39results about How to "Prolong metabolic time" patented technology

The invention belongs to the technical field of biological pharmacy, and relates to a tumor targeting polypeptide-medicine coupling derivative, and a preparation method and application thereof. The tumor targeting polypeptide-medicine coupling derivative comprises targeting polypeptides, long effect polypeptides and medicine molecules, wherein the targeting polypeptides are connected onto the endC of the long effect polypeptides through flexible connecting peptides; fusion peptides are used as carriers of the medicine molecules; the medicine carriers and the long effect polypeptides in the fusion peptides are connected through chemical bonds; and the long effect polypeptides are polypeptide or protein structural domains having the affine mutual effects with human serum albumin. The tumortargeting polypeptide-medicine coupling derivative can be combined with the human serum albumin; the remaining half-life period in the blood circulation system can be obviously prolonged; the long-term effectiveness in the body is realized; the targeting and seepage into the tumor tissues or cells can be realized; then, free effect molecules are released in tumor tissue micro acid environments orin cells in through an acid hydrolysis mechanism; and a better anti-tumor efficiency is achieved.

The invention belongs to the medical technical field, and discloses 7-ethyl-10-hydroxycamptothecine liposome freeze-dried powder injection and a preparation method thereof. The 7-ethyl-10-hydroxycamptothecine liposome freeze-dried powder injection comprises the following components: 1-10g of 7-ethyl-10-hydroxycamptothecine, 30-60g of phospholipids, 10-40g of cholesterol, 2-8g of VE, 100-300g of a freeze drying protectant, 2000-8000ml of an organic solvent, 1000-4000ml of alkaline buffer salt solution and 1000-4000ml of acid buffer salt solution. The preparation method comprises the following steps: dissolving liposoluble components in the organic solvent and water-soluble components in the alkaline buffer salt; transferring the organic solvent, and then adding the alkaline buffer salt for hydration; and carrying freeze drying in vacuum, re-dissolving with the acid buffer salt, incubating, filtering, sterilizing, and carrying out freeze drying again to obtain the 7-ethyl-10-hydroxycamptothecine liposome freeze-dried powder injection for injection. The invention solves the problems of low solubility and fast in-vivo metabolism of the 7-ethyl-10-hydroxycamptothecine, thus lowering toxic reaction, eliminating side reaction, having higher target distribution characteristics, prolonging metabolism time and improving solubility and bioavailability.

The invention aims to provide a preparation method for improving liposome entrapment efficiency. The preparation method comprises the following steps: dissolving liposoluble components in an organic solvent, and dissolving water-soluble components in alkalescent or acidulous buffer salt; transferring the organic solvent, and adding buffer salt solution for hydration; and after vacuum freeze drying, redissolving the components in the alkalescent or acidulous buffer salt, and incubating to obtain a medicament-containing liposome. Acid compounds are easily dissolved in alkaline solution, and alkaline compounds are easily dissolved in acid solution; and in the method, the liposome is prepared by utilizing the characteristic of solubility change due to the acid-base difference, so that the entrapment efficiency of the compounds in the liposome is improved greatly, and a novel idea for preparing the liposome for indissoluble compounds is provided.

The invention relates to a sarafloxacin hydrochloride sustain-released injection and a preparation method thereof, belongs to a medicinal preparation field. The sarafloxacin hydrochloride sustain-released injection is composed of sarafloxacin hydrochloride, an emulsifier, a suspending agent, a stabilizing agent, an antioxidant, plant oil for injection, and injection water. The preparation method comprises the following steps of: heating sieved sarafloxacin hydrochloride raw material drug, the plant oil for injection, the emulsifier and the antioxidant in a constant temperature magnetic stirrer, to obtain a mixture A; heating the suspending agent, a water-soluble emulsifier, the stabilizing agent and the injection water in the constant temperature magnetic stirrer, to obtain a mixture B; continuously adding the mixture A into the mixture B, mixing and shearing to obtain colostrums; complementing margin of the colostrum with injection water, then homogenizing, loading, and disinfecting with cobalt 60 ray, to obtain the product. The sarafloxacin hydrochloride injection with obvious sustain-released effect on intramuscular injection of livestock and poultry, can reduce stress reaction, mitigates culture labor intensity, and raises economic benefits and social benefits for livestock and poultry culture.

The invention discloses a magnetic hydrogel device. According to the magnetic hydrogel device, hydrogel is used as a main body structure, and a plurality of magnetic nanoparticles are filled in the hydrogel. The invention further discloses a preparation method of the magnetic hydrogel device and application of the magnetic hydrogel device in nerve magnetic stimulation. Compared with a single magnetic nanoparticle, the magnetic hydrogel device has stronger superparamagnetism, is not easy to diffuse and metabolize in a living body (the metabolism time of a magnetic material in the living body is prolonged), the problem that the single magnetic nanoparticle is easy to diffuse and metabolize in the living body can be solved, the magnetic effect time of the magnetic nano-particles in the living body is further prolonged, damage caused by frequent injection of nano-drugs in nerve regulation and control is reduced, the magnetic nano-particles can exert the electromagnetic effect and the force effect at the same time, and then the ion channel activation capacity of nerve cells is cooperatively improved.

The invention relates to deuterium labelled 1-substituted phenyl-4-substituted anilinomethyl-1,2,3-triazole derivatives. The derivatives have the structure shown as general formula (I) in the description, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 can be -F, -Cl, -Br, -I, -OCD3, -NO2, -SO3D, -D, deuterium labelled alkyl groups with 1-18 carbon atoms, deuterium labelled substituted phenyl,deuterium labelled substituted benzyl or deuterium labelled heterocyclic substituents. The invention further discloses a preparation method of the derivatives and an application of the derivatives topreparation of tumor treating or preventing drugs. Compared with the prior art, the deuterium labelled 1-substituted phenyl-4-substituted anilinomethyl-1,2,3-triazole derivatives have the effect of inhibiting cancer cells, and are convenient to synthesize.

The invention relates to neural stem cells traced by fluorescence and SPECT/CT double-image functional microspheres. The neural stem cells endocytose the fluorescence and SPECT/CT double-image functional microspheres. The fluorescence and SPECT/CT double-image functional microspheres comprise the following components, by mass, of 70%-99.9% of polymers, 0.05%-20% of cyclic metal iridium compounds and 0.05%-10% of I125 agents, wherein the polymers are degradable. The invention further discloses an application of the neural stem cells in preparation of tracers and/or therapeutic agents for a spiral neuronal injury or a neurodegenerative disease. According to the prepared neural stem cells traced by the fluorescence and SPECT/CT double-image functional microspheres, a noninvasive, dynamic, visual, simple and convenient method is provided for tracing tissue engineering seed cells implanted into a living body or a human body, and an observing and repairing technology aiming at the neurodegenerative disease is provided.

The invention relates to the technical field of fine chemicals, and provides a preparation method of a deuterated aromatic compound. The method comprises the following steps: mixing arylboronic acid, a photocatalyst, a Lewis base catalyst, a mercaptan catalyst, deuterated water and an organic solvent, and carrying out deboration deuteration reaction under a visible light irradiation condition to obtain the deuterated aromatic compound. According to the method, the deboration deuteration reaction of arylboronic acid is synergistically catalyzed by adopting visible light, Lewis alkali and mercaptan, the deuterated aromatic compound can be obtained in one step, the deuteration rate is high, the selectivity is good, and the product yield is high; by adopting the method disclosed by the invention, deuterated modification of complex arylboronic acid molecules and drugs can be realized. The result of the embodiment shows that the yield of the deuterated aromatic compound prepared by the preparation method provided by the invention can reach 90%.

The invention discloses a polynuclear compound which is of the structure as indicated in the general formula (1).The invention further discloses a preparation method of the polynuclear compound and application of the polynuclear compound to preparation of medicine for treating diabetes.According to the methylated polynuclear compound, under the condition that medicine effects are maintained unchanged, stability of the polynuclear compound is improved.

The present invention relates to the controllable degradation, filling-type complex bone implant of multivariant amino acid polymer-organic calcium/phosphorus salts, as well as to the preparative method thereof. The complex bone implant is consisted of multivariant amino acid polymers and medically acceptable organic calcium/phosphorus salts, while the content of organic calcium/phosphorus salts is 20-90% based on the total mass of composite material; the multivariant amino acid polymer is polymerized by ε-aminocaproic acid and at least two other amino acids, in which the molar content of ε-aminocaproic acid is at least 50% of the total molar quantity of amino acid polymers, while the amounts of other amino acids are at least 0.5% of the total molar quantity of amino acid polymers.

The invention relates to the field of public health, particularly relates to chemical risk assessment, and especially relates to a physiological poison metabolism kinetic model for adults exposed to bisphenol A through mouths. The construction method of the model comprises the following steps: S1, determining a kinetic process of absorption, distribution, metabolism and excretion of the bisphenolA orally taken in a human body; S2, determining a physiological poison metabolism kinetic model structure of the adults exposed to bisphenol A through the mouths; S3, establishing a mathematical model, and compiling a differential equation; S4, acquiring human physiological parameters, bisphenol A biochemical parameters and bisphenol A toxicokinetic parameters; and S5, carrying out simulation andparameter optimization on the physiological poison metabolism kinetic model of the bisphenol A. The model and the method disclosed by the invention are helpful to establish bisphenol A internal and external exposure association of the human body, simulate the content level of bisphenol A in a target organ, and further clarify an effect mechanism and a dose-reaction relationship of the bisphenol Ain combination with an effect index of the bisphenol A, so that the health risk that people are exposed to bisphenol A through the mouths can be evaluated more accurately, and important scientific basic data are provided for making and correcting bisphenol A limit values.

The invention discloses a radionuclide-labeled estrogen receptor molecular targeting compound and application thereof. The structural formula of the radionuclide-labeled estrogen receptor molecular targeting compound is described in the descriptions of the invention, contains an estrogen structure and has good estrogen receptor targeting in vitro and vivo; radioactive iodine isotopes (123I, 124I,125I or 131I) and 18F are used as radioactive signal groups to perform SPECT or PET development on estrogen receptors in organs or tissues of human or animals and treat positive tumors of the estrogenreceptors.