CN103622935A - Preparation method of triptolide nano coating agent - Google Patents
Preparation method of triptolide nano coating agent Download PDFInfo
- Publication number
- CN103622935A CN103622935A CN201310605864.1A CN201310605864A CN103622935A CN 103622935 A CN103622935 A CN 103622935A CN 201310605864 A CN201310605864 A CN 201310605864A CN 103622935 A CN103622935 A CN 103622935A
- Authority
- CN
- China
- Prior art keywords
- preparation
- radix tripterygii
- tripterygii wilfordii
- wilfordii lactone
- film coating
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Landscapes
- Medicinal Preparation (AREA)
Abstract
The invention discloses a preparation method of a triptolide nano coating agent. The triptolide nano coating agent is prepared by the following steps: preparation of nanoparticles, freeze drying, preparation of a sol, and preparation of the nano coating agent. The coating agent prepared by the preparation method disclosed by the invention is convenient to use, so that the long-acting control-released medicine effect can be realized, the bioavailability of the medicine is improved, the use level of the medicine is reduced, the toxic and side effects of triptolide are effectively reduced, and the officinal dosage forms of triptolide are enriched.
Description
Technical field
The invention belongs to the research field of preparation technique of traditional Chinese medicine, be specifically related to the preparation method of Radix Tripterygii Wilfordii lactone alcohol nano-film coating agent.
Background technology
Liniment (film coating agent) is the external use semi-solid varnish that macromolecule filming material and medicine dissolution are made in organic solvent.Liniment is applied to affected part, until organic solvent, can forms thin film on surface, affected part fast after volatilization, affected part is played a protective role, meanwhile, contained drug slowly discharges and plays therapeutical effect, is therefore specially adapted to treating for skin disease.
Radix Tripterygii Wilfordii lactone alcohol (triptolide), claims again Triptolide, triptolide, is from Celastraceae Thunder God Calamus Radix Tripterygii Wilfordii
tripterygium wilfordiihook. F., Tripterygium hypoglaucum
t. hypoglaucuml é vl Hutch., Tripterygium Forretii Dicls
t. forrestiidicls and Tripterygium regelii Spragus et Takeda
t. regeliiisolated Diterpene compound in Sprague et Takrda.Radix Tripterygii Wilfordii lactone alcohol biological activity is stronger, is mainly used in the treatment of the autoimmune diseasees such as rheumatoid arthritis, lupus erythematosus, and has the biological activitys such as antiinflammatory, antitumor.But because it has larger toxic and side effects to digestive system, urinary system and blood system etc., its application is very limited.The present invention adopts Chinese traditional herbs combining nano controlled-release technology, prepares the agent of Radix Tripterygii Wilfordii lactone alcohol nano-film coating, can reduce drug dose, effectively reduces the toxic and side effects of triptolide.
Summary of the invention
The object of the present invention is to provide the preparation method of a kind of Radix Tripterygii Wilfordii lactone alcohol nano-film coating agent, the Radix Tripterygii Wilfordii lactone alcohol nano-film coating agent making is easy to use, can reach the drug effect of long-acting slow-release, improve drug bioavailability, reduce drug dose, effectively reduce the toxic and side effects of triptolide.
For achieving the above object, the present invention adopts following technical scheme:
The agent of Radix Tripterygii Wilfordii lactone alcohol nano-film coating, is characterized in that: its preparation method comprises the following steps:
The preparation of step 1) nanoparticle: Radix Tripterygii Wilfordii lactone alcohol, lecithin and stearic acid are dissolved in organic solvent, stir, add in the aqueous solution containing surfactant, 1.5 * 10
6even 5 times of Pa stimulating milk secretion, solvent evaporated under reduced pressure is separated out nanoparticle from suspended emulsion;
Step 2) lyophilization: adopt vacuum lyophilization, by nanoparticle pre-freeze 1 ~ 3h at-20 ~-40 ℃, then regulate pressure 5 ~ 10Pa, 20 ~ 25 ℃ of dry 15 ~ 20h of temperature, dried Radix Tripterygii Wilfordii lactone alcohol nanoparticle subpackage is standby;
The preparation of step 3) colloidal sol: the Pioloform, polyvinyl acetal of usining mixes as substrate and is added to the water with PEG400,90 ℃ of water-bath swellings are gel, Borneolum Syntheticum, glycerol, azone are added in gel after being dissolved in dehydrated alcohol, are stirred well to completely and dissolve;
The preparation of step 4) nano-film coating agent: nanoparticle is added after dehydrated alcohol redissolution, more dropwise add in colloidal sol, fully stir, obtain colourless thickness clear liquid, by every 10 grams of subpackages, obtain the agent of Radix Tripterygii Wilfordii lactone alcohol nano-film coating.
In step 1), the volume ratio of organic solvent and aqueous solution is 30 ~ 35:10 ~ 12; Described organic solvent comprises acetone, dichloromethane, chloroform;
Step 1) adds Radix Tripterygii Wilfordii lactone alcohol, lecithin and the stearic weight portion in organic solvent to be respectively: 5 ~ 10 parts of Radix Tripterygii Wilfordii lactone alcohols, 50 ~ 56 parts, lecithin, 34 ~ 45 parts of stearic acid;
In aqueous solution, the mass fraction of surfactant is 0.1% ~ 0.3%.
Step 2) in, the diameter of Radix Tripterygii Wilfordii lactone alcohol nanoparticle is 100 ~ 200nm.
In step 3), the mass percent of each component is:
Pioloform, polyvinyl acetal 30 ~ 40%;
PEG400 17~25%；
Water 18 ~ 26%;
Borneolum Syntheticum 1 ~ 3%;
Glycerol 4 ~ 8%;
Azone 1 ~ 3%;
Dehydrated alcohol 10 ~ 16%;
The mass percent sum of each component is 100%.
In step 4), the mass ratio of nanoparticle and dehydrated alcohol is 0.5 ~ 1:1.5 ~ 2.
remarkable advantage of the present invention is:
(1) adopt Chinese traditional herbs combining nano controlled-release technology, can reach the drug effect of long-acting slow-release, improve drug bioavailability, reduce drug dose, effectively reduce the toxic and side effects of triptolide;
(2) Radix Tripterygii Wilfordii lactone alcohol is prepared into liniment and can effectively avoids liver first-pass effect, and interruption of the administration with oneself, adverse effect and toxic and side effects reduced.
The specific embodiment
embodiment mono-
The agent of Radix Tripterygii Wilfordii lactone alcohol nano-film coating, is characterized in that: its preparation method comprises the following steps:
The preparation of step 1) nanoparticle: 0.1g Radix Tripterygii Wilfordii lactone alcohol, 0.6g lecithin and 0.1g stearic acid are dissolved in 150mL acetone, 1.5 * 10
6even 5 times of Pa stimulating milk secretion, adds 100mL to contain in the aqueous solution that mass fraction is 0.1% surfactant, and solvent evaporated under reduced pressure is separated out nanoparticle from suspended emulsion;
Step 2) lyophilization: adopt vacuum lyophilization, by nanoparticle pre-freeze 3h at-20 ℃, then regulate pressure 8Pa, 20 ℃ of dry 15h of temperature, dried Radix Tripterygii Wilfordii lactone alcohol nanoparticle diameter is 100nm, and subpackage is standby;
The preparation of step 3) colloidal sol: the Pioloform, polyvinyl acetal of usining mixes as substrate and is added to the water with PEG400,90 ℃ of water-bath swellings are gel, Borneolum Syntheticum, glycerol, azone are added in gel after being dissolved in dehydrated alcohol, are stirred well to completely and dissolve; In step 3), the mass percent of each component is:
Pioloform, polyvinyl acetal 30%;
PEG400 20%；
Water 26%;
Borneolum Syntheticum 2%;
Glycerol 8%;
Azone 2%;
Dehydrated alcohol 12%;
The preparation of step 4) nano-film coating agent: nanoparticle 100g is added after the redissolution of 300g dehydrated alcohol, more dropwise add in colloidal sol, fully stir, obtain colourless thickness clear liquid, by every 10 grams of subpackages, obtain the agent of Radix Tripterygii Wilfordii lactone alcohol nano-film coating.
embodiment bis-
The agent of Radix Tripterygii Wilfordii lactone alcohol nano-film coating, is characterized in that: its preparation method comprises the following steps:
The preparation of step 1) nanoparticle: 80g Radix Tripterygii Wilfordii lactone alcohol, 550g lecithin and 370g stearic acid are dissolved in 160mL dichloromethane, 1.5 * 10
6even 5 times of Pa stimulating milk secretion, adds 50mL to contain in the aqueous solution that mass fraction is 0.2% surfactant, and solvent evaporated under reduced pressure is separated out nanoparticle from suspended emulsion;
Step 2) lyophilization: adopt vacuum lyophilization, by nanoparticle pre-freeze 2h at-30 ℃, then regulate pressure 10Pa, 23 ℃ of dry 16h of temperature, dried Radix Tripterygii Wilfordii lactone alcohol nanoparticle diameter is 150nm, and subpackage is standby;
The preparation of step 3) colloidal sol: the Pioloform, polyvinyl acetal of usining mixes as substrate and is added to the water with PEG400,90 ℃ of water-bath swellings are gel, Borneolum Syntheticum, glycerol, azone are added in gel after being dissolved in dehydrated alcohol, are stirred well to completely and dissolve; In step 3), the mass percent of each component is:
Pioloform, polyvinyl acetal 35%;
PEG400 17%；
Water 21%;
Borneolum Syntheticum 3%;
Glycerol 5%;
Azone 3%;
Dehydrated alcohol 16%;
The preparation of step 4) nano-film coating agent: nanoparticle 160g is added after the redissolution of 340g dehydrated alcohol, more dropwise add in colloidal sol, fully stir, obtain colourless thickness clear liquid, by every 10 grams of subpackages, obtain the agent of Radix Tripterygii Wilfordii lactone alcohol nano-film coating.
embodiment tri-
The agent of Radix Tripterygii Wilfordii lactone alcohol nano-film coating, is characterized in that: its preparation method comprises the following steps:
The preparation of step 1) nanoparticle: 10og Radix Tripterygii Wilfordii lactone alcohol, 56og lecithin and 340g stearic acid are dissolved in 175mL chloroform, 1.5 * 10
6even 5 times of Pa stimulating milk secretion, adds 60mL to contain in the aqueous solution that mass fraction is 0.3% surfactant, and solvent evaporated under reduced pressure is separated out nanoparticle from suspended emulsion;
Step 2) lyophilization: adopt vacuum lyophilization, by nanoparticle pre-freeze 1h at-40 ℃, then regulate pressure 5Pa, 25 ℃ of dry 20h of temperature, dried Radix Tripterygii Wilfordii lactone alcohol nanoparticle diameter is 200nm, and subpackage is standby;
The preparation of step 3) colloidal sol: the Pioloform, polyvinyl acetal of usining mixes as substrate and is added to the water with PEG400,90 ℃ of water-bath swellings are gel, Borneolum Syntheticum, glycerol, azone are added in gel after being dissolved in dehydrated alcohol, are stirred well to completely and dissolve; In step 3), the mass percent of each component is:
Pioloform, polyvinyl acetal 40%;
PEG400 25%；
Water 18%;
Borneolum Syntheticum 1%;
Glycerol 4%;
Azone 1%;
Dehydrated alcohol 11%;
The preparation of step 4) nano-film coating agent: nanoparticle 200g is added after the redissolution of 400g dehydrated alcohol, more dropwise add in colloidal sol, fully stir, obtain colourless thickness clear liquid, by every 10 grams of subpackages, obtain the agent of Radix Tripterygii Wilfordii lactone alcohol nano-film coating.
Radix Tripterygii Wilfordii lactone alcohol nano-film coating agent solvent evaporates prepared by the present invention is fast, good permeability, and drug treating time is long, and the treatment of rheumatoid arthritis, lupus erythematosus is had to good curative effect, and toxic and side effects reduces.
The foregoing is only preferred embodiment of the present invention, all equalizations of doing according to the present patent application the scope of the claims change and modify, and all should belong to covering scope of the present invention.
Claims (7)
1. the preparation method of Radix Tripterygii Wilfordii lactone alcohol nano-film coating agent, is characterized in that: described preparation method comprises the following steps:
The preparation of step 1) nanoparticle: Radix Tripterygii Wilfordii lactone alcohol, lecithin and stearic acid are dissolved in organic solvent, stir, add in the aqueous solution containing surfactant, 1.5 * 10
6even 5 times of Pa stimulating milk secretion, solvent evaporated under reduced pressure is separated out nanoparticle from suspended emulsion;
Step 2) lyophilization: adopt vacuum lyophilization, by nanoparticle pre-freeze 1 ~ 3h at-20 ~-40 ℃, then regulate pressure 5 ~ 10Pa, 20 ~ 25 ℃ of dry 15 ~ 20h of temperature, dried Radix Tripterygii Wilfordii lactone alcohol nanoparticle subpackage is standby;
The preparation of step 3) colloidal sol: the Pioloform, polyvinyl acetal of usining mixes as substrate and is added to the water with PEG400,90 ℃ of water-bath swellings are gel, Borneolum Syntheticum, glycerol, azone are added in gel after being dissolved in dehydrated alcohol, are stirred well to completely and dissolve;
The preparation of step 4) nano-film coating agent: nanoparticle is added after dehydrated alcohol redissolution, more dropwise add in colloidal sol, fully stir, obtain colourless thickness clear liquid, by every 10 grams of subpackages, obtain the agent of Radix Tripterygii Wilfordii lactone alcohol nano-film coating.
2. the preparation method of Radix Tripterygii Wilfordii lactone alcohol nano-film coating according to claim 1 agent, is characterized in that: in step 1), the volume ratio of organic solvent and aqueous solution is 30 ~ 35:10 ~ 12; Described organic solvent comprises acetone, dichloromethane, chloroform.
3. the preparation method of Radix Tripterygii Wilfordii lactone alcohol nano-film coating according to claim 1 agent, it is characterized in that: step 1) adds Radix Tripterygii Wilfordii lactone alcohol, lecithin and the stearic weight portion in organic solvent to be respectively: 5 ~ 10 parts of Radix Tripterygii Wilfordii lactone alcohols, 50 ~ 56 parts, lecithin, 34 ~ 45 parts of stearic acid; In aqueous solution, the mass fraction of surfactant is 0.1% ~ 0.3%.
4. the preparation method of Radix Tripterygii Wilfordii lactone alcohol nano-film coating according to claim 1 agent, is characterized in that: step 2) in the diameter of Radix Tripterygii Wilfordii lactone alcohol nanoparticle be 100 ~ 200nm.
5. the preparation method of Radix Tripterygii Wilfordii lactone alcohol nano-film coating according to claim 1 agent, is characterized in that: in step 3), the mass percent of each component is:
Pioloform, polyvinyl acetal 30 ~ 40%;
PEG400 17~25%；
Water 18 ~ 26%;
Borneolum Syntheticum 1 ~ 3%;
Glycerol 4 ~ 8%;
Azone 1 ~ 3%;
Dehydrated alcohol 10 ~ 16%;
The mass percent sum of each component is 100%.
6. the preparation method of Radix Tripterygii Wilfordii lactone alcohol nano-film coating according to claim 1 agent, is characterized in that: in step 4), the mass ratio of nanoparticle and dehydrated alcohol is 0.5 ~ 1:1.5 ~ 2.
7. the Radix Tripterygii Wilfordii lactone alcohol nano-film coating agent that the preparation method of a Radix Tripterygii Wilfordii lactone alcohol nano-film coating as claimed in claim 1 agent makes.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310605864.1A CN103622935B (en) | 2013-11-26 | 2013-11-26 | The preparation method of Radix Tripterygii Wilfordii lactone alcohol nano-film coating agent |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310605864.1A CN103622935B (en) | 2013-11-26 | 2013-11-26 | The preparation method of Radix Tripterygii Wilfordii lactone alcohol nano-film coating agent |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103622935A true CN103622935A (en) | 2014-03-12 |
| CN103622935B CN103622935B (en) | 2015-10-28 |
Family
ID=50204624
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310605864.1A Expired - Fee Related CN103622935B (en) | 2013-11-26 | 2013-11-26 | The preparation method of Radix Tripterygii Wilfordii lactone alcohol nano-film coating agent |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103622935B (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103908484A (en) * | 2014-03-20 | 2014-07-09 | 浙江工业大学 | Tripterygium wilfordii plastic for treating rheumatoid arthritis and preparation method thereof |
| CN105434446A (en) * | 2015-11-21 | 2016-03-30 | 中南大学湘雅医院 | Triptolide traditional Chinese medicine compound film coating agent and preparation method and application thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1543932A (en) * | 2003-11-25 | 2004-11-10 | 华中科技大学 | Application of solid lipid nanoparticles in the preparation of drugs for iontophoresis transdermal delivery |
| CN101658545A (en) * | 2009-09-16 | 2010-03-03 | 中国药科大学 | Preparation method of tripterygium glycosides solid lipid nanoparticle |
| CN101991585A (en) * | 2009-08-25 | 2011-03-30 | 福建省医学科学研究所 | Percutaneous absorption film coating agent for treating rheumatoid arthritis and preparation method thereof |
-
2013
- 2013-11-26 CN CN201310605864.1A patent/CN103622935B/en not_active Expired - Fee Related
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1543932A (en) * | 2003-11-25 | 2004-11-10 | 华中科技大学 | Application of solid lipid nanoparticles in the preparation of drugs for iontophoresis transdermal delivery |
| CN101991585A (en) * | 2009-08-25 | 2011-03-30 | 福建省医学科学研究所 | Percutaneous absorption film coating agent for treating rheumatoid arthritis and preparation method thereof |
| CN101658545A (en) * | 2009-09-16 | 2010-03-03 | 中国药科大学 | Preparation method of tripterygium glycosides solid lipid nanoparticle |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103908484A (en) * | 2014-03-20 | 2014-07-09 | 浙江工业大学 | Tripterygium wilfordii plastic for treating rheumatoid arthritis and preparation method thereof |
| CN103908484B (en) * | 2014-03-20 | 2017-05-03 | 浙江工业大学 | Tripterygium wilfordii plastic for treating rheumatoid arthritis and preparation method thereof |
| CN105434446A (en) * | 2015-11-21 | 2016-03-30 | 中南大学湘雅医院 | Triptolide traditional Chinese medicine compound film coating agent and preparation method and application thereof |
| CN105434446B (en) * | 2015-11-21 | 2018-03-02 | 中南大学湘雅医院 | Triptolide traditional Chinese medicine compound film coating agent and preparation method and application thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| CN103622935B (en) | 2015-10-28 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| TW201002334A (en) | Andrographis paniculata extract | |
| CN103655519A (en) | Curcumin solid lipid nanoparticle with P-gp inhibiting effect and preparation method thereof | |
| CN103622935B (en) | The preparation method of Radix Tripterygii Wilfordii lactone alcohol nano-film coating agent | |
| WO2017092230A1 (en) | Biflavone compound and uses thereof for treating cancers and preparing drugs | |
| RU2016150868A (en) | ORAL PHARMACEUTICAL COMPOSITION OF ISOTRETINOIN | |
| JP2015522649A5 (en) | ||
| CN105748436B (en) | Paeonol vesicle cream for external use and preparation method thereof | |
| WO2017070515A3 (en) | Methods of preventing and treating inflammatory bowel disease with branched fatty acid esters of hydroxy fatty acids (fahfas) | |
| JP2015511618A5 (en) | ||
| CN102716080B (en) | Suspension containing andrographolide solid lipid nanoparticles as well as preparation method and application of suspension | |
| CN102525954B (en) | Lyophilized emulsion preparation for injection of levo-gossypol and acetate of levo-gossypol | |
| CN105853378A (en) | Resveratrol trinocotinate nanocrystal quick release capsule preparation and preparation technology thereof | |
| CN105816428B (en) | A kind of triptolide nano liposomes and preparation method thereof | |
| RU2016103313A (en) | LIPID NANOPARTICLE WITH POLYMIXINS | |
| CN107929265A (en) | Preparation method of medicinal transdermal material | |
| CN103405383B (en) | Clindamycin phosphate gel and preparation method thereof | |
| CN104825466A (en) | Applications of cleistanone O-(benzimidazolyl) ethyl derivative in preparation of drugs for preventing or treating pancreatic fibrosis | |
| WO2016161683A1 (en) | Statin pharmaceutical composition, and capsule formulation and preparation method thereof | |
| CN102512371A (en) | Preparation method for forsythiaside lipidosome | |
| CN104667284B (en) | Oleanolic acid is used to modify application of the Emodin Liposome in medicine is prepared | |
| CN104188974A (en) | Application of 2-methoxyestradiol in treatment of systemic lupus erythematosus | |
| Lee et al. | Eupatilin ameliorates cathelicidin-induced skin inflammation in mouse model of rosacea | |
| Xu et al. | Synthesis and potent cytotoxic activity of diosgenin derivative FZU-0021-194-P2 and its phytosomes against non-small-cell lung cancer cells | |
| CN104825522A (en) | Application of safflower extract in preparation of 5 alpha-reductase inhibitors | |
| Deng et al. | Extraction issues of paclitaxel in nanocrystals |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20151028 Termination date: 20191126 |
|
| CF01 | Termination of patent right due to non-payment of annual fee |