51 results about "Spirolactone" patented technology

The invention relates to a fluorescence detection method and provides a fluorescent probe which has high sensitivity and high selectivity and is used for detecting intracellular hypochloric acid and an application of thiospirolactone in intracellular hypochloric acid detection. The structure of the fluorescent probe for detecting the intracellular hypochloric acid is a triphenylmethane fluorescent probe with a Xanthone ring parent structure; and the fluorescent probes of the thiospirolactone all adopt corresponding spirolactones as raw materials. The thiospirolactone has high-sensitivity fluorescent response characteristics on hypochloric acid, and when being used in the fluorescent probe for detecting the intracellular hypochloric acid, the selectivity is high. The probe has strong lightstability, no illumination self oxidation, rapid response to an aimed compound, good cell permeability and no strong cytotoxicity, and a product formed by combining the fluorescent probe and the aimed compound has strong photobleaching resistance. The thiospirolactone used for detecting the hypochloric acid of the aimed compound has high sensitivity and strong specificity and other active oxygen in cells has no interference on the detection.

The invention relates to a Rhodol derivative dye and a photoacoustic imaging PA (polyamide) probe and in particular to preparation and application of the Rhodol derivative dye and the photoacoustic imaging PA probe. A novel Rhodol derivative dye Rhodol-NIR is designed and synthesized, has novel Rhodol-NIR chromophore which has a large mole extinction coefficient, excellent photostability and an ideal quantum yield, and has excellent optical physical properties when a high-contrast activated PA probe. Tests prove that the Rhodol-PA probe designed and synthesized by the invention has high sensitivity and high selective detection on hNQO1 in in-vitro PA absorption and fluorescent measurement. By adopting the Rhodol derivative dye, the high-contrast activated PA probe is developed through a spirolactone open-loop conversion policy in China for a first time. The related policy of the invention is a generally applicable design, and a new platform can be provided for developing the high-contrast activated PA probe.

The invention provides spirolactone composition freeze-dried tablets and a preparation method thereof, and relates to the technical field of medicine and medicine production. The spirolactone composition freeze-dried tablets comprise spirolactone, starch and sucrose; the starch and sucrose are used as accessories, common corn starch is processed by a heating process, the bonding and disintegration effects of the starch in the tablets can be improved, the formability of the tablets is increased, and only two accessories, namely starch and sucrose, are needed in the spirolactone composition freeze-dried tablets. A freeze-drying process of two-time reduction and two-time increase is adopted for the spirolactone composition freeze-dried tablets, the formability of the tablets is better through two-time reduction and two-time increase of temperature, and the dissolubility of the tablets is improved so as to improve the bioavailability of the tablets; the tablets overcome the shortcomings of common spirolactone tablets, and the types and amount of accessories in the spirolactone tablets are reduced; and moreover, the dissolubility and bioavailability of the tablets are high, and the curative effect and safety of clinical medication are guaranteed.

This application relates to para-quinol derivatives, such as analogues of manumycins, aranorosins and gymnastatins. This application also relates to methods of synthesizing and using the para-quinol derivatives. In one embodiment of the invention a compound having the chemical structure (I) is provided wherein X₁ and X₂ are carbon atoms either joined by double bond or joined by a single bond and comprising constituents of an epoxide ring or a hydroxyethylene moiety; X₃ and X₄ are carbon atoms either joined by double bond or joined by a single bond and comprising constituents of an epoxide ring; R₁ is selected from the group consisting of branched alkyl chains, unbranched alkyl chains, cycloalkyl groups, aromatic groups, alcohols, ethers, amines, and substituted or unsubstituted ureas, esters, aldehydes and carboxylic acids; and R₂ is selected from the group consisting of H, OH and NHR₃ wherein R₃ is a nitrogen protecting group. In a particular embodiment of the invention R₁ is a polyunsaturated carbon chain as found in biologically active manumycins. The applicant's synthetic method may involve diasteroselective formation of a spirolactone in an oxidative spiroannulation process using tyrosine or a tyrosine derivative having a chiral centre as a starting material.

The invention discloses a diabetes treating compound medicine for reducing side effect of rosiglitazone and a preparation method thereof, and belongs to the field of medicine preparation. The compound medicine consists of rosiglitazone and a diuretic medicine, wherein the ratio of rosiglitazone to the diuretic medicine by weight is 1:(0.04-1). The diabetes treating compound medicine is compounded and matched with any one of spirolactone, amiloride, compound amiloride, ergosterol, triamterene, ethacrynic acid, hydroflumethiazide and bumetanide which can better eliminate side effect of rosiglitazone with rosiglitazone so as to form the compound medicine which not only can reduce the side effect of rosiglitazone, but also better treats diabetes.

The invention discloses a compound spirolactone nanoemulsion drug. The nano drug is prepared from the following materials in mass percentage: 1%-15% of spirolactone, 15%-35% of surfactant, 5%-20% of cosurfactant, 5%-20% of oil, 0.5%-10% of hawthorn extract, 0.5%-10% of asarum extract and the balance of distilled water, wherein the sum of the mass percentages of the ingredients is 100%. According to the invention, after the spirolactone is prepared into nanoemulsion dosage form, the ability of penetrating blood brain barrier is obviously increased, the bioavailability of active compound is obviously improved, the half-life period of the drug is prolonged, and the administration times are reduced. The dissolving and penetrating abilities of the drug of the spirolactone are improved by the nanoemulsion, and the stability of the spirolactone is increased. The spirolactone nanoemulsion drug has obvious synergistic effect after being combined with aqueous extract of the hawthorn and asarum, and the curative effect of the drug is brought into full play.

This invention relates to a process for making spirolactone compounds of general formula I, having an improved IA/IB ratio, according to the following shceme.

The invention belongs to the technical field of medicines and in particular relates to lacidipine-spirolactone co-amorphous solid dispersion and a preparation method thereof. According to the preparation method, lacidipine and spirolactone, which have a cooperative blood pressure lowering effect, are carriers for each other, and the co-amorphous solid dispersion is prepared by adopting a solvent volatilization method. The co-amorphous solid dispersion is formed by combining the lacidipine and the spirolactone according to the mol ratio of 1 to (1 to 9); Cu-Kalpha radiation is utilized, and a powder X-ray diffraction spectrum shown as a 2theta angle does not have a sharp diffraction peak; peak positions and peak strength of the co-amorphous solid dispersion are obviously changed in a Fourier infrared spectrum. Compared with a lacidipine crystal and a spirolactone crystal, the co-amorphous solid dispersion has the advantages that the dissolution rates and dissolvability of the lacidipineand the spirolactone are remarkably improved. The preparation method of the solid dispersion is simple and feasible and has good repeatability; amplified production is easy to carry out and industrial transformation is carried out; the preparation method has a good clinical application prospect.

The invention relates to a cleansing cream for preventing and curing acnes, comprising plant extracts, thiamphenicol, spirolactone, hydracrylic acid, lecithin, deionized water, pearl powder and 75% of ethanol; the product is obtained by mixing the components; the cleansing cream has better anti-acne effect; at least 95% of effective ingredients can be absorbed; the active ingredients can be delivered to dried and damaged part of skin in a prioritizing manner; the curative effect is improved; the preparation process is simple and does not need any special device; and the cream can be prepared by the production line for common cosmetics.

The invention relates to a hybridoma cell strain secreting spirolactone and metabolite monoclonal antibodies thereof, the hybridoma cell strain is named as a monoclonal cell strain PRM, and the hybridoma cell strain is preserved in China General Microbiological Culture Collection Center on May 13, 2021, the preservation address is No.3, Yard 1, Beichen West Road, Chaoyang District, Beijing, and the preservation number is CGMCC No.22341. The hybridoma cell strain disclosed by the invention can efficiently and stably secrete the monoclonal antibody of the spirolactone and the metabolite of the spirolactone, provides a powerful detection method and means for detecting the residual quantity of the spirolactone and the metabolite of the spirolactone in animal-derived food and cosmetics, and has relatively good sensitivity and specificity.

The invention relates to the technical field of medicine synthesis, in particular to a synthesis process of a steroid compound, canrenone and spirolactone. An embodiment of the invention provides thesteroid compound. The steroid compound has a structural formula as shown in the specification. In the structural formula, R is selected from H or an alkyl group. The steroid compound can be used for synthesizing canrenone and spirolactone, synthesis conditions are mild, synthesis efficiency is high, the amount of wastewater is small, the quality of the formed products is high, and production costcan be effectively reduced.

The invention discloses tinidazole and spirolactone cream and a preparation method thereof, in order to solve problems of current tinidazole and spirolactone cream, such as poor stability and moderate sensitization. According to the formula, the cream comprises tinidazole, spirolactone, laurocapram, stearic acid, albolene, sorbitol anhydride monostearate, hexadecanol, light liquid paraffin, lauryl sodium sulfate, polysorbate-80, propylene glycol, sodium benzoate and purified water. The cream disclosed by the invention can inhibit formation of acne through such links as inhibiting bacteria, diminishing inflammation and reducing sebum secretion, and has an excellent curative effect on inflammatory skin lesion and non-inflammatory skin lesion caused by acne.

The invention provides a method for preparing spirolactone intermediate canrenone. The method comprises the following operation steps: a lactone substance (I) is dissolved in an organic solvent, a catalyst and an auxiliary agent are added, and the mixture is stirred at 50-80 DEG C to prepare the canrenone (II), wherein the organic solvent is at least one of cyclohexane, toluene or methyl tetrahydrofuran; the auxiliary agent is at least one of dimethyl formamide, N,N - dimethyl acetamide and N-methyl pyrrolidone; and the catalyst is poly-4-vinylpyridine. The reaction route is shown in the specification. Compared with the prior art, the method has the advantages that the reaction temperature is low, pressurization is not needed, the quality of canrenone can be improved, the energy consumption can be effectively reduced, and the production cost can be reduced.

The invention discloses a combined combination drug for resisting heart failure and application of a steroid aldosterone receptor antagonist and beta-cyclodextrin in preparation of a drug for resisting heart failure. The combined drug contains a diluent, an adhesive, a disintegrating agent, an antioxidant, an emulsifier, a solubilizer, the steroid aldosterone receptor antagonist and beta-cyclodextrin. According to the combined combination drug for resisting heart failure, compared with drugs such as spirolactone, beta-cyclodextrin, nebivolol and amlodipine which are independently used, the combined combination drug of the steroid aldosterone receptor antagonist and beta-cyclodextrin can significantly increase the cell survival rate, can reduce the ROS content in cells treated by adriamycin, can significantly improve the antioxidant ability of the cells, and can further greatly improve the anti-heart failure effect of the drug.

The invention relates to a medicine for treating diastolic cardiac insufficiency and a preparation method of the medicine. The medicine contains metoprolol lipidosome, hydrochlorothiazide, spirolactone, filler, a disintegrating agent and a surfactant, wherein metoprolol lipidsome comprises metoprolol, cholesterol, soybean lecithin, (distearoyl-phosphatidylethanolamine)-polyethylene glycol, propylgallate and Span. The medicine has the advantages that the accumulative dissolutive degree is high, the medicine is slowly and constantly released, the biological utilization rate is high, the stability is good, the medicine has a remarkable treatment effect on diastolic cardiac insufficiency, a preparation process is simple and suitable for industrial production and the like.

The invention discloses a method for preparing spirolactone by a chemical-enzyme method, and belongs to the technical field of organic synthesis. According to the method for preparing the spirolactone through the chemical-enzymatic method, 4AD serves as a raw material, and the spirolactone is obtained through enol etherification, epoxidation, lactonization, enzymatic dehydrogenation and sulfo-reaction. The enzymatic dehydrogenation method adopted by the spirolactone synthesis process route is good in specificity, mild in condition, free of special equipment and high in catalytic rate; the reaction product in each step involved in the method is easy to purify, the total mass yield of the final product is higher than 92%, and the HPLC purity is higher than 99.8%; the method is low in cost and suitable for industrial large-scale production, and has good economic benefits.

The invention provides a binary co-amorphous substance and a preparation method and application thereof, the co-amorphous substance comprises a spirolactone/L-tryptophan or a spirolactone/L-phenylalanine co-amorphous substance, and the co-amorphous substance is formed by spirolactone and L-tryptophan as well as L-phenylalanine according to a molar ratio of 1: 1. Compared with a spirolactone bulk drug crystal, the spirolactone/L-tryptophan co-amorphous substance has the advantages that the solubility is improved by 3.22 times, and the dissolution rate is improved by 2.45 times; compared with a spirolactone bulk drug crystal, the spirolactone/L-phenylalanine co-amorphous substance has the advantages that the solubility is improved by 1.76 times, and the dissolution rate is improved by 1.59 times. The compound has a wide treatment prospect in the aspects of treating edema diseases, hypertension, primary aldosteronism and the like. The preparation method of the spirolactone/L-tryptophan and the spirolactone/L-phenylalanine binary co-amorphous substance is simple, no toxic organic solvent is added, the energy consumption is low, the efficiency is high, the preparation method is green and environment-friendly, and the application prospect is wide.