Water-soluble realgar solid dispersions as well as preparation method and application thereof

A solid dispersion, water-soluble technology, applied in the field of medicine, can solve the problems of the increase of highly toxic by-products, and the production cannot be completed in one step, and achieves improved bioavailability, improved bioavailability and anti-leukemia activity, and improved bioavailability. Effect

Active Publication Date: 2016-12-21
THE INST OF BASIC MEDICAL SCI OF CHINESE ACAD OF MEDICAL SCI
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, this process must first prepare nano-realgar and then mix it with polymers, which cannot solve the problem of increasing the highly toxic by-products faced in the preparation process of nano-realgar
In addition, the production of this method cannot be completed in one step, and the nano-realgar particles are only mixed in the polymer matrix by a common stirring process, and exist in agglomeration mode (Guo Teng. Research on the influence of solid dispersion technology on the stability and in vitro dissolution of nano-realgar [ J]. Chinese Journal of Traditional Chinese Medicine, 2013,38(17):2782-7.)

Method used

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  • Water-soluble realgar solid dispersions as well as preparation method and application thereof
  • Water-soluble realgar solid dispersions as well as preparation method and application thereof
  • Water-soluble realgar solid dispersions as well as preparation method and application thereof

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Embodiment

[0037] The water-soluble realgar solid dispersions of Examples 1-10 were prepared by the following preparation methods, only the composition of the raw materials and the preparation process parameters were adjusted, and the specific adjustments were shown in Table 1 (mentioned in Table 1). The specific preparation method is as follows: weighing a certain weight of realgar and macromolecule (and surfactant), stirring and mixing in a container to form materials, and then adding them into an extruder. The temperature in the extruder is set at 50-200° C., and the screw speed is 5-100 r / min. The material is extruded from the die hole of the machine head, and an orange-yellow solid product is obtained after cooling at room temperature.

[0038] Table 1 The raw material composition and preparation process parameters of water-soluble realgar solid dispersion of the present invention

[0039]

experiment example

[0041] The comparative example 1 among the experimental examples is the raw material liquid realgar.

[0042] In the following experimental examples, only the experimental process and data of some embodiments are listed, and the same experiments are also done in other embodiments, and the experimental results are the same as those of the listed embodiments.

experiment example 1

[0043] Experimental Example 1: Water Solubility Evaluation

[0044] Take by weighing embodiment 1 product 32mg and comparative example 1 powder 8mg (both contained As 2 S 2 Content is 8mg), respectively placed in test tubes, add 8mL pure water, after ultrasonic treatment 10min, obtain embodiment 1 aqueous dispersion and comparative example 1 aqueous dispersion, such as figure 1 As shown, after the product of Example 1 is ultrasonically treated, the aqueous dispersion is orange-yellow, indicating that realgar in the product can be dissolved in a large amount and enter the water phase to form a stable aqueous dispersion; after the powder of Comparative Example 1 is processed by ultrasonic in water, realgar Still precipitated at the bottom of the test tube (shown by the white arrow), the water phase is still in a colorless and transparent state, showing that realgar is difficult to enter the water phase in Comparative Example 1.

[0045] The above experimental results show that...

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Abstract

The invention discloses water-soluble realgar solid dispersions as well as a preparation method and an application thereof. The dispersions comprise the following components in parts by weight: 1 part of realgar, 1-20 parts of macromolecule, and 0-5 parts of a surfactant. The realgar solid dispersions solve the problem of low bioavailability due to difficult dissolution of realgar in water, effectively improve dissolution rate and accumulated dissolution of realgar in water, improve bioavailability of realgar, prolong cycling time of arsenic in blood, and therefore enhance efficacies of anti-leukemia drugs. The preparation processing process is simple, production efficiency is high, and the preparation process and a subsequent crushing or shaping process of the solid dispersions can be directly connected. In a clinic application, dosage of realgar can be effectively reduced, especially in an intensive treatment period or a consolidation treatment period, taking frequency and dosage can be reduced; compliance of patients can be improved, risks for health brought by toxic and side effects of large dosage of taking for a long time can be reduced, and treatment cost can be substantially reduced.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a water-soluble realgar solid dispersion and a preparation method and application thereof. Background technique [0002] The main component of realgar is arsenic disulfide (As 2 S 2 ), the clinical use of realgar in traditional Chinese medicine has a history of more than two thousand years. Currently commonly used Chinese patent medicines such as Niuhuang Jiedu Tablets, Angong Niuhuang Pills, Liushen Pills, Zijindan and Chansu Pills contain realgar. [0003] Studies have found that the application of realgar to chronic myelogenous leukemia (also known as chronic myelogenous leukemia, Chronic Myelogenous Leukemia, CML) can make the patient's complete remission rate reach 72%. Tablet) in the treatment of promyelocytic leukemia (Acute Promyelocytic Leukemia, APL) has a complete remission rate of 98.3%, and there is no obvious bone marrow suppression. Compared with the currently commonly ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K33/36A61K47/32A61K47/34A61K9/00A61P35/02
Inventor 许海燕刘健马强王川孟洁
Owner THE INST OF BASIC MEDICAL SCI OF CHINESE ACAD OF MEDICAL SCI
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