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Saxagliptin medicinal composition and preparation method thereof

A composition and drug technology, which is applied in the direction of drug combination, non-active ingredients of polymer compounds, sugar-coated pills, etc., can solve problems such as the stability of saxagliptin preparations, hygroscopic weight gain of crystalline forms, and high impurity content, and achieve improvement. The effect of in vitro dissolution, simple operation and mature process

Inactive Publication Date: 2015-05-27
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Saxagliptin has great advantages in terms of effectiveness and safety, but in the actual production process, the applicant found that there are difficulties in purification, high impurity content, crystal forms protected by patents and There are certain problems such as moisture absorption and weight gain
In order to solve the above problems, the inventor has surprisingly discovered a new pharmaceutical composition of saxagliptin through a large number of long-term experiments, and the composition is prepared, stored, and its lactone is degraded under high humidity conditions. Products, oxidative degradation products, and photodegradation products are no longer increased, which can ensure the stability of long-term storage, thus solving the problem that has been plagued by the stability of saxagliptin preparations

Method used

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  • Saxagliptin medicinal composition and preparation method thereof
  • Saxagliptin medicinal composition and preparation method thereof
  • Saxagliptin medicinal composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0105] Embodiment 1 (comparative embodiment)

[0106] Saxagliptin 15-25g

[0107] Croscarmellose Sodium 40-80g

[0108] Microcrystalline cellulose 150-250g

[0109] Lactose 180-360g

[0110] Pregelatinized starch 15-30g

[0111] Talc powder 1-2g

[0112] Appropriate amount of 5% povidone absolute ethanol solution

[0113] Coating powder 100-200g

[0114] Makes 1000 pieces

[0115] The preparation method goes through the following steps:

[0116] 1) Sieve saxagliptin, microcrystalline cellulose, lactose, croscarmellose sodium, pregelatinized starch, and talcum powder separately, and set aside;

[0117] 2) Mix the raw and auxiliary materials evenly and set aside;

[0118] 3) Take 5% povidone anhydrous ethanol solution in 2), mix well, make 50-60 mesh granules, dry below 50°C, granulate, add lubricant, mix evenly, and compress into tablets;

[0119] 4) Put the sample prepared in 3) into the coating pan, coat it, and get it.

Embodiment 2

[0121] Composition 1

[0122] Saxagliptin 25g

[0123] Beta cyclodextrin 80g

[0124] Sodium hydroxide 0.03g

[0125] Composition 2

[0126] Croscarmellose Sodium 60g

[0127] Microcrystalline cellulose 250g

[0128] Lactose 360g

[0129] Pregelatinized starch 30g

[0130] Talc powder 2g

[0131] Appropriate amount of 5% povidone absolute ethanol solution

[0132] Coating Composition

[0133] Coating powder 200g

[0134] Makes 1000 pieces

[0135] The preparation method goes through the following steps:

[0136] 1) Put saxagliptin, beta cyclodextrin and sodium hydroxide in a mortar, add a small amount of water and grind them into a paste,

[0137] Dried below 50°C, crushed into 150-250 mesh fine powder, set aside;

[0138] 2) Sieve microcrystalline cellulose, lactose, croscarmellose sodium, pregelatinized starch, and talcum powder respectively, and set aside;

[0139] 3) Add the prescribed amount of excipient 2) into 1), mix well, and set aside;

[0140] 4) Take...

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PUM

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Abstract

The invention relates to a preparation method of a saxagliptin medicinal composition. The form of the above preparation can be safely applied to patients, can improve the stability of saxagliptin, and also can improve the gastrointestinal tract absorption. The invention concretely relates to a preparation method of a medicinal composition containing amorphous saxagliptin and beta-cyclodextrin. The preparation method comprises the following steps: grinding saxagliptin and beta-cyclodextrin under an alkaline condition, drying, crushing to obtain 150-250 mesh fine powder, mixing the powder with an appropriate auxiliary material to prepare granules, tabletting, and dressing to obtain the composition. The saxagliptin composition greatly improves the in vitro release in order to improve the bioavailability, can effectively treat type II diabetes, and has the advantages of convenient oral administration, covering of bad taste, fast disintegration, fast absorption and convenient carrying.

Description

technical field [0001] The invention relates to a preparation method of a saxagliptin pharmaceutical composition. Dispersing saxagliptin in beta-cyclodextrin can greatly increase the release rate in vitro, thereby improving the bioavailability. Background technique [0002] Diabetes mellitus is a group of metabolic diseases mainly characterized by elevated blood sugar. The main pathophysiological basis is the disorder of sugar, protein, and fat metabolism caused by insulin secretion disorder and (or) insufficient insulin action, followed by the imbalance of water and electrolyte metabolism. [0003] Diabetes can be divided into two types: Type I-insulin-dependent diabetes, which is caused by the destruction of pancreatic beta cells and lack of insulin secretion, resulting in hyperglycemia; type II-non-insulin-dependent diabetes, which is caused by low beta-cell function and relative lack of insulin And insulin action links are not perfect and cause blood sugar levels to ri...

Claims

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Application Information

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IPC IPC(8): A61K9/28A61K47/40A61K31/403A61P3/10
Inventor 严洁李轩
Owner TIANJIN HANKANG PHARMA BIOTECH
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