transmission electron microscopy show that the nanoparticles in the present invention are uniformly distributed, about 40-60 nm; in vitro cytotoxicity experiments show that the nanoparticles coated with platinum prodrug can significantly inhibit tumor cells (MDA-MB-468 and HT- 29); in vivo experiments show that, compared with cisplatin injection, on the basis of reducing systemic toxicity, it has the effect of inhibiting subcutaneous tumor MDA-MB-468, and has good market prospects and clinical application value.

The invention discloses a method for preparing matrine slow-release tablets by applying attapulgite, which comprises the following steps of: dissolving matrine by using hydrochloric acid with the mass concentration of 0.1 percent to obtain 2-5mg / ml of matrine solution; adsorbing the matrine solution through modified attapulgite for 4-6 hours according to the proportion by weight of 1:2; filteringand drying to obtain the attapulgite loading the matrine; and adding 2 percent by weight of talcum powder into the attapulgite loading the matrine, granulating by a dry method, and tabletting to obtain the matrine slow-release tablets. A modifying method of the attapulgite comprises the following steps of: weighing 20g of attapulgite, placing the attapulgite into 1000ml of aqueous solution, stirring for 12 hours, settling, removing upper water, adding purified water, stirring for 12 hours, settling, taking an intermediate fine particle layer, adding concentrated hydrochloric acid, settling for 24 hours, filtering through suction, washing with water to be neutral, drying at the temperature of 105DEG C, finely grinding and screening with a 120-mesh screen to obtain acid modified attapulgite. The invention adopts the principle of adsorption separation and selects the modified attapulgite which can be taken as an adsorbent for adsorbing the matrine, the matrine slow-release tablets are slowly released under the desorption action of a body fluid, operation steps are simple, and the production period of traditional Chinese medicine preparations is shortened.

The invention discloses freeze-dried azacitidine powder for injection. The freeze-dried azacitidine powder comprises azacitidine, mannitol and sodium acetate. Meanwhile, the invention discloses a preparation method of freeze-dried azacitidine powder injection for injection and aims to solve the problems of instability of azacitidine aqueous solution, non-uniform particle distribution, substandardsuspending uniformity, small settling volume and the like through adding sodium acetate, sieving bulk drug, controlling preparation temperature, optimizing freeze-drying curve and the like. A productproduced according to the technical scheme provided by the invention is stable in quality, good in redissolving performance, and uniform in particle distribution; the particle size of prepared suspension satisfies the requirements of clinical medication, the settling speed is low, caking does not exist after settling, and particles can disperse uniformly after being shaken gently.