A kind of indirubin self-microemulsifying preparation and preparation method thereof

A self-microemulsification and self-microemulsion technology, which is applied in the fields of pharmaceutical formula, emulsion delivery, and medical preparations containing active ingredients, etc., can solve the problem of unsatisfactory water solubility and fat solubility, affecting clinical effects, and low bioavailability, etc. problems, to achieve the effect of facilitating absorption, reducing the frequency of taking, and taking accurate doses

Inactive Publication Date: 2017-07-18
CHONGQING ACAD OF CHINESE MATERIA MEDICA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Indirubin is a bisindole compound extracted from the traditional Chinese medicine Qingdai. It is an active ingredient for the treatment of acute and chronic myeloid leukemia. Its water solubility and fat solubility are not ideal. affect its clinical efficacy

Method used

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  • A kind of indirubin self-microemulsifying preparation and preparation method thereof
  • A kind of indirubin self-microemulsifying preparation and preparation method thereof
  • A kind of indirubin self-microemulsifying preparation and preparation method thereof

Examples

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Embodiment 1

[0034] Example 1 Optimization and preparation of indirubin SMEDDS blank prescription of the present invention

[0035] In this study, self-emulsifying excipients were screened by solubility test, and on this basis, a ternary phase diagram was drawn to preliminarily determine the proportion range of the prescription composition, and then the star point design-response surface method was used to optimize the SMEDDS prescription, and the appearance characteristics, particle size, Zate Potential, drug loading, stability and dissolution rate are the evaluation indicators for preliminary quality evaluation of indirubin SMEDDS.

[0036] 1. Screening of self-emulsifying auxiliary materials

[0037] Take about 2mL of different oil phases, surfactants, and co-surfactants, and place them in a 5mL centrifuge tube. Add excess indirubin API, vortex to disperse, and place at 37℃, 200r / min constant temperature shaking box. Dissolve equilibrium is reached at 24h, take it out, centrifuge at 10000r / mi...

Embodiment 2

[0125] Example 2 Preparation of indirubin self-microemulsion sustained-release microcapsules

[0126] Sodium alginate (SA) is a natural polysaccharide polymer material extracted from marine plants such as kelp and Sargassum. It is non-toxic, non-irritating, and has unique physical and chemical properties and good biocompatibility. It is widely used in pharmaceutical preparations, clinical treatment cell culture, food and other fields. Sodium alginate can be complexed and cross-linked with metal ions with more than two valences (such as calcium ions) to produce calcium alginate gel with water and acid insolubility, non-toxic, and sufficient toughness and strength. Calcium alginate gel can be used as Carriers for enzyme immobilization, oral administration of protein and polypeptide drugs, and slow and controlled release administration.

[0127] In the present invention, the indirubin self-microemulsion is used as the core of the microcapsules, and the calcium alginate microcapsules ...

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Abstract

The invention provides an indirubin self-microemulsifying preparation, which is prepared from the active ingredient indirubin, an oil phase, an emulsifier and a co-emulsifier. The invention also provides a preparation method of the indirubin self-microemulsion preparation, and a self-microemulsion sustained-release microcapsule containing the indirubin self-microemulsion preparation. The solubility of the indirubin self-microemulsifying preparation in the present invention is at least 97.39 times higher than that of the indirubin crude drug, and the quality evaluation result of the in vitro preparation is good, and the purpose of solubilizing the indirubin is achieved. The present invention aims to use self-emulsification as a drug-loading system to achieve the purpose of solubilizing and promoting penetration of indirubin, and uses microencapsulation technology to conduct slow-release research on indirubin self-emulsifying preparations to reduce the number of times of taking and prolong the drug effect. time, with the aim of enhancing patient compliance.

Description

Technical field [0001] The invention relates to an indirubin self-microemulsifying preparation and a preparation method thereof. Background technique [0002] Indirubin is a bis-indole compound extracted from the traditional Chinese medicine Indigo Naturalis. It is an effective ingredient for the treatment of acute and chronic myeloid leukemia. Its water solubility and fat solubility are not ideal, and its oral administration has low bioavailability and slower efficacy. Affect its clinical effect. (Ji Xiujuan, Zhang Furong. Study on the anti-tumor effect and structure-activity relationship of indirubin compounds[J].Acta Pharmaceutica Sinica,1985,20(2):137-139.) Because the gastrointestinal absorption of indirubin belongs to Passive diffusion mechanism can improve its mucosal permeability by improving its solubility. Wu Zhenghong, et al. Transmembrane transport of indirubin self-emulsifying drug delivery system and its pharmacokinetic process in dogs, Chinese Journal of New Drug...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/404A61K9/52A61K47/44A61P35/02
Inventor 杨荣平王云红蒋瑶秦伟瀚刘楠郭响香周文杰
Owner CHONGQING ACAD OF CHINESE MATERIA MEDICA
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