Dasatinib liposome preparation, and preparation method thereof

A technology of dasatinib and nilipids, which is applied in the field of nano-drug delivery, can solve the problems of large effective dose, limited bioavailability, and high frequency of medication, and achieves improved encapsulation efficiency, bioavailability, and biological phase. Good capacitive effect

Active Publication Date: 2017-10-20
SHANGHAI JIAO TONG UNIV
View PDF3 Cites 12 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As an oral tablet, its effective dose is large and the frequency of medication is high, and its bioavailability is limited

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Dasatinib liposome preparation, and preparation method thereof
  • Dasatinib liposome preparation, and preparation method thereof
  • Dasatinib liposome preparation, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0072] The preparation method of Dasatinib liposome preparation

[0073] The preparation method of dasatinib liposome preparation of the present invention, comprises the steps:

[0074] (1) prepare the blank liposome that inner water phase and outer water phase all contain ammonium saline solution;

[0075] (2) preparing blank liposomes whose inner water phase contains an ammonium salt solution and whose outer water phase contains a physiological isotonic solution;

[0076] (3) Mix the blank liposome obtained in step (2) with dasatinib soluble saline solution, incubate, remove free dasatinib soluble salt, and obtain dasatinib liposome.

[0077] In step (1) and step (2), the concentration of the ammonium salt in the ammonium salt aqueous solution may be 50-500 mM. The concentration of the ammonium salt in the ammonium salt aqueous solution may also be 50-300 mM. The concentration of the ammonium salt in the ammonium salt aqueous solution may also be 300-500 mM.

[0078] The...

Embodiment 1

[0095] Embodiment 1, establish dasatinib detection method

[0096] In this embodiment, a standard curve of dasatinib was established, as follows.

[0097] Using ultraviolet (ultraviolet, UV) detection and analysis method: the detection instrument is TECAN 200PRO; the detection wavelength is 325nm; the detection temperature is 24°C; the detection orifice plate is 96well plates, UV-transparent; the detection volume is 200μl.

[0098] Accurately weigh 2.5002mg of dasatinib hydrochloride and dissolve it in a 25ml volumetric flask to obtain a dasatinib hydrochloride aqueous solution with a concentration of 0.1000mg / ml; mix the dasatinib hydrochloride aqueous solution with ultrapure water, Gradual dilution to obtain a series of dasatinib hydrochloride standard solutions with concentrations of 25 μg / ml, 20 μg / ml, 15 μg / ml, 10 μg / ml, 7.5 μg / ml, 5 μg / ml, and 2.5 μg / ml. The dasatinib hydrochloride standard solution of the above-mentioned concentration was detected by UV detection a...

Embodiment 2

[0102] Embodiment 2, investigate the precipitation reaction of different salt solutions and dasatinib

[0103] Sodium citrate, sodium acetate, sodium sulfate, sodium chloride, ammonium sulfate, ammonium phosphate, ammonium chloride, and ammonium acetate used in this example were all purchased from Sinopharm Chemical Reagent Co., Ltd.; Ammonium isethionate and ammonium isethionate were purchased from Sigma-Aldrich.

[0104] This embodiment investigates the precipitation reaction of sodium salt solution and dasatinib, and the specific process is as follows:

[0105] (1) Precisely weigh 0.8823g sodium citrate and dissolve in 10ml double distilled water (ddH 2 (2) in, obtain the sodium citrate aqueous solution that concentration is 300mM; Accurately weigh 5.06mg dasatinib hydrochloride and be dissolved in the sodium citrate aqueous solution of 1ml 300mM;

[0106] (2) Precisely weigh 0.4082g sodium acetate and dissolve in 10ml ddH 2 In O, obtain the sodium acetate aqueous soluti...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
Particle sizeaaaaaaaaaa
Login to view more

Abstract

The invention relates to a dasatinib liposome preparation, and a preparation method thereof. The dasatinib liposome preparation is high in biocompatibility; target modification can be carried out; sustained and controlled release of dasatinib can be realized; and it is beneficial for maintenance of relatively high plasma drug concentration in a long term, improvement of drug distribution, and increasing of drug bioavailability. The dasatinib liposome preparation possesses excellent lipophilic performance, is capable of passing through phospholipid bilayer in a molecular form and entering into inner water phase; pH value of liposome inner water phase is relatively low, the dasatinib moleculars are capable of bonding with hydrogen ions so as to form dasatinib ions, and combination with anions in an ammonium salt solution and forming of insoluble salts are realized, diffusion of dasatinib in the inner water phase into an outer water phase is inhibited, dasatinib is coated by the liposome inner water phase steadily, encapsulation efficiency and storage stability are improved, and excellent in-vitro slow release effect is achieved.

Description

technical field [0001] The invention relates to the technical field of nano drug delivery, in particular to a dasatinib liposome preparation and a preparation method thereof. Background technique [0002] Dasatinib (dasatinib), the chemical name is N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]- 2-Methyl-4-pyrimidinyl]amino]-5-thiazole carboxamide monohydrate is a tyrosine protein kinase inhibitor. Dasatinib is approved by the U.S. Food and Drug Administration (FDA) for the treatment of adults with chronic, accelerated, myeloid or lymphoid chronic myelogenous leukemia ( Chronic myelogenous leukemia (CML), mainly inhibits the excessive proliferation of white blood cells in the bone marrow of patients, and is often used to treat leukemia caused by BCR-ABL kinase mutations. [0003] The currently marketed dasatinib products are only oral tablets. For patients with Ph+ chronic phase CML, the recommended starting dose is 100 mg once a day. As an oral tab...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): A61K9/127A61K31/506A61K47/04A61K47/20A61P35/00
CPCA61K9/0019A61K9/1271A61K9/1278A61K31/506A61K47/02A61K47/20
Inventor 魏晓慧缪旭光徐宇虹
Owner SHANGHAI JIAO TONG UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap