18 results about "Calcitriol" patented technology

A single unit oral dose pharmaceutical composition for use as a medicament for separate, sequential or simultaneous administration with an agonist of a 5-hydroxytryptamine (5-HT) receptor;wherein the single unit oral dose pharmaceutical composition comprises a first active ingredient and a second active ingredient;wherein the first active ingredient is for absorption in the gastrointestinal tract from the oesophagus onwards and the second active ingredient is for absorption in the oral cavity; andwherein the first active ingredient is naltrexone in an amount of 0.01 to 10 mg and the second active ingredient is calcitriol in an amount of 80 to 200 ug.

The invention discloses a method for constructing a zebrafish osteoporosis model by using levothyroxine sodium, and belongs to the field of biological medicines. An existing zebrafish osteoporosis model has the problems of high toxicity, poor specificity and the like, and is solved through the following steps that 5 dpf normally-developed wild type AB line zebrafish juvenile fish is selected, a levothyroxine sodium E3 culture medium with the concentration of 7.81-250 mg / mL is used for continuous treatment from 5 dpf to 8 dpf, the model is verified by detecting the vertebra fluorescence area, brightness and number, and the zebrafish osteoporosis model is obtained. The toxicity is evaluated by combining indexes such as body weight and body length. The result shows that the vertebra mineralization of the model is obviously reduced, and the phenotype can be obviously reversed by the positive drug calcitriol. The model provided by the invention has the characteristics of strong skeleton specificity, low toxicity and reversibility, and is suitable for osteoporosis mechanism research and drug screening.

The invention discloses a calcitriol impurity B and a preparation method thereof, and belongs to the technical field of medicines. The preparation method of the calcitriol impurity B comprises the following steps: S1, mixing an intermediate 3, a first solvent and alkali, and then heating for reflux reaction to obtain an intermediate 4; and S2, dissolving the intermediate 4 in a second solvent, cooling to 0-5 DEG C, adding a photosensitizer, and reacting under the illumination condition to obtain the calcitriol impurity B. The calcitriol impurity B prepared by the preparation method provided by the invention is high in yield, and the purity of the product can reach 99% or above.

This invention provides ACE2 expression inhibitors and their application in ACE2-mediated diseases. It uses human RXRα as a target protein for virtual drug screening and employs computer molecular docking technology to screen compounds with high affinity for the human RXRα receptor. Combined with cell experiments, it screens compounds that inhibit ACE2. The ACE2 expression inhibitors are at least one of ten drugs selected from ursolic acid, phlorizin, resveratrol, triamcinolone, budesonide, fluticasone propionate, vitamin D2, vitamin D3, calcitriol, and alfacalcidol. The ACE2 inhibitors screened by this invention can serve as targeted drugs for ACE2-mediated diseases, providing more drug options for the prevention or treatment of these diseases.

The invention provides a synthesis method of an intermediate for preparing a fluorocalcitriol 23, 24-double bond derivative, and relates to the field of organic chemistry, beta unsaturated acid ester is used as a trans-double bond side chain donor reagent and is subjected to a coupling reaction with an upstream substrate to obtain a beta trans-double bond terminal ester group compound, the technical prejudice is broken through, and the yield of the intermediate is improved. A target product is obtained with high selectivity, the yield can reach 92%, the technical problem of synthesis of a terminal ester compound with beta trans-double bonds is solved, the terminal ester compound with beta trans-double bonds is reacted to generate a final CD ring intermediate with 23 and 24-double bonds, and a process route of the CD ring intermediate with 23 and 24-double bonds is broken through, so that the fluorine calcitriol 23, 24-double bonds are synthesized, and the yield of the fluorine calcitriol 23, 24-double bonds is increased. According to the invention, a key intermediate is provided for a 2, 4-difluoro-1, 4, 24-double bond derivative, a material basis is provided for the provision of a fluorocalcitriol impurity reference substance and the discovery of a bone metabolism drug, and the economic cost is reduced.

The invention discloses a preparation method of a fluorine bone triol intermediate, which comprises the following steps: (20S)-3beta-acetoxy-20-methyl-21-iodo-pregna-5-ene as shown in a formula II is taken as a raw material, and 26, 26, 26, 27, 27, 27-hexafluoro-25-hydroxycholesterol is prepared through four steps of reaction, namely coupling, ester hydrolysis, trifluoromethyl substitution and trifluoromethyl addition, and the reaction formula is as shown in the specification. The method has the advantages of simple process, cheap and easily available reagents, and suitableness for industrial production.

The application discloses a kind of calcitriol soft capsule content in vitro evaluation method and its application, belong to the technical field of pharmaceutical analysis.The method uses diffusion cell device, under certain conditions, the dissolution and penetration behavior of calcitriol soft capsule content is simulated and determined.Specifically, acidic or buffered salt medium solution containing specific proportion alcohol is added to diffusion cell, so that liquid surface is flush with filter membrane;The sample to be measured content is placed above filter membrane;At specified temperature, rotation speed, sample is taken from the lower part of diffusion cell at different time points, and the concentration of calcitriol is determined.The method of the application can accurately and conveniently evaluate the in vitro release behavior of calcitriol soft capsule content prepared by different prescriptions or processes, has high correlation degree with in vivo effectiveness, and has good repeatability, to provide reliable in vitro evaluation tool for product quality control and prescription screening.

The invention discloses the application of the Chinese wolfberry fruit-glossy privet fruit and calcitriol composition in the medicine for treating postmenopausal osteoporosis for the first time, and through three-layer research of'in vitro cell-animal model-molecular pathway ', it is clear that the composition can bidirectionally regulate and control kidney vitamin D metabolic enzyme by activating'PI3K-AKT' signal pathway for the first time, so that the curative effect on postmenopausal osteoporosis is achieved. Further, the serum 25 hydroxyl vitamin D and blood calcium level are improved, and the bone mineral density is improved. The mechanism provides a modern molecular biology support for the traditional Chinese medicine theory of'kidney dominating bone ', and also establishes a new path of'regulating kidney metabolic enzyme to treat osteoporosis'. By optimizing the metabolic bone protection effect of the vitamin D, bone loss of ovariectomized mice is effectively delayed, meanwhile, the vitamin D and calcitriol play a synergistic effect, and the vitamin D has a multi-target bone protection effect in postmenopausal PMOP, has anti-osteoporosis activity and can be used for treating the PMOP.

The invention discloses a medicine for treating anxiety and depression symptoms, which comprises calcitriol, and also discloses an application of the medicine for treating anxiety and depression symptoms in construction of an anxiety and depression symptom model. According to the medicine for treating anxiety and depressive symptoms and the application thereof, mice with anxiety and depressive symptoms are intervened with nasal drop calcitriol, animal experiment evidences are provided for supplementing calcitriol to intervene autism spectrum disorders in the early stage of clinical experiments, and a new thought is provided for early prevention and treatment of neurodevelopment disorders of clinical children.

The invention discloses application of vitamin D in preparation of a protection medicine for avoiding ovarian injury caused by chemotherapy, and belongs to the technical field of biology. It is found for the first time that in an experiment of intraperitoneal injection of calcitriol (the active form of vitamin D) and retinoic acid in newborn mice, DNA damage caused by chemotherapeutic drugs cyclophosphamide and adriamycin can be partially reversed when calcitriol and retinoic acid are independently used; the number of primordial follicle apoptosis caused by chemotherapeutic drugs (including cyclophosphamide and adriamycin) is remarkably reduced, and the effect of combined medication (calcitriol and retinoic acid) is better. The discovery expands the application of vitamins in the female reproductive system, provides a new thought for preventing ovarian follicle development from being damaged by chemotherapy drugs and in-vivo protection of fertility, and also has important significance for protecting the life quality of female patients after chemotherapy.

The present invention refers to food compositions comprising selenium, preferably in an amount of at least 4 μg / g, and a set of different ingredients selected from retinyl palmitate, calcitriol (1,25(OH)2 Vitamin D3), phylloquinone (phytomenadione, Vitamin K1), tocopherol (preferably a-tocopherol), or ubiquinol. The invention particularly refers to chocolate bars comprising selenium and the set of different ingredients. Consumption of the food compositions of the invention can reverse, reduce or slow signs of aging in a subject. The invention also relates to methods of producing cacao fruits, cacao beans, cacao mass, and cacao powder with an increased selenium content.

1. Name of the product in this design: Packaging Box (Calcitriol Soft Capsules). 2. Intended use of this design: pharmaceutical packaging. 3. The key design features of this product are the combination of shape and pattern. 4. The image or photograph that best illustrates the design's key points: a 3D model.

Provide improved means for transdermally delivering a pesticidal or other toxic agent from a composition containing the toxic agent to a target animal, particularly into its bloodstream. **Solution**: A composition for killing animals, such as rodents, comprising (i) one or more toxic agents toxic to the animal, such as cholecalciferol or 25-hydroxy cholecalciferol (vitamin D3), as a toxic component, and (ii) a carrier system for the toxic component, wherein the carrier system (ii) comprises (a) at least one solvent or dispersion medium for the toxic component, such as an alcohol like ethanol, and (b) at least one skin disrupting component, such as dimethyl sulfoxide (DMSO). The composition enhances the skin penetration of the toxicant into or through the skin of the animal where the composition is sprayed or delivered, for example, in a trap or other device. ​

Use of vitamin D in the preparation of a protective drug for avoiding chemotherapy-induced ovarian injury, pertaining to the field of biotechnology. It has been discovered for the first time that in experiments involving intraperitoneal injection of calcitriol (the active form of vitamin D) and retinoic acid into newborn mice, both calcitriol and retinoic acid, when used individually, can partially reverse the DNA damage caused by the chemotherapeutic drugs cyclophosphamide and doxorubicin, and significantly reduce the number of primordial follicle apoptosis induced by chemotherapeutic drugs (including cyclophosphamide and doxorubicin); the combined drug use (calcitriol + retinoic acid) has a better effect. This discovery expands the application of vitamins in the female reproductive system, provides new ideas for preventing damage to ovarian follicle development caused by chemotherapeutic drugs and for the in vivo protection of fertility, and is also of great significance for safeguarding the quality of life of female patients after chemotherapy.

The present invention relates to a formulation comprising a combination of sodium pentaborate pentahydrate and calcitriol (active form of vitamin D), which exerts an anti-cancer effect in the treatment of hepatocellular carcinoma. The purpose of the present invention is to provide an anti-cancer effect on hepatocellular carcinoma by a preparation obtained from a combination of sodium pentaborate pentahydrate and calcitriol.

The invention belongs to the technical field of cancer treatment, and discloses a method for inducing mitochondrial apoptosis and remodeling an immunosuppressive tumor microenvironment to inhibit CRPC by targeting DHCR7 and cooperating with enzalutamide. It is found that drug-resistant cells show remarkable cholesterol accumulation and cholesterol ester reduction, meanwhile, 7-DHC depletion is accompanied, the level of 7-DHC can be recovered through drug treatment, mitochondrial damage dependent on reactive oxygen species (ROS) is caused, and tumors are sensitive to enzalutamide again. Calcitriol and enzalutamide act synergistically to overcome drug resistance and activate anti-tumor immunity, associating epidemiological observations about the association between vitamin D deficiency and invasive prostate cancer over tens of years with viable treatment strategies. The results not only expand the understanding of metabolic heterogeneity in castration resistant prostate cancer (CRPC), but also provide a biomarker-based framework for using existing therapies to resist fatal treatment drug resistance.

The application discloses a C1, 25-position double-hydroxylase mutant of vitamin D3 and a genetically engineered bacterium and application thereof, and belongs to the technical field of enzyme engineering. In the application, the glutamic acid at position 81 of vitamin D3 double-hydroxylase of Bacillus megaterium H-1 is mutated into alanine to obtain a vitamin D3 double-hydroxylase mutant; pMA5 is used as an expression plasmid to realize heterologous expression of the vitamin D3 double-hydroxylase mutant in Bacillus subtilis; and the application of the engineered bacterium of the application to the synthesis of calcitriol has the effects of improving the product concentration accumulation amount and shortening the reaction time consumption, and meets the production demand of shortening the time cost in industrial production.