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Oral solid preparation of canagliflozin and preparation method thereof

A solid and filler technology, which is applied in the direction of medical preparations containing active ingredients, pill delivery, pharmaceutical formulations, etc., and can solve problems such as crystal transformation and poor compressibility

Active Publication Date: 2014-03-26
CHONGQING PHARMA RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Through a lot of research, it was unexpectedly found that by controlling the particle size of the raw material drug, the compressibility and dissolution rate of canagliflozin can be effectively improved without the use of granulation solvents, which effectively solves the problem of the transfer of canagliflozin in the amorphous form during the preparation process. The important technical problem of crystal and poor compressibility

Method used

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  • Oral solid preparation of canagliflozin and preparation method thereof
  • Oral solid preparation of canagliflozin and preparation method thereof
  • Oral solid preparation of canagliflozin and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1~6

[0052] The prescription of embodiment 1~6 sees table 1:

[0053]

[0054] Preparation Process:

[0055] 1. Get the amorphous canagliflozin raw material of the above-mentioned volume average particle size for subsequent use;

[0056] 2. Pass the lactose, microcrystalline cellulose, croscarmellose sodium and magnesium stearate through an 80-mesh sieve for later use;

[0057] 3. Mix the bulk drug, lactose, microcrystalline cellulose, croscarmellose sodium of 70% prescription quantity and magnesium stearate of 70% prescription quantity of each embodiment, and the mixed material is added into dry process Dry granulation in the granulator, the prepared granules are mixed with 30% prescription amount of magnesium stearate and 30% prescription amount of croscarmellose sodium to obtain semi-finished products;

[0058] 4. Determine the content of the semi-finished product and calculate the tablet weight. The tablet weight was adjusted according to the content of the semi-finished ...

Embodiment 7~13

[0069] The prescription of embodiment 7~13 sees table 4:

[0070]

[0071] Preparation Process:

[0072] 1. Take the canagliflozin raw material with the above-mentioned volume average particle size for subsequent use;

[0073] 2. Lactose, mannitol, starch, pregelatinized starch, microcrystalline cellulose, croscarmellose sodium, crospovidone, carboxymethyl starch sodium, sodium lauryl sulfate, Silica and magnesium stearate are passed through an 80-mesh sieve for subsequent use;

[0074] 3. Mix all the excipients except silicon dioxide and magnesium stearate in the above prescriptions evenly, add the mixed materials into the dry granulator for dry granulation, and add the silicon dioxide of the respective prescription amount to the prepared granules Mix with magnesium stearate to get a semi-finished product;

[0075] 4. Determine the content of semi-finished products and calculate the tablet weight. According to the content of the semi-finished product, adjust the tablet...

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Abstract

The invention relates to an oral solid medicine composition of canagliflozin and a preparation method thereof. The composition comprises canagliflozin and pharmaceutic adjuvants, wherein the canagliflozin is in an amorphous form, and the average grain size of particles is 2.5-30 microns. The composition can be used for effectively solving the technical problems that the crystal transformation and the compressibility of the canagliflozin in the amorphous form are poor in the preparation process of the solid preparation.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a canagliflozin oral solid pharmaceutical composition and a preparation method thereof. technical background [0002] Canagliflozin, generic name canagliflozin, chemical name: 1-(β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienyl Methyl] benzene, its structural formula is as shown in formula I. [0003] [0004] Canagliflozin is a selective type 2 sodium glucose cotransporter (SGLT2) inhibitor, which has been approved by the United States and the European Union for the treatment of type 2 diabetes. [0005] Normally, the kidneys play an important role in the regulation of blood sugar. Glucose is completely reabsorbed back into the blood when it passes through the renal tubules, so there is almost no glucose in the final urine, and blood sugar is kept stable. Glucose is an uncharged organic substance, and its reabsorption is an active reabsorption process...

Claims

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Application Information

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IPC IPC(8): A61K31/351A61K9/20A61P3/10
Inventor 王立张涛邓杰
Owner CHONGQING PHARMA RES INST
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