Medicine development and preparation using absorbed and metabolized natural medicine component as main component

A technology of natural medicines and medicines, which is applied to medical preparations containing active ingredients, plant/algae/fungus/moss ingredients, pharmaceutical formulations, etc., and can solve problems such as insignificant effects, difficulty in determining active ingredients, and complex chemical ingredients.

Active Publication Date: 2006-01-04
大连弘毅生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] (1) Although the isolated single compound may have biological activity and can be developed into a drug, it fundamentally loses the essence of the combination and complementarity of the multi-compound pharmacodynamics of traditional Chinese medicine, so this is actually just the westernization of traditional Chinese medicine rather than Modernization of traditional Chinese medicine in the real sense
[0013] (2) Due to the extremely complex chemical composition in traditional Chinese medicine, usually more than one compound has pharmacological effects. In most cases, it is impossible to separate and purify hundreds of compounds and find out the pharmacological mechanism of each compound one by one.
Therefore it is difficult to determine which compounds are necessary active ingredients
Therefore, this method is almost infeasible in most cases, especially for the research of compound Chinese medicine
[0014] (3) Since the absorption and metabolism of the drug by the human body determine which components can have an effect on the body, the monomeric compound obtained by chemical separation in traditional Chinese medicine, even if it is confirmed to have biological activity in the pharmacological test in vitro, but in vivo Often not active at all or exhibit a completely different effect
[0017] In view of the characteristics of unclear structure and insignificant effect of Chinese medicine extracts in the development of medicines that use purified Chinese medicines or monomeric compounds as active ingredients in the prior art, the inventors combined the theories of Chinese medicine serum pharmacology and Chinese medicine metabolic chemistry, Developed a new drug development method using effective metabolites of traditional Chinese medicines in vivo as active ingredients of drugs

Method used

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  • Medicine development and preparation using absorbed and metabolized natural medicine component as main component
  • Medicine development and preparation using absorbed and metabolized natural medicine component as main component
  • Medicine development and preparation using absorbed and metabolized natural medicine component as main component

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] Example 1. Research on the Metabolites of Ginseng Extract (Total Saponins) Rat Intestinal Bacteria and Its Absorption into the Blood

[0069] The main component in ginseng extract (total saponins) is Rb1 (ginsenoside Rb1), which is protopanaxadiol group saponins. According to previous studies by many scholars, Rb1 can be metabolized into a series of compounds under the action of human and rat intestinal bacteria, and its metabolic mode is Rb1→Rd→F2→compound K(C2K)→20(S)protopanaxadiol (aPPD), which is its final metabolite. The purpose of this experiment is to detect the blood components of the metabolites of total saponins. On the basis of previous in vitro and in vivo metabolic studies of intestinal bacteria, the more sensitive electrospray ionization mass spectrometry (Electrospray Ionization Mass Spectrometry, ESIMS) method was used to detect the absorption of metabolites into blood after rats were given total saponins.

[0070] experimental method:

[0071] Drugs...

Embodiment 2

[0080] Example 2: Research on ginseng metabolism and absorption into blood components

[0081] a. Study on the components of Chinese ginseng (Panax ginseng C.A.Meyer) absorbed into the blood by human metabolism

[0082] experimental method:

[0083] Medicines: 20 grams of ginseng is purchased from the market, identified as Chinese ginseng root of Panax ginseng C.A.Meyer6 age;

[0084] Instruments and materials: trypsin, thin-layer chromatography (TLC); Finnigan MAT company LCQ electrospray mass spectrometry (ESI-MS) instrument (USA);

[0085] 20 grams of ginseng was processed into a decoction, which was given to healthy adult volunteers orally, and 20 mL of blood was collected 1.5, 2, 4 and 6 hours after taking the medicine, and 24 hours of urine were collected at the same time. Take 3 mL of the above serum sample, add 10 mL of Tris buffer solution (pH 8) containing 0.001 mol·L-1 CaCl2, put it in a 50 mL iodine bottle, add 10-20 mL of trypsin under stirring, mix well, and ke...

Embodiment 3

[0101] Example 3: aPPD can induce cancer cell apoptosis through multiple mechanisms

[0102] Apoptosis is a very special way of cell death. Experiments have confirmed that, unlike many common anticancer drugs, aPPD can activate multiple tumor killing mechanisms at the same time, and each mechanism can induce cancer cells to enter apoptosis; therefore, aPPD It kills cancer cells in a multi-faceted, multi-targeted manner. Figure 3 shows the typical morphology of apoptosis after the action of aPPD; the group of small vacuoles indicated by the arrows in the figure are apoptotic bodies of cancer cell remains after treatment with aPPD.

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Abstract

The present invention relates to Chinese medicine developing method and its application in preparing medicine, and is especially the medicine developing method with human body or aninal body absorbed and metabolized medicine components as medicine, the application of the method and developed medicine. The medicine developing process includes the following five steps: 1. metabolizing Chinese medicine in biological filtering system to obtain metabolized monomers; 2. separating and identifying the metabolized monomers and separated pharmacological analysis; 3. determining effective monomer components; 4. extracorporeal synthesis or extraction of the effect monomers; and 5. mixing the effective metabolized monomers to obtain new type selective metabolized single-monomer medicine.

Description

technical field [0001] The present invention relates to a development method of a new type of traditional Chinese medicine and its application in the preparation of medicines. In particular, the present invention relates to the metabolism and absorption of traditional Chinese medicines and Chinese medicine compound prescriptions (traditional Chinese medicine varieties identified in the Pharmacopoeia), or natural medicines in humans or animals. A drug development method in which the obtained active ingredient is used as a drug, the application of the method in the preparation of a drug, and the drug obtained by using the method to prepare a metabolite active ingredient as an active ingredient. Background technique [0002] With the development of society, the medical model has changed from simple disease treatment to a combination of prevention, health care, treatment and rehabilitation. Various alternative medicine and traditional medicine are playing an increasingly importan...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/00
Inventor 贾韦国
Owner 大连弘毅生物技术有限公司
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