112 results about "Repaglinide" patented technology

The invention discloses an oral solid drug composition containing metformin hydrochloride repaglinide, which contains pharmaceutically acceptable carriers. The preparation process is simple, the problem of chipping is effectively solved, and simultaneously, the repaglinide has good content uniformity and dissolution; and the oral solid drug composition is used for treating type II diabetes.

This invention discloses a process for synthesizing repaglinide by using 4-carboxymethyl-3-ethoxybenzoate as raw material to produce acyl chloride. Compared to other process, this invention is characterized of high efficiency, low toxicity, easy obtained and cheap raw material, simple operation, and high yield with 80.9% total yield rate in two-step reaction, which makes it a good repaglinide systhesis process with good industrialization future.

The invention relates to a pharmaceutical combination with repaglinide and metformin as active components and a preparation method thereof. The pharmaceutical combination comprises 0.1-10 weight portions of repaglinide and 100-1500 weight portions of metformin as active components and pharmaceutic adjuvants, wherein, the pharmaceutic adjuvants comprise filler, disintegrating agent, adhesive, flavoring agent, lubricant and swelling accessory, and the repaglinide is repaglinide crystal. The invention adopts the repaglinide crystal with small particle size, metformin and pharmaceutic adjuvants to prepare the pharmaceutical combination, so as to realize the purpose of simultaneous release. Since the particle size of the repaglinide used in the invention is small, the dissolvability is improved, so that the dissolution is improved and the bioavailability is increased.

The Present invention relates to a process for the preparation of (RS) 3-methyl-1-(2-piperidinyl phenyl) butyl amine of formula 1. (RS) 3-Methyl-1-(2-piperidinyl phenyl butyl amine having formula 1 is an important key intermediate for the synthesis of repaglinide of formula 2 an oral hypoglycemic agent.

The invention relates to an oral troche which contains repaglinide or pharmaceutically acceptable derivatives of repaglinide as well as a preparation method of the oral troche. According to the preparation method, powder of repaglinide or pharmaceutically acceptable derivatives of repaglinide is directly pressed into troche, so that the production cost is remarkably lowered, and the disintegration and the dissolution rate are greatly improved. The bioavailability and the stability of the medicine can be improved, and the problem of low content uniformity of existing small-dose medicines formed by the direct pressing method is overcome, so that the quality of the troche is better guaranteed.

The invention relates to a preparation method of a drug for treating diabetes mellitus, that is, repaglinide. The preparation method comprises the following steps: a (S) type compound as shown in formula (II) and a compound as shown in formula (III) are subject to an amidation reaction in the presence of a condensing agent to generate a (S) type compound as shown in formula (IV); R2 radical is removed from the (S) type compound of the formula (IV) in the presence of alkali, and R1 radical is removed in the presence of acid. The (S) type compounds as shown in the formula (II), the formula (III) and the formula (IV), and the R1 radical and the R2 radical are defined in the specification. In the preparation method, the introduction of the R1 radical and deprotection improvement shorten the reaction time, increase the yield and enhance safety, thus the method is more suitable for industrialized production.

This invention relates to a method for preparing repaglinide. Compared with other methods, the method has such advantages as high efficiency, low toxicity, high safety, easy operation, wide raw materials, and low cost, thus is suitable for industrialization.

The invention relates to the field of medicine medicinal preparation, in particular to a stable method for preparing repaglinide compressed tablets, which is characterized in that the pelletizing process includes the following steps: adding repaglinide into adhesive solution and making the pellets with fillers through a fluidized bed in ejecting mode. Particles of the repaglinide tablets can rapidly disperse when the epaglinide tablets disintegrate, and active ingredient repaglinide evenly dispersed in the particles can rapidly dissolve out. The prepared repaglinide particles can be evenly mixed with auxiliary materials such as disintegrating agents, lubricating agents and the like and pressed into tablets. Tablet cores can completely disintegrate within two minutes.

The present invention relates to a cost effective and industrially advantageous process for the preparation of repaglinide.

The invention relates to a preparation method of a medicinal preparation of repaglinide. The preparation method comprises the following steps: (a) dissolving meglumine and repaglinide in alcohol and water to prepare an adhesive solution; (b) mixing pharmaceutically acceptable adjuvant materials to prepare a mixture; (c) adding the adhesive solution to the mixture obtained in the step b, and performing wet granulation; and (d) preparing the medicinal preparation. The invention further relates to application of meglumine as a repaglinide stabilizer in the medicinal preparation containing repaglinide.

The invention belongs to the field of pharmaceutical compositions for treating non-insulin dependent diabetes mellitus (NIDDM), and in particular relates to a novel pharmaceutical composition for repaglinide and dimethyldiguanide tablets and a preparation method thereof. The pharmaceutical composition is equivalent to PrandiMet in dissolving-out characteristic on the basis that good content uniformity of repaglinide is ensured, and related substances are superior to the existing products. The preparation method is suitable for industrialized production.

The invention relates to a preparation and refining method of repaglinide. The preparation method comprises the steps that: (S)-3-Methyl-1-(2-piperidinophenyl)butylamine glutamate (II) is adopted as a raw material, and is subjected to hydrolysis and an acylation reaction; an obtained material is subjected to an amidation reaction with 4-ethoxycabonyl-3-ethoxyphenylacetic acid (IV) under the existence of a condensing agent, such that 4-ethoxycabonyl-3-ethoxyphenylacetic ester (V) is obtained; the material V is hydrolyzed under an alkaline condition, such that a repaglinide crude product is obtained; the repaglinide crude product is subjected to ethanol-water solvent crystallization, such that repaglinide (I) is obtained. According to the invention, (S)-3-Methyl-1-(2-piperidinophenyl)butylamine glutamate is adopted as an initial raw material; the reaction conditions are optimized; the yield is improved; and good safety is ensured. An ethanol-water refining method is adopted, such that the product quality is improved, and environment pollution is reduced. Therefore, the method is suitable for industrialized productions.

The invention discloses a qualitative analysis detection method for illegally mixed high-polar chemical anti-diabetic components in anti-diabetic traditional Chinese medicine products. The method comprises the following steps that: 1) high efficient liquid phase chromatography conditions: an ammonium acetate-triethylamine-acetonitrile moving phase system and a C18 chromatographic column with certain specification are used, the wavelength is detected by ultraviolet, and the flow rate is 1.0ml/min; 2) analysis result: glibenclamide, glipizide, gliclazide, glimepiride, gliquidone, repaglinide, nateglinide, rosiglitazone and pioglitazone hydrochloride can realize the complete separation; 3) result judgment: when retention time of a chromatographic peak in an anti-diabetic traditional Chinese medicine product is consistent with that of anti-diabetic medicine in the step 2) and the apparent absorption is shown out, which indicate that the anti-diabetic medicine is contained in the sample to be tested. The method has the advantages of quickness, simplicity, convenience, high sensitivity, strong specialization, broad coverage and so on.

The invention relates to a method for synthesizing a repaglinide key intermediate, namely 4-ethoxycarbonyl-3-ethyoxy phenylacetic acid. The method comprises the following steps: by taking 3-ethyoxy-4-ethoxycarbonyl-benzyl cyanide as an initial raw material, performing hydrolysis, esterification, selective hydrolysis and the like, thereby obtaining the important intermediate 4-ethoxycarbonyl-3-ethyoxy phenylacetic acid of repaglinide. According to the key intermediate, the impurities of the product is less, the purity of the product is high and can reach over 99.7%, so that the quality of the subsequently synthesized repaglinide product is improved, the 100 percent first-pass yield of the subsequently synthesized repaglinide product can be basically reached, a refining step is avoided, and the synthetic yield is effectively improved. The process is easy and convenient to operate, the yield is high, the molar yield is 69.1 percent, the production cost is low, and the method is suitable for industrial production.

The present invention relates to intranasally deliverable compositions comprising a hypoglycemic agent, for example, repaglinide, and to methods of using such compositions in the treatment of various disorders, including, for example, type-2 diabetes.

The invention relates to a one-pot method for synthesizing repaglinide. In the method, commercial (S)-3-methyl-1[2-(1-piperidyl) phenyl] butyl amine L-N-acetylglutamate and 4-ethoxycarbonyl-3-ethoxy phenylacetic acid are used as raw materials to prepare repaglinide, thereby greatly shortening the reaction route and facilitating the production stability and continuity; and in esterification reaction, an acylating agent/acid-binding agent replaces triphenyl phosphorus/carbon tetrachloride to perform reaction, the intermediate does not needed to be crystallized, direct hydrolysis is performed according to the one-pot method, the intermediate meeting the requirements is obtained by a crude product recrystallization method, the column chromatographic separation is not needed, waste liquid is easy to treat, the yield is greatly improved, and the industrial production is facilitated.

The invention discloses a preparation of repaglinide chitosan sustained and controlled release microspheres and a preparation method thereof. The core-shell microsphere preparation is formed in the capsule material formed by condensation and cross-linking of polysaccharides. The preparation has slow and controlled release of drugs, and significantly improves the stability of repaglinide. The capsule material prepared by natural cross-linking agent and chitosan has good biocompatibility without any cytotoxicity, and can promote the absorption of drugs , improve the bioavailability of the drug. The invention is used for preparing repaglinide chitosan sustained and controlled release microspheres, and the medicine in dosage form is mainly used for preventing and treating type Ⅱ diabetes mellitus with high blood sugar.

The invention relates to a repaglinide tablet and a preparation method thereof. According to the preparation method, a wet granulation process is used, calcium hydrophosphate, microcrystalline cellulose and pregelatinized starch are used as filling agents, and meglumine, poloxamer and povidone are matched to prepare a binder to carry out wet granulation, so that the prepared repaglinide tablet is uniform in content and favorable to release; compared with the prior art, the wet granulation process is capable of solving the problems of non-uniform content and low dissolution rate in the preparation process; and meanwhile, the dissolution rate and the stability of the prepared preparation are consistent with those of the original contrast drug so that the drug quality is ensured.