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CN1562275A - Stauntonvine general glycoside and injection - Google Patents

Stauntonvine general glycoside and injection Download PDF

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Publication number
CN1562275A
CN1562275A CN 200410026547 CN200410026547A CN1562275A CN 1562275 A CN1562275 A CN 1562275A CN 200410026547 CN200410026547 CN 200410026547 CN 200410026547 A CN200410026547 A CN 200410026547A CN 1562275 A CN1562275 A CN 1562275A
Authority
CN
China
Prior art keywords
caulis
injection
folium stauntoniae
sodium
general glycoside
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.)
Pending
Application number
CN 200410026547
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Chinese (zh)
Inventor
傅卫国
王伟
曾韶辉
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
GUANGZHOU ANJIAN INDUSTRIAL DEVELOPMENT Co Ltd
Original Assignee
GUANGZHOU ANJIAN INDUSTRIAL DEVELOPMENT Co Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by GUANGZHOU ANJIAN INDUSTRIAL DEVELOPMENT Co Ltd filed Critical GUANGZHOU ANJIAN INDUSTRIAL DEVELOPMENT Co Ltd
Priority to CN 200410026547 priority Critical patent/CN1562275A/en
Publication of CN1562275A publication Critical patent/CN1562275A/en
Pending legal-status Critical Current

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Abstract

A papaside and its injection is prepared from wild papaya through extracting in alcohol to obtain the papaside, and preparing its injection or the injection of its water-soluble salt.

Description

Caulis et folium stauntoniae general glycoside and injection thereof
Technical field
The present invention relates to a kind of injection of forming by effective site Caulis et folium stauntoniae general glycoside or its water soluble salt of Lardizabalaceae plant Caulis et folium stauntoniae.
Background technology
Caulis et folium stauntoniae (Stauntonia chinensis DC) has another name called false Fructus Litchi, around tievine, be Lardizabalaceae Caulis et folium stauntoniae platymiscium.Pharmacological evaluation proof Caulis et folium stauntoniae whole plant and extract thereof all have analgesia, calmness and spasmolysis, are used for the treatment of rheumatic arthritis, traumatic injury, various neuropathic pains.But life-time service and continuous use, dosage becomes positive correlation with effectiveness, and analgesic activity does not influence people's consciousness and sensation, has no drug resistance, addiction is not a kind of effective Chinese medicine analgesic.Having gone on the market at present, to be used for clinical injection be stauntonvine injection, is to make with the method for traditional water extract-alcohol precipitation with crude drug, and extracts active ingredients is incomplete, the impurity content height.The different places of production, the raw materials quality difference in different picking seasons is bigger, makes that quality and the curative effect between each batch of stauntonvine injection is all stable inadequately.And side effect is big, has certain potential safety hazard.
Therefore,, be necessary to develop a kind of quality and curative effect and all stablize at the above-mentioned shortcoming of stauntonvine injection, and the little injection of forming by Caulis et folium stauntoniae effective site of side effect.
Summary of the invention
The object of the present invention is to provide a kind of injection of forming by the effective site Caulis et folium stauntoniae general glycoside of Caulis et folium stauntoniae
The present invention is achieved in that
Caulis et folium stauntoniae total glycoside injection of the present invention is to be made by following raw material:
Caulis et folium stauntoniae general glycoside or its water soluble salt
Injection additive commonly used; Comprise polysorbas20 or polysorbate40 or Tween 80 or, water for injection or polyvinylpyrrolidone or yolk phospholipid or lecithin or NaTDC or pluronic F-86 or acetic acid or sodium acetate or citric acid or sodium citrate or lactic acid or tartaric acid or sodium tartrate or sodium hydrogen phosphate or sodium dihydrogen phosphate or sodium carbonate or sodium acid carbonate or sodium carbonate or or gelatin or methylcellulose or sodium cellulose glycolate or pectin or sorbierite or creatinine or glycine or nicotinic acid amide or sodium sulfite or sodium hydrogensulfite or sodium pyrosulfite or phenmethylol or butyl p-hydroxybenzoate or ethyl-para-hydroxybenzoate or phenol or anesin or procaine hydrochloride or lidocaine or above material in two or more.
These adjuvants are respectively solubilizing agent, wetting agent, buffer agent, stabilizing agent, antioxidant, antibacterial, local anesthetic'ss (analgesic) commonly used in the injection.
With two or more raw material mix homogeneously, even with solvent, packing, Caulis et folium stauntoniae general glycoside injection is made in sterilization.
With two or more raw material mix homogeneously, lyophilization or sterilization solvent crystallization or spray drying are made the Caulis et folium stauntoniae injectable sterile powder.
Two or more raw materials are mixed, even with the solvent preparation, filter, embedding forms the transfusion of Caulis et folium stauntoniae general glycoside
Solvent in above-mentioned injection and the transfusion comprises the injection common solvent, i.e. water for injection or oil for injection or ethanol or glycerol or propylene-glycol-based Polyethylene Glycol or mannitol or benzyl benzoate or dimethyl acetylamide.
The used Caulis et folium stauntoniae general glycoside of Caulis et folium stauntoniae general glycoside injection of the present invention is to make in order to the below method: get Caulis et folium stauntoniae (whole plant) coarse powder, at first the rare alcohol with 5-20 times of volume of Caulis et folium stauntoniae coarse powder soaked Caulis et folium stauntoniae 2-12 hour, reflux, extract, is 1-5 time then, merge extractive liquid,, rare alcohol is reclaimed in distilling under reduced pressure, get the rare alcohol extract of Caulis et folium stauntoniae, get rare alcohol extract of 1 part of thing Caulis et folium stauntoniae then, get combining extraction liquid 1-5 time with the mixed extractant solvent of two or more compositions of the doubly water saturated butanols of reuse 1-10 or amylalcohol or hexanol or enanthol or capryl alcohol or nonyl alcohol or decanol or above various pure apoplexy due to endogenous wind behind the water dissolution of 1-10 branch.Obtain the Caulis et folium stauntoniae general glycoside behind the vacuum distillation recovered solvent.Or get commercially available Caulis et folium stauntoniae and mention 1 part of thing, with the mixed extractant solvent of two or more compositions of the doubly water saturated butanols of reuse 1-10 behind the water dissolution of 1-10 part or amylalcohol or hexanol or enanthol or capryl alcohol or nonyl alcohol or decanol or above various pure apoplexy due to endogenous wind 1-5 time, combining extraction liquid.Obtain the Caulis et folium stauntoniae general glycoside behind the vacuum distillation recovered solvent.In preparation preparation process, get the Caulis et folium stauntoniae general glycoside and add suitable quantity of water, hydro-oxidation sodium or potassium hydroxide solution to solution is the clarification shape and promptly gets Caulis et folium stauntoniae general glycoside water soluble salt then.
The present invention is guidance with the pharmacological evaluation, by extract Caulis et folium stauntoniae effective site Caulis et folium stauntoniae general glycoside with special solvent, and make injection, reduced impurity in injection content and improved content of effective, the quality of injection and curative effect be improved
Pharmacological action
17-19 restrains female mice, is placed on before the test on 55 ± 0.5 ℃ of thermostat water baths, licks the index of metapedes as pain reaction with mice, measures the pain threshold of mice, rejects irritated and unresponsive mice (less than 10 seconds, greater than 30 seconds persons).To predict that qualified mice is divided into 3 groups, every group 10, give lumbar injection Caulis et folium stauntoniae general glycoside injection, stauntonvine injection and normal saline respectively, measure its pain reaction after 1 hour, compare the threshold of pain, medication front and back difference with statistical method, Caulis et folium stauntoniae general glycoside injection shows the analgesic effect (P<0.05) that is better than stauntonvine injection significantly as a result.
The specific embodiment:
The preparation method of Caulis et folium stauntoniae general glycoside raw material
1, with 75% soak with ethanol Caulis et folium stauntoniae of 20 times of volumes of Caulis et folium stauntoniae 12 hours, reflux, extract, was 4 times then, merge extractive liquid,, ethanol is reclaimed in distilling under reduced pressure, rare alcohol extract.Get 1 part of rare alcohol extract then, be dissolved in 3 parts of water, again with 3 parts of water saturated n-butanol extractions 5 times, combining extraction liquid, the reclaim under reduced pressure n-butyl alcohol, the gained solid drying is pulverized, and promptly gets Caulis et folium stauntoniae effective site Caulis et folium stauntoniae general glycoside.
2, the preparation method of Caulis et folium stauntoniae general glycoside injection
The preparation of Caulis et folium stauntoniae general glycoside raw material is with embodiment 1.
Prescription 1:
Caulis et folium stauntoniae general glycoside 200g
Polysorbas20 1g
Water for injection is added to 2000ml
Make 1000 every altogether and contain principal agent 200mg
Prescription 2:
Caulis et folium stauntoniae general glycoside 200g
Polysorbate40 1g
Carboxymethyl cellulose sodium 1g
Add ethanol to 2000ml
Make 1000 altogether, every contains principal agent 200mg
Prescription 3:
Caulis et folium stauntoniae general glycoside 200g
Tween 80 1g
Methylcellulose 1g
Add Polyethylene Glycol to 2000g
Make 1000 altogether, every contains principal agent 200mg
The Caulis et folium stauntoniae general glycoside is added an amount of water for injection, add the adjuvant of recipe quantity, mixes all, fully dissolving adds the injection water to recipe quantity, filters, and embedding is sterilized, promptly.
Prescription 4:
Caulis et folium stauntoniae general glycoside 200g
1% sodium hydroxide solution is an amount of
Water for injection is added to 2000ml
Make 1000 every altogether and contain principal agent 200mg
The Caulis et folium stauntoniae general glycoside is added an amount of water for injection, and it is clear and bright to solution to add 1% sodium hydroxide solution, adds the injection water to recipe quantity, and fully dissolving filters, embedding, and sterilization, promptly.
3, the preparation method of Caulis et folium stauntoniae general glycoside injectable sterile powder
The preparation of Caulis et folium stauntoniae general glycoside raw material is with embodiment 1.
Prescription 1:
Caulis et folium stauntoniae general glycoside 200g
Mannitol 140g
Benzyl alcohol 20g
Make 1000 altogether
Prescription 2:
Caulis et folium stauntoniae general glycoside 200g
Mannitol 140g
Ethylparaben 0.2
Make 1000 every altogether and contain principal agent amount 200mg
Prescription 3:
Caulis et folium stauntoniae general glycoside 200g
Mannitol 140g
Lignocaine 1g
Glycine 2g
Make 1000 every altogether and contain principal agent 200mg
Being prepared as of Caulis et folium stauntoniae general glycoside injectable sterile powder: with the adjuvant mix homogeneously of purified Caulis et folium stauntoniae general glycoside raw material and recipe quantity, lyophilization, packing (before the packing with bottle and plug sterilization) replenishes sterilization, pack Caulis et folium stauntoniae general glycoside injectable sterile powder.4, the preparation method of Caulis et folium stauntoniae general glycoside transfusion
Prescription 1:
Caulis et folium stauntoniae general glycoside 0.2g
Water for injection 100g
Ethylparaben 0.01g
Creatinine 0.7g
Make the 100ml/ bottle
Prescription 2:
The total Saponin 0.2g of Caulis et folium stauntoniae
Water for injection 100g
Benzyl alcohol 1g
Glycine 1.5g
Make the 100ml/ bottle
Prescription 3:
Caulis et folium stauntoniae general glycoside 0.2g
Water for injection 100g
Butyl p-hydroxybenzoate 0.01g
Nicotinic acid amide 1.5g
Make the 100ml/ bottle
Being prepared as of Caulis et folium stauntoniae general glycoside transfusion: the Caulis et folium stauntoniae general glycoside is dissolved in the dosing, adds the adjuvant mix homogeneously of recipe quantity, filter, embedding, sterilization is packed to such an extent that the Caulis et folium stauntoniae general glycoside is infused.

Claims (10)

1, Caulis et folium stauntoniae total glycoside injection is characterized in that it is to be made by following material:
Caulis et folium stauntoniae general glycoside or its water soluble salt
The injections in common use additives; Comprise polysorbas20 or polysorbate40 or Tween 80, two or more in water for injection or polyvinylpyrrolidone or yolk phospholipid or lecithin or NaTDC or pluronic F-86 or acetic acid or sodium acetate or citric acid or sodium citrate or lactic acid or tartaric acid or sodium tartrate or sodium hydrogen phosphate or sodium dihydrogen phosphate or sodium carbonate or sodium acid carbonate or sodium carbonate or gelatin or methylcellulose or sodium cellulose glycolate or pectin or sorbierite or creatinine or glycine or nicotinic acid amide or sodium sulfite or sodium hydrogensulfite or sodium pyrosulfite or phenmethylol or butyl p-hydroxybenzoate or ethyl-para-hydroxybenzoate or phenol or anesin or procaine hydrochloride or lidocaine or the above material.
Above-mentioned a kind of raw material and one or more additives are made injection or injectable sterile powder or transfusion.
2, as the mentioned Caulis et folium stauntoniae general glycoside of claim 1 with after proper amount of water for injection is mixed, hydro-oxidation sodium solution or potassium hydroxide solution to mixture is the water soluble salt that clear and bright solution promptly gets the Caulis et folium stauntoniae general glycoside.
3, require 1 described Caulis et folium stauntoniae total glycoside injection as profit, it is characterized in that each unit injection contains Caulis et folium stauntoniae general glycoside 0.1mg to 5000mg.
4, yemuoside injection as claimed in claim 1 is characterized in that raw material and additives mix homogeneously, and is even with solvent, packing, and Caulis et folium stauntoniae general glycoside injection is made in sterilization
5, Caulis et folium stauntoniae injection as claimed in claim 1 is characterized in that raw material is mixed with additives, is dissolved in solvent, and lyophilization or sterilization solvent crystallization or spray drying are built in Caulis et folium stauntoniae general glycoside injectable sterile powder.
6, such as claim 1 the Caulis et folium stauntoniae total glycoside injection of art, it is characterized in that raw material is mixed with additives, with the solvent preparation evenly, filter, embedding forms the transfusion of Caulis et folium stauntoniae general glycoside
7, as claim 4 and 6 used solvents, it is characterized in that comprising the injection common solvent, i.e. water for injection or oil for injection or or ethanol or propylene glycol or Polyethylene Glycol or mannitol or benzyl benzoate or dimethyl acetylamide.
8, as effective site Caulis et folium stauntoniae general glycoside mentioned in the claim 1, it is characterized in that obtaining: with the rare alcohol extract or the commercially available extract of Caulis et folium stauntoniae, with the 1-5 of reuse aqueous solution volume behind the 1-5 water dissolution doubly water saturated butanols or the mixed extractant solvent of two or more compositions of amylalcohol or hexanol or enanthol or capryl alcohol or nonyl alcohol or decanol or above various pure apoplexy due to endogenous wind and getting doubly in order to following method.
9, the rare alcohol mentioned as claim 8 is meant that two or three concentration of forming with water by the aqueous solution of methanol or ethanol or propanol or above alcohol is the solution of 10%-90%.
10, as claim 8 and 9 mentioned propanol, butanols, amylalcohol, hexanol, enanthol, capryl alcohol, nonyl alcohol, decanol all comprise various isomers.
CN 200410026547 2004-03-22 2004-03-22 Stauntonvine general glycoside and injection Pending CN1562275A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN 200410026547 CN1562275A (en) 2004-03-22 2004-03-22 Stauntonvine general glycoside and injection

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN 200410026547 CN1562275A (en) 2004-03-22 2004-03-22 Stauntonvine general glycoside and injection

Publications (1)

Publication Number Publication Date
CN1562275A true CN1562275A (en) 2005-01-12

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Family Applications (1)

Application Number Title Priority Date Filing Date
CN 200410026547 Pending CN1562275A (en) 2004-03-22 2004-03-22 Stauntonvine general glycoside and injection

Country Status (1)

Country Link
CN (1) CN1562275A (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103826651A (en) * 2011-08-18 2014-05-28 财团法人全南生物产业振兴院 Medical composition containing stauntonia hexaphylla extract
CN106109404A (en) * 2016-08-09 2016-11-16 成都佳迪璐莎生物科技有限公司 A kind of medicinal composition for injections improving Caulis et folium stauntoniae drug injection preparation stability

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103826651A (en) * 2011-08-18 2014-05-28 财团法人全南生物产业振兴院 Medical composition containing stauntonia hexaphylla extract
US9370542B2 (en) 2011-08-18 2016-06-21 Jeonnam Bioindustry Foundation Medical composition containing Stauntonia hexaphylla extract
CN108392501A (en) * 2011-08-18 2018-08-14 财团法人全南生物产业振兴院 Medical composition containing Caulis et folium stauntoniae extract
CN106109404A (en) * 2016-08-09 2016-11-16 成都佳迪璐莎生物科技有限公司 A kind of medicinal composition for injections improving Caulis et folium stauntoniae drug injection preparation stability

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