43results about How to "Low drug load" patented technology

A coating and method for a coating an implantable device or prostheses are disclosed. The coating includes an undercoat of polymeric material containing an amount of biologically active material, particularly heparin, dispersed herein. The coating further includes a topcoat which covers less than the entire surface of the undercoat and wherein the topcoat comprises a polymeric material substantially free of pores and porosigens. The polymeric material of the topcoat can be a biostable, biocompatible material which provides long term non-thrombogenicity to the device portion during and after release of the biologically active material.

This invention pertains to the enhanced delivery of orally administered pharmaceutical agents and methods, dosage forms and devices thereof. In particular, the invention is directed to methods including providing a low solubility drug having a pKa between about 6 and about 9; dissolving the low solubility drug in an aqueous solution, wherein a pH of the aqueous solution is less than about 6.0; dissolving a hydrophilic polymer in the aqueous solution, wherein the weight ratio of the hydrophilic polymer to the low solubility drug is less than or equal to about 0.15; lyophilizing the aqueous solution to obtain a lyophilized powder. Also disclosed are drug formulations made according to the method, and dosage forms that include the drug formulations.

The invention discloses a drug-loaded microsphere and the preparation method, belonging to the technical field of biomedicine, which comprises following steps: adopting water/oil/water multiple emulsion technology and self-assembly technology of protein to fully mix the water soluble medicine and regenerated silk fibroin solution; adding the mixture in oil phase with emulsifier with certain amount during stirring for emulsification; adding organic solvent and stirring, thereby the silk fibroin is denaturalized and Beta structured to form milky crystalline silk fibroin fine particle, and the medicine is embedded; removing supernatant liquid through centrifugal effect; adding organic solvent; further crystallizing the silk fibroin and embedding the medicine; removing solvent and residual oil phase through centrifugal effect and collecting the microsphere. The average particle size of the silk fibroin drug-loaded microsphere is between 5.84 to 86.27Mum, the embedding rate is 42 to 99%, the drug loading dosage is 2.5 to 8.5%. The drug-loaded microsphere has the advantages of applicability to requirements for different purposes and wide application prospect.

The invention belongs to the new technical field of a drug preparation and in particular relates to a precursor liposome containing a glycyrrhetinic acid and a method for preparing the same. The precursor liposome containing the glycyrrhetinic acid consists of glycyrrhetinic acid, phospholipids, cholesterol, a surfactant and a water-soluble material; a suspension solution of the glycyrrhetinic acid liposome is prepared by an ethanol injection method or a thin-film dispersion method; and solid liposome powder is prepared by a freeze drying method or a spray drying method. The precursor liposome has simple process and good repeatability, is suitable for industrialized production; through drug administration by intravenous injection, the precursor liposome has long-circulating function, can remarkably reduce the toxicity of drug and achieve the function of prolonging the drug effect; and through oral administration, a solid preparation of the liposome can increase absorption and improve bioavailability by three to five times.

The invention relates to the field of nanometer drug carriers, and concretely relates to an asymmetric magnetic mesoporous silica rod supporting chemotherapeutic and gene drugs and application thereof to tumor diagnosis and treatment. The asymmetric magnetic mesoporous silica rod is prepared by employing spherical magnetic ferrite nanoparticles and ethyl orthosilicate through a sol-gel method, and the asymmetric magnetic mesoporous silica rod is subjected to surface functionalization modification, and is successively loaded with a chemotherapeutic drug, coated by a positive high-molecular polymer and loaded with a gene drug, so that a target product is obtained. The chemotherapeutic drug is connected with the silica rod through functionalization of the mesoporous surface, and the silica rod is endowed with the pH-responsive drug release characteristic, also the biocompatibility of the composite material is increased and the in-vivo cycling time is prolonged, and gene is supported in an electrostatic adsorption mode. The composite material is injected into a living body via an intravenous route, the characteristics of nanoparticle in-vivo passive targeting, gene guiding and pH-responsive drug release of the composite material are utilized, also the cooperativity of the multidrug resistant gene and the chemotherapeutic drug is utilized, and in-vitro magnetic targeting, NMR imaging and other technologies are applied to diagnosis and treatment of malignant tumors.

The invention discloses an antibody conjugated medicine and a preparation method and application thereof. The antibody conjugated medicine is formed by connecting an antibody and a medicine through a connecting arm. The antibody is an anti-CD20 monoclonal antibody with heavy chain containing LPXTG sequence. The medicine is aplysiatoxin or a derivative thereof. The connecting arm contains a short-peptide linker for connecting the antibody and a self-elimination linker for connecting the medicine. The short-peptide linker contains at least 1-3 continuous glycines. The antibody conjugated medicine has high uniformity and can achieve higher in-vitro and in-vivo antineoplastic activity with less drug loading capacity (DAR) than CD20 targeting ADC prepared by other chemical methods. IC50 (median inhibitory concentration) for Ramos cells can reach 0.005 nanogram/milliliter.

The invention provides a crystal form A of sofosbuvir and a preparation method thereof. The crystal form A is characterized in that an X-ray powder diffraction spectrum has characteristic peaks at the 2[theta] value being 12.4 +/- 0.2 degrees, 19.4 +/- 0.2 degrees, 27.1 +/- 0.2 degrees, 13.5 +/- 0.2 degrees, 25.5 +/- 0.2 degrees and 16.8 +/- 0.2 degrees. The crystal form A is higher in solubility in a bio-medium, is beneficial to drug efficiency increasing, can reduce the carrying amount of the drug, is low in hygroscopicity and is not liable to deliquesce due to high humidity, so that the drug can be stored for a long time conveniently.

A solid pharmaceutical composition comprises a solid adsorbate comprising a hydrophobic drug, a lipophilic vehicle, and a porous substrate, wherein the hydrophobic drug and lipophilic vehicle are adsorbed to the porous substrate.

The invention particularly relates to an acid-responsive polymer drug based on dextran and application of the acid-responsive polymer drug. In a molecular formula of the polymer drug, the value rangeof x is 3 to 30, and m and n separately indicate polymerization degrees of a hydrophobic block and a hydrophilic block. A method comprises the following synthetic steps: (1) using dextran to synthesize an ATRP initiator (Dextran-Br); (2) introducing the hydrophilic and hydrophobic blocks by utilizing ATRP polymerization reaction; (3) using N2H4-H2O to substitute an ester group on MGMA, thus obtaining an acid-responsive precursor; and (5) using amino and carbonyl on doxorubicin to react to form hydrazone bonds to synthesize an acid-responsive polymerization prodrug. In a cancer cell weak acid environment, the polymerization prodrug can be selectively released and has the advantages of higher micelle stability, high drug loading amount and the like, and can effectively overcome the defects in a drug delivery system of the nano technology that hydrophobic drug molecules are poor in solubility, high in toxicity and side effects and the like.

The invention provides a water-soluble cyclodextrin derivative clathrate of fluorouracil, and an in-situ gel film agent containing the clathrate and having biological adhesion and a preparation method thereof. According to the invention, cyclodextrin derivative-hydroxypropyl-beta-cyclodextrin is used to include fluorouracil hardly soluble in water so as to allow the solubility of fluorouracil in water to be improved and fluorouracil to have a slow release effect, so the in-situ gel film agent is prepared; the in-situ gel film agent is a novel cavity drug delivery preparation and comprises the hydroxypropyl-beta-cyclodextrin clathrate of fluorouracil, a temperature-sensitive gel skeletal material and a biologically adhesive material. The preparation is a freely flowable solution before usage, rapidly forms a gel film on the surface of a cavity, has a great drug release area, good biological compatibility and good gel strength and biological adhesion, is capable of firmly adhering on the mucous membrane of the cavity, prolongs action time, realizes uniform drug distribution, is beneficial for absorption of the drug and diffusion of the drug to peripheral tissue and improves bioavailability and treatment effects of the drug.

The new nano Chinese medicine threwingnut/Tripteerygium preparation consists of threwingnut/Tripterrygium extraction, general lactone or general alkaloid 0.1-0.6 wt%, carrier 0.1-0.8 wt%, surfactant 0.8-3.8 wt% and water. The preparation process includes dissolving threwingnut/Tripteerygium extraction, general lactone or general alkaloid in alcohol, dissolving carrier in cyclohexane, mixing through stirring, depression rotary evaporation to eliminate organic solvent and to form medicine film onto the wall of flask, vacuum drying to eliminate organic solventm, dissolving surfactant in water and adding it to the film, and final supersonic treatment to obtain yellow transparent colloid solution.

The invention relates to an interventional or implantable medical instrument drug coating and a preparation method thereof. The core of the interventional or implantable medical instrument drug coating is a grafted drug copolymer. The preparation method comprises the following steps: under the action of a catalyst, an active drug is covalently connected with a hydrophilic matrix to prepare the grafted drug copolymer, the grafted drug copolymer is dissolved and dispersed in a solvent, and then covered on the surface of an interventional or implantable medical instrument, and drying is performed. The covalent linkage manner can enhance the homogeneity of the drug and the matrix coating, improve the hydrophilicity and hydrophobicity balance of the drug and the adhesion-release balance of thedrug coating and the surface of the medical instrument, and enhance the efficiency that the drug is absorbed by tissues, penetrates through tissue stroma, and is taken in by cells. The homogeneity, uniformity and stability of the medical instrument drug coating are enhanced, the drug loading capacity is reduced, the drug loss is reduced, the drug entering blood circulation is reduced, and the absorption of the drug in target tissues and cells is increased, so that the toxicity is reduced, and the drug efficacy is improved.

The invention relates to a rheumatic bone-setting transdermal patch which is formed by dactylicapnos root, cortex picrasmae, paniculate swallowwort root and rhizoma panacis M which are extracted, andeffective parts are refined, and then transdermal patch excipients are added to prepare the transdermal patch; the transdermal patch obtained by the invention has the characteristics of being convenient for carrying and using, high transdermal adsorption ratio, high effective ingredients and strong treating effect.

The present invention provides a protective agent for nano-emulsion, which can improve the drug loading of nano-emulsion and the stability of nano-emulsion. Adding the protective agent into nano-emulsion can improve the drug loading of nano-emulsion. The influence factor of the preparation being investigated, no medicinal crystallization occurs when the nano-emulsion is in the refrigerated condition even in the freezing condition, and therefore the invention can not only improve the quality of medicine but also in favor of the storage and transportation of medicine.

The invention discloses poloxamer-adriamycin conjugate (DOX-P) micelle with anti-tumor drug resistance and a preparation method of the DOX-P micelle. The synthetic process of the DOX-P comprises the steps of firstly, reacting poloxamer with succinic anhydride to obtain high-molecular polymer of which the tail end contains carboxyl; and then, directly bonding the carboxyl at the tail end of the polymer with primaquine group in the adriamycin in an amido bond mode. The DOX-P has the capability of forming the micelle; and compared with the adriamycin bulk drug, the adriamycin subjected to covalent binding in the DOX-P micelle has the advantages that the anti-tumor activity of the adriamycin is maintained, the drug resistance of the tumor is overcome, and the stability of the adriamycin is better than that of poloxamer micelle.

The invention discloses a preparation method of a hard-core soft-membrane type nano slow-release drug delivery system for injection. The preparation method comprises the following steps of: S1, preparing hydroxyapatite; S2, preparing a soft-membrane material PEG-PSI; S3, mixing a drug to be delivered with the prepared hydroxyapatite in a solution, then adding the PEG-PSI dissolved in dimethyl sulfoxide for injection, uniformly mixing, and then centrifuging a preparation at a high speed; and S4, washing, then re-suspending in pure water, and carrying out freeze drying to obtain a final product. According to the preparation method disclosed by the invention, polyethylene glycol modified polysuccinimide with different molecular weights is used as an organic coating material, the hydroxyapatite is used as a drug carrying core, the drug is adsorbed, and a nano preparation form with a hard-core soft-membrane structure is formed through a coating effect of the polysuccinimide on the hydroxyapatite, so that the drug carrying capacity of a nano preparation is increased, the burst release of the nano preparation is avoided, the aggregation of nano particles is reduced, and the physical and chemical stability is improved.