CN1858070A - Use of trimethyl chitosan - Google Patents
Use of trimethyl chitosan Download PDFInfo
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- CN1858070A CN1858070A CN 200610019277 CN200610019277A CN1858070A CN 1858070 A CN1858070 A CN 1858070A CN 200610019277 CN200610019277 CN 200610019277 CN 200610019277 A CN200610019277 A CN 200610019277A CN 1858070 A CN1858070 A CN 1858070A
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- trimethyl chitin
- transdermal
- trimethyl
- transdermal absorption
- absorption enhancer
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Abstract
The present invention discloses the use of trimethyl chitosan. Trimethyl chitosan in quaternary ammoniation degree of 40%-60% is used as transdermal absorption promoter in transdermal absorption system. The extracorporeal and intracorporeal transdermal experiments show that trimethyl chitosan in quaternary ammoniation degree of 40%-60% is water soluble and high in biocompatibility, can promote the transdermal absorption of medicine effectively, and may be used as transdermal absorption promoter in transdermal absorption system.
Description
Technical field
The present invention relates to a kind of purposes of trimethyl chitin, belong to polymer chemistry and field of medicaments.
Background technology
Percutaneous absorption enhancer (penetration enhancers) is meant that those can reduce the percutaneous resistance of medicine, quicken the material of medicine transdermal, be transdermal absorption system (Transdermal TherapeuticSystem, TTS) in indispensable integral part.To development, the exploitation of novel Percutaneous absorption enhancer, can promote the development of TTS at pharmacy field, for many chronic diseases and topical therapeutic and prevention provides simply, convenient and effective preparation variety, have broad application prospects.
At present, Chang Yong Percutaneous absorption enhancer can be divided into following a few class: 1. tensio-active agent: cationics, anionic agent, non-ionic type and Yelkin TTS; 2. organic solvent class: ethanol, propylene glycol, ethyl acetate, dimethyl sulfoxide (DMSO) and dimethyl formamide; 3. laurocapram and homologue thereof; 4. organic acid, lipid acid: oleic acid, linolic acid and lauryl alcohol; 5. cutin is preserved moisture and tenderizer: urea, Whitfield's ointment and pyrrolones; 6. terpenes: menthol, camphor, limonene etc.Amino acid and some water soluble proteins, phosphatide and drug-loaded liposome also can increase the skin absorption of many medicines.But all there is weak point separately respectively in these Percutaneous absorption enhancers commonly used, and for example life-time service can have pungency, whole body absorption meeting toxic to organ in the health to skin, and production cost is more high.
Summary of the invention
The objective of the invention is to deficiency at Percutaneous absorption enhancer existence commonly used in the prior art, a kind of new purposes of trimethyl chitin is provided, be about to quaternary ammoniated degree and be 40%～60% trimethyl chitin as Percutaneous absorption enhancer, no matter quaternary ammoniated degree is neutral, acid, or all can promote medicine to pass through intercellular transhipment of keratoderma and the high advantage of biological safety in the alkaline environment if being that 40%～60% trimethyl chitin has as Percutaneous absorption enhancer.
The technical scheme that realizes the object of the invention is: with general formula of molecular structure be:
, quaternary ammoniated degree is that 40%～60% trimethyl chitin is used for transdermal absorption system, as Percutaneous absorption enhancer.
And the quaternary ammoniated degree as the trimethyl chitin of Percutaneous absorption enhancer is preferably 60%, and quaternary ammoniated degree is 60% trimethyl chitin (TMC60) when using as Percutaneous absorption enhancer, and its mass percentage content is 1～20%.
Trimethyl chitin (N-trimethyl chitosan, TMC) be chitosan (molecular structural formula is as follows for chitosan, a kind of artificial-synthesis derivant CS):
The present invention adopt ATR-FTIR spectrum and the method research TMC that deconvolutes to the keratic effect of stratum corneum, through studies show that in a large number, no matter be neutral, acid, still in the alkaline environment, TMC all can promote medicine to pass through the intercellular transhipment of keratoderma, thereby improve in the absorption and the bioavailability, particularly neutrality and alkaline environment of medicine, promoter action is better than CS and its esters.The mechanism of action of TMC be positively charged on the C-2 position of protonated TMC quaternary ammonium group can with the electronegative composition effect of skin keratin confluent monolayer cells, thereby opening iuntercellular combines closely, promote the absorption of medicine greatly, this mechanism of action has illustrated that also TMC promotes that the size of sorption is relevant with its quaternary ammoniated degree, quaternary ammoniated degree is high more, the TMC positive charge is many more, promotes that sorption is strong more.And the inside and outside toxicological effect studies show that TMC is high as the biological safety of absorption enhancer, and itself can not be absorbed, and does not disturb the corneocyte film, so almost there is not any cytotoxicity.Therefore TMC can be used as a kind of novel Percutaneous absorption enhancer, is used for not containing the various TTS of anionic component.And through we a large amount of contrast experiment, show that quaternary ammoniated degree is that 40%～60% trimethyl chitin is used for transdermal absorption system, result of use as Percutaneous absorption enhancer is better, particularly mass percentage content be 1～20%, quaternary ammoniated degree be 60% trimethyl chitin TMC60 during as Percutaneous absorption enhancer its promoter action especially remarkable.
Embodiment
Embodiment is with the positive contrast of azone, and testosterone is a model drug, by the inside and outside transdermal experiment, has verified that quaternary ammoniated degree is 40%, 60% TMC, and promptly TMC40, TMC60 are to the infiltration promoter action of skin.
Embodiment 1
The preparation of model drug testosterone gel: get an amount of TMC60 and testosterone respectively and at room temperature be dissolved in 67% ethanol, be cooled to 4 ℃, again poloxamer P407 slowly is added in the solution, continuously stirring, 4 ℃ of placements form until settled solution.Each component content is respectively in the gel: testosterone: P407: TMC60 (1: 25: 5).By the inside and outside transdermal experiment, show that TMC60 is soluble in water, good biocompatibility can effectively promote to can be used as the Transdermal absorption of medicine novel cutaneous permeable agent and be used for TTS.
Embodiment 2
Get an amount of TMC40 by the step of embodiment 1 and prepare the model drug testosterone gel, by the inside and outside transdermal experiment, show that TMC40 is soluble in water, good biocompatibility, can promote the Transdermal absorption of medicine, can be used as novel cutaneous permeable agent and be used for TTS, but the percutaneous rate of the Transdermal absorption of promotion medicine is lower slightly than TMC60.
Claims (3)
1, a kind of purposes of trimethyl chitin, the general formula of molecular structure of this trimethyl chitin is:
, it is characterized in that: quaternary ammoniated degree is that 40%～60% trimethyl chitin is used for transdermal absorption system, as Percutaneous absorption enhancer.
2, the purposes of trimethyl chitin according to claim 1 is characterized in that: the optimum value as the quaternary ammoniated degree of the trimethyl chitin of Percutaneous absorption enhancer is 60%.
3, the purposes of trimethyl chitin according to claim 1 and 2 is characterized in that: quaternary ammoniated degree is 60% trimethyl chitin (TMC60) when using as Percutaneous absorption enhancer, and its mass percentage content is 1～20%.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200610019277 CN1858070A (en) | 2006-06-07 | 2006-06-07 | Use of trimethyl chitosan |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200610019277 CN1858070A (en) | 2006-06-07 | 2006-06-07 | Use of trimethyl chitosan |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1858070A true CN1858070A (en) | 2006-11-08 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200610019277 Pending CN1858070A (en) | 2006-06-07 | 2006-06-07 | Use of trimethyl chitosan |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1858070A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104798823A (en) * | 2015-04-30 | 2015-07-29 | 山东大学齐鲁医院 | Bactericide for clinical laboratory |
-
2006
- 2006-06-07 CN CN 200610019277 patent/CN1858070A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104798823A (en) * | 2015-04-30 | 2015-07-29 | 山东大学齐鲁医院 | Bactericide for clinical laboratory |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
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| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |