30results about How to "Improve membrane permeability" patented technology

The invention describes combinations of at least three amphipatic substances forming aggregate suspensions in a polar liquid. Judicious choice of system components, which differ at least 2-times to 10-times in solubility, ensures said aggregates to have extended, unusually adaptable surfaces. This is probably due to simultaneous action on said aggregates of at least two more soluble substances amongst said three system components, at least one of which is an active ingredient and preferably a drug; the third component, alternatively, can take the role of a drug. The patent further deals with the use of said combinations in pharmaceutical preparations capable of transporting drugs into the body of warm blood creatures. This is made possible by the drug loading capability of said aggregates with the highly flexible and deformable coating, which renders the resulting drug carriers highly adaptable. The patent finally reveals suitable methods and favourable conditions for carrier manufacturing and application.

The present invention is directed to a therapeutic composition in which human PDGF is bound directly to peptides that self assemble into a biologically compatible gel. When implanted in a patient's body, the composition provides for the slow, sustained release of PDGF. The composition will be especially useful in treating patients who have undergone a myocardial infarction.

The present invention provides a lactam compound, a sugar transport enhancement agent containing this compound as an active ingredient, an agent for the prevention and / or treatment of diabetes mellitus, diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic macrovascular disease, glucose tolerance anomaly, obesity and the like. In addition, the present invention also provides a preparation method for the novel lactam compound, and a preparation intermediate thereof.

Methods and compositions for increasing membrane permeability are provided. One aspect provides protein resulting from a fusion between a membrane-active peptide and second peptide. Nucleic acids and vectors encoding the pore forming fusion proteins are also provided.

The invention discloses a self-microemulsion, in particular to a curcumin self-microemulsion and a preparation method thereof. The curcumin self-microemulsion is characterized by the following components by weight percent: 0.05%-10% of curcumin, 1%-35% of oil phase, 20%-80% of surfactant, and 2%-40% of cosurfactant. The curcumin self-microemulsion and the preparation method thereof has the benefits that: a curcumin self-microemulsion release system increases the solubility of drugs, protects the drugs dissolved in oil drops, and improves the stability in a body; and the surfactant can change the flowability of cell membranes, improve membrane permeability of the drugs, enhance the absorption of the drugs in the body and increase the relative bioavailability of oral drugs.

The invention provides a high permeance and high selectivity facilitated transport membrane comprising a very small pore, nanoporous polyethersulfone (PES) / polyvinylpyrrolidone (PVP) blend support membrane, a hydrophilic polymer inside the very small nanopores on the skin layer surface of the support membrane, a thin, nonporous, hydrophilic polymer layer coated on the surface of the support membrane, and metal salts incorporated in the hydrophilic polymer layer coated on the surface of the support membrane and the hydrophilic polymer inside the very small nanopores, a method of making this membrane, and the use of this membrane for olefin / paraffin separations, particularly for propylene / propane and ethylene / ethane separations.

The invention belongs to the field of organic synthesis and relates to ( Z )- β ‑Trifluoromethyldehydrotryptophan compounds, especially (Z)‑β ‑Trifluoromethyl dehydrotryptophan compound and its synthesis method and application. Weigh 3-trifluoroacetylindole compounds, isocyanate compounds, catalysts and solvents in proportion, stir and react at 20-40°C for 15-60 hours, after the reaction is completed, obtain ( Z )- β ‑Trifluoromethyl dehydrotryptophans. The present invention uses 3-trifluoroacetyl indole as a trifluoromethyl source, and through the reaction with isocyanate, it is simple and efficient to construct ( Z )- β ‑Trifluoromethyl dehydrotryptophans. The introduction of trifluoromethyl groups can effectively improve the membrane permeability of cyclic active peptides containing dehydrotryptophan, increase the oil-water separation coefficient, enhance lipophilicity and metabolic stability, and improve the cyclic activity of dehydrotryptophan-containing peptides. Biological activity of active peptides.

The invention discloses a 1,3,4-oxadizaole structure unit-containing Rhodamine B pH fluorescence probe, the structure of which is shown as the formula (I) in the specification. The invention further discloses applications of the probe to monitoring the change of pH values and specifically marking lysocome in living cells. The probe does not emit fluoresce under the neutral and alkaline conditions; after the pH value is smaller than 7, the fluorescence intensity is fast enhanced along with the reduction of the pH value and can achieve the maximum value when the pH value is about 4.4; the pH sensitivity of the fluorescence detection ranges from 6.7 to 4.4, and the fluorescence intensity and the pH are in linear relation from pH 4.7 to 5.7; good capability of interference resistance to various metal ions can be achieved under acidity condition; and the probe is very suitable for monitoring the pH value under the complicated interior environment of the living cells in real time, especially specifically marking lysocome and monitoring the change of pH value in the lysocome.

The invention belongs to the field of using microorganisms to produce high value-added products, and in particular relates to a method for fermenting and culturing Schizophyllum polysaccharides from Schizophyllum, the method comprising the following steps: using basic culture medium to carry out deep layer liquid culture of Schizophyllum, and then adding ring Pentanone fatty acids continued to be cultured. The fermentation medium and the cyclopentanone fatty acid additive provided by the invention can shorten the fermentation cycle of the schizophyllum hyphae and greatly increase the content of high value-added products produced by the unit mycelium.

A fluorescent carbon dot for cell nucleus staining. The carbon dot is prepared by the following steps: 1) dissolving folic acid and m-phenylenediamine in water and heating for reaction; 2) after the reaction, centrifugation, and silica gel column chromatography to collect yellow The green fluorescent part was evaporated, transferred to water, and freeze-dried. The carbon dots prepared by the invention emit green light under ultraviolet excitation, have a large Stokes shift, and the optimal excitation position is consistent with the existing commercial 405 laser, and can be well applied to laser confocal microscopy.

The present invention provides a novel category of naphthalene-based two-photon fluorescent probes having a general formula I, wherein: X is selected from the X1, X2, X3 and X4; The mentioned two-photon fluorescent probes have a low fluorescence background in the non-tumor cells and tissues, and have a strong and specific fluorescent signal in the tumor cells and tissues. These probes have a certain level of water-solubility, while having good membrane permeability. In addition, they have a bigger effective two-photon absorption cross section. The compounds of the present invention also have a lower biotoxicity, phototoxicity and photobleaching. There is sufficient difference between the spectral range thereof and that of a biological sample.

The invention belongs to the technical field of medicines and especially relates to a medicinal application of collagen protein peptide, a cucurbitacin oral micelle, and a preparation method thereof.The application is that the collagen protein peptide is used as a medicine transmembrane tool in preparation of the oral medicine preparation, wherein the collagen protein peptide carries positive charges. The invention provides the cucurbitacin oral micelle containing the collagen protein peptide, which comprises, by weight, 8-15 parts of cucurbitacin, 30-70 parts of lecithin, 50-75 parts of octanoic decanoic polyethylene glycol glyceride, 25-50 parts of polyethylene glycol 15-hydroxystearate and 80-100 parts of the collagen protein peptide carrying the positive charges. The collagen proteinpeptide, cooperated with other carrier materials, can improve membrane-permeability of the medicine and reduce excretion of the medicine, so that the collagen protein peptide can be used as the medicine transmembrane tool. For solving problems about oral bioavailability of the cucurbitacin, the invention provides the technology of collagen protein peptide coating nano-micelle, wherein by means ofthe characters of the collagen protein peptide, the problem of low bioavailability of medicines, such as the cucurbitacin, is solved.

Since a compound represented by formula (I) wherein all of the symbols are the same as defined in the specification, a salt thereof, a solvate thereof, a prodrug thereof, a mixture with a diastereomer thereof in an arbitrary ratio, or a cyclodextrin clathrate thereof have a contracting activity of bladder detrusor and a relaxing activity of urethral sphincter, they can ameliorate bladder contraction dysfunction and / or urethral relaxation dysfunction, and for example, are effective for underactive bladder. Additionally, the compound of the present invention has little risk of side effects on the urinary system, the circulatory system and the digestive system, and exhibits excellent pharmacokinetics, such as oral absorbability etc. Therefore, the compound of the present invention is useful as a superior agent for preventing, treating and / or ameliorating underactive bladder.