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A kind of metabolism and efflux dual-inhibition anpentesin nanoemulsion and its preparation method

An pentogen and nanoemulsion technology, which can be used in metabolic diseases, pharmaceutical formulations, emulsion delivery, etc., can solve the problems of limited clinical application value, low bioavailability, and poor water solubility of pentogen, and achieve widen clinical application. Application value, non-irritating, beneficial to promotion and application

Inactive Publication Date: 2020-11-03
GUANGZHOU JINAN BIOMEDICINE RES & DEV CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, the currently extracted anpentapene has poor water solubility, and is easily metabolized by metabolic enzymes in the body to generate secondary metabolites, resulting in extremely low bioavailability, which greatly limits its clinical application value

Method used

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  • A kind of metabolism and efflux dual-inhibition anpentesin nanoemulsion and its preparation method
  • A kind of metabolism and efflux dual-inhibition anpentesin nanoemulsion and its preparation method
  • A kind of metabolism and efflux dual-inhibition anpentesin nanoemulsion and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Embodiment 1, a kind of metabolism and efflux dual-inhibition type anpentene nanoemulsion

[0037] The metabolism and efflux double-inhibited anpentesin nanoemulsion consists of the following components and their contents:

[0038] Anpentapene 30mg, sodium oleate 120mg, soybean lecithin 100mg and medium chain triglyceride 1000mg.

[0039] Preparation:

[0040] S1 Weigh sodium oleate and add it into ultrapure water, the solid-to-liquid ratio of the sodium oleate to the ultrapure water is 16mg:1ml, ultrasonically treat until the sodium oleate is completely dissolved, and the ultrasonic frequency is 20KHz to obtain an aqueous phase;

[0041] S2 Mix anpentapene, soybean lecithin and medium-chain triglycerides uniformly to obtain a mixture I, then add dehydrated ethanol to the mixture I, the solid-to-liquid ratio of the dehydrated alcohol and the mixture I is 2.19g:5ml , ultrasonic treatment for 3 to 6 minutes until completely dissolved, the ultrasonic frequency is 20KHz, ...

Embodiment 2

[0044] Embodiment 2, a kind of metabolism and efflux dual inhibition type anpentene nanoemulsion

[0045] The metabolism and efflux dual-inhibition anpentapene nanoemulsion consists of the following components and parts by weight:

[0046] Anpentapene 40mg, sodium oleate 160mg, soybean lecithin 150mg and medium chain triglyceride 2000mg.

[0047] The preparation method is similar to Example 1.

Embodiment 3

[0048] Embodiment 3, a kind of metabolism and efflux dual-inhibition type anpentene nanoemulsion

[0049] The metabolism and efflux dual-inhibition anpentapene nanoemulsion consists of the following components and parts by weight:

[0050]Anpentapene 50mg, sodium oleate 180mg, soybean lecithin 200mg and medium chain triglyceride 3000mg.

[0051] The preparation method is similar to Example 1.

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Abstract

The invention belongs to the technical field of medicine preparations and in particular relates to a metabolism and excretion dual inhibition type anwuligan nano emulsion and a preparation method thereof. The metabolism and excretion dual inhibition type anwuligan nano emulsion provided by the invention mainly consists of anwuligan, sodium oleate, soybean lecithin and medium chain triglyceride. Byadopting the metabolism and excretion dual inhibition type anwuligan nano emulsion provided by the invention, the consequence that anwuligan is metabolized by metabolic enzymes in bodies to generatesecondary metabolite can be avoided, anwuligan excretion can be also avoided, the bioavailability of the anwuligan can be improved, meanwhile, the anwuligan nano emulsion has the advantages of being good in stability and high in solubility, and the clinical application values of the anwuligan are greatly increased.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a double-inhibited metabolism and efflux anpentesin nanoemulsion and a preparation method thereof. Background technique [0002] Nutmeg is the dry seed kernel of the Myristicaceae plant Nutmeg. It has the effects of warming the middle and promoting qi, astringent intestines and relieving diarrhea. It is used in the treatment of digestive disorders, vomiting, diarrhea, rheumatism, cholera, flatulence, palpitation and mental confusion. Modern research has found that anpentapene is the main functional ingredient in nutmeg, and the structural formula of anpentapene is: [0003] Anpentesin has been proven to have a wide range of pharmacological activities, such as antibacterial, anti-inflammatory, anti-cancer, anti-diabetic, liver protection, etc.; more importantly, it also has the effect of protecting nerves, and has a role in neurodegenerative dise...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/36A61K47/12A61P1/16A61P3/10A61P25/28A61P29/00A61P31/04A61P35/00
CPCA61K9/1075A61K31/36A61K47/12A61P1/16A61P3/10A61P25/28A61P29/00A61P31/04A61P35/00
Inventor 王一飞董栋王巧利吴宝剑李志杰全恩希
Owner GUANGZHOU JINAN BIOMEDICINE RES & DEV CENT