阅读说明：本技术 一种格列吡嗪片及其用途 (Glipizide tablets and application thereof ) 是由 林凡儒 郭增光 王明涛 刘倩 于 2019-10-28 设计创作，主要内容包括：本发明属于制药技术领域,公开了一种格列吡嗪片,其原料组成如下：格列吡嗪,牛蒡苷,一水乳糖,微晶纤维素,玉米淀粉,二氧化硅,硬脂酸。本发明片剂中通过添加牛蒡苷活性成分,与格列吡嗪共同起作用,效果更佳,可考虑进行进一步的临床试验来进行验证。(The invention belongs to the technical field of pharmacy, and discloses a glipizide tablet which comprises the following raw materials: glipizide, arctiin, lactose monohydrate, microcrystalline cellulose, corn starch, silicon dioxide and stearic acid. The tablet disclosed by the invention has better effect by adding the arctiin active ingredient to act together with glipizide, and can be verified by considering further clinical tests.)

1. The glipizide tablet comprises the following raw materials: glipizide, arctiin, lactose monohydrate, microcrystalline cellulose, corn starch, silicon dioxide and stearic acid.

2. The glipizide tablet of claim 1, wherein the glipizide tablet comprises the following raw materials by weight for producing 1 ten thousand tablets: 50g of glipizide, 10g of arctiin, 1640g of lactose monohydrate, 180g of microcrystalline cellulose, 100g of corn starch, 20g of silicon dioxide and 40g of stearic acid.

3. A glipizide tablet according to claims 1-2, wherein the glipizide tablet is prepared by the following steps:

1) pretreatment: taking the raw materials, and sieving stearic acid by a sieve of 80 meshes for later use;

2) weighing: weighing glipizide, arctiin, lactose monohydrate, microcrystalline cellulose, corn starch and stearic acid according to the formula for later use;

3) mixing: putting 50g of weighed glipizide into a three-dimensional motion mixer, then adding 100g of lactose monohydrate, mixing for 5min, then adding 200g of lactose monohydrate, mixing for 5min, then adding 400g of lactose monohydrate, mixing for 5min, and finally putting the rest of lactose monohydrate into the three-dimensional motion mixer for mixing for 1 h; taking out, sieving with a 30-mesh sieve, mixing in a three-dimensional motion mixer for 3h, adding 10g of arctiin, 180g of microcrystalline cellulose and 100g of corn starch, and continuously mixing for 30min to obtain an intermediate product;

4) total mixing:

averagely dividing the intermediate product obtained in the step 3) into two parts, adding 20g of stearic acid and 10g of silicon dioxide into each part, and then adding the two parts into a three-dimensional motion mixer together for mixing at the rotating speed of 12rpm for 5 min;

5) tabletting:

selecting a phi 8.0mm circular punch and a die; tabletting with a rotary tablet press, controlling the tablet weight difference within + -5.0%, and controlling the hardness within 80-120N.

4. A glipizide tablet according to claim 3, wherein the rotation speed of the three-dimensional motion mixer in the step 3) is 12 rpm.

5. Use of glipizide tablets as claimed in claims 1-4 for the treatment of diabetes.

6. Use according to claim 5, wherein the diabetes is type II diabetes.

Technical Field

The invention belongs to the technical field of pharmacy, and particularly relates to a glipizide tablet and application thereof.

Background

Glipizide (Glipizide), chemical name 1-cyclohexyl-3- {4- [2- (5-methylpyrazine-2-amide) -ethyl ] benzenesulfonyl } urea, molecular formula: C21H27N5O4S, molecular weight 445.54. Glipizide (Glipizide) is a second generation sulfonylurea oral hypoglycemic agent. It can promote the pancreatic islet beta cells to secrete insulin and enhance the action of the insulin on target tissues; it also can stimulate islet alpha cells to inhibit glucagon secretion, and has effects of inhibiting hepatic glycogenolysis, promoting muscle utilization and consuming glucose.

After the common glipizide preparation is taken, the blood sugar fluctuation is large, the adverse reaction is more, and the patient needs to take the medicine for many times every day, and the compliance is poor. The prior art is mostly improved from the preparation per se, including preparation of sustained-release preparations and the like. Arctiin is a chemical substance with molecular formula of C27H34O 11. Arctiin is one of the important active substances of burdock and is originally derived from burdock extract. Modern pharmacological research results show that the active ingredient in the burdock is arctigenin, and the arctiin can be quickly converted into the arctigenin under the action of intestinal bacteria when the arctigenin is orally taken. Because the medicinal materials have less free arctigenin, the arctiin in the great burdock fruit is used as an index component. Alpha-glucosidase can break down complex carbohydrates into monosaccharides that can be absorbed by the body, while alpha-glucosidase inhibitors can delay or reduce postprandial blood glucose elevation by inhibiting the activity of this enzyme. At present, researches show that arctiin can be used as an inhibitor of alpha-glucosidase and can reduce blood sugar by inhibiting the activity of the alpha-glucosidase. In the prior art, a scheme for reducing blood sugar by combining glipizide and arctiin, and a scheme for preparing the glipizide and the arctiin into tablets together are not available.

Disclosure of Invention

The invention provides a glipizide tablet by combining glipizide and arctiin.

The invention is realized by the following technical scheme.

The glipizide tablet comprises the following raw materials: glipizide, arctiin, lactose monohydrate, microcrystalline cellulose, corn starch, silicon dioxide and stearic acid.

Further, according to the production of 1 ten thousand tablets, the glipizide tablet comprises the following raw materials: 50g of glipizide, 10g of arctiin, 1640g of lactose monohydrate, 180g of microcrystalline cellulose, 100g of corn starch, 20g of silicon dioxide and 40g of stearic acid.

Specifically, the glipizide tablet is prepared according to the following steps:

1) pretreatment: taking the raw materials, and sieving stearic acid by a sieve of 80 meshes for later use;

2) weighing: weighing glipizide, arctiin, lactose monohydrate, microcrystalline cellulose, corn starch and stearic acid according to the formula for later use;

3) mixing: putting 50g of weighed glipizide into a three-dimensional motion mixer, then adding 100g of lactose monohydrate, mixing for 5min, then adding 200g of lactose monohydrate, mixing for 5min, then adding 400g of lactose monohydrate, mixing for 5min, and finally putting the rest of lactose monohydrate into the three-dimensional motion mixer together for mixing for 1 h; the rotating speed of the three-dimensional motion mixer is 12 rpm;

taking out, sieving with a 30-mesh sieve, mixing in a three-dimensional motion mixer for 3h, adding 180g of microcrystalline cellulose and 100g of corn starch, and continuously mixing for 30min to obtain an intermediate product;

4) total mixing:

averagely dividing the intermediate product obtained in the step 3) into two parts, adding 20g of stearic acid and 10g of silicon dioxide into each part, and then adding the two parts into a three-dimensional motion mixer together for mixing at the rotating speed of 12rpm for 5 min;

5) tabletting:

selecting a phi 8.0mm circular punch and a die; tabletting with a rotary tablet press, controlling the tablet weight difference within + -5.0%, and controlling the hardness within 80-120N.

The invention also claims the application of the glipizide tablet in treating diabetes.

Preferably, the diabetes is type II diabetes.

Compared with the prior art, the invention has the advantages that the following aspects are mainly included but not limited:

the invention improves all indexes of the tablet by optimizing the formula and the process; the product of the invention has less impurities, good uniformity and excellent dissolution effect in four media; the tablet disclosed by the invention has better effect by adding the arctiin active ingredient to act together with glipizide, and can be verified by considering further clinical tests.

Detailed Description

In order to make those skilled in the art better understand the technical solutions in the present application, the technical solutions in the present application will be clearly and completely described below with reference to specific embodiments of the present application, and it is obvious that the described embodiments are only a part of the embodiments of the present application, and not all embodiments. All other embodiments, which can be derived by a person skilled in the art from the embodiments given herein without making any creative effort, shall fall within the protection scope of the present invention.