30results about How to "Improve release behavior" patented technology

The invention belongs to the technical field of biological medicines and particularly provides an anti-tumor platinum pro-drug and a nanometer hydrogel drug and a preparation method thereof.The pro-drug is obtained by conducting hydrogen peroxide oxidation on an anti-tumor platinum drug to obtain a Pt(IV) sexadentate complex and then making the sexadentate complex react with anhydride or carboxylic acid containing double bonds.The pro-drug can be in self-polymerization or can be copolymerized with other hydrophilic monomers for the preparation of drug micro-spheres having high drug loading capacity.The micro-spheres are uniform in particle size and controllable in size and can keep long-term stability in an aqueous solution by using a stabilizer.The preparation method is simple, an obtained nanometer hydrogel drug carrier has glutathione stimulus responsibility, so that nanometer hydrogel is kept stable in a low-glutathione-concentration environment outside tumor cells, the drug is rarely leaked after long-time cycle, the nanometer hydrogel is rapidly degraded in the reducing environment within the tumor cells and converted into a linear chain of small molecular weight, the drug is quickly released, and the targeted killing effect on the target tumor cells is achieved.

The invention relates to a medicament eluting stent, which consists of a bare stent and a coating coated on the bare stent. The medicament eluting stent is characterized in that the coating at least comprises a polymer layer and a resin layer, wherein the polymer layer comprises polylactic-co-glycolic acid (PLGA) and medicaments; and the resin layer is coated on the surface of the polymer layer. A resin of the invention is coated on the surface of the medicament-loaded polymer coating. Due to the sustained release effect of the resin, on the premise of guaranteeing medicament dosage, the dosage of the polymer is reduced so as to obvious reduce an inflammatory reaction, reduce the generation of adverse reactions such as late intravascular restenosis and the like, and avoid forming late thrombosis.

The invention provides a sustained release microsphere containing risperidone and risperidone analogues and a preparation method thereof, wherein the sustained release microsphere containing the risperidone and the risperidone analogues can be used for injections. The sustained release microsphere comprises an active substance risperidone, the risperidone analogues, biodegradable medicinal high polymer materials, plasticizers, antioxygen and the like. The preparation method of the sustained release microsphere containing the risperidone and the risperidone analogues can be an emulsion process, a spray drying process, a low-temperature spray extraction method, a supercritical fluid method and the like. A blank medicinal high polymer material layer can also be wrapped on the surface of the microsphere on the basis. The microsphere preparation solves the problems, of dumping, lag phase and the like, existing in a reported or a listed product. The composition is mainly used in treating acute and chronic mental diseases.

The invention relates to a metformin hydrochloride sustained-release tablet and a preparation method thereof, and belongs to the technical field of medicine. The metformin hydrochloride sustained-release tablet is composed of sustained-release granules, sustained-release microcapsules and a lubricant, and is prepared through tabletting, wherein the weight ratio of the metformin hydrochloride in the sustained-release granules and the metformin hydrochloride in the sustained-release microcapsules is (3:7)-(6:4), and the lubricant is selected from superfine silica powder or magnesium stearate. According to the preparation method, a traditional spray drying method is improved, by combining a dry granulation process, the sustained-release microcapsules and sustained-release granules of different processes are prepared, tabletting is further carried out to prepare the metformin hydrochloride sustained-release tablet, the specific ratio of the sustained-release microcapsules prepared by the spray drying process to the sustained-release granules prepared by the dry granulation process is explored, and the metformin hydrochloride sustained-release tablet of which the inner portion has the structure of the sustained-release microcapsules and the sustained-release granules is finally obtained. The metformin hydrochloride sustained-release tablet and the preparation method thereof achievea good release behavior of the sustained-release tablet, overcome the shortcomings of sudden release and incomplete release, obtain a better release curve, and also greatly reduce the impurity content.

The present invention relates to a tofacitinib or tofacitinib salt sustained release preparation, which sequentially comprises a permeation tablet core composition containing a release accelerant, a controlled release coating, and an unnecessary aesthetic coat from inside to outside, wherein based on the total weight of the tablet core composition, the tablet core composition comprises 6.4wt%-16wt% of a pharmaceutical active component, 20wt%-77wt% of the release accelerant, 0wt%-56wt% of an osmotic pressure accelerant, 16wt%-50wt% of an adhesive and 0.5wt%-7wt% of other pharmaceutical auxiliary materials; and the release accelerant is a cyclic oligosaccharide cyclodextrin derivative. The tofacitinib sustained release preparation prepared from the osmotic tablet core composition containingthe release accelerant can increase the in-vivo exposure amount of tofacitinib and has improved bioavailability.

An electromechanical brake booster having a plunger rod for connecting a brake pedal lever to a brake master cylinder, a gear motor, which is coupled with the plunger rod, and a control device for driving the gear motor. A pedal force variable representing the pedal force and a plunger rod motion variable representing the motion of the plunger rod are supplied to the control device as input variables. The control device is configured to determine a setpoint return velocity for the plunger rod with the aid of the plunger rod motion variable and an actual return velocity for the plunger rod and the pedal force variable from the setpoint return velocity and to generate an activation signal for the gear motor. This makes it possible to improve the brake release behavior and to reduce high Bernoulli forces at the end stop for the starting position of the brake pedal lever.

The invention discloses a method used for modifying cyclodextrin with fluorescent probe fluorescein isothiocyanate (FITC) so as to solve technical problems of the prior art that cyclodextrin content determination method is low in sensitivity, and evaluation of endocytosis behavior is impossible to realize. According to the method, molecule mole ratio of FITC/ cyclodextrin is 0.1-20:1, preferably 0.5-10:1, and most preferably 1:1, and hydroxypropyl-beta-cyclodextrin is used preferably. Compared with the prior art, drug inclusion effects are not influenced by the FITC-modified cyclodextrin, cyclodextrin content can be determined via FITC fluorospectrophotometry, concentration lower limit of cyclodextrin ranges from 27.5 to 110ng/ml, and sensitivity is increased substantially compared with that cyclodextrin determination using a high performance liquid chromatography-differential refraction detector (concentration lower limit is 0.1mg/ml). The method is capable of solving a technical problem that cyclodextrin quantification is difficult to realize; and application in cyclodextrin new dosage form content determination, pharmaceutical property evaluation such as releasing rate evaluation, and cyclodextrin endocytosis action and target drug delivery effect is wide.

The invention relates to a chilo venosatus sex pheromone liquid slow-release agent and a preparation method thereof. The liquid slow-release agent is prepared from the following raw materials in partsby weight: 0.7-1.2 parts of chilo venosatus sex pheromone, 3-6 parts of a biodegradable polymer, 0.7-1.5 parts of an oily anti-UV agent, 0.7-1.5 parts of a water-based anti-UV agent, 0.7-1.5 parts ofbutyl hydroxyl anisole, and 130-160 parts of a solvent, wherein the biodegradable polymer is selected from polylactic acid and/or poly(butylene succinate); and the solvent is a mixed solution of dichloromethane and a hydroxypropyl methyl cellulose aqueous solution, the mass ratio of the dichloromethane to the hydroxypropyl methyl cellulose aqueous solution is 1:(1-2), and the mass concentration of the hydroxypropyl methyl cellulose in the hydroxypropyl methyl cellulose aqueous solution is 0.7-1.3%. The liquid slow-release agent provided by the invention has a long release lasting period, caneffectively prevent and control chilo venosatus pests, and can save labor and time through mechanical spraying.

The invention relates to a polyethylene glycol modified doxorubicin prodrug as well as a preparation method and application thereof, and belongs to the technical field of biological pharmacy. The polyethylene glycol modified doxorubicin prodrug contains a novel connecting arm of a hydrazide fragment connected by a piperazine heterocyclic ring, the prodrug has an excellent selective slow release behavior, and the preparation method of the prodrug has the advantages of mild reaction conditions, high yield, simplicity and convenience in operation and environmental friendliness. The polyethylene glycol modified doxorubicin prodrug disclosed by the invention has a good application prospect.

Provided is a method for producing a rumen-bypassing preparation which is produced at a low cost and simultaneously achieves the objects of protecting an active ingredient from release and decomposition in the first stomach and increasing release behavior in a target internal organ. A granular agent obtained thereby is also described. The method includes a step of applying vibration to a die head containing a melt of a coating agent for the rumen-bypassing preparation and a nutrient to bypass a rumen and having at least one injection port or to the melt, thereby injecting the melt from the injection port.

The invention relates a method for preparing a recombinant human vascular endothelial inhibin composition slow-release microsphere, which belongs to the technical field of pharmaceuticals. The constituents of the slow-release microsphere include recombinant human vascular endothelial inhibin which accounts for 1-30% in terms of weight percentage, hydrophilic substances 1-30% and lactic acid-glycolic acid polymers 69-98%. The preparation comprises the following steps: (a), adding the hydrophilic substance into a recombinant human vascular endothelial inhibin solution for free drying so as to obtain composition powder from the recombinant human vascular endothelial inhibin and the hydrophilic substance; (b), then suspending the power obtained in an organic solvent containing the lactic acid-glycolic acid polymers, which allows the power to disperse therein; (c), after dispersion, adding the solvent into a water phase containing emulsifier, stirring the solvent in a normal pressure or decompression environment to enable the solvent to be volatile and to change into microspheres, and keeping the temperature unchanged at a proper temperature as the solvent becomes volatile; and (d), subjecting the obtained microspheres to cleaning and drying so as to obtain slow-release microsphere preparations in the form of finished products. The preparation method provided by the invention can ensure that the recombinant human vascular endothelial inhibin can take a relatively stable form which effectively allows the recombinant human vascular endothelial inhibin to be encapsulated in the microspheres, thereby reducing the risk of possible degradation of the recombinant human vascular endothelial inhibin during the preparation process.