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Arsenic trioxide sustained-release pellet and preparation method thereof

A technology of arsenic trioxide and sustained-release pellets, which is applied in the fields of medical technology and pharmaceutical preparations, can solve the problems of low bioavailability, low patient compliance, and long administration time, and achieves easy industrial production, simple preparation process, and reduced administration. effect of times

Active Publication Date: 2020-05-22
哈尔滨医大药业股份有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The present invention will solve the problems of long administration time of ATO injection, low patient compliance, frequent administration of oral preparations, low bioavailability, easy to cause gastrointestinal adverse reactions, and transiently high blood drug concentration. Problems that limit applications such as cell damage

Method used

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  • Arsenic trioxide sustained-release pellet and preparation method thereof
  • Arsenic trioxide sustained-release pellet and preparation method thereof
  • Arsenic trioxide sustained-release pellet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] In the arsenic trioxide sustained-release pellets provided in this embodiment, the prescription composition and preparation method of the drug pellet core are as follows:

[0033] Table 1 Drug bolus core prescription composition

[0034]

[0035] Ball core preparation method: adopt extruding spheronization method to prepare the medicine ball core of above each prescription, concrete operation is as follows: after main drug and adjuvant are mixed by prescription ratio, add binding agent (with deionized water PVP is mixed with concentration 10% solution as adhesive). After the soft material is made, it is extruded in the extruder through the screen of the extruder, and the obtained strips are rounded in the spheronizer, then taken out and dried, and sieved to obtain small pellets of 18-35 mesh for later use. The pellet core yields prepared by each prescription are not less than 90%.

Embodiment 2

[0037] In the arsenic trioxide sustained-release pellets provided in this example, the coating solution formulation and preparation method of the sustained-release layer are as follows:

[0038] Table 2 Coating Solution Prescription Composition

[0039]

[0040] Coating process: the coating solution of above different prescriptions is wrapped outside the drug ball core, and concrete operation is as follows: open the fluidized bed, will prepare the ATO ball core (18 mesh to 35 Mesh) 500g into the fluidized bed, spray coating solution, after coating, respectively at 50°C (coating solution prescription 1), 40°C (coating solution prescription 2), 25°C (coating solution prescription 3) and 40°C (coating solution prescription 4) oven for aging for 24h.

Embodiment 3

[0042] In this embodiment, an appropriate amount of slow-release pellets with different polymer wrapping amounts is taken, packed into capsules, and the release degree is measured. The specific results are as follows: figure 1 shown;

[0043] The release rate refers to the general rules of Part 4 of the 2015 edition of the "Chinese Pharmacopoeia", using the device of the first method of the dissolution and release rate determination method, using 1000ml of phosphate buffer solution with pH 7 as the solvent, and the speed is 100 rpm. Operate according to the law.

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Abstract

The invention belongs to the fields of medical technology and pharmaceutical preparations, and relates to an arsenic trioxide sustained-release pellet, as well as a preparation method and applicationthereof. The arsenic trioxide sustained-release pellet is prepared from a drug pellet core containing arsenic trioxide and a sustained-release coating layer wrapped around the pellet core, the drug pellet core is composed of the arsenic trioxide, a filler and a binder, and the sustained-release coating layer is composed of an enteric polymer material or water-insoluble polymer material, a plasticizer, a pore forming agent and / or an anti-sticking agent. The arsenic trioxide sustained-release pellet can realize 10%-30% (0.5-2 h), 40%-60% (4-8 h) and >=90% (24 h) release ranges; and the preparedsustained-release pellet is used for preparing an oral drug for treating acute non-lymphocytic leukemia, has a most remarkable curative effect on acute promyelocytic leukemia, and is used for preparing oral drugs for treating chronic myeloid leukemia, and chronic blastic phase liver cancer, lung cancer, pancreatic cancer, colon cancer, breast cancer and cervical cancer.

Description

technical field [0001] The invention belongs to the field of medical technology and pharmaceutical preparations, and relates to an arsenic trioxide sustained-release pellet and a preparation method and application thereof. Background technique [0002] The prior art discloses that arsenic trioxide (ATO) has been widely used in the treatment of acute promyelocytic leukemia (APL), and a large number of experimental studies have shown that the use of this drug in the treatment of APL has a significant effect. Studies have shown that ATO has a dose-dependent dual effect on acute promyelocytic leukemia cells. A low concentration of ATO can induce partial differentiation of cells for a long time, and high concentration can induce cell apoptosis; low concentration (0.1-0.5 μmol / L) is applied to In cell lines, ATO can induce the differentiation of human acute promyelocytic leukemia cells by attacking the PML part of the PML-RARα fusion product and destroying the chimeric protein. A...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K47/32A61K47/38A61K33/36A61P35/02
CPCA61K9/5042A61K9/5026A61K33/36A61P35/02Y02A50/30
Inventor 周晋姜嫣嫣刘晓周萍高建华海鑫
Owner 哈尔滨医大药业股份有限公司
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