35 results about "Voglibose" patented technology

The present invention relates to the use of a combination of a certain DPP-4 inhibitor and an alpha-glucosidase inhibitor for use in therapy, e.g. for use in treating and/or preventing a metabolic disease such as type 2 diabetes mellitus and/or conditions related thereto. The invention also relates to the use of such combination for improving body weight control, reducing body weight, inducing satiety, inhibiting gastric emptying and/or reducing food intake, in a patient in need thereof.

The invention relates to a voglibose dispersible tablet and capsule and a preparation method thereof. The voglibose dispersible tablet comprises: 0.01-5 percent of voglibose, 1-99 percent of disintegrating agent, 0-98 percent of diluting agent; 0.5-20 percent of lubricant and fluidizer, 0.1-20 percent of bonding agent; wherein, the disintegrating agent is one or more selected from starch, modified starch, cellulose, microcrystalline cellulose, cross-linked polyvinyl pyrrolidone, sodium carboxymethyl starch, cross-linked sodium carboxymethyl cellulose, low-substituted hydroxypropyl cellulose, alginic acid and colloid magnesium aluminum silicate; the diluting agent is one or more selected from lactose, mannitol, sorbitol, sucrose, calcium sulfate, kaolin, dextrine and sodium chloride. The capsule preparation does not contain the bonding agent. The invention has the advantages that the voglibose dispersible tablet disintegrates swiftly and disperses evenly, the voglibose dispersible tablet can be disintegrated swiftly into fine particles and scattered evenly after being taken orally, which is beneficial for the dissolution and the absorption of the voglibose dispersible tablet with the short onset time. Disintegrated swiftly in three minutes; after being taken orally, the capsule shell quickly swells and splits, which conceals the discomfort caused by the capsule taken in mouth.

The invention relates to a pharmaceutical composition having alpha-glucosidase inhibition activity, wherein the pharmaceutical composition comprises a flavone compound and an alpha-glucosidase inhibitor, the flavone compound is at least one selected from a monomer such as baicalein, quercetin, luteolin, baicalein-7-O-glucoside and catechin, an organic salt of the monomer, and an inorganic salt of the monomer, and the alpha-glucosidase inhibitor is at least one selected from a monomer such as acarbose, voglibose and miglitol, an organic salt of the monomer, and an inorganic salt of the monomer. According to the present invention, the pharmaceutical composition can effectively reduce postprandial blood glucose, can inhibit the activity of alpha-glucosidase adopting starch, maltose and sucrose as substrates, and less uses the alpha-glucosidase inhibitor, such that the efficacy can be improved, the side effect of the alpha-glucosidase inhibitor can be effectively reduced, and hypoglycemia and other problems easily caused by drug combination are effectively solved.

The present invention relates to crystallized (1S)-(1(hydroxy), 2, 4, 5/1, 3)-2, 3, 4-tri-oxo-benzyl-5-[(2-hydroxy-1-(hydroxymethyl) ethyl) amino]-1-carbo-methylbenzylmethyl-1, 2, 3, 4-cyclohexane tetrol, which has smelting point of 89.7 deg.c; monocrystalline X ray diffraction data of orthorhombic system, P2(1)2(1)2(1) space groupp, unit cell parameters a=7.8487, b=20.746, c=20.988 and R 0.0748; and X ray diffraction peak of crystal powder of 16.76, 18.90 and 24.00+/-0.15 deg. It is prepared through dissolving oily tetrabenzyl voglibose in one kind of polar non-protonic solvent, adding one other kind of non-polar solvent via stirring at room temperature to crystallize, stilling, filtering and vacuum drying to obtain the crystal. Compared with oily tetrabenzyl voglibose, the crystallized tetrabenzyl voglibose has higher purity, convenient transportation and maintenance and easy application.

The invention provides a method for preparing voglibose particles. The particles are prepared through a one-step prilling process,the friability is low,and the roundness is good. Voglibose can be dissolved out fast,the content uniformity is good,and the voglibose particles are suitable for being further prepared into capsules,tables (including dispersible tablets and orally disintegrating tablets)and granules. According to the preparation idea,the voglibose is added into a polar solvent containing a water-soluble adhesive,and the mixture is sprayed into a one-step pelletizer containing a diluent and a disintegrating agent in a top spraying prilling mode. The preparation method is easy to operate,the labor intensity is reduced,and the preparation method is suitable for large-scale production.

The invention relates to processes for the preparation of pure voglibose. The invention also relates to the preparation of acid addition salts of voglibose. More particularly, it relates to the preparation of crystalline hydrochloride salt of voglibose. The invention also relates to pharmaceutical compositions that include the pure voglibose or voglibose hydrochloride and use of said compositions for treatment or prevention of hyperglycemic symptoms and various disorders caused by hyperglycemia such as diabetes, obesity, and hyperlipemia.

The invention provides a pharmaceutical composition for improving complications of high-fat and high-sugar diet. The pharmaceutical composition comprises flavonoid and an alpha-glucosidase inhibitor, wherein the flavonoid is at least one selected from the group consisting of monomer baicalein, monomer chrysin, organic salts of the monomers and inorganic salts of the monomers, and the alpha-glucosidase inhibitor is one selected from the group consisting of monomer acarbose, monomer voglibose, monomer migltol, organic salts of the monomers and inorganic salts of the monomers. The composition provided by the invention can effectively reduce the dosage of the alpha-glucosidase inhibitor; desired effects can be obtained by mixing the flavonoid with the alpha-glucosidase inhibitor with a dosage 0.01 to 0.75 time of a normal dosage; the disadvantages of a great dosage and great side-effects in individual usage of the alpha-glucosidase inhibitor are overcome; the disadvantages of unobvious hypoglycemic effect, a great dosage, a long administration period and the like in individual usage of the flavonoid are overcome; and the disadvantages of complex components and difficult quality control of a traditional Chinese medicine compound drug are overcome.

The invention provides a synthesis method of voglibose, and solves the technical problems that in an existing synthesis method of voglibose, raw materials are difficult to obtain, high in price, large in investment, low in yield and not suitable for industrial production. The synthesis method comprises the steps: synthesizing a compound V by taking glucose monohydrate and sodium acetate as raw materials through eleven reaction steps; and preparing a compound VIII from the compound V through an addition reaction, a ring-opening reaction and an aldol condensation reaction, and thus obtaining voglibose through amination reduction of the compound VIII. The synthesis method of voglibose can be widely applied to the technical field of voglibose synthesis methods.

The present invention discloses a glipizide/voglibose hypoglycemic oral preparation composition and a preparation method thereof, and the glipizide/voglibose hypoglycemic oral preparation composition comprises the following raw materials: 2-6% by weight of main components, 50-90% by weight of a filler, 5-15% by weight of a disintegrant, 0.1-3% by weight of a binder, 0.01-5% by weight of a lubricant. The main components comprise 2.5mg-5mg of glipizide and 0.1mg-0.3mg of voglibose, and auxiliary materials comprises the filler, the disintegrant, the binder and the lubricant. The glipizide/voglibose hypoglycemic oral preparation composition has the advantages of complementary main material action mechanism, multi targets, good patient compliance, and the like, and is more applicable to type 2 diabetes patients of which blood-glucose rises after meals and fasting blood-glucose rises insignificantly.

The invention discloses a preparing method for tetra-benzyl-voglibose, namely, (1S)-(1(hydroxyl),2,45/1,3)-2,3,4-trioxyl-benzyl-5-[(2-hydroxyl-1-(hydroxymethyl)ethyl)amino]-1-carbon-benzyloxy methyl-1,2,3,4-cyclohexane tetraol or benzene sulfonate thereof. The method comprises the steps that (2R, 3S, 4S, 5S)-5-hydroxyl-2,3,4-tri(benzyloxy)-5-[(benzyloxy)methyl]-cyclohexanone reacts with serinol in protonic solvent under organic acid catalysis to be prepared into an intermediate amine compound, and the intermediate amine compound is reduced to be tetra-benzyl-voglibose. The method has the advantages that reaction reagent is low in price, safety is good, solvent toxicity is low, reaction time is short, aftertreatment is simple, the product yield is large, purity is high, and the method is suitable for industrial production.

The invention discloses a voglibose tablet capable of being quickly dissolved out and a preparation method of the voglibose tablet, and belongs to the technical field of pharmaceutical preparations. According to the voglibose tablet, firstly, a solid dispersion of voglibose and a carrier material is prepared by adopting a solvent method and a spray drying technology, and then the solid dispersion is uniformly mixed with a filling agent, a disintegrating agent and a lubricating agent and is directly tableted. According to the voglibose tablet prepared by the method, the dissolution rate and the content uniformity are improved, meanwhile, the quality is stable and controllable, and the voglibose tablet is suitable for industrial large-scale production.

The invention belongs to the field of medicines, and particularly relates to a medicine composition for treating or preventing adiposis and metabolic syndrome and application thereof. Active ingredients of the medicine composition are orlistat and voglibose, wherein the mass ratio of the orlistat to the voglibose is (10 to 30) to 0.1. According to the medicine composition, the metabolism and endocrine system drug voglibose is creatively combined with the conventional antiobesity drug orlistat for use, and the purposes of remarkably reducing postprandial blood sugar and enabling the postprandial blood sugar to be stable can be realized by greatly reducing the dosage of the single drugs, so that the pressure of islet cells is lowered, and the probability of diabetic complication of an adiposis patient is retarded or prevented. When the composition is used for treating or preventing the adiposis and the metabolic syndrome, not only obvious advantage is shown on the treating and preventing of the adiposis, but also effective control is performed on the indexes of blood fat, blood glucose and the like, and the positive treating and preventing effects are realized on the metabolic syndrome.

A preparation method of voglibose capsules belongs to the field of pharmaceutical preparations and comprises five steps of preparation of original liquid medicine, coating drying, micronization, freeze drying and capsule filling. The voglibose capsule with high dissolution rate and good voglibose content uniformity is prepared, the dissolution rates in 5 minutes, 15 minutes and 30 minutes are respectively 53.8 to 55.9 percent, 93.6 to 96.7 percent and 99.9 to 100 percent, and the voglibose content uniformity is 0.35 to 0.43; according to the voglibose capsule preparation and the preparation method thereof, the polyvinylpyrrolidone and the superfine silica powder are added into the voglibose aqueous solution, and the rapid evaporation operation of coating drying is matched, so that the crystallization phenomenon in the voglibose precipitation process is inhibited, the voglibose in an amorphous powder state is obtained, and the final capsule preparation has excellent dissolution rate and content uniformity.