118 results about "Amphotericin B" patented technology

Amphotericin B (AmB) is the gold standard for treatment of life-threatening systemic fungal infections. To develop cost-effective AmB formulations with reduced toxicity, embodiments disclosed introduce controlled number of phenylboronic acid (PBA) moieties into telodendrimer (TD) nanoplatform for optimizing AmB conjugation via reversible boronate ester strategy. This multivalent flexible boronate TD nanoplatform can also be applied in developing prodrugs for different cis-diol containing or α- or β- hydroxyl ketone-containing drug molecules.

The present application is directed to a cochleate composition including one or more cochleates and at least two anti-fungal compounds selected from amphotericin B, 5-flucytosine, fluconazole, ketoconazole, ravuconazole, albaconazole, itraconazole, posaconazole, isavuconazole and / or voriconazole. Methods of using the antifungal cochleate formulations are also disclosed.

The invention relates to a 4-hydroxymethylphenylboronic acid modified amphotericin B derivative as well as a preparation method and application thereof, and belongs to the technical field of medicine preparation. Amino groups on trehalose amine in amphotericin B molecules are modified through 4-hydroxymethyl phenylboronic acid, and the amphotericin B derivative with a novel structure is obtained. Compared with amphotericin B, the derivative has the characteristics of low hemolysis toxicity, low kidney cell toxicity and low acute toxicity. In addition, the invention also provides a preparation method of the derivative, and the prepared derivative has better antifungal activity and has a wide market prospect in the aspect of treating systemic deep fungal infection.

The invention discloses a macrophage-polymer lipid nanoparticle composite drug delivery system, a preparation method thereof and application of the macrophage-polymer lipid nanoparticle composite drug delivery system in cryptococcus infection resistance. According to the drug delivery system, alpha-linolenic acid (ALA), high molecular weight chitosan oligosaccharide (HCOS) and amphotericin B (AmB) are used as raw materials to construct nanoparticles AmB-PLHNs, the nanoparticles are loaded in macrophages through the phagocytosis of the macrophages, and the AmB-PLHNs (at) M1 is constructed. AmB is a common medicine for clinically treating Cn infection, but has the problems of toxic and side effects on kidney and incapability of being transferred into the center. The AmB-PLHNs (at) M1 carries AmB-PLHNs to be transferred into the brain according to the blood-brain barrier penetrating characteristic of M1 type macrophages, and the brain entering efficiency of the medicine is improved. By combining the phagocytosis of macrophages on cryptococcus, the inflammation immune regulation function of the macrophages and the bacteriostatic action of the drug-loaded nanoparticles, the drug-loaded nano-particles are used for treating Cn central infection, and the toxic and side effects of AmB are reduced.

The invention provides a low-temperature-resistant inactivated guanidine salt virus preservation solution and a preparation method thereof, and relates to the field of virus preservation solutions. Comprising the following raw materials: NaCl, KCl, glucose, KH2PO4, Na2HPO4, guanidine hydrochloride, penicillin, streptomycin, amphotericin B and glycerol. The raw materials are mixed and uniformly stirred. The preserving fluid is suitable for being used in a low-temperature environment, can preserve a liquid state within several hours in the low-temperature environment, can significantly inactivate pathogens, can also maintain completeness of subsequent nucleic acid extraction, and has no significant influence on amplification and the like.

Disclosed are compositions comprising a lipid polymer excipient and AmB or an AmB derivative. The lipid polymer excipient can form micelles when formulated with AmB or the AmB derivative and can solubilize and stabilize the drug. Also disclosed are methods of treating a fungal infection using the compositions.

The invention discloses a tissue preservation solution in organoid construction as well as a preparation method and application thereof. The tissue preservation solution is prepared from the following components: an Advanced DMEM / F12 culture medium, a mycillin / amphotericin B three-antibody mother solution, Glutamax-1, an HEPES buffer solution and a Y-27632 mother solution. The preparation method of the tissue preserving fluid comprises the following steps: adding an Advanced DMEM / F12 culture medium into a centrifugal tube on a super clean bench; then sequentially adding a mycillin / amphotericin B three-antibody mother solution, Glutamax-1, an HEPES buffer solution and Y-27632, and uniformly mixing, so as to obtain the tissue preservation solution. After uniformly mixing, filtering and sterilizing by using a disposable needle type filter, and collecting the preserving fluid into a centrifugal tube; the invention also discloses an application of the tissue preserving fluid in organoid construction. According to the tissue preserving fluid obtained by the invention, in the transportation process, the cell viability in the tissue is improved, the cell damage is reduced, and the success rate of primary cell adherent culture and organoid construction is increased.

A hydrogel composition for intranasal delivery of an antifungal (amphotericin B) at an infection site, specifically the nasal mucosa and upper respiratory tract.

Compositions comprising a lipid polymer excipient and an AmB or an AmB derivative are disclosed. The lipid polymer excipient can form micelles when formulated with AmB or an AmB derivative, and can solubilize and stabilize the drug. Also disclosed are methods of treating a fungal infection comprising administering to a subject in need thereof a therapeutically effective amount of the composition.

The invention discloses a composition, preparation method and application of a bionic nanosystem loaded with amphotericin B; the composition comprises AmB, PLGA nanoparticles and vaginal epithelial cell membranes; wherein AmB is encapsulated in PLGA nanoparticles, and the entire encapsulation is wrapped by vaginal epithelial cell membranes; the preparation method is to separate and purify the cell membranes of vaginal epithelial cells; encapsulate AmB in PLGA nanoparticles; wrap the cell membranes of vaginal epithelial cells on the surface of PLGA nanoparticles containing AmB; and the application is to treat Candida albicans infection. The scheme of the invention can overcome the poor targeting and retention time of drugs in the preparations in the prior art, and reduce the problem of toxic and side effects caused by injecting large doses of drugs for therapeutic effects.

The invention discloses a culture medium and a culture method of a breast cancer organoid. The culture medium comprises an Advanced DMEM / F12 basal culture medium and an additive, the additive is prepared from penicillin streptomycin / amphotericin B, a B-27 additive, L-glutamine amide, HEPES (Hydroxyethyl PES), N-Acetylcysteine, nicotinamide, SB202190, A83-01, FGF10 (Fibroblast Growth Factor 10), EGF (Epidermal Growth Factor), human Hergulin beta-1, Y27632, WNT-3A, R-spondin 1, NOGGIN (Nitrogen Growth Factor IN), FGF7 (Fibroblast Growth Factor 7) and beta-estradiol. The culture method of the breast cancer organoid comprises the step of using the breast cancer organoid culture medium, and the method specifically comprises the steps of tissue sample taking, primary tissue construction, breast cancer organoid liquid changing and breast cancer organoid subculture. According to the prepared breast cancer organoid culture medium, tumor cells taken from breast cancer tumors grow fast, the cell speed is high, and follow-up medicine screening experiments can be facilitated; after the breast cancer organoid culture medium is used for culturing the breast cancer organoid, the cellular morphology and the protein expression condition of the organoid are identified through HE and immunohistochemistry, and it can be seen that the organoid can well reduce the pathological characteristics of the tissue.

The invention discloses a preparation method of amphotericin B sustained release microspheres, which comprises the following steps: S1, suspending AmB in methanol to prepare an AmB suspension; s2, dissolving BSA in water to prepare a BSA aqueous solution; s3, uniformly mixing the AmB suspension with the BSA aqueous solution to obtain a water phase; s4, taking liquid paraffin as an oil phase, adding an emulsifier, then adding the water phase into the oil phase under a mechanical stirring condition, emulsifying to obtain W / O type primary emulsion, and naturally volatilizing to remove methanol; s5, a glutaraldehyde solution with the concentration being 8 wt% is added into the primary emulsion for curing; s6, the cured substance is washed and freeze-dried, and the amphotericin B sustained release microspheres are prepared. The amphotericin B sustained-release microsphere can reduce the administration frequency, alleviate the dose-dependent toxic and side effects and reduce the cost of pharmaceutic adjuvants and preparations.

Disclosed are C16 amide derivatives of C2'-epi-amphotericin B (C2'epiAmB) and salts thereof, characterized by improved clinical efficacy and reduced toxicity compared to AmB. Also disclosed are pharmaceutical compositions comprising any of the disclosed compounds or salts thereof, as well as treatment methods and therapeutic uses of the pharmaceutical compositions.

Provided are an amphotericin B amide derivative and a use thereof. The amphotericin B amide derivative is as shown in formula (I). The compound has good antifungal activity, is effective against various fungi, has good water solubility, is adapted to be developed into an injection dosage form, has excellent metabolic stability in animals (such as mice, rats, dogs, and monkeys), has a long half-life period, can effectively reduce the frequency of administration, has weak inhibition on CYP enzymes, and has a low risk of drug interaction.

The invention provides an amphotericin B amide derivative and application thereof. The amphotericin B amide derivative is shown as a formula (I), has good antifungal activity, is effective to various fungi, has good water solubility, is suitable for being developed into injections, has excellent metabolic stability in animal bodies (such as mice, rats, dogs and monkeys), is long in half-life period, can effectively reduce the administration frequency, is weak in CYP enzyme inhibition, and can be used for preparing the antifungal drugs. The drug interaction risk is low.

Disclosed are pharmaceutical compositions, comprising: (i) amphotericin B or a pharmaceutically acceptable salt or hydrate thereof; (ii) cholesterol; (iii) phospholipids, comprising hydrogenated soy phosphatidylcholine and distearoylphosphatidylglycerol; and (iv) calcium chloride (CaCl2)). Also disclosed are methods of using the pharmaceutical compositions for treating a disease or disorder (e.g., cystic fibrosis), increasing the pH of airway surface liquid, increasing bicarbonate secretion into airway surface liquid, and increasing a subject's forced expiratory volume in one second.

The invention discloses a culture medium and a culture method of araliaceae plant embryogenic stem cells and a method for producing saponin at high yield by using the araliaceae plant embryogenic stem cells. The culture medium comprises a basic culture medium, and 200 mg / L-500 mg / L of cerium nitrate is added into the basic culture medium; the basic culture medium is selected from one of an MS culture medium and a B5 culture medium. The MS culture medium is further added with amphotericin B with the concentration of 0.8 to 1.3 mg / L and double antibodies with the mass concentration of 0.9 to 1.2 percent, and the double antibodies are 100X mycillin mixed liquor, 6-BA with the concentration of 0.8 to 1.2 mg / L and NAA with the concentration of 0.8 to 1.3 mg / L; or 0.098 mg / L to 0.120 mg / L of 6-BA, 13 mg / L to 18 mg / L of cane sugar, 0.48 mg / L to 0.52 mg / L of methyl jasmonate and 0.099 mg / L to 0.130 mg / L of triacontanol are also added into the B5 culture medium. The cerous nitrate is added into the culture medium of the araliaceae plant embryonic stem cells, the culture of the araliaceae plant embryonic stem cells is obviously promoted, and the culture quantity of the embryonic stem cells can be obviously increased, so that efficient and rapid culture is realized, and the culture medium has universality.

The invention belongs to the technical field of biological medicines, and in particular relates to an application of hyssopus rigidus var. Cupidus essential oil in preparation of an antibiotic antibacterial sensitizer and / or preparation of an antibiotic combined medicine, and further relates to an application of the hyssopus rigidus var. Cupidus essential oil in preparation of the antibiotic antibacterial sensitizer and / or the antibiotic combined medicine. It is found that the hyssop officinalis essential oil can enhance the antibacterial sensitivity of various antibiotics including fluconazole and amphotericin B, the hyssop officinalis essential oil and the antibiotics are combined for use, the synergistic antibacterial activity is achieved, and the better antibacterial effect is achieved while the dosage of the antibiotics is reduced; important technical support is provided for improving the current situation of drug resistance of fungi.

The present invention provides semisynthetic derivatives of amphotericin B, their preparation methods, and uses. Specifically, the present invention discloses compounds having a structure as shown in Formula V, as well as water-soluble salts and complexes, pharmaceutical compositions, and plant and body therapeutic products containing the derivatives, and their use as antifungal antibiotics. The present invention also discloses methods for preparing the aforementioned compounds. #imgabs0#

The invention relates to the technical field of plant tissue culture, in particular to application of amphotericin B in inhibition of endophyte pollution of ancient cinnamomum camphora stem tissue culture. It is found that amphotericin B can effectively inhibit endophyte pollution in the ancient cinnamomum camphora stem tissue culture process, meanwhile, it is avoided that high-concentration antibiotics generate a toxic effect on stem induction, the stem induction endophyte pollution rate in the tissue culture process is effectively reduced and can be reduced to 6%, the stem induction rate can still reach 78%, and the tissue culture cost is reduced. The bottleneck problem of endophyte pollution in the ancient cinnamomum camphora stem tissue culture process is solved, and technical support is provided for efficient propagation and preservation of precious germplasm resources of ancient cinnamomum camphora.

A composition comprising a lipid polymer excipient and AmB or an AmB derivative is disclosed. The lipid polymer excipient can form micelles when formulated with AmB or an AmB derivative, solubilizing and stabilizing the drug. Also disclosed is a method of treating fungal infections using this composition.

The invention relates to a process for obtaining an amphotericin B (AmB) formulation in liposomes containing dicetyl phosphate (DCP), based on incorporation of the drug into the membrane of preformed liposomes, combining the effects of pH on the solubility of amphotericin B and of temperature on the insertion of the drug into the liposome membrane. The technology also relates to use of the process and of the formulation for the manufacture of medicaments for the treatment of leishmaniasis and sporotrichosis, for oral or topical administration.

The invention discloses a brain-targeted nasal-spray amphotericin B phospholipid complex and a preparation method and application thereof, and belongs to the technical field of pharmaceutical preparations, the brain-targeted nasal-spray amphotericin B phospholipid complex is prepared by adopting a film dispersion method, and the preparation method comprises the following steps: dissolving 15-hydroxystearic acid polyethylene glycol ester, phospholipid, cholesterol, amphotericin B and optional other auxiliary components in a solvent, removing the solvent until a film is formed, and drying to obtain the brain-targeted nasal-spray amphotericin B phospholipid complex. And carrying out hydration dispersion to obtain the amphotericin B-loaded phospholipid complex. According to the amphotericin B sodium deoxycholate injection, the problems that the traditional amphotericin B sodium deoxycholate injection is high in renal toxicity, the intrathecal injection is poor in solubility, and low in bioavailability and patient compliance, large in side effect and the like due to the fact that the traditional amphotericin B sodium deoxycholate injection is difficult to penetrate through a blood brain After nasal administration, the drug is quickly delivered into the brain, so that the slow release of the drug is realized, the intracerebral bioavailability of the drug is improved, high brain targeting and low systemic toxic and side effects are realized, and good clinical application value and market prospect are achieved.

The invention relates to an amphotericin B nano-composite based on sphingosine coupled polyethylene glycol carrier as well as a preparation method and application thereof, and belongs to the technical field of pharmaceutical preparations. The water-soluble sphingosine-polyethylene glycol conjugate is obtained by carrying out coupling reaction on amino on sphingosine and polyethylene glycol activated ester. The amphotericin B / sphingosine nano-composite is used as a carrier material, and forms a nano-composite in a highly aggregate form with drug molecules under the intermolecular acting force of amphotericin B and sphingosine. Compared with the prior art, the amphotericin B compound can effectively reduce hemolytic toxicity, kidney cell toxicity and acute toxicity of amphotericin B, and has good in-vivo and in-vitro antifungal activity. In addition, the invention also provides a preparation method of the carrier and the nano-composite, and the carrier and the nano-composite have a wide market prospect in the aspect of treating systemic deep fungal infection.

Provided are a combination of an inositol phosphorylceramide synthase inhibitor and amphotericin B and use thereof. The use includes preparing a pharmaceutical composition, which includes an inositol phosphorylceramide synthetase inhibitor and amphotericin B or a salt thereof. Inositol phosphorylceramide is an important and conserved component of fungal plasma membranes. In the pharmaceutical composition according to an embodiment of the present disclosure, due to the presence of the inositol phosphorylceramide synthase inhibitor, the interaction between the inositol phosphorylceramide synthase inhibitor and amphotericin B not only enhances the inhibitory ability of the inositol phosphorylceramide synthase inhibitor on the synthesis of inositol phosphorylceramide in Cryptococcus, but also effectively reduces the dosage of amphotericin B and prolongs the half-life of amphotericin B, facilitating to reduce the adverse reactions of amphotericin B. The pharmaceutical composition exhibits superior fungicidal effect and safety compared to the currently used clinical combination of 5-fluorocytosine and amphotericin B.

The invention discloses a nano-robot based on tear driving, a preparation method of the nano-robot and application of the nano-robot in eye drops. The preparation method comprises the following steps: step 1, loading ophthalmic disease treatment drugs such as amphotericin B, voriconazole and natamycin into nano-particles such as polylactic acid-glycolic acid copolymer, chitosan and sodium alginate; 2, coupling urease on the surfaces of the nano-particles to obtain a nano-robot with autonomous movement ability; step 3, performing morphology characterization on the obtained nanometer robot driven by the tear liquid; and step 4, dispersing the prepared tear-driven nano-robot in a buffer solution to prepare the eye drops. The tear-driven nano-robot can utilize urea in tears as fuel to generate cluster motion on the cornea surface, so that the retention time is remarkably prolonged, the drug retention amount is increased, and the treatment effect is improved. The nano-robot eye drops based on tear driving have biocompatibility and treatment safety, and have wide application prospects in the field of ophthalmic local administration.

Disclosed is a simplified, readily scalable series of individual methods that collectively constitute a method for the synthesis of C2'epiAmB, an efficacious and reduced-toxicity derivative of amphotericin B (AmB), beginning from AmB. Also provided are various compounds corresponding to intermediates in accordance with the series of methods.

The invention discloses a method for detecting the total number of mould and saccharomycetes of amphotericin B. The method comprises the following steps: (1) preparing mould and / or saccharomycetes to be detected into a bacterium suspension; (2) adding a sulfydryl-containing neutralizer into the SDA culture medium to obtain a neutralizer-containing SDA culture medium; (3) weighing an amphotericin B sample, and diluting the amphotericin B sample with a buffer solution to obtain a test solution; and (4) adding a test solution into the bacterial suspension, uniformly mixing, injecting into a neutralizer-containing SDA culture medium, culturing, and counting to obtain the total number of mould and / or saccharomycetes of amphotericin B. According to the method, a technology combining a dilution method and a neutralization method is adopted, a test sample is diluted, a sulfydryl-containing neutralizer is added into an SDA culture medium, amphotericin B molecules are effectively wrapped, and contact between the amphotericin B molecules and fungal microorganism cell membranes is reduced, so that the bacteriostatic activity of the amphotericin B molecules is eliminated, the inhibition effect of the amphotericin B on sensitive fungi is solved, the recovery rate is effectively increased, and the method is suitable for industrial production. And accurate microbial limit detection is realized.

The present application relates to the use of amphotericin B or its combination in the preparation of anti-tumor drugs. The present application first confirms that amphotericin B directly binds to Toll-like receptor 2 and activates the downstream signaling pathway as a Toll-like receptor 2 agonist, thereby enhancing the phagocytic ability of macrophages to tumor cells; it is first confirmed that amphotericin B combined with therapeutic antibodies can produce a synergistic anti-tumor effect, and the above synergistic effect is mainly due to the regulatory effect of amphotericin B on macrophage function, including enhancing Fc gamma receptor expression and polarizing macrophages to M1 direction, which provides a solid foundation for the clinical transformation of amphotericin B and is expected to provide new treatment options for cancer patients.

The invention discloses a culture medium and a culture method of orchid stem cells. The culture medium comprises a basic culture medium, and 100-300 mg / L of lanthanum nitrate is added into the basic culture medium; the basic culture medium is selected from one of an MS culture medium and a B5 culture medium. The basic culture medium is an MS culture medium, 0.9-1.2 mg / L of amphotericin B and a double antibody with the volume concentration of 0.8%-1.3% are further added, and the double antibody is a 100X mycillin mixed solution, 0.9-1.1 mg / L of 6-BA and 0.9-1.2 mg / L of NAA; or the basic culture medium is a B5 culture medium, and 0.099 mg / L to 0.130 mg / L of 6-BA, 12 mg / L to 17 mg / L of cane sugar, 0.49 mg / L to 0.54 mg / L of methyl jasmonate and 0.098 mg / L to 0.120 mg / L of triacontanol are also added into the basic culture medium. Lanthanum nitrate with the concentration of 100-300 mg / L is added into the culture medium for culturing the orchid stem cells, and experiments show that a large number of stem cells can be cultured within a short time by adding lanthanum nitrate with the concentration range, the cell dispersion degree is increased, the number of the cells is increased, and a foundation is provided for subculture multiplication culture in the next step.