33 results about "Nateglinide" patented technology

Provided is a process for preparation of an intermediate in the synthesis of nateglinide. Trans-4-isopropylcyclohexane acid chloride is formed by reacting 4-isopropylcyclohexanecarboxyl acid with thionyl chloride in the presence of an effective amount of an organic amide.

Also provided are processes for preparation of nateglinide by acylation of a suitable salt of D-phenylalanine with trans-4-isopropylcyclohexane acid chloride in both a single and a two phase system, and in water free of a co-solvent.

Provided are crystalline forms of nateglinide, labeled Forms A, C, D, F, G, I, J, K, L, M, N, O, P, Q, T, U, V, Y, α, β, γ, δ, ε, σ, θ and Ω, processes for their preparation and processes for preparation of other crystalline forms of nateglinide. Also provided are their pharmaceutical formulations and methods of administration.

Provided are crystalline forms of nateglinide, labeled forms A, C, D, F, G, I, J, K, L, M, N, O, P, Q, T, U, V, Y, alpha, beta, gamma, delta, epsilon, sigma, theta and omega, processes for their preparation and processes for preparation of other crystalline forms of nateglinide. Also provided are their pharmaceutical formulations and methods of administration.

Provides are crystalline forms of nateglinide, labeled Forms A, C, D, F, G, I, J, K, L, M, N, 0, P, Q, T, U, V, Y, α, β, γ, δ, ε, σ, θ and Ω, processes for their preparation and processes for preparation of other crystalline forms of nateglinide. Also provided are their pharmaceutical formulations and methods of administration.

The invention relates to Nateglinide tablets and a preparation method thereof; in Nateglinide, 30-60% of filler is 3-15% of starch and 10-30% of microcrystalline cellulose, bonding agent is 1-10% of low substituted hydroxypropyl methylcellulose, disintegrant is 15-50% of sodium carboxymethyl starch, fluidizer is 0.1-5% of silica, and lubricant is 0.1-1% of magnesium stearate; the preparation method comprises the following steps: sieving raw materials for standby use; weighing Nateglinide with prescription amount, adding appropriate purified water, blending to prepare soft material, pelletizing and drying to prepare granules of main drug; evenly mixing microcrystalline cellulose, starch and part of sodium carboxymethyl starch, adding substituted hydroxypropyl methylcellulose by equivalently progressive method, evenly mixing to prepare soft material, pelletizing and drying; mixing granules of main drug with granules of accessories, adding residual sodium carboxymethyl starch, magnesium stearate and silica to be evenly mixed, pelletizing and tabletting. The invention has the characteristics of few components, available accessories, capability of fully disintegration in 3 minutes, above 95% of dissolution rate and suitability for long term storage.

There is provided methods for producing nateglinide crystals, which comprises the steps of adding an acid(s) to a reaction mixture containing nateglinide to make it acidic, the reaction mixture being obtained by reacting trans-4-isopropylcyclohexylcarbonyl chloride with D-phenylalanine in a mixed solvent of ketone solvent and water in the presence of an alkali; and then adjusting the temperature of the mixture to 58° C. to 72° C. and the concentration of ketone solvent to more than 8 wt % and less than 22 wt % to conduct precipitation of nateglinide crystals. This producing method is the industrially beneficial methods for crystallization of nateglinide.

Provided are crystalline forms of nateglinide and processes for their preparation.

Provides are crystalline forms of nateglinide, labeled Forms A, C, D, F, G, I, J, K, L, M, N, O, P, Q, T, U, V, Y, α, β, γ, δ, ε, σ, θ and Ω, processes for their preparation and processes for preparation of other crystalline forms of nateglinide. Also provided are their pharmaceutical formulations and methods of administration.

Provides are crystalline forms of nateglinide, labeled Forms A, C, D, F, G, I, J, K, L, M, N, O, P, Q, T, U, V, Y, α, β, γ, δ, ε, σ, θ and Ω, processes for their preparation and processes for preparation of other crystalline forms of nateglinide. Also provided are their pharmaceutical formulations and methods of administration.

The invention relates to a synthesis method of a nateglinide, in particular to the synthesis of the nateglinide by a one-pot method. Original material D-phenylalanine is used as raw material in the method, D-phenylalanine esterified substance (II) is obtained through esterification, a compound (IV) is obtained through acylation of isopropylcyclohexanecarboxylic acid (III), and then the compound (IV) is ester hydrolyzed so as to obtain the nateglinide. The technique of the method has simple technique process and easy and convenient post-treatment; meanwhile, the method has the advantages of strong operability, being easy to be industrialized and cost saving.

The invention discloses a dapagliflozin solid-form compound as well as a preparation method and application thereof. The compound is in a solid form formed by dapagliflozin, nateglinide, candesartan cilexetil, anagliptin or enalapril. The invention also comprises a preparation method and application of the dapagliflozin solid compound. According to the dapagliflozin solid compound, the two components are combined in a hydrogen bond or other non-covalent bond mode on the basis that original molecular covalent bonds are not damaged, a new eutectic or amorphous substance is formed, the two active components exist in a specific stoichiometric ratio, no organic solvent is contained, and the preparation method is simple. And good biocompatibility is achieved. Different from a mixture obtained by simply and physically mixing the two active ingredients, the compound provided by the invention can effectively improve various physicochemical properties of the medicine, improve the stability, solubility and bioavailability of the medicine and effectively improve the hygroscopicity of the medicine.

The present invention discloses, as a immediate-release preparation useful as an antidiabetic, a nateglinide-containing preparation comprising nateglinide as an active ingredient wherein the nateglinide is amorphous.

The invention discloses a nateglinide tablet and a method for preparing the nateglinide tablet through a direct compression method, wherein each one thousand of nateglinide tablets are prepared from 30g of nateglinide, 45g of diluent, 35g of disintegrating agent, 1g of lubricating agent and 3g of flow aid, the preparation method for preparing the nateglinide tablet through direct compression by using a compressible auxiliary material comprises a process of weighing and matching, screening, mixing, tabletting, inner packing and packing under the D level condition, the nateglinide tablet and the method, provided by the invention solve the problems of cracking tablet, rough tablet, sticking and the like of a nateglinide tablet prepared through a traditional wet method.

The invention relates to a compound nateglinide valsatan medicinal composition, which is a dual-layer tablet and comprises a first layer of nateglinide and a second layer of valsatan, wherein the first layer is delivered from a self-soluble tablet to be immediately released; and the second layer is released from a self-disintegration or corroded tablet matrix.

The invention discloses an additive for improving plastic plasticity, which comprises the following components according to the ratio of parts by weight: 20-40 parts of potassium sulfate solution, and 12-20 parts of modified glycerin epoxy resin , 0.3-0.7 parts of sodium carbonate, 0.01-0.03 parts of ammonium chloride, 0.01-0.02 parts of methyl formate, 0.1-0.4 parts of regulator, 0.02-0.03 parts of nateglinide and 1-3 parts of potassium dihydrogen phosphate. The additive for improving the plasticity of the present invention can effectively improve the plasticity of the plastic, increase its transverse and longitudinal tensile stress, so that the plastic has a better plasticizing effect; further, the raw materials of the present invention are easy to obtain, and the preparation method is simple and easy. operate.