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Apixaban sustained-release tablets and preparation method thereof

A technology for apixaban and sustained-release tablets, applied in the field of apixaban sustained-release tablets and its preparation, can solve the problems of poor drug effect, weight loss, vision loss, etc., achieve stable therapeutic effect and reduce absorption Good speed and drug stability

Inactive Publication Date: 2015-03-04
HARBIN SHENGJI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The mechanism of hyperphagia is not very clear. Most scholars tend to be caused by the decrease of glucose utilization rate (difference in glucose concentration in arterial and venous blood before and after entering and leaving tissue cells). Normal people fasting When the glucose concentration difference in the arteriovenous blood decreases, it stimulates the feeding center and produces hunger. After eating, the blood sugar rises, the concentration difference in the arteriovenous blood increases (greater than 0.829mmoL / L), the feeding center is inhibited, and the satiety center is excited. Food intake requirements disappear, but due to the absolute or relative lack of insulin or tissue insensitivity to insulin, the ability of tissues to absorb and utilize glucose decreases in diabetics. Being in a "starvation state" stimulates the feeding center, causing hunger and overeating. In addition, the body cannot make full use of glucose, and a large amount of glucose is excreted from the urine, so the body is actually in a semi-starved state, and the lack of energy also causes hyperphagia
[0010]4. Weight loss
[0011] Although the appetite and food intake of diabetic patients are normal or even increased, the weight loss is mainly due to the absolute or relative lack of insulin or insulin resistance, and the body cannot fully utilize glucose to generate energy. Cause fat and protein decomposition to strengthen, excessive consumption, negative nitrogen balance, weight loss gradually, and even emaciation. Once diabetes is properly treated and well controlled, weight loss can be controlled or even rebounded. Sustained weight loss or significant emaciation during treatment, suggesting poor metabolic control or other chronic wasting diseases
[0012]5. Fatigue
[0014]6. Vision loss
[0016]There are many drugs on the market to treat diabetes, but most of them are not very effective

Method used

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  • Apixaban sustained-release tablets and preparation method thereof

Examples

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Effect test

Embodiment 1

[0041] An apixaban sustained-release tablet and a preparation method thereof, which are made of apixaban, a sustained-release framework material, and a lubricant, wherein, in parts by weight, 5 parts of apixaban, 50- 95 parts, lubricant 3-20 parts.

[0042] According to the optimal parts by weight, there are 5 parts of apixaban, 93 parts of slow-release matrix material and 5 parts of lubricant.

[0043] The sustained-release matrix material is hypromellose.

[0044] The hypromellose is one or a mixture of 75hd100cr hypromellose, 75hd4000cr hypromellose, 75hd15000cr hypromellose, 100000cr hypromellose.

[0045] Described lubricant is magnesium stearate, talcum powder, silicon dioxide or a mixture of both.

Embodiment 2

[0047] A kind of Apixaban slow-release tablet and preparation method thereof, the concrete steps of its preparation method are:

[0048] Step 1, material preparation: pulverize apixaban with a pulverizer, pass through a 100-mesh sieve, and set aside;

[0049] Step 2: Total mixing: weigh apixaban and hypromellose in parts by weight, put them in a three-dimensional mixer and mix them for 30 minutes, take them out for later use;

[0050] Step 3: Granulation: Put the mixed fine powder of raw and auxiliary materials into the wet granulator, use pure water as the binder, put the binder into the liquid supply tank, turn on the machine, adjust the parameters, and start adding the moistening Wet agent, open the shearing flying knife at the same time, 2-5 minutes, discharge, use a swing granulator, granulate with a 20-mesh nylon screen, dry with a fluidized bed dryer, first dry with cool wind, wait After the skin is completely dry, turn on the hot air heating, the air inlet tem...

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Abstract

The invention relates to apixaban sustained-release tablets. The apixaban sustained-release tablets are prepared from the raw materials in parts by weight: 5 parts of apixaban, 50-95 parts of sustained-release framework material and 3-20 parts of lubricant. A preparation method of the apixaban succinate sustained-release tablets comprises the steps of preparing materials, mixing, granulating, mixing, tabletting and carrying out aluminum-plastic packaging. According to the apixaban sustained-release tablets, postprandial hyperglycemia related symptoms of type 2 diabetes patients (only limited to the patients, of which blood sugar cannot be effectively controlled by dietotherapy and kinesitherapy, or the patients, of which the blood sugar cannot be effectively controlled yet after an alpha-glucosidase inhibitor is applied based on the dietotherapy and the kinesitherapy) can be effectively improved, novel sustained-release preparations are adopted, and sustained release means delaying the drug release rate of a drug from a dosage form, lowering the organism entering absorption rate of the drug and thus exerting a more stable treatment effect; the apixaban sustained-release tablets have the advantages of good drug stability, convenience in packaging, transportation and storage and the like; the preparation method of the apixaban sustained-release tablets is simple and easy and is applicable to industrial production.

Description

technical field [0001] The invention belongs to the field of chemical drug sustained-release preparations, in particular to an apixaban sustained-release tablet and a preparation method thereof. Background technique [0002] Diabetes is a group of metabolic diseases characterized by hyperglycemia. Hyperglycemia is caused by defective insulin secretion or impaired biological action, or both. The long-term high blood sugar in diabetes leads to chronic damage and dysfunction of various tissues, especially the eyes, kidneys, heart, blood vessels, and nerves. Obesity caused by overeating and reduced physical activity is the most important environmental factor for type 2 diabetes, which makes individuals with genetic susceptibility to type 2 diabetes prone to onset. [0003] The symptoms of diabetes can be divided into two categories: one category is related to metabolic disorders, especially the "three more and one less" related to hyperglycemia, which is more common in type 1 ...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K31/4545A61K47/38A61P3/10
Inventor 马玉国
Owner HARBIN SHENGJI PHARMA
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