147 results about "Prednisolone" patented technology

The invention features a method for treating a patient having an inflammatory disorder, by administering to the patient (i) a tricyclic antidepressant (e.g., amoxapine); and (ii) a corticosteroid (e.g., prednisolone) simultaneously or within 14 days of each other in amounts sufficient to reduce or inhibit inflammation.

Disclosed herein are compositions comprising cyclodextrin derivatives and prednisolone and prodrugs thereof, and methods related thereto. The use of soluble polyanionic polymers such as hydroxypropylmethylcellulose and others in relation to these compositions is also disclosed. Delivery of these prednisolone-related compounds to the back of the eye via topical ophthalmic administration is also disclosed.

The invention teaches derivatives of ascomycin and methods of preparing immunogens and other conjugates useful in immunoassays for quantitatively measuring concentrations of tacrolimus in patient specimens. Antibodies produced from the disclosed immunogens capable of binding to tacrolimus with cross-reactivity of no more than 5% with each of 15-O-demethyl tacrolimus, 31-O-demethyl tacrolimus, and 13,31-O-didemethyl tacrolimus, less than 40% with 13-O-demethyl tacrolimus, and less than 1% with cyclosporin, rapamycin, mycophenolic acid, prednisone, hydrocortisol, and prednisolone are described. Further, immunoassays for measuring the concentration of tacrolimus using such antibodies are taught.

The invention relates to a preparation method of a steroid compound, in particular to the preparation for prednisolone and the derivative thereof, which takes 17-hydroxyl-1, 4, 9-triene- pregna-3, 20-diketone as the initiator and is improved by 9, 11th and 21st to obtain the prednisolone and the derivative thereof, such as prednisolone acetic ester, isoflupredone, and the like. The invention further provides the application of a compound (I) in the preparation of a compound (II). As the production process adopts the existing intermediate of the company as the initiator, the line is concise, the material is easy to obtain, expensive auxiliary materials are saved, and the yield and the cost are obviously superior to the historical synthetic method of the prednisolone and the derivative thereof; in addition, the adoption of the existing intermediate realizes the doubling production of the triamcinolone products and the prednisolone products, thus greatly reducing the production cost and industrial conditions. R1 is equal to H, F, Cl and Br; R2 is equal to H, OH and OCOR3, wherein, R3 is equal to the alkyl with less than 11carbon atoms.

The invention discloses a preparation method of an adrenal cortex hormone medicament and particularly relates to a preparation method of a high-purity R-budesonide isomer. According to the method disclosed by the invention, prednisolone is used as an original raw material and the budesonide acetic ester is prepared by cyclization, ring opening, esterification, elimination, oxidation, cyclization and hydrolysis. The method disclosed by the invention has a simple process and high yield and is suitable for industrial production.

The invention discloses a veterinary suspension containing amoxicillin, colistin sulfate and prednisolone and a preparation method thereof. The veterinary suspension adopts the amoxicillin, the colistin sulfate and the prednisolone as active ingredients. The preparation method of the veterinary suspension containing the amoxicillin, the colistin sulfate and the prednisolone comprises the following steps of: (1) dissolving or dispersing a suspending agent, an antioxidant and a preservative in a hot dispersion medium to obtain a solution (A); (2) adding 40-80 percent of dispersion medium in a formula ratio in a colloid mill, starting the colloid mill, then slowly adding the solution (A) and adding a wetting agent while stirring after the solution (A) is fully added; (3) sequentially adding the amoxicillin, the colistin sulfate and the prednisolone after fully adding all the accessories, and grinding by adopting two alternate modes, i.e. an endless grinding mode and a non-endless grinding mode; and (4) detecting the grain fineness, stopping grinding when the grain fineness accords with the requirement, adding the dispersion medium to the formula ratio, mixing, canning, sealing and sterilizing to obtain the veterinary suspension containing the amoxicillin, the colistin sulfate and the prednisolone.

The invention discloses a preparation method of budesonide. The budesonide is prepared sequentially through the following steps of: carrying out an esterification reaction on a starting material and acetic anhydride, wherein the starting material is prednisolone; carrying out a degreasing reaction in the presence of a catalyst which can be alkali or an alkali metal salt ; carrying out an oxidizing reaction with potassium permanganate in acid environment; carrying out an ester exchange reaction with alcohol in alkaline environment; carrying out a condensation reaction with n-butanal, and the like. In the preparation method, appropriate catalysts are added in the reactions, and reaction conditions are appropriately controlled so as to achieve the purposes of increasing the reaction rates inall the steps and improving the yield of intermediate products, and the product quality conforms to the standard of the European Pharmacopoeia. Meanwhile, all the steps have moderate reaction condition and easy control, low energy consumption, high product yield, small pollution, easy reaction raw material obtaining and low production cost.

Methods and compositions for enhancing the activity and / or duration of action of soft anti-inflammatory steroids of the haloalkyl 17α-alkoxy-11β-hydroxyandrost-4-en-3-one-17β-carboxylate type and the corresponding Δ1,4 compounds and of anti-inflammatory steroids of the hydrocortisone and prednisolone type are described. The enhancing agents have the formula: wherein R is H or C1-C4 alkyl; Z1 is carbonyl or β-hydroxymethylene; X1 is —O— or —S—; R5 is —OH, —OR6, —OCOOR6 or —OCOR7 wherein R6 is C1-C4 alkyl and R7 is C1-C4 alkyl, fluoromethyl or chloromethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated; with the proviso that when R is C1-C4 alkyl, then R5 is —OH.

Pharmaceutical ophthalmic compositions are described, the compositions consisting essentially of a therapeutically effective quantity of an anti-bacterial agent (such as moxifloxacin), a therapeutically effective quantity of an anti-inflammatory agent (such as prednisolone), at least one pharmaceutically acceptable excipient and a pharmaceutically acceptable carrier. Methods for fabricating the compositions and using them are also described.

The invention discloses a perfusion medicament for treating milk cow mastitis and a preparation method thereof. The perfusion medicament is prepared from the following raw materials by weight: 0.9-4.3g of cefquinome sulphate, 0.15-0.25g of prednisolone, 0.5-1.3g of flunixin meglumine, 1-1.5g of glycerin monostearate, 3-8g of Vaseline, 0.05g of ethylparaben and 65-70g of whiteruss. The preparationmethod comprises the following specific steps of: (1) putting one tenth of the liquid paraffin into a burdening tank in a certain weight ratio; (2) adding one third of the liquid paraffin into a heating tank; and (3) putting the rest of the liquid paraffin left after the steps (1) and (2) and auxiliary materials in the step (2) into an emulsifying tank, adding 0.9-4.3g of cefquinome sulfate in a certain weight ratio, and stirring till uniform distribution to obtain the perfusion medicament for treating milk cow mastitis. The perfusion medicament has the advantages of no induction of endotoxemia in a milk cow mastitis treating process, remarkable curative effect on mastitis and freeness from medicament tolerance.

The invention provides a synthesis method of 16alpha-hydroxy prednisolone, belonging to the technical field of fine chemical synthesis method. The synthesis method comprises the following steps: using prednisolone with a structure as shown in formula (I) as a raw material, performing dehydration reaction to generate a double-bond compound under the action of gemini surfactant as shown in formula (II), then adding aqueous hydrogen peroxide solution for further reaction, and adding water to hydrolyze after finishing reaction so as to obtain the target product 16alpha-hydroxy prednisolone, wherein the gemini surfactant is diphenylmethane gemini surfactant. According to the synthesis method, gemini surfactant is simultaneously used as a reaction medium and a catalyst, and can be recovered and reused after reaction finishes, the process is simple, the after-treatment is convenient, the obtained products have the characteristics of high productivity, good efficiency, and less waste, the yield is greater than 85%, and the gemini surfactant can be recycled, and therefore the synthesis method is an economical, practical and environment-friendly technology and is suitable for popularization and application.

This invention relates to a method for preparing superfine prednisolone powder, and belongs to the field of micronization. Open question at present: particle diameter of prednisolone is small but can not obtain dry powder, or the dry powder has wide size distribution, bad redispersibility, and instability in water. The invention is to realize the preparation of prednisolone granule with controllable particle diameter, narrow particle size distribution, and superfine or nano-graded quadrilate and hexagon through inverse solvent recrystallization.the prednisolone of the invention has the advantages of controllable particle diameter, narrow particle size distribution, good redispersibility, stable micropowder, and good dissolving effect; and has prodigious dominance in the development of drug effect and new medicament form.

The invention discloses a method for preparing a sterides compound 17-alpha ester. The method comprises the following steps of: dissolving 17 alpha, 21-dihydroxyl sterides compound serving as a raw material in a cyclic ester solvent; adding an ester and a catalyst into the mixture and reacting the mixture to prepare a cyclic ester; and dissolving the prepared cyclic ester in a hydrolysis solvent, adding an orientation reagent and a hydrolysis reagent into the mixed solution and hydrolyzing the cyclic ester into the 17-alpha ester. The sterides compound is hydrocortisone, prednisolone, prednisone, hexadecadrol or betamethasone. The method has selective hydrolysis effect,, and can effectively enhance the conversion rate of a product, greatly increase product yield and greatly promote the preparation capability of a sterides medicament.

The invention discloses a method for preparing 6 beta-methylprednisolone. The method comprises the following steps: taking 6-methyl epoxides as raw materials, after Grignard reaction, hydrolysis, elimination, generating 6 beta-methyl elimination, and then after dehydrogenation by fermentation, iodine putting, replacement, hydrolysis, preparation of liquid phase purification, obtaining 6 beta-methylprednisolone. A reaction formula is as follows: the formula is shown in the description, the 6 beta-methylprednisolone of the invention is a major synthetic impurity in methylprednisolone, separation and purification of the 6 beta-methylprednisolone have great significance on impurity analysis.

The invention relates to a method for directly generating prednisolone through bio-fermentation in one step by using cortisone acetate as a raw material and Arthrobacter Simple ATCC 21032.

The invention relates to a preparation method of a steroid compound, in particular to the preparation of fluorometholone and the derivative thereof, which takes 6-methyl-17-hydroxyl-1, 4, 9-triene-pregna-3, 20-diketone as the initiator to design a brand new process line for synthesizing the fluorometholone and the derivative (III) thereof and further provides the application of a compound (I) in the preparation of the fluorometholone and the derivative (III) thereof. As the production process adopts the existing intermediate of the company as the initiator, the line is concise, the material is easy to obtain, expensive auxiliary materials are saved, and the yield and the cost are obviously superior to the historical synthetic method of the prednisolone and the derivative thereof; in addition, the adoption of the existing intermediate realizes the doubling production of the hexamethylprednisolone products and the fluorometholone products, thus greatly reducing the production cost and industrial conditions. Meanwhile, in the line for preparing a fluorometholone esterified ester, the disadvantages of easy esterification of 11th and too much side products are avoided. R1 is equal to the alkyl with less than 5 carbon atoms; R2 is equal to H, OH, the alkyl with less than 5 carbon atoms; R3 is equal to H, COR4, wherein, R4 is equal to the alkyl with less than 11 carbon atoms.

A gatifloxacin and prednisolone topical ophthalmic pharmaceutical compositions for prevention and treatment of ophthalmic bacterial infections and inflammatory conditions associated with pre-surgical and / or post surgical ocular surgeries.

The present invention provides cancer treatment preparations of excellent targetability. The sugar chain-modified liposomes of the present invention, which contain an aromatase inhibitor, anti-androgenic agent, lyase inhibitor, GnRH agonist, GnRH antagonist, anti-angiogenic agent, tyrosine kinase inhibitor, serine-threonine kinase inhibitor, antibody having an anticancer activity, ansamitocin, capecitabine, celmoleukin, docetaxel hydrate, gemcitabine hydrochloride, oxaliplatin, prednisolone, tegafur-uracil mixtures, zinostatin stimalamer or arsenic trioxide may be used as cancer treatment preparations having an excellent targetability.

Disclosed is a one-pot process for the preparation of a prednisolone derivative of formula I, comprising reacting the compound of formula II with the compound of formula III and the compound of formula IV The process does not need to separate and purify the intermediate formed, and therefore the process reduces the reaction time and increases the yield of the product compared to the prior art.

The invention relates to a preparation method of prednisolone. The preparation method comprises the steps of sequentially carrying out 3, 20-keto protective reaction, 11-keto reduction reaction, 21-hydroxyl esterification reaction, 3, 20-keto deprotection reaction and 21-acetic ester hydrolysis reaction by taking prednisone acetate as a raw material to obtain prednisolone. The invention provides a novel synthesis route sequentially comprising the steps of esterifying and deprotecting; nitrosification quenching reaction and resin hydrolysis reaction are omitted in the deprotection process; and ester hydrolysis reaction is finished under the protection of a mixed solvent and inert gases, so that the condition that byproducts are produced by hydrolysis reaction is avoided. The preparation method is novel in process route, simple and rapid in operation process, low in production cost and suitable for large-scale industrial production.

The invention discloses a pharmaceutical composition for the treatment of chronic obstructive pulmonary disease (COPD) and bronchial asthma, which is composed of a glucocorticoid, a bronchodilator and a pharmaceutically acceptable auxiliary material or carrier; the composition is a preparation for oral use. The glucocorticoid in the inventive pharmaceutical composition is selected from prednisone, prednisolone, methylprednisolone, betamethasone, decamethasone or hydrocortisone; the bronchodilator is selected from formoterol, clenbuterol, procaterol or theophylline. The inventive composition has better therapeutic effect on the COPD and the bronchial asthma than independent administration of two ingredients, and has synergistic effect. The composition has easily-available raw materials, inexpensive price and increased medicine taking compliance as well as plays a significant role in preventing and treating the COPD and the bronchial asthma of patients in vast rural areas and patients in low-income class of the city in China.

The invention provides an anti-cancer sustained-release agent co-carrying glucocorticoid and chemotherapeutic drugs and belongs to sustained-release injections. The anti-cancer sustained-release agent comprises sustained-release microspheres and a solvent, wherein, the sustained-release microspheres comprise anti-cancer active components and sustained-release auxiliary materials; and the solvent is a particular solvent containing a suspending agent. The glucocorticoid is selected from prednisolone, methylprednisolone, dexamethasone, betemethasone, triamcinolone acetonide or triamcinolone acetonide; the chemotherapeutic drugs are selected from phosphoinositide 3-kinase inhibitor, pyrimidine analogues and the like; the sustained-release auxiliary materials are biocompatible high-polymers, such as polylactic acid and the copolymers thereof, polyethylene glycol, carboxyl-terminated polylactic acid copolymers, polyfatty acid dimer-sebacic acid copolymers, poly(erucic acid dimer-sebacic acid), poly(fumaric-co-sebacic acid), polifeprosan and the like; and the suspending agent with the viscosity being 100cp to 3,000cp (at the temperature of 20 to 30 DEG C) is selected from sodium carboxymethyl cellulose and the like. The anti-cancer active components and the sustained-release microspheres can further be prepared into sustained-release implants which can effectively inhibit the growth of tumors, alleviate edema and improve the curative effects of radiotherapy and chemotherapy by intra-tumor or peri-tumor injection or placement.

This invention relates to a novel process of manufacture of nanoparticles of substantially water insoluble materials from emulsions. The emulsions have the ability to form a single liquid phase upon dilution of the external phase, instantly producing dispersible solid nanoparticles. The formed nanoparticles have average diameter of about 10 to 200 nm and are suitable for drug delivery and targeting of water insoluble therapeutic or diagnostic agents. Examples of such agents are methotrexate, progesterone, testosterone, prednisolone, and ibuprofen. Such agents can be used in a wide range of therapeutic and diagnostic treatments including treatment for cancer, hormonal therapy, and pain management.

The invention discloses a method for preparing prednisolone. The method comprises the steps as follows: a dihydroxyprogesterone dehydrogenated substance is adopted as a raw material, an alpha hydroxyl in the 11th position is firstly transformed into beta hydroxyl, then reactions including iodination, replacement and the like are performed, and prednisolone and a derivative of prednisolone are obtained; the equation is shown in the specification. According to the method, the dihydroxyprogesterone dehydrogenated substance is adopted as the raw material for the first time for preparing prednisolone and the derivative of prednisolone, the total yield is 80% or higher, the production cost is reduced, and the method is applicable to large-scale industrial production.

The invention discloses a methylprednisolone intermediate debrominated product and a preparation method thereof. According to the preparation method, a compound shown as a formula I is used as a raw material, and a dechlorination reaction, a bromination reaction, a debromination reaction and an oxidation reaction are sequentially performed to prepare a compound (debrominated substance) shown as aformula V. The preparation method has the advantages of short synthetic route, high yield, low cost and easily available raw materials, is suitable for industrial production, and has very high industrial value.

Methods and compositions for enhancing the activity and / or duration of action of soft anti-inflammatory steroids of the haloalkyl 17α-alkoxy-11β-hydroxyandrost-4-en-3-one-17β-carboxylate type and the corresponding Δ1,4 compounds and of anti-inflammatory steroids of the hydrocortisone and prednisolone type are described. The enhancing agents have the formula:wherein R is H or C1-C4 alkyl; Z1 is carbonyl or β-hydroxymethylene; X1 is —O— or —S—; R5 is —OH, —OR6, —OCOOR6 or —OCOR7 wherein R6 is C1-C4 alkyl and R7 is C1-C4 alkyl, fluoromethyl or chloromethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated; with the proviso that when R is C1-C4 alkyl, then R5 is —OH.

The present invention provides a method for treating a mammal with immunological disorders, particularly autoimmune disease, and most preferably systemic lupus erythematosus (SLE). The method includes oral administration of germination activated Ganoderma lucidum spores (“GLSs”) to the mammal. Additionally, a corticosteroid, such as prednisolone, can be co-administered with the GLSs to the mammal to achieve synergistic effect of treatment.

The invention relates to the field of medicinal chemistry, in particular to a preparation method of new R budesonide, which is characterized in that a budesonide product is synthesized by carrying out microwave catalytic reaction on the 16-alpha hydroxyl prednisolone and n-butanal in the presence of a mixed catalyst, wherein the content of the R budesonide is more than 95 percent.