CN1879649A - Application of chitosan quaternary ammonium salt in absorption of bile acid - Google Patents
Application of chitosan quaternary ammonium salt in absorption of bile acid Download PDFInfo
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- CN1879649A CN1879649A CN 200610013724 CN200610013724A CN1879649A CN 1879649 A CN1879649 A CN 1879649A CN 200610013724 CN200610013724 CN 200610013724 CN 200610013724 A CN200610013724 A CN 200610013724A CN 1879649 A CN1879649 A CN 1879649A
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- chitosan
- quaternary ammonium
- bile acid
- ammonium salt
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Abstract
The invention discloses the use of chitosan quaternary ammonium salts in adsorbing bile acid, wherein the chitosan quaternary ammonium salts include iodine form quaternary ammonium salt of chitosan, N-trimethyl chitosan chloride and 2-hydroxypropyltrimethyl ammonium chloride chitosan.
Description
Technical field
The present invention relates to a kind of application of chitosan quaternary ammonium salt in absorption of bile acid, belong to the chitosan quaternary ammonium salt application technology.
Background technology
Chitosan is made by de-acetyl chitin as an emerging in recent years family macromolecule chemical compound, and reserves are only second to cellulose, have rich in natural resources and cheap price.Chitosan quaternary ammonium salt is that the amino of chitosan is converted to quaternary ammonium salt or a low molecule quaternary ammonium salt is received the amino class chitosan derivatives that obtains of going up by introducing group.Chitosan quaternary ammonium salt is applied to environmental protection flocculating agent, environmental protection antibacterial, paper grade (stock) fluidizer filter aid at present more.Research through decades; find not only avirulence of chitosan; and has an excellent biological compatibility; higher antibacterial and bactericidal activity; especially gastrointestinal mucosa had protective effect; can effectively stop digestive system to absorb cholesterol and triglyceride too much, prevent that cholesterol and fatty acid from accumulating in vivo, promote these materials in body, to discharge.Chitosan is made the adsorbent of hemoperfusion clinically, the materials such as low density lipoprotein, LDL by in the method removing blood of blood purification illustrate that it possesses very high biocompatibility and blood compatibility.After in chitosan, introducing cation group, the electropositive of chitosan quaternary ammonium salt and cation intensity improve greatly, and bile acid possesses stronger anionic group, therefore chitosan quaternary ammonium salt can be made ion exchange resin type as the absorption of bile acid chelating agen, simultaneously because the chitosan excellent biological compatibility has reduced the generation of untoward reaction.
Atherosclerosis is a kind of disease of serious harm human life health, and its characteristics of lesion is that lipid deposits in endarterium in the blood, forms medicated porridge sample thing, makes the arterial wall hardening.It is generally acknowledged that the generation of primary disease and lipid metabolic disorder and hyperlipemia relation is very close.Bile acid is an important metabolite in the human body, be the hyperlipemia main diseases because of.Present antiatherogenic medicine is a lot, mainly based on blood lipid regulation---reduce LDL-C (LDL-C), while high density lipoprotein increasing-cholesterol (HDL-C), represent medicine as influencing the cholesterol absorption medicine, influence cholesterol and triglyceride metabolism medicine, influencing that cholesterol distributes and the transhipment medicine, occurred newtype drug such as HMG-CoA reductase inhibitor etc. in recent years again.There are many untoward reaction in the fat-reducing medicament of clinical practice because medicine time is long, as gastrointestinal reaction and liver dysfunction etc., has limited the performance of curative effect.And oral adsorbent is a kind of Therapeutic Method novel, effective, easy to use, its principle is: after oral adsorbent arrives human body intestinal canal, absorption is accumulated in intravital bile acid, the formation complex excretes, avoid bile acid heavily to be absorbed by intestinal wall, the enterohepatic circulation of blocking-up bile acid is because bile acid is the primary raw material that forms cholesterol, therefore can reach and alleviate the hyperlipemia symptom, suppress the purpose that the state of an illness further worsens.Be applied to the hydrochloric acid colesevelam (colesevelamhydrochloride) that this type of clinical oral adsorbent mainly contains ion exchange resin type bile acid chelating agent-colestyramine (cholestyramine), colestipol (colestipol) and up-to-date listing at present, its principle is by the exchange anionic group, in intestinal, combine with the bile salt anion, forming complex discharges with feces, the enterohepatic circulation of bile acid is interfered, promoted the conversion of cholesterol in hepatocyte, reached effect for reducing fat thereby blood plasma cholesterol level is descended.Such medicine is not absorbed, and does not enter systemic circulation, and is safe and reliable but have simultaneously following shortcoming yet: 1. dosage is excessive and the ammonia stink is arranged, and makes patient be difficult to stand, and is non-critical patient especially, often is reluctant to take medicine; 2. significantly intestines and stomach side effect, as dyspepsia, constipation, feel sick, stomachache, hemorrhoid, anal fissure, hernia aggravation etc., bring difficulty to long-term prescription.
Summary of the invention
The object of the present invention is to provide a kind of application of chitosan quaternary ammonium salt in absorption of bile acid, this chitosan quaternary ammonium salt pair bile acid high adsorption capacity.
The present invention is realized by following technical proposals, a kind of application of chitosan quaternary ammonium salt in absorption of bile acid, and described chitosan quaternary ammonium salt comprises iodate N-N-trimethyl chitosan TMC, chlorination N-N-trimethyl chitosan TMC and hydroxypropyltrimethyl ammonium chloride chitosan.It is characterized in that with this chitosan quaternary ammonium salt be the adsorbents adsorb bile acid.
The invention has the advantages that: convenient sources, cheap, preparation is simple, fast to the bile acid rate of adsorption, binding ability is strong, toxic and side effects is little.
The specific embodiment
With embodiment the present invention is illustrated below.
Example 1
Precision takes by weighing iodate N-N-trimethyl chitosan TMC 50mg and places the 50ml conical flask, the bile acid solution 20ml that adds 3mmol/l, placing 37 ℃ constant temperature oscillator then, utilize furfural-concentrated sulphuric acid method reaction back to measure the absorbance of 60min under 605nm, is 2.4mg/g through calculating absorbability.
Example 2
Precision takes by weighing chlorination N-N-trimethyl chitosan TMC 50mg and places the 50ml conical flask, the bile acid solution 20ml that adds 3mmol/l, placing 37 ℃ constant temperature oscillator then, utilize furfural-concentrated sulphuric acid method reaction back to measure the absorbance of 60min under 605nm, is 2.4mg/g through calculating absorbability.
Example 3
Precision takes by weighing hydroxypropyltrimethyl ammonium chloride chitosan 50mg and places the 50ml conical flask, the natrii tauroglycocholas solution 20ml that adds 3mmol/l, place 37 ℃ constant temperature oscillator then, utilize furfural-concentrated sulphuric acid method reaction back under 605nm, to measure the absorbance of 60min.Through calculating absorbability is 1.0mg/g.
Example 4
At first feed and set up hyperlipemia model of rats with high lipid food, feed with iodate N-N-trimethyl chitosan TMC modeling success back, dosage is fed with 160mg iodate N-N-trimethyl chitosan TMC according to the per kilogram rat every day, after 2 weeks, raise 50% through measuring rat HDL-C, LDL-C reduces by 43.0%, and TC reduces by 27.4%.Illustrate that iodate N-N-trimethyl chitosan TMC has significant lipid-lowering effect to hyperlipemia.
Example 5
Iodate N-N-trimethyl chitosan TMC is carried out acute toxicity testing, and dosage is fed with 4.50g iodate N-N-trimethyl chitosan TMC according to the per kilogram mice every day, and the result shows iodate N-N-trimethyl chitosan TMC avirulence, has the basis of clinical practice.
Claims (1)
1. the application of a chitosan quaternary ammonium salt in absorption of bile acid, described chitosan quaternary ammonium salt comprises iodate N-N-trimethyl chitosan TMC, chlorination N-N-trimethyl chitosan TMC and hydroxypropyltrimethyl ammonium chloride chitosan, it is characterized in that: with this chitosan quaternary ammonium salt is the adsorbents adsorb bile acid.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200610013724 CN1879649A (en) | 2006-05-17 | 2006-05-17 | Application of chitosan quaternary ammonium salt in absorption of bile acid |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200610013724 CN1879649A (en) | 2006-05-17 | 2006-05-17 | Application of chitosan quaternary ammonium salt in absorption of bile acid |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1879649A true CN1879649A (en) | 2006-12-20 |
Family
ID=37518150
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200610013724 Pending CN1879649A (en) | 2006-05-17 | 2006-05-17 | Application of chitosan quaternary ammonium salt in absorption of bile acid |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1879649A (en) |
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2006
- 2006-05-17 CN CN 200610013724 patent/CN1879649A/en active Pending
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| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |