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865results about How to "Improve oral bioavailability" patented technology

Milled particles

A process for milling a solid substrate in the milling chamber of a dispersion or media mill in the presence of a two or more compositions of milling media bodies is disclosed wherein all milling media bodies contribute to the grinding of the solid substrate and wherein at least one composition of media bodies provides fragments of milling media bodies that are retained with the milled solid substrate particles in the form of a synergetic commixture produced in the milling process. More specifically, a process is disclosed for preparing a synergetic commixture comprising small particles of a solid substrate and small particulates of a first material of a desired size comprising the steps of (a) providing to the milling chamber of a media mill a contents comprising a pre-mix of a solid substrate, a fluid carrier, a plurality of milling bodies of a first material having a fracture toughness Kc1, and a plurality of milling bodies of a second material having a fracture toughness Kc2; (b) operating the media mill to grind the solid substrate and degrade at least a portion of the milling bodies of first material to produce a dispersion in the fluid carrier comprising a synergetic commixture of small particulates of the first material and small particles of the solid substrate having a desired size equal to or less than a size Sp; (c) separating the dispersion from any milling bodies and solid substrate particles having a size larger than Sp; and (d) optionally removing the fluid carrier from the dispersion to form a synergetic commixture free of fluid and comprising the particles and the small particulates, wherein KC2 is greater than KC1.
Owner:RTP PHARMA +1

Novel nanoemulsion formulations

An oil-in-water nanoemulsion delivery system that includes at least one oil having a concentration of greater than or equal to 2% (w / w) of at least one polyunsaturated fatty acid, preferably of the omega-3 or omega-6 family, is disclosed. The delivery system further includes at least one emulsifier and also an aqueous phase. Preferably, one or more hydrophobic therapeutic, monitoring and / or diagnostic agents are dispersed in the oil phase. The nanoemulsions may optionally contain other conventional pharmaceutical aids such as stabilizers, preservatives, buffering agents, antioxidants, polymers, proteins and charge inducing agents. The invention also relates to a process for preparing the nanoemulsions and to their use in the oral, parenteral, opthalmic, nasal, rectal or topical delivery of hydrophobic therapeutic, monitoring or diagnostic agents.
Owner:NORTHEASTERN UNIV +1

Matrix compositions for controlled delivery of drug substances

A novel matrix composition for pharmaceutical use. The matrix composition has been designed so that it is especially suitable in those situation where an improved bioavailability is desired and / or in those situation where a slightly or insoluble active substance is employed. Accordingly, a controlled release pharmaceutical composition for oral use is provided in the form of a coated matrix composition, the matrix composition comprising i) a mixture of a first and a second polymer that have plasticizing properties and which have melting points or melting intervals of a temperature of at the most 200° C., the first polymer being selected from the group consisting of polyethylene glycols and polyethylene oxides, and the second polymer being selected form block copolymer of ethylene oxide and propylene oxide including poly(ethylene-glycol-b-(DL-lactic acid-co-glycolic acid)-b-ethylene glycol (PEG-PLGA PEG), poly((DL-lactic acid-co-glycolic acid)-g-ethylene glycol) (PLGA-g-PEG), poloxamers and polyethylene oxide-polypropylene oxide (PEO-PPO), ii) a therapeutically, prophylactically and / or diagnostically active substance, the matrix composition being provided with a coating having at least one opening exposing at one surface of said matrix, wherein the active substance is released with a substantially zero order release.
Owner:EGALET LTD

Estrogenic compounds in combination with progestogenic compounds in hormone-replacement therapy

One aspect of the present invention relates to a method of hormone replacement in mammals, which method comprises the oral administration of an estrogenic component and a progestogenic component to a mammal in an effective amount to prevent or treat symptoms of hypoestrogenism, wherein the estrogenic component is selected from the group consisting of substances represented by the above formula in which formula R1, R2, R3, R4 independently are a hydrogen atom, a hydroxyl group or an alkoxy group with 1-5 carbon atoms; each of R5, R6, R7 is a hydroxyl group; and no more than 3 of R1, R2, R3, R4 are hydrogen atoms; precursors capable of liberating a substance according to the aforementioned formula when used in the present method; and mixtures of one or more of the aforementioned substances and / or precursors. Another aspect of the invention concerns a pharmaceutical kit comprising oral dosage units that contain the aforementioned estrogenic component and a progestogenic component as well as an androgenic component.
Owner:ESTETRA SRL

2-Substituted and 4-substituted aryl nitrone compounds

InactiveUS20050182060A1High oral bioavailabilityLow toxicityBiocideOrganic chemistryNitroneMedicinal chemistry
The present invention provides aryl nitrones, compositions comprising the same and methods of their use for the treatment or prevention of oxidative, ischemic, ischemia / reperfusion-related and chemokine mediated conditions.
Owner:RENOVIS

Matrix compositions for controlled delivery of drug substances

A novel matrix composition for pharmaceutical use. The matrix composition has been designed so that it is especially suitable in those situation where an improved bioavailability is desired and / or in those situation where a slightly or insoluble active substance is employed. Accordingly, a controlled release pharmaceutical composition for oral use is provided in the form of a coated matrix composition, the matrix composition comprising i) a mixture of a first and a second polymer that have plasticizing properties and which have melting points or melting intervals of a temperature of at the most 200° C., the first polymer being selected from the group consisting of polyethylene glycols and polyethylene oxides, and the second polymer being selected form block copolymer of ethylene oxide and propylene oxide including poly(ethylene-glycol-b-(DL-lactic acid-co-glycolic acid)-b-ethylene glycol (PEG-PLGA PEG), poly((DL-lactic acid-co-glycolic acid)-g-ethylene glycol) (PLGA-g-PEG), poloxamers and polyethylene oxide-polypropylene oxide (PEO-PPO), ii) a therapeutically, prophylactically and / or diagnostically active substance, the matrix composition being provided with a coating having at least one opening exposing at one surface of said matrix, wherein the active substance is released with a substantially zero order release.
Owner:EGALET LTD

Cell-penetrating peptide modified nanoparticle and its preparation method

InactiveCN102988295AIncreased cellular uptakeImprove biostability in vivoPowder deliveryPeptide/protein ingredientsSide effectWhole body
The invention belongs to the medicinal preparation field, relates to a cell-penetrating peptide modified nanoparticle, and concretely relates to a nanoparticle delivery system for oral polypeptide and protein medicines, and its preparation method. The medicine delivery system is composed of the nanoparticle, cell-penetrating peptides modified on the surface of the nanoparticle, and the polypeptide protein medicines sealed by the nanoparticle, wherein the average particle size range of the medicine delivery system is 10-500nm. The cell-penetrating peptide modified nanoparticle and glucosaminoglycan having electronegative cell surfaces undergo electric property attraction and then undergo endocytosis, so the cell-penetrating peptide modified nanoparticle and the glucosaminoglycan are integrally taken into cells; and the cell-penetrating peptide modified nanoparticle has an alimentary canal mucous membrane penetrating capability after the cell-penetrating peptide modified nanoparticle is orally taken, and can deliver the polypeptide protein medicines carried by the cell-penetrating peptide modified nanoparticle to the whole body for blood circulation, so the oral biological utilization degree of the medicines are improved. The cell-penetrating peptide modified nanoparticle has the advantages of improvement of the stability of polypeptide and protein medicines in the alimentary canal, reduction of the application amount of cell-penetrating peptides, and reduction of possible toxic side effects caused by the cell-penetrating peptides.
Owner:FUDAN UNIV
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