36 results about "Voglibose" patented technology

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 voglibose tablet and a preparation method thereof. The voglibose tablet is prepared from 1 part by weight of voglibose, 450-550 parts by weight of lactose, 130-170 parts by weight of starch, 20-30 parts by weight of high substituted hydroxypropyl fibers, 3-4 parts by weight of magnesium stearate, 0.1-0.5 parts by weight of propolis, 5-10 parts by weight of sodium lauryl sulfate, 4-6 parts by weight of polysorbate 80, 30-40 parts by weight of a co-solvent and 40-50 parts by weight of a disintegrant. The voglibose is used as the main drug, and high-substituted hydroxypropyl fiber, propolis, polysorbate 80 synergistic voglibose, lactose, starch, magnesium stearate and sodium lauryl sulfate are used in a good ratio so that the tablet dissolution degree is greatly improved, the disintegration time limit is optimized and the drug efficacy is improved. The voglibose tablet has a good dissolution degree and good disintegration effects, can well exert the efficacy of the voglibose tablet and can improve the drug efficiency. Through combination of the initial mixing process and low / high-speed agitation, the tablet dissolution degree is further improved and the quality of the tablet is improved.

The invention discloses a preparation method of voglibose capsules, belonging to the field of pharmaceutical preparations, comprising five steps of preparation of original medicinal liquid, film drying, micronization, freeze drying and capsule filling. The invention prepares voglibose capsules with high dissolution rate and good uniformity of voglibose content, and the dissolution rates in 5 minutes, 15 minutes and 30 minutes are respectively 53.8-55.9%, 93.6-96.7% and 99.9%. ~100%, the voglibose content uniformity is 0.35~0.43; the present invention inhibits voglibose by adding polyvinylpyrrolidone and micropowder silica gel to the voglibose aqueous solution and cooperating with the rapid evaporation operation of coating film drying. The crystallization phenomenon during the precipitation process of boose yields voglibose in an amorphous powder state, so that the final capsule preparation has excellent dissolution and content uniformity.

The invention discloses a voglibose film and a preparation method thereof. The voglibose film comprises the following components by weight percent: 0.2-15% of voglibose, 40-99.8% of high molecular filming material, 0-20% of plasticizer, 0-5% of titanium pigment and 0-20% of flavouring agent, wherein the molecular weight of the high molecular filming material is 20000-300000. The invention is the voglibose film prepared by a solid dispersion technology, the medicine is highly dispersed in a carrier material and is encircled by the sufficient molecules of the carrier material, the high dispersivity of the medicine is ensured, the dissolving out of the medicine is quickened, the medicine enters the digestive tract along with saliva quickly, and the medicine effect is exerted.

The invention discloses a method for determining related substances in voglibose raw materials and preparations. The present invention utilizes 1-phenyl-3-methyl-5-pyrazolone to carry out pre-column derivatization of voglibose and its related substances, and adopts high-performance liquid chromatography to measure voglibose in raw materials and preparations related substances. The invention can separate the related substances of voglibose, and effectively control the quality of voglibose raw materials and preparations. The determination method of the invention has strong specificity, high accuracy, high precision, good durability, and convenient operation, and can effectively control the quality of raw materials and preparations in actual production.

For controlling the condition of type 2 diabetes, a pharmaceutical including a combination of mitiglinide, a pharmacologically acceptable salt thereof or a hydrate thereof and an α-glucosidase inhibitor such as voglibose or acarbose, and a therapeutic method using the pharmaceutical are provided. The pharmaceutical according to the present invention has an extremely strong effect of decreasing a morning fasting blood glucose level, a postprandial blood glucose level and HbA1C of a patient with type 2 diabetes, and can improve glucose spike, insulin resistance and lipid metabolism.

The invention discloses a biological preparation method of valienamine. The preparation method comprises a step of biologically converting valienone into valienamine by using amino transferase (WecE), or integrating WecE gene into bacterial strains that can generate the precursor compounds of valienone so that the bacterial strains integrated with WecE gene can directly produce valienamine through fermentation. The conventional chemical synthesis method has the disadvantages such as many reaction steps, low yield, strict reaction conditions, organic reagent pollution, and the like, and the provided biological preparation method overcomes the abovementioned problems. The biological preparation method is based on amino transferase catalyzed amino transferring reactions, the direct biological synthesis is convenient and high efficient, the stereo-selectivity is high, and the valienamine can be used as a synthetic intermediate for synthesis of voglibose for treating II type diabetes, synthesis of acarbose, and development of glycosidase inhibitors.

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 present invention provides a kind of preparation method of voglibose impurity I hydrochloride, comprising the steps of: (S)-(oxirane methyl) carbamate tert-butyl ester and tetrabenzyl Jinggang mycosamine Amination of epoxide to obtain the compound of formula III; the hydroxyl group of the compound of formula III is protected by benzyl group to obtain the compound of formula IV; the amino protecting group of the compound of formula IV is deprotected to obtain the compound of formula V; 5S)-5-hydroxyl-2,3,4-tris(benzyloxy)-5-[(benzyloxy)methyl]-cyclohexanone undergoes a condensation reduction reaction to obtain a compound of formula VI. The preparation method of voglibose impurity I hydrochloride provided by the present invention has a simple process flow and fills up the gap in the current technology for preparing voglibose impurity I. The prepared voglibose impurity I hydrochloride The salt can be used for qualitative and quantitative research on impurities in the production of voglibose, which can improve the quality standard of voglibose, thereby improving the drug safety of voglibose.