108 results about "Hydroxyvitamins D" patented technology

Vitamin D compounds of formula (I) with a label attached to a spacer group in the 3 position are disclosed.In the above formula (I), X is an optionally substituted hydrocarbon group with a length of 0.8-4.2 nm, optionally containing the heteroatoms S, O, N or P; Y is H or OH; A is a label capable of binding with high affinity to a protein; R is an optionally substituted hydrocarbon side chain of a D vitamin or a D vitamin metabolite. Also disclosed is the preparation of formula (I).

Methods for treating and preventing obesity, inhibiting adipocyte differentiation, inhibiting increased SCD-1 gene transcription, and / or reducing body fat in a subject include administering at least one analog of 1α,25-dihydroxyvitamin D3 or 1α,25-dihydroxyvitamin D2 or a pharmaceutical composition that includes such an analog to a subject in need thereof. The analog may be a 19-nor vitamin D analog such as a compound of formula IA, a compound of formula IB, or a mixture thereof where the variables R1, R2, and R3 have the values described herein.

Provided are methods of detecting the presence or amount of a dihydroxyvitamin in D metabolite in a sample using mass spectrometry. The methods generally comprise ionizing a dihydroxyvitamin D metabolite in a sample and detecting the amount of the ion to determine the presence or amount of the vitamin D metabolite in the sample. In certain preferred embodiments the methods include immunopurifying the dihydroxyvitamin D metabolites prior to mass spectrometry. Also provided are methods to detect the presence or amount of two or more dihydroxyvitamin D metabolites in a single assay.

The present invention relates to pharmaceutical products containing progestins in combination with the 25 hydroxy Vitamin D compounds. The 25 hydroxy Vitamin D compounds are preferably administered with the progestins. In OC and HRT regimens, the 25 hydroxy Vitamin D compounds can be administered daily, or on a non-daily basis, and if so, preferably when the progestin dosages are the highest in the cycle.

The present invention relates to pharmaceutical products containing progestins in combination with the 25 hydroxy Vitamin D compounds. The 25 hydroxy Vitamin D compounds are preferably administered with the progestins. In OC and HRT regimens, the 25 hydroxy Vitamin D compounds can be administered daily, or on a non-daily basis, and if so, preferably when the progestin dosages are the highest in the cycle.

A method for treatment of diseases caused by deficiency or overproduction of the vitamin D3 metabolites by administering analogs of 1 alpha ,25-dihydroxyvitamin D3. These analogs are selective agonists or antagonists for the genomic and rapid nongenomic cellular responses. A pharmaceutical composition comprising 1 alpha ,25-dihydroxyvitamin D3 analog.

The invention provides a detection reagent for detecting hydroxy vitamin D, a preparation method of the detection reagent and application of the detection reagent to immunological detection of 25-hydroxy vitamin D. The detection reagent comprises a conjugate substance and a magnetic sphere, wherein the conjugate substance is formed by 25-hydroxy vitamin D antigen derivatives and protein carriers; the magnetic sphere is coated with the conjugate substance. By modifying the 25-hydroxy vitamin D antigen derivatives, the stability of the produced reagent is obviously improved, and the specificity and accuracy in the detection of the 25-hydroxy vitamin D are also improved. The invention further provides a kit for detecting 25-hydroxy vitamin D; the kit comprises the detection reagent, and the kit is good in stability, high in accuracy and high in universality.

Provided are methods of detecting the presence or amount of a dihydroxyvitamin D metabolite in a sample using mass spectrometry. The methods generally comprise ionizing a dihydroxyvitamin D metabolite in a sample and detecting the amount of the ion to determine the presence or amount of the vitamin D metabolite in the sample. In certain preferred embodiments the methods include immunopurifying the dihydroxyvitamin D metabolites prior to mass spectrometry. Also provided are methods to detect the presence or amount of two or more dihydroxyvitamin D metabolites in a single assay.

The embodiment of the invention provides a method for detecting 25(hydroxyl)vitamin D by using a high-pass liquid chromatography-tandem mass spectrometry. The method comprises the following steps of: adding an acetonitrile solution containing an internal standard substance of the 25(hydroxyl)vitamin D into a human serum sample to carry out protein precipitation; sufficiently and uniformly mixing the solution, and then, adding an n-hexane extracting solvent; sufficiently and uniformly mixing the solution, then centrifuging the solution, movably taking a supernatant and drying the supernatant, and adding a complex solution to obtain a sample to be detected; detecting the sample to be detected by using a high-pass liquid chromatography-tandem quadrupole mass spectrometer; and quantifying according to the relative retention time of 25(hydroxyl)vitamin D2 and / or 25(hydroxyl)vitamin D3 and the detected abundance ratio of quantitative ion pairs by using an internal standard curve method. According to the embodiment of the invention, the method has the advantages of simplicity in pretreatment, strong specificity and matrix interference resistance, short detection time, high pass, high detection precision and low cost.

A method of treating and preventing secondary hyperparathyroidism in CKD by increasing or maintaining blood concentrations of both 25-hydroxyvitamin D and 1,25-dihydroxyvitamin Din a patient by administering 25-hydroxyvitamin D3 with or without 25-hydroxyvitamin D2 and, as necessary, 1,25-dihydroxyvitamin D2 as a Vitamin D hormone replacement therapy.

The invention provides 24-hydroxyvitamin D compounds and methods for their use in the treatment and prophylaxis of hyperparathyroidism and hyperproliferative diseases, and in the modulation of the immune and inflammatory responses as well as the treatment of bone depletive disorders.

The invention provides a method for detecting 25-hydroxy-vitamin D through a high-sensitivity high-throughput ultra-performance liquid chromatography-tandem mass spectrometry device. The method comprises adding an internal standard substance of 25-hydroxy-vitamin D into a serum sample, adding a zinc sulfate solution and a methanol solution into the mixture so that protein deposition is realized, carrying out full mixing, adding a n-hexane solvent into the mixture, carrying out extraction, carrying out full mixing, carrying out centrifugation, taking the supernatant, carrying out nitrogen blowing drying, adding a compounded solution into the supernatant to obtain a sample to be detected, detecting the sample to be detected through an ultra-performance liquid chromatography-tandem quadrupole mass spectrometry device and carrying out quantitation through an internal standard curve method based on 25-hydroxy-vitamin D2 and / or 25-hydroxy-vitamin D3 quantitative and qualitative ion pair retention time as qualitative basis. The method has advantages of simple pre-treatment process, good specificity, good matrix interference resistance, short detection time, high throughput, high detection precision, high sensitivity and low cost.

The invention relates to a liquid chromatogram tandem mass spectrum detection method for 25-hydroxy vitamin D in a dry blood sample. The pretreatment technique mainly comprises the processes of sample pretreatment, deriving and redissolving, and meanwhile, the multi-reaction monitoring MRM scanning mode is adopted. According to the method, the high-flux liquid chromatogram tandem mass spectrum detection method for 25-hydroxy vitamin D in the dry blood sample can be realized; the problems of large demanded quantity of samples and inconvenience in sampling and transporting of the traditional liquid chromatogram tandem mass spectrum method are solved; through the improvement for the detection technique, the detection for the 25-hydroxy vitamin D in the dry blood sample is realized, the detector can voluntarily collect at home, the demanded quantity of samples is small and the sampling and transporting are convenient.

The invention relates to a method for detection of 25-hydroxyvitamin D in serum. The method comprises sample pretreatment: adding an acetonitrile solution containing a 25-hydroxyvitamin D internal standard substance into a serum sample, carrying out protein precipitation, carrying out centrifugation, taking the supernatant and diluting the supernatant through acetonitrile to obtain a sample to be detected, wherein a volume ratio of the serum sample to the acetonitrile solution is 1: 1-4 and a volume ratio of the supernatant to acetonitrile is 1: 1-4, and enrichment, separation and detection: carrying out enrichment, separation and detection on the sample to be detected through a two-dimensional liquid chromatography-tandem quadrupole mass spectrometer. The method is simple, greatly shortens the detection time, improves the detection flux of the sample and has a high detection precision, a low cost, specificity and strong matrix interference resistance.

The invention discloses a high performance liquid chromatography tandem mass spectrometry detection method of 25-hydroxy vitamin D in serum. The method comprises the following steps that (1) a sampleis pre-treated, specifically, an internal standard working solution and a sodium hydroxide solution are sequentially added into a serum sample and mixed to be uniform; (2) solid-liquid extraction treatment is conducted, specifically, the sample treated in the step (1) is loaded to an SLE 96 pore plate, and eluted with normal hexane, and then the eluant is blown to be dried by using nitrogen; (3) aderivatization reaction is conducted, a derivatization reagent 4-phenyl-1,2,4-triazoline-3,5-diketone (PTAD) solution is added to redissolve, a thermostatic reaction is conducted, then ethyl alcoholis added to terminate the reaction, and the product is blown to be dried by using nitrogen; and (4) redissolution is conducted, and analytical detection is conducted by adopting the high performance liquid chromatography tandem mass spectrometry based on a multiplexing system (MPX). The high performance liquid chromatography tandem mass spectrometry detection method is high in detection sensitivity, high in specificity and low in cost, meanwhile, the pre-treatment time and analysis time of the sample are effectively shortened, and the detection efficiency of the sample is improved.

The invention provides a liquid chromatography-tandem mass spectrometry detection method of 25-hydroxyvitamin D in serum or blood plasma. The method comprises the following steps: 1, preprocessing a sample: adding 10[mu]l of an internal standard solution and 200[mu]l of human serum to a centrifuge tube, uniformly mixing, adding 600[mu]l of acetone, uniformly mixing, standing the obtained solution at a low temperature for 15min, adding the solution to a centrifuge, centrifuging the solution at 13000rpm for 5min, taking the obtained supernatant to a second centrifuge tube, drying the supernatant with 50DEG C nitrogen until the supernatant is dry, adding 200[mu]l of acetonitrile to redissolve the dried supernatant, uniformly mixing, adding the obtained acetonitrile solution to the centrifuge, centrifuging the acetonitrile solution at 13000rpm for 2-4min, and taking the obtained supernatant; and 2, detecting the finally obtained supernatant through liquid chromatography-tandem mass spectrometry in a multi-reaction monitoring MRM scanning manner. A preprocessing technology is improved, so the preprocessing process in the invention is simple and fast, and bath processing can be realized.

The invention provides a blood 25-hydroxy vitamin D3 adenocarcinoma assay kit and a preparation method thereof, and relates to an assay kit. The kit comprises calibrators of different concentrations, an ELISA (enzyme-linked immuno sorbent assay) plate of a 25-hydroxy vitamin D3 coated antibody, horse radish peroxidase marked 25-hydroxy vitamin D3, a quality control product, a substrate chromogenic solution, a reaction stop buffer and a washing fluid. By adopting a series of chemical modification, the 25-hydroxy vitamin D3 is modified into 25-hydroxy vitamin D3 hemisuccinate ester. Hapten is transformed into complete antigen by an improved carbodiimide method and protein vector BSA (bovine serum albumin) protein coupling. Furthermore, the blood25-hydroxy vitamin D3 adenocarcinoma assay kit is developed by combining the ELISA method. The kit can be used in cancer assay in clinical application.

The invention discloses a novel industrial preparation method for a medicament 1-alpha-hydroxyl vitamin D2 or D3, namely paricalcitol and doxercalciferol, for treating osteoporosis. Site 1 of the vitamin D is subjected to microbial transformation by using pseudonocardia CGMCC No. 5098 to directly obtain 1-alpha-hydroxyl vitamin D in one step. The method is milder than a chemical method; protection is not required and toxic selenium dioxide is not required to be used for oxidation; the method has regional selectivity; radical protection is not required; the biotransformation yield reaches 40-50 percent; the method is environmentally-friendly; the process route is greatly shortened through one-step transformation reaction, the yield is improved, and the preparation cost is reduced; the known chemical reaction of about six steps for synthesizing the paricalcitol and the doxercalciferol is shortened into one-step reaction; and the total yield is increased to be 40-50 percent.

The invention discloses a chemiluminiscence immuno-assay kit for 25-hydroxyl vitamin D and a preparation method thereof. The chemiluminiscence immuno-assay kit herein includes: carboxylated magnetic micro-particles that are coated by a 25-hydroxyl vitamin D monoclonal antibody and a chemiluminiscence marker that is marked by a vitamin D derivative. The chemiluminiscence immuno-assay kit, with a full-auto chemiluminiscence immuno-analysis instrument as a detection tool, completes the detection on the 25-hydroxyl vitamin D. A test proves that the kit reaches 0.2 ng / ml in detection sensitivity, which is improved by at least 10 times than that of a conventional detection method of the 25-hydroxyl vitamin D. The chemiluminiscence immuno-assay kit has high detection precision.

The invention discloses a method for simultaneously detecting vitamin A and 25-hydroxyl vitamin D in blood. The method comprises the following steps: firstly, centrifuging a whole blood sample, and taking supernate to obtain serum or plasma for later use; secondly, calibrating a standard solution; thirdly, pretreating a sample; fourthly, taking 80mu L of to-be-detected supernate sample treated in the third step, putting the to-be-detected supernate sample into an automatic sample feeding bottle, and analyzing by liquid chromatography-tandem mass spectrometry; meanwhile, quantitatively detecting the contents of the vitamin A and the 25-hydroxyl vitamin D in the blood. The method for simultaneously detecting the vitamin A and the 25-hydroxyl vitamin D in the blood, disclosed by the invention, has the advantages of high specificity, high accuracy, high flexibility and short analysis time.

Oral and topical pharmaceutical compositions, kits and methods of treatment thereof for treating various skin disorder including acne, psoriasis, ichthyosis, photoaging, photodamaged skin, and, skin cancer. Exemplary vitamin D analogs as active pharmaceutical ingredients include 2-methylene-19-nor-20(S)-1α-hydroxy-bishomopregnacalciferol, 19-nor-26,27-dimethylene-20(S)-2-methylene-1α,25-dihydroxyvitamin D3, 2-methylene-1α,25-dihydroxy-(17E)-17(20)-dehydro-19-nor-vitamin D3, 2-methylene-19-nor-(24R)-1α,25-dihydroxyvitamin D2, 2-methylene-(20R,25S)-19,26-dinor-1α,25-dihydroxyvitamin D3, 2-methylene-19-nor-1α-hydroxy-pregnacalciferol, 1α-hydroxy-2-methylene-19-nor-homopregnacalciferol, (20R)-1α-hydroxy-2-methylene-19-nor-bishomopregnacalciferol, 2-methylene-19-nor-(20S)-1α-hydroxy-trishomopregnacalciferol, 2-methylene-23,23-difluoro-1α-hydroxy-19-nor-bishomopregnacalciferol, 2-methylene-(20S)-23,23-difluoro-1α-hydroxy-19-nor-bishomopregnancalciferol, (2-(3′hydroxypropyl-1′,2′-idene)-19,23,24-trinor-(20S)-1α-hydroxyvitamin D3, 2-methylene-18,19-dinor-(20S)-1α,25-dihydroxyvitamin D3, a stereoisomer thereof, a prodrug thereof in oral compositions, a salt thereof, and / or a solute thereof. Compounds that activate retinoic acid receptors, such as retinoyls and retinoyl esters, include 13-cis-retinoic acid, all-trans-retinoic acid, (2E,4E,6Z,8E)-3,7-dimethyl-9-(2,6,6-trimethyl-1-cyclohexeneyl)nona-2,4,6,8-tetraenoic acid, 9-(4-methoxy-2,3,6-trimethyl-phenyl)-3,7-dimethyl-nona-2,4,6,8-tetraenoic acid, 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-napthoic acid, 4-[1-(3,5,5,8,8-pentamethyl-tetralin-2-yl)ethenyl]benzoic acid, retinobenzoic acid, ethyl 6-[2-(4,4-dimethylthiochroman-6-yl)ethynyl]pyridine-3-carboxylate, retinoyl t-butyrate, retinoyl pinacol, retinoyl cholesterol, an isomer thereof, a prodrug thereof for oral compositions, an ester thereof, a salt thereof, and / or, a solute thereof. Combinations of such active ingredients demonstrate synergistic efficacy.

The invention relates to a quantitative-detection test paper strip for 25-hydroxyvitamin D and application of the quantitative-detection test paper strip and belongs to the field of medical reagents. The test paper strip comprises a sample pad, a combining pad, an NC film, a water absorbing pad and a PVC lining plate, wherein the sample pad is coated with latex microparticles activated by 25-OH VD and / or latex microparticles activated by 1, 25-(OH)2VD; the combining pad is coated with colloidal-gold-labeled anti-25-OH VD monoclonal antibodies and anti-VDBP monoclonal antibodies; the NC film comprises a T line and a C line in sequence; the T line is coated with 25-OH VD-BSA and partially-expressed human VDBP; and the C line is coated with goat-anti-mouse antibodies. With the adoption of the test paper strip, the content of vitamin D in a sample can be quickly and accurately determined without pretreating the sample.

Provided are a detection agent for detecting hydroxy vitamin D, preparation method thereof, and use thereof in 25-hydroxy vitamin D immunological detection. The detection agent comprises a conjugate formed by a 25-hydroxy vitamin D antigen derivative and protein carrier, and magnetic spheres coated by the conjugate. Also provided is a 25-hydroxy vitamin D detection kit comprising the detection agent.

The invention discloses a method for preparing 25-hydroxyvitamin D by microbial transformation. The method utilizes Streptomycessp. wsbee2009112 which is preserved in the China general microbiological culture collection center and has a preservation number of CGMCC No.5831 to carry out 25-hydroxy transformation of vitamin D. The method comprises the following steps of inoculating a medium with a prepared spore suspension, carrying out culture on a shaking table at a temperature of 22 to 30 DEG C at a rotation rate of 200 to 280rpm for 2 to 5 days, adding a mixture of one or more cyclodextrins, vitamin D, a surfactant and an organic solvent into the medium, carrying out culture for 1 to 10 days, and filtering to obtain a finished product. The method realizes direct hydroxylation at a 25 site of vitamin D, and has a high yield, simple production processes and a low cost.

We disclose compositions comprising Vitamin D (cholecalciferol and / or ergocalciferol) and 25-OH D3 (calcifediol), and use of those compositions to affect at least concentration, bioavailability, metabolism, or efficacy of vitamin D in a human. Forms and dosages of the composition, as well as processes for manufacturing a spray-dried formulation, are also disclosed.

The invention discloses a high-performance liquid chromatography (HPLC)-tandem mass spectrometry detection method of 25-hydroxy vitamin D in dried blood spots. The method comprises the following steps: (1) ultrasonic extraction: taking a dried blood spots sample, adding an extraction solvent, ultrasonically extracting, and then adding an internal standard working solution, performing vortex-mixing, centrifuging, taking upper extraction liquid, drying through nitrogen; (2) derivatization reaction: adding the sample processed in the step (1) into a PTAD derivatization working solution to redissolve, reacting at constant temperature, and adding the ethanol to terminate the reaction, and drying through the nitrogen; and (3) redissolving: performing analysis detection by adopting the HPLC-tandem mass spectrometry. The method disclosed by the invention is high in efficiency, high in flux, low in cost, simple for operation, high in accuracy, and high in sensitivity, free form conflict limitation on other detection projects, and suitable for fast detecting batch of clinical samples; and meanwhile, the wound on the subject is small by adopting the dried blood spots method, the amount of collecting blood is less, the sample is convenient for collection and transportation, and easy to save, the stabiligy is good, and the method is especially suitable for the detection on the population (such as infants) difficult for venous blood collection.