Dasatinib nanopreparation and preparation method thereof

A dasatinib and nano-preparation technology, which is applied in the direction of pharmaceutical formulas, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of long preparation process, complicated preparation process, uneven distribution, etc. , to achieve the effects that are beneficial to the efficacy of the drug, increase the concentration of the drug, and the production process is simple

Active Publication Date: 2017-09-15
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

For example, in the Chinese invention patent application document with the publication number CN103845332A, a dasatinib pharmaceutical composition and its preparation method are disclosed. The blocker in the invention can improve the microenvironment of the solid preparation, and can improve the Stability and dissolution rate; its defect is: the particle size of dasatinib used in this invention is micron order, only optimizing the formula can not solve the problem of insoluble drug itself
In the Chinese invention patent application document with the publication number CN105560247A, a dasatinib composition tablet and its preparation method are disclosed. The dasatinib composition tablet in this invention has high dissolution rate and good stability. Low moisture and impurity content; the disadvantage is that the preparation process is time-consuming and difficult to produce in large quantities
In the Chinese invention patent application document with the publication number CN105106159A, a drug dasatinib composition tablet for the treatment of blood cancer is disclosed. The invention uses a new crystal form of dasatinib to prepare the tablet. The dissolution rate of the existing technology has been improved; the disadvantage is that the improvement effect of the dissolution rate and bioavailability of the drug is limited by adjusting the formulation of the preparation and changing the crystal form of the active ingredient of the drug.
[0008] In summary, the above-mentioned existing methods have the disadvantages of large particle size and uneven distribution of the drug, it is difficult to greatly increase the dissolution rate of the drug, the preparation process is complicated, and the production cost is high.

Method used

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  • Dasatinib nanopreparation and preparation method thereof
  • Dasatinib nanopreparation and preparation method thereof
  • Dasatinib nanopreparation and preparation method thereof

Examples

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Embodiment 1

[0049] A dasatinib oral nano-preparation, comprising the following components:

[0050] Dasatinib 600mg, excipients 800mg, additives 600mg;

[0051] Among them, the auxiliary materials include 600 mg of microcrystalline cellulose and 200 mg of crospovidone; the additive is mannitol.

[0052] A preparation method of dasatinib oral nano-preparation, the steps are as follows:

[0053] S1, Dasatinib bulk drug (scanning electron microscope picture as shown in figure 1 shown) and N,N-dimethylformamide to form 20mL of Dasatinib N,N-dimethylformamide solution with a concentration of 30mg / mL;

[0054] S2. Mix mannitol and deionized water into 400 mL of 1.5 mg / mL mannitol aqueous solution, and simultaneously add 15 mg of sodium lauryl sulfate to the mannitol aqueous solution to obtain a mixed solution;

[0055] S3. Add the dasatinib N,N-dimethylformamide solution obtained in step S1 to the mixed solution obtained in step S2, stir with a magnetic stirrer for 35 minutes, and control th...

Embodiment 2

[0065] A dasatinib oral nano-preparation, comprising the following components:

[0066] Dasatinib 800mg, excipients 1100mg, additives 800mg;

[0067] Among them, the auxiliary materials include 1000 mg of polyvinylpyrrolidone and 100 mg of hypromellose; the additive is lactose monohydrate.

[0068] A preparation method of dasatinib oral nano-preparation, the steps are as follows:

[0069] S1, Dasatinib bulk drug and dimethyl sulfoxide are made into 20 mL of dasatinib dimethyl sulfoxide solution with a concentration of 40 mg / mL;

[0070] S2, polyvinylpyrrolidone and deionized water are made into 500mL of polyvinylpyrrolidone aqueous solution of 2mg / mL;

[0071] S3. Open the internal circulation high-gravity rotating packed bed, add the dasatinib dimethyl sulfoxide solution obtained in step S1 and the aqueous solution of pharmaceutical excipients obtained in step S2 into the high-gravity rotating packed bed at the same time, adjust the speed to 2800rpm, and circulate The time...

Embodiment 3

[0077] A dasatinib oral nano-preparation, comprising the following components:

[0078] Dasatinib 500mg, excipients 510mg, additives 300mg;

[0079] Wherein, the auxiliary materials include 10 mg sodium dodecyl sulfonate, 400 mg microcrystalline cellulose, 50 mg carboxymethyl cellulose sodium and 50 mg hypromellose; the additive is mannitol.

[0080] A preparation method of dasatinib oral nano-preparation, the steps are as follows:

[0081] S1. Dasatinib bulk drug and N, N-dimethylacetamide were formulated into 10 mL of Dasatinib N, N-dimethylacetamide solution with a concentration of 50 mg / mL;

[0082] S2. Mannitol and deionized water are mixed into 200 mL of 1.5 mg / mL mannitol aqueous solution, and 10 mg of sodium dodecylsulfonate is added to the mannitol aqueous solution at the same time to obtain a mixed solution

[0083] S3. Add the dasatinib N,N-dimethylacetamide solution obtained in step S1 to the mixed solution obtained in step S2, stir for 15 minutes using a high-sp...

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Abstract

The invention discloses a dasatinib nanopreparation, which consists of dasatinib, auxiliary material and additive; the dasatinib is 5 to 40 parts by weight, the auxiliary material is 30 to 80 parts by weight, the additive is 10 to 40 parts by weight, and the grain size of the dasatinib is less than 1Mu m. The invention further discloses a preparation method for the preparation. The invention optimizes the grain size and dissolubility of the nanodrug by adjusting the composition of the auxiliary material, concentration and preparation process parameters, so that the dissolubility of the drug is greatly increased, and the dissolution rate of the drug in 15 minutes reaches 91 to 94 percent; moreover, the production process is simple, the dasatinib nanopreparation can be mass-produced, methods, such as high temperature, high pressure and chemical reaction, which can easily destroy the ingredients of the drug are not needed, the process conditions are mild, and thereby industrialization is benefited.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a dasatinib nano-preparation and a preparation method thereof. Background technique [0002] Dasatinib (Dasatinib), developed by Bristol-Myers Squibb (BMS) of the United States, with a trade name of Sprycel, was first listed in the United States in tablet form in 2006, and is used for the treatment of imatinib mesylate resistance. Drugs, or intolerant Philadelphia chromosome positive (Ph+) chronic myeloid leukemia (CML) adult patients in chronic phase, accelerated phase and blast phase. At present, the drug has been approved for marketing in most countries around the world. [0003] Dasatinib chemical name: N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl -4-pyrimidinyl]amino]-5-thiazolecarboxamide. Its molecular formula is C 22 h 28 N 7 ClO 3 S, with a relative molecular mass of 488.2, has the following structural formula: ...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/506A61K47/38A61K47/26A61P35/02
CPCA61K9/19A61K31/506A61K47/26A61K47/38
Inventor 乐园陈鹏沈煜栋林谡轩戴田晨
Owner BEIJING UNIV OF CHEM TECH
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