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Invokana sustained release preparation and preparation method thereof

A slow-release preparation, the technology of canagliflozin, which is applied in the direction of pharmaceutical formulas, medical preparations with no active ingredients, medical preparations containing active ingredients, etc., can solve the problems of no canagliflozin sustained-release preparations, etc., and achieve The effect of being easy to industrialized production, reducing adverse reactions, and reducing the number of administrations

Active Publication Date: 2015-06-10
CHENGDU HENGRUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But at present there is no canagliflozin sustained-release preparation at home and abroad

Method used

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  • Invokana sustained release preparation and preparation method thereof
  • Invokana sustained release preparation and preparation method thereof
  • Invokana sustained release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] A canagliflozin sustained-release preparation, which is composed of the following raw materials:

[0036] Canagliflozin with a purity of 99.0% is 80g; polymethacrylate is 40g; sodium polymethacrylate is 20g; lactose is 50g; micronized silica gel is 10g;

[0037] First pass canagliflozin through a 100-mesh sieve, polymethacrylate, sodium polymethacrylate, lactose, and micropowdered silica gel through a 80-mesh sieve, then mix the above-mentioned raw materials, and then directly press into tablets with a hardness of 50N-80N to obtain The canagliflozin sustained-release preparation. In this embodiment, the canagliflozin sustained-release preparation was made into 80 mg / tablet.

Embodiment 2

[0039] A canagliflozin sustained-release preparation, which is composed of the following raw materials:

[0040] Canagliflozin with a purity of 99.0% is 100g; polymethacrylate is 40g; sodium polymethacrylate is 20g; lactose is 30g; micronized silica gel is 10g;

[0041] First pass canagliflozin through a 100-mesh sieve, polymethacrylate, sodium polymethacrylate, lactose, and micropowdered silica gel through a 80-mesh sieve, then mix the above-mentioned raw materials, and then directly press into tablets with a hardness of 50N-80N to obtain The canagliflozin sustained-release preparation. In this embodiment, the canagliflozin sustained-release preparation was made into 0.1 g / tablet.

Embodiment 3

[0043] A canagliflozin sustained-release preparation, which is composed of the following raw materials:

[0044] Canagliflozin with a purity of 99.0% is 120g; polymethacrylate is 40g; sodium polymethacrylate is 10g; lactose is 30g; micronized silica gel is 10g;

[0045] First pass canagliflozin through a 100-mesh sieve, polymethacrylate, sodium polymethacrylate, lactose, and micropowdered silica gel through a 80-mesh sieve, then mix the above-mentioned raw materials, and then directly press into tablets with a hardness of 50N-80N to obtain The canagliflozin sustained-release preparation. In this embodiment, the canagliflozin sustained-release preparation was made into 0.12 g / tablet.

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Abstract

The invention discloses an invokana sustained release preparation and a preparation method thereof. The invokana sustained release preparation is composed of the following raw materials in parts by weight: 40-60 parts of invokana, 8-30 parts of polymethacrylate, 5-30 parts of sodium polymethacrylate, 5-60 parts of lactose and 1-5 parts of aerosil. The invokana sustained release preparation prepared according to the invention reduces the administration frequency, lowers the untoward effect of drugs on gastrointestinal tracts, reduces the side effect of drugs on the human body, and can achieve the maximum drug efficacy with the minimum dose of drugs; and the preparation method disclosed by the invention is simple in process and can be put into industrial production easily.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to a canagliflozin sustained-release preparation and a preparation method thereof. Background technique [0002] Canagliflozin, trade name Inovokana, is the first SGLT2 inhibitor approved by the FDA for the treatment of type 2 diabetes in adult patients. Sodium-glucose linked transporter (SGLT) is a glucose transporter with two subtypes, SGLT1 and SGLT2, which are distributed in the small intestinal mucosa and renal tubules respectively, and can transport glucose into the blood. Canagliflozin can inhibit SLCT2, so that the glucose in the renal tubule cannot be smoothly reabsorbed into the blood and excreted with the urine, thereby reducing the blood sugar concentration. [0003] Since glucose is excreted into urine through the kidneys, it is accompanied by side effects such as renal dysfunction, symptomatic hypotension, and fungal infection. 9 clinical trials involving 10,285 patients w...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/22A61K31/381A61K47/32A61P3/10
Inventor 朱德其沈桦
Owner CHENGDU HENGRUI PHARMA
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