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Dasatinib dispersoid, preparation method thereof and application thereof in tablets

A technology of dasatinib and dispersion, which is applied in the directions of non-active ingredient medical preparations, medical preparations containing active ingredients, and pill delivery, etc., can solve the problem of incomplete drug release, low bioavailability, and easy stickiness It can improve the bioavailability, reduce the production cost and make it easy to take.

Active Publication Date: 2012-12-26
NANJING SANHOME PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The dosage forms of dasatinib currently on the market are mainly oral tablets, see WO2006121742, WO2007035874; studies have found that such oral tablets are prone to sticking during the release process, resulting in incomplete drug release, which will cause partial bioavailability. Low

Method used

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  • Dasatinib dispersoid, preparation method thereof and application thereof in tablets
  • Dasatinib dispersoid, preparation method thereof and application thereof in tablets
  • Dasatinib dispersoid, preparation method thereof and application thereof in tablets

Examples

Experimental program
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Effect test

Embodiment 1

[0047] The preparation of dasatinib solid dispersion, the specific steps are: take dasatinib and polyvinylpyrrolidone PVP with a mass ratio of 1: (0.5-10), and fully dissolve them in N, N -Dimethylformamide (DMF) solution, the solution is weighed according to the amount of 1 part of Dasatinib by mass and 4 to 30 parts by volume of the solution. After the dissolution is complete, the obtained solution is slowly dropped into the stirring In the precipitant mixed with ethyl acetate or ethyl acetate and petroleum ether, the volume ratio of the solution to the precipitant is 1: (5-40). With the continuous dripping of the solution, the precipitate is continuously precipitated from the precipitant until the precipitation is complete. Finally, filter out the precipitate, vacuum filter to remove the organic solvent contained in the precipitate, then place it in an oven at 50-60°C for drying, and sieve the dry powder to obtain the Dasatinib solid dispersion. Partition, the detailed sele...

Embodiment 2

[0061] The preparation of dasatinib solid dispersion tablets specifically includes: (1) weighing the prescribed amount of dasatinib solid dispersion and tablet excipients; Select the appropriate punch for the required specifications, and test the tablet to adjust the hardness; (4) Compress the tablet; (5) Coat with 3% Opadry ethanol solution, and the weight of the coating increases by 3%. In different tablet specifications, the detailed selection ratio of each component and solution is as follows, but the preparation ratio is not limited to the following:

[0062] 1.1 Tablet Specification Tablet weight 160mg, dasatinib solid dispersion 40mg, of which dasatinib content is 20mg, microcrystalline cellulose 105.6mg, croscarmellose sodium 12.8mg, magnesium stearate 1.6mg . 3% Opadry ethanol solution coating weight gain 3%. The tablet hardness of this specification is 13.35kg.

[0063] 1.2 Tablet specifications Tablet weight 400mg, dasatinib solid dispersion 100mg, of which dasat...

Embodiment 3

[0067] In vitro dissolution test, in vitro dissolution test according to the dissolution test regulations of the Chinese Pharmacopoeia 2010 edition, using the paddle method and the big cup method, the test time is 2 hours, the speed is 50rpm in the first hour, 200rpm in the next hour, and the temperature is 37℃±0.5 ℃, the dissolution medium is 0.1M hydrochloric acid. The specifications obtained by detecting Example 2 respectively are tablet weight 160mg-containing drug 20mg, tablet weight 400mg-containing drug 50mg, tablet weight 400mg-containing drug 70mg, tablet weight 500mg-containing drug 100mg tablet in vitro dissolution rate, the dissolution rate 106.8%, 98.8%, 99.8%, 97.8% respectively, the dissolution curve is shown in Figure 3-Figure 6 , each tablet met the dissolution rate standard.

[0068]

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Abstract

The invention belongs to the field of medicinal preparations and in particular relates to a Dasatinib dispersoid, a preparation method thereof and an application thereof in preparation of Dasatinib dispersible tablets. Dasatinib solid dispersoid is prepared by using Dasatinib as an active ingredient and is prepared into tablets of different specifications. The Dasatinib solid dispersible tablets overcome the defects of incomplete release of the medicine and low bioavailability caused by that the dispersible common oral tablets are easy to adhere in the medicine releasing process, so that the bioavailability of the Dasatinib medicine can be further improved and the therapeutic effect of the medicine can be effectively exerted. The preparation process is simple, convenient and practical.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a dispersion of dasatinib and a preparation method thereof, and a dispersible tablet of dasatinib prepared by using the dispersion. [0002] Background technique [0003] Dasatinib, trade name Sprycel TM , is an oral tyrosine kinase inhibitor developed by Bristol-Myers Squibb. The drug was granted priority approval by the US FDA on June 28, 2006. It is used for patients with all stages of adult chronic myeloid leukemia (CML) who have failed or are intolerant to previous treatment, and is also used for the treatment of patients who are resistant to other therapies. Adult patients with Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ALL) who are drug-resistant or intolerant. Its chemical name is N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4- Pyrimidinyl] amino] -5-thiazole carboxamide, the chemical structural formula...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/506A61K47/32A61K47/34A61K9/28
Inventor 王勇张仓陈跃坚邢臻真张文萍沈振涛
Owner NANJING SANHOME PHARMACEUTICAL CO LTD
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