2868results about How to "High drug loading" patented technology

The present invention provides pharmaceutical compositions for controlled release of pharmaceutically active agents, especially those with a high water solubility, high dose, and / or short half-life. In addition, the present application provides methods for preparing and using such pharmaceutical compositions.

A drug conjugate is provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -LD-D, the protein based recognition-molecule being connected to the polymeric carrier by LP. Each occurrence of D is independently a therapeutic agent having a molecular weight≦5 kDa. LD and LP are linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.

A transdermal drug delivery system for the topical application of one or more active agents contained in one or more polymeric and / or adhesive carrier layers, proximate to a non-drug containing polymeric backing layer which can control the delivery rate and profile of the transdermal drug delivery system by adjusting the moisture vapor transmission rate of the polymeric backing layer.

The present invention is a magnetic nanoparticle composition with enhanced drug delivery characteristics. The magnetic nanoparticle composition is composed of a magnetic particle core surrounded by a fatty acid and surfactant corona. Methods for increasing the efficacy of therapeutic agents and facilitating diagnostic imaging are also provided.

Methods for preparing monomeric cytotoxic drug / carrier conjugates with a drug loading significantly higher than in previously reported procedures and with decreased aggregation and low conjugate fraction (LCF) are described. Cytotoxic drug derivative / antibody conjugates, compositions comprising the conjugates and uses of the conjugates are also described. Monomeric calicheamicin derivative / anti-CD22 antibody conjugates, compositions comprising the conjugates and uses of the conjugates are also described.

Provided herein are water-soluble prodrugs. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are covalently attached to an active agent, e.g., a small molecule. The conjugates of the invention provide an optimal balance of polymer size and structure for achieving improved drug loading, since the conjugates of the invention possess three or more active agents releasably attached to a multi-armed water soluble polymer. The prodrugs of the invention are therapeutically effective, and exhibit improved properties in-vivo when compared to unmodified parent drug.

Iodinated and / or brominated derivatives of aromatic dihydroxy monomers are prepared and polymerized to form radio-opaque polymers. The monomers may also be copolymerized with other dihydroxy monomers. The iodinated and brominated aromatic dihydroxy monomers can be employed as radio-opacifying, biocompatible non-toxic additives for other polymeric biomaterials. Radio-opaque medical implants and drug delivery devices for implantation prepared from the polymers of the present invention are also disclosed.

The invention is directed to modified polymers with increased drug-loading including compounds of formula (I): wherein Z is a poly(lactic-co-glycolic acid) (PLGA) polymer having molecular weight from 1-15 kDa and where the ratio of lactide to glycolide in the PLGA polymer is from 1:10 to 10:1; formula (II) R1 are independently H, R2, OH, O-alkyl, —O—R2, NH—R2, -linker-R2, or -and R2 are independently one or more therapeutic agents. The invention is also directed to nanoparticle drug delivery systems including a PLGA-b-PEG block copolymer; and a stabilizer and to drug delivery systems including PLGA-b-PEG block copolymer polyvinyl alcohol (PVA) nanoparticle; and the modified polymer substantially as described herein.

The present invention relates to compositions and methods for treating diseases and disorders including cancer and various other angiogenic-dependent diseases, vascular malfunctions, arteriovenous malformations (AVM), hemorrhagic processes and treatment of pain, in particular tumor-related pain by drug delivery and / or therapeutic embolization using microspheres. More particularly the invention relates to microspheres containing non-ionic contrast agents, to compositions comprising these microspheres, as well as methods for preparing and using such compositions for embolization therapy. The invention further relates to compositions and methods using detectable microspheres for targeted drug delivery, irrespective of whether embolization is also needed.

The invention discloses biologically related substances modified by a multifunctional H-type polyethylene glycol derivative. The derivative comprises a linear main axis LPEG and four PEG branched chains, and n1, n2, n3 and n4 are polymerization degrees of the branched chains, respectively; U1 and U2 are trivalent branching groups connecting the main axis LPEG with two PEG branched chains; F1 and F2 contain functional groups or their protected forms R01, and the number of R01 is one or more than one. Any linking group in the molecule or linking groups formed with adjacent heteroatom groups are stable or degradable; any PEG chain segment in the molecule independently shows polydispersity or monodispersity. One H-type molecule can modify multiple types of or multiple biologically related substances; the modified product has a flexible branching structure, a high drug loading capacity, optimized pharmacokinetics and tissue distribution, and can also carry two biologically related substances with different functions, so as to generate fluorescence property or targeting function.

The invention discloses a multifunctional H-type polyethylene glycol derivative and a preparation method thereof. The structure is as shown in formula (1) in the description, wherein a linear main axis LPEG and four PEG branched chains are included, and n1, n2, n3 and n4 are polymerization degrees of the branched chains, respectively; U1 and U2 are trivalent branching groups connecting the main axis LPEG with two PEG branched chains; F1 and F2 contain functional groups or their protected forms R01, and contain or do not contain branching groups G, and correspondingly, the number of R01 is one or more than one; F1 is the same as or different from F2; any linking group in the molecule or linking groups formed with adjacent heteroatom groups are stable or degradable; any PEG chain segment in the molecule independently shows polydispersity or monodispersity. The functionalized polyethylene glycol is diverse in branching structure and branching arm length, is adjustable and easily-controllable in various parameters and performance indexes, and is wide in application.

The invention relates to a method for preparing protein nanoparticles for delivering pharmacological active substances inside human bodies, and belongs to the field of delivery of pharmacological active substances inside human bodies and clinical application of delivery of the pharmacological active substances inside the human bodies. The method has the advantages that the pharmacological active substances are wrapped in the protein nanoparticles by means of unfolding and then refolding proteins and polypeptide or automatically assembling the proteins and the polypeptide, so that the pharmacological active substances can be delivered inside the human bodies.

The present invention is directed to aqueous drug coatings that include at least one insoluble drug, wherein the drug accounts for about 85 wt % to about 97 wt % of the drug coatings. A drug coating according to the present invention may include only one insoluble drug, two or more insoluble drugs, or one or more insoluble drugs in combination with one or more soluble drugs. The present invention also includes drug coating formulations suitable for providing drug coatings according to the present invention and dosage forms that include a drug coating according to the present invention.

A hot-melt extruded composition having finely divided drug-containing particles dispersed within a polymeric and / or lipophyllic carrier matrix is provided. The carrier softens or melts during hot-melt extrusion but it does not dissolve the drug-containing particles during extrusion. As a result, a majority or at least 90% wt. of the drug-containing particles in the extrudate are deaggregated during extrusion into essentially primary crystalline and / or amorphous particles. PEO is a suitable carrier material for drugs insoluble in the solid state in this carrier. Various functional excipients can be included in the carrier system to stabilize the particle size and physical state of the drug substance in either a crystalline and / or amorphous state. The carrier system is comprised of at least one thermal binder, and may also contain various functional excipients, such as: super-disintegrants, antioxidants, surfactants, wetting agents, stabilizing agents, retardants, or similar functional excipients. A hydrophilic polymer, such as hydroxypropyl methylcellulose (HPMC E15), polyvinyl alcohol (PVA), or poloxamer, and / or a surfactant, such as sodium lauryl sulfate (SLS), can be included in the composition. A process for preparing the extrudate is conducted at a temperature approximating or above the softening or melting temperature of the matrix and below the point of solubilization of drug-containing particles in the carrier system, and below the recrystallization point in the case of amorphous fine drug particles.

A super-porous aqueo-gel of an interpenetrating network polymer used for the orally applying system of protein polypeptide to suppress proteinase and break the close linking between epithelial cells contains two polymers: a cross-linked polymer and a cross-linked polyose polymer. Its preparing process includes such steps as mixing at least one unsaturated enylmonomer, at least one polyenyl cross-linking agent, a linear polyose polymer and a foaming agent to generate the super-porous aqueo-gel of semi-interpenetrating network polymer, and cross-linking with linear polyose.

The present invention provides a preparation method of protein nanoparticles for in vivo delivery of pharmacologically active agents, wherein the methods are to encase pharmaceutically active agents into proteins or peptides to form nanoparticles by unfolding the protein, and subsequently refolding or assembling the protein to produce a pharmacologically active agent encased within a protein nanoparticle.

The present invention provides a pharmaceutical dosage formulation, and more particularly, to a pharmaceutical dosage formulation comprising an HIV protease inhibitor.

A polymeric scaffold useful for conjugating with a protein based recognition-molecule (PBRM) to form a PBRM-polymer-drug conjugate is described herein. The scaffold includes one or more terminal maleimido groups. Also disclosed is a PBRM-polymer-drug conjugate prepared from the scaffold. Compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions are also described.

The invention provides a risperidone slow-release microsphere, a preparation method and an application thereof. The microsphere comprises risperidone or 9-hydroxy risperidone or the salt thereof and anon-end-capped lactide-glycollide copolymer. The risperidone slow-release microsphere provided by the invention has higher medicine-carrying quantity, no in-vivo sudden-release phenomenon, stable blood concentration and no medicine release lag period, reduces the administration frequency of a patient greatly, reduces the administration volume of each time, enhances the conformance of the patientand reduces the generation of adverse reactions.

The invention relates to a health product oral fast-release preparation and a production method thereof. The basic raw material of the preparation comprises main material and auxiliary material. The main material is health product raw material. The auxiliary material is oily dispersant mainly, and water-soluble dispersant, flavouring and emulsifier are added when necessary. The weight percentage of the main material is 0.1 percent to 80 percent, and the weight percentage of the auxiliary material is 20 percent to 99.9 percent. The method comprises the following steps: (1) preparing materials;(2) preparing slurry, including thinning and liquidizing, the finial fineness of the thinning is that 80 percent of the weight of the preparation is less than 300 microns, and the liquidizing processis that solid particles are dispersed in the oily dispersant in a stirring way. The weight percentage of the addition quantity of the oily dispersant can satisfy that the oil content in a finished product is not less than 15 percent; (3) molding that a finished product preparation is manufactured by a cooling molding method or a powder molding method. The health product oral fast-release preparation of the invention improves the dispersing speed of health product component in mouth under the precondition of achieving good flavor and is convenient for people to take without drinking water.

Pharmaceutical compositions suitable for oral administration comprising paclitaxel, a solvent, a surfactant, a substituted cellulosic polymer, and optionally but preferably a P-glycoprotein inhibitor. The composition may further comprise a diglyceride or mixture of diglyceride and monoglyceride. The composition generates a supersaturated paclitaxel microemulsion upon contact with water resulting in improved oral bioavailability of paclitaxel.

A blend of at least two polymers in combination with a drug provides a pressure-sensitive adhesive composition for a transdermal drug delivery system in which the drug is delivered from the pressure-sensitive adhesive composition and through dermis when the pressure-sensitive adhesive composition is in contact with human skin.

The invention discloses an adsorption method for preparing hydroxyapatite pesticide and slow-release fertilizer compound, which comprises the following steps: soaking a nano hydroxyapatite carrier in phosphate buffer solution, then adding a starting material into the buffer solution and continuously stirring the mixture to form compound solution, finally centrifuging the compound solution to obtain sediment, and drying the sediment to obtain the compound. By using a porous structure of the nano hydroxyapatite self to embed medicaments into an internal grid of the carrier, the burst effect of the medicaments is avoided, the medicinal effect is long, the medicament residue is greatly reduced, and the medicaments are safer. A product obtained by using the nano hydroxyapatite as a pesticide and fertilizer carrier has the advantages of reliable quality, strong stability, safe use and low cost, greatly improves the medicament loading amount and adsorption amount, is easy for continuous production, and has good application prospect.

The invention belongs to the field of pharmaceutical agents, relates to a polymer micelle lyophilized agent encapsulating an insoluble antitumor drug as well as a preparation method and an application thereof. The polymer micelle lyophilized agent is prepared by carrying out molecular self-assembly on a methoxy poly(ethylene glycol) 2000-polyester block copolymer to form micelles, and then encapsulating the insoluble antitumor drug in a hydrophobic core formed by the polyester. The lyophilized agent has high encapsulation rate, high drug loading and small particle size, can significantly improve the water solubility of the insoluble drug and result in passive targeting of more antitumor drugs to concentrate in the tumor tissues, thus improving an anti-tumor treatment effect and reducing the toxic and side effects of drugs, and can be used to prepare the drugs used for the treatment of lung cancer, intestinal cancer, mammary cancer, ovarian cancer, etc. The lyophilized agent can also be quickly dissolved and dispersed to form a transparent micellar solution after water for injection, normal saline solution and the like are added, and is used for the preparation of the drugs for treating primary intestinal cell carcinoma.

This invention pertains to the formulation of small-particle suspensions of anticonvulsants and antidementia, particularly carbamazepine, for pharmaceutical use. This invention also pertains to the formulation of small-particle suspensions of immunosuppressive agents, particularly cyclosporin, for pharmaceutical use.

The invention relates to a medical used hot melt pressure-sensitive adhesive type base material and its preparing method which provides a hot melt pressure-sensitive adhesive and an adhesive used paste preparation. The main element of the hot melt pressure-sensitive adhesive is styrenic thermoplastic elastomer SIS (phenylethene -isoprene -phenylethene three block copolymers) with adhesive resin (such as petroleum resin, terpenes polymer, polyisobutylene), flexing oil (such as liquid petrolatum) and aging retarder (such as propyl gallate, BZ) and so on.

The invention relates to biodegradable fluorouracil(Fu) polyester drug-bearing manoparticles with a coating material of polylactic acid, polylactic acid-glycolic acid, polylactic acid-polyethylene glycol block copolymer or polylactic acid-glycolic acid-polyethylene glycol block copolymer and the producing method including: firstly, fully dissolving the copolymer in the dichloromethane, under the ultrasonic shock, injecting the fluorouracil NaOH solution in the dichloromethane solution, dispersing uniformly, forming W / O primary latex, and beating up the primary latex and injecting into the fluorouracil saturated water solution containing 5 wt% of polyvinylalcohol (PVA), and storing in the refrigeratory after freeze-dry. The drug-bearing manoparticle has a drug content which is 10-25% of the microparticle mass, and has a smooth surface, an even diameter distribution, a remarkable slow release function and not adhesive. The micropartical size is 100-1000nm.

The invention relates to a method for preparing environment-responsive mesoporous silicon nanoparticles. The mesoporous silicon nanoparticles with the particle size of 20 to 1,000nm, the pore size of 2 to 50nm, the specific surface area of 500 to 1,500m<2> / g and a controlled structure are prepared by a template extraction method and subjected to surface functionalization by a self-assembly technology. A medicine sustained-release system prepared by the method is high in biocompatibility and medicine loading rate, can be released intelligently and controllably and has good application prospects in fields of growth factor and gene release, enzyme immobilization, cancer treatment and the like in tissue engineering, the preparation method is simple, reaction conditions are mild, and experiment raw materials are low in cost.

The invention discloses a paclitaxel lipid complex. The paclitaxel lipid complex consists of paclitaxel and lipid material. The weight proportion of the paclitaxel and the lipid material is 1 to 1 - 19, the preferential proportion is 1 to 2 - 10, and the more preferential proportion is 1 to 3 - 6. The lipid material is selected from natural lipid and synthetic lipid or the mixture thereof. The paclitaxel lipid complex can also contain antioxidation stabilizer. The invention also discloses a preparation method of the paclitaxel lipid complex and the application in the preparation of injection submicron emulsion and dry emulsion. The paclitaxel lipid complex has high solubility in oil, and the prepared submicron emulsion has the advantages of high drug loading quantity, high stability, high safety and low irritability.