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Medicine composition and application thereof, medicine inclusion compound, vein preparation and preparation method thereof

一种组合物、包合物的技术，应用在药物组合物,静脉制剂及制备领域，能够解决不适KX2-361开发成本有效、增溶方式和增溶用试剂不理想等问题，达到载药量优化、成本经济、提高溶解度的效果

Active Publication Date: 2017-06-30
GUANGZHOU XIANGXUE PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] However, the inventors of the present invention have found that during the drug development process of KX2-361, the specific solubilization methods and solubilization reagents disclosed in document WO2006 / 071960 are not ideal, and are not suitable for the further development of KX2-361 to effectively Administered to patients efficiently, cost-effective pharmaceutical preparations

Method used

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  • Medicine composition and application thereof, medicine inclusion compound, vein preparation and preparation method thereof
  • Medicine composition and application thereof, medicine inclusion compound, vein preparation and preparation method thereof
  • Medicine composition and application thereof, medicine inclusion compound, vein preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0155] Example 1: Preparation and evaluation of KX2-361 besylate freeze-dried agent for injection and reconstitution solution (HP-β-CD concentration is 30%, high drug loading)

[0156] Prepare a prescription of the following composition:

[0157]

[0158] Note: The molecular weight of HP-β-CD is 1431~1806, so when calculating the molar ratio, the upper and lower limits of its molecular weight are used for calculation.

[0159] Follow the steps below to prepare the above prescription:

[0160] 1) Put 1.8mL of concentrated hydrochloric acid in a 200mL volumetric flask, and dilute to 200mL with distilled water to obtain a hydrochloric acid solution with a pH of about 1.2 (concentration is 0.1mol / L, the same below).

[0161] 2) Weigh HP-β-CD according to the above-mentioned prescription quantity, and add three 50mL volumetric flasks respectively. Add the solution obtained in 1), dissolve with ultrasonic (ultrasonic frequency 59kHz) and dilute to about 46mL with the above hydr...

Embodiment 2

[0192] Example 2: Preparation and evaluation of KX2-361 besylate freeze-dried agent for injection and reconstitution solution (HP-β-CD concentration is 30%, low drug loading)

[0193] Prepare a prescription of the following composition:

[0194]

[0195] Note: The molecular weight of HP-β-CD is 1431~1806, so when calculating the molar ratio, the upper and lower limits of its molecular weight are used for calculation.

[0196] Follow the steps below to prepare the above prescription:

[0197] 1) Put 1.8mL of concentrated hydrochloric acid in a 200mL volumetric flask, and dilute to 200mL with distilled water to obtain a hydrochloric acid solution with a pH of about 1.2.

[0198] 2) Weigh HP-β-CD according to the above-mentioned prescription amount, and add three 25mL volumetric flasks respectively. Add the solution obtained in 1), dissolve with ultrasonic (ultrasonic frequency 59kHz) and dilute to about 23mL with the above hydrochloric acid solution.

[0199] 3) Weigh the ...

Embodiment 3

[0260] Example 3: Preparation and evaluation of KX2-361 besylate freeze-dried agent for injection and reconstitution solution (HP-β-CD concentration is 20%, higher drug loading)

[0261] Prepare a prescription of the following composition:

[0262]

[0263] Note: The molecular weight of HP-β-CD is 1431~1806, so when calculating the molar ratio, the upper and lower limits of its molecular weight are used for calculation.

[0264] Follow the steps below to prepare the above prescription:

[0265] 1) Put 1.8mL of concentrated hydrochloric acid in a 200mL volumetric flask, and dilute to 200mL with distilled water to obtain a hydrochloric acid solution with a pH of about 1.2.

[0266] 2) Weigh HP-β-CD according to the above-mentioned prescription amount, and add to two 25mL volumetric flasks respectively. Add the solution obtained in 1), dissolve with ultrasonic (ultrasonic frequency 59kHz) and dilute to about 23mL with the above hydrochloric acid solution.

[0267] 3) APIs w...

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Abstract

The invention provides a medicine composition and application thereof, a medicine inclusion compound, a vein preparation and a preparation method thereof. The medicine composition comprises hydroxypropyl-beta-cyclodextrin and an active ingredient, wherein the active ingredient is KX2-361 or a medicinal salt thereof, wherein the KX2-361 is expressed by a formula I which is shown in the description. The medicine composition has the advantages that the hydroxypropyl-beta-cyclodextrin and the KX2-361 or the medicinal salt thereof are mixed to form the inclusion compound, so that the dissolvability of the insoluble medicine KX2-361 is greatly improved; the medicine can be prepared into multiple types of medicine preparations which are clinically applied to patients, such as vein preparations and oral preparations; the stability of the medicine preparations is good, the safety is high, the absorbing property is good, the bioavailability is high, and the cost is more economic.

Description

technical field [0001] The invention belongs to the field of pharmacy, and specifically relates to a pharmaceutical composition and its application, a drug inclusion compound, an intravenous preparation and a preparation method. Background technique [0002] KX2-361 is a small molecule compound developed by Kinex Pharmaceuticals in the United States that can be used to treat cell proliferation diseases (especially cancer). This compound may treat cell proliferation diseases through tyrosine kinase inhibition (see patent document WO2006 / 071960). The Chinese chemical name of KX2-361 is N-(3-fluorobenzyl)-2-(5-(4-morpholinephenyl)pyridin-2-yl)acetamide, and the English chemical name is N-(3-Fluorobenzyl )-2-(5-(4-Morpholinophenyl)pyridin-2-yl)-acetamide), the molecular formula is C 24 h 24 FN 3 o 2 , the molecular weight is 405.46g / mol, and the structural formula is shown in formula 1: [0003] [0004] KX2-361 is in the form of free base, and its pharmaceutically acc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K9/08A61K9/19A61K9/20A61K31/5377A61P35/00
CPCA61K9/0019A61K9/08A61K9/19A61K9/2054A61K31/5377A61K47/40A61K9/20A61K47/6951A61P35/00A61P35/02A61K9/205
Inventor 施水萍张庆勇赵荣华陈惠红曾仑欧达欣刘炎
Owner GUANGZHOU XIANGXUE PHARMA CO LTD
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