Regorafenib dispersible tablet and preparation method thereof

A technology of regorafenib and dispersible tablets, applied in the field of regorafenib dispersible tablets and its preparation, can solve the problems of difficult treatment of patients, influence on drug absorption, low dissolution rate, etc., and achieve good drug safety and good human body absorption , the effect of taking convenience

Inactive Publication Date: 2017-06-23
PEKING UNIV FOUNDER GRP CO LTD +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The main problem with regorafenib is that it has a low dissolution rate after being made into tablets because it is slightly soluble in water.
Ordinary tablets have the disadvantage of slow disintegration speed, which affects the absorption of drugs; in addition, ordinary tablets have a large volume, or often need to use multiple tablets (grains) at a time, and need to be washed with water, which is inconvenient to take, especially for the elderly. , young and patients with swallowing dysfunction have certain difficulties in treatment

Method used

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  • Regorafenib dispersible tablet and preparation method thereof
  • Regorafenib dispersible tablet and preparation method thereof
  • Regorafenib dispersible tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Prescription (Specification: 20mg)

[0032]

[0033] Preparation:

[0034] (1) Treatment of raw and auxiliary materials: the Dv90 of the co-micronized active ingredient regorafenib and mannitol is 21.8 μm, and the rest of the auxiliary materials are passed through an 80-mesh sieve for later use;

[0035] (2) making soft material: after taking the co-micronized product of recipe quantity, microcrystalline cellulose, 2% carboxymethyl starch sodium and mixing evenly, make soft material with water;

[0036] (3) Granulation: get above-mentioned soft material and granulate with 18 mesh screens;

[0037] (4) Drying: dry the wet granules, control the temperature of the material at 50±5°C, and make the moisture of the granules reach about 2%;

[0038] (5) Grain sizing: the dried granules are sieved with a 24-mesh sieve;

[0039] (6) Total blending: the granulated granules are added to the converted magnesium stearate and 1% sodium carboxymethyl starch and mixed evenly. The...

Embodiment 2

[0042] Prescription (Specification: 40mg)

[0043]

[0044] Preparation:

[0045] (1) Treatment of raw and auxiliary materials: the Dv90 of the active ingredient regorafenib and mannitol co-micronized powder is 22.5 μm, and the rest of the auxiliary materials are passed through an 80-mesh sieve for later use;

[0046] (2) making soft material: after taking the co-micronized product of recipe quantity, microcrystalline cellulose, 2% carboxymethyl starch sodium and mixing evenly, make soft material with water;

[0047] (3) Granulation: get above-mentioned soft material and granulate with 18 mesh screens;

[0048] (4) Drying: dry the wet granules, control the temperature of the material at 50±5°C, and make the moisture of the granules reach about 2%;

[0049] (5) Grain sizing: the dried granules are sieved with a 24-mesh sieve;

[0050] (6) Total blending: the granulated granules are added to the converted magnesium stearate and 1% sodium carboxymethyl starch and mixed even...

Embodiment 3

[0053] Prescription (Specification: 20mg)

[0054]

[0055] Preparation:

[0056] (1) Treatment of raw and auxiliary materials: the Dv90 of the active ingredient regorafenib and mannitol co-micronized powder is 18.6 μm, and the rest of the auxiliary materials are passed through an 80-mesh sieve for later use;

[0057] (2) making soft material: after taking the co-micronized product of prescription quantity, mannitol, microcrystalline cellulose, 2% carboxymethyl starch sodium and mixing evenly, make soft material with water;

[0058] (3) Granulation: get above-mentioned soft material and granulate with 18 mesh screens;

[0059] (4) Drying: dry the wet granules, control the temperature of the material at 50±5°C, and make the moisture of the granules reach about 2%;

[0060] (5) Grain sizing: the dried granules are sieved with a 24-mesh sieve;

[0061] (6) Total blending: the granulated granules are added to the converted magnesium stearate and 1% sodium carboxymethyl starc...

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Abstract

The invention provides a regorafenib dispersible tablet and a preparation method of the regorafenib dispersible tablet. The dispersible tablet is composed of the active ingredient, namely, regorafenib, and the pharmaceutic adjuvants including a filler, disintegrating agent and a lubricant. The prepared regorafenib dispersible tablet can completely disintegrate rapidly, so that the time for reaching the peak is shortened, the dissolution rate achieves 90% or above, the taking is convenient, the efficiency release is rapid, the bioavailability is high, in addition, the preparation process is simple, the control is easy, the operation is convenient, and the preparation method is suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of medicines, and in particular relates to a regorafenib dispersible tablet and a preparation method thereof. Background technique [0002] Regorafenib, the chemical name is 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N -Methylpyridine-2-carboxamide·monohydrate. Its molecular formula is C 21 h 15 CIF 4 N 4 o 3 ·H 2 O, molecular weight is 500.83, its compound structural formula is as follows: [0003] [0004] It mostly exists in the form of salt, such as hydrochloride, methanesulfonate and phenylsulfonate, which is an effective anticancer and antiangiogenic agent, including VEGFR, PDGFR, raf, p38 and / or flt- 3 inhibitory activity of kinase signaling molecules, and it can be used in the treatment of various diseases and disorders, such as hyperproliferative diseases, such as cancer, tumor, lymphoma, sarcoma and leukemia. Its film-coated tablet Stivarga (specification 40mg) w...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/44A61P35/00
CPCA61K9/0095A61K9/2059A61K31/44
Inventor 易崇勤王海超冀蕾
Owner PEKING UNIV FOUNDER GRP CO LTD
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