CN108653203A - The 3beta,6alpha,12beta-Trihydroxydammar-20's preparation and preparation method that can be used for being injected intravenously - Google Patents
The 3beta,6alpha,12beta-Trihydroxydammar-20's preparation and preparation method that can be used for being injected intravenously Download PDFInfo
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Abstract
The present invention relates to a kind of 3beta,6alpha,12beta-Trihydroxydammar-20's preparation that can be used for being injected intravenously and preparation methods, said preparation includes 3beta,6alpha,12beta-Trihydroxydammar-20's injection and 3beta,6alpha,12beta-Trihydroxydammar-20's freeze drying powder injection, cosolvent when prepared by 3beta,6alpha,12beta-Trihydroxydammar-20's injection includes NaCl and glucose, and is aided with heating；Cosolvent is beta cyclodextrin in 3beta,6alpha,12beta-Trihydroxydammar-20's freeze drying powder injection.Preparation method provided by the invention can effectively improve the bioavilability and effect of 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside, not only solve the problems, such as that existing saponin(e powder-injection is since drug effect difference and shelf-life caused by complicated component are short on the market, the solubility of saponin(e in the injection and powder-injection is improved simultaneously, it no longer needs to be dissolved with the special cosolvent such as ethyl alcohol when use, with the patient suitable for ethyl alcohol allergy.
Description
Technical field
The present invention relates to biological fields, and in particular to it is a kind of can be used for be injected intravenously 3beta,6alpha,12beta-Trihydroxydammar-20's preparation and preparation
Method.
Background technology
Ginseng is a kind of traditional Chinese medicine that medical value is very high, is had thousands of years in oriental medicinal history,
With keep fit and healthy, intelligence development, improving eyesight, the multiple efficacies such as tranquilizing the mind.Ginsenoside is the significant ingredient of ginseng, be by sapogenin with
Sugar is connected the glucoside compound of composition, content about 4%.Multinomial experimental study shows ginsenoside because having higher anticancer
Activity receives people's concern, some scholars have made certain research with extracorporeal anti-tumor effect in animal body to it, they
By inhibiting growth of cancer cells, promotes cancer cell-apoptosis, inhibit invasion and transfer, autophagy, angiogenesis inhibiting, blocks cellular week
Phase, metabolite anticancer, overriding resistance effect and drug combination, the modes such as oxidative stress effectively inhibit the further deterioration of tumour,
Good effect is achieved, and has part saponin(e in China by as commercial drug and health products.
3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside is a kind of triol group rare ginsenoside.3beta,6alpha,12beta-Trihydroxydammar-20's polarity is than ginsenoside Rg1 and people
It is all small to join saponin(e Rh1, according to the higher research experience of the smaller activity of polarity, 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside there should be very high biology living
Property and pharmacological activity.And also repeatedly point out that 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside has protection cardiac muscle cell, anti-liver neoplasm thin in pertinent literature
Born of the same parents' proliferation function, and there is immunoloregulation function, anti-platelet aggregation effect and anti-malignant cell increment effect.Market at present
On with medicament made of saponin(e mainly have XUESAITONG JIAONANG, XUESAITONG PIAN, XUESAITONG ZHUSHEYE etc., what these medicaments mainly used
Be arasaponin be raw material.And arasaponin is multiple target point drug, the various saponin constituents, ratio in drug are all different,
It must lead to total saposins injection difference in drug effect, and the saponin injection property of high concentration is highly unstable, leads
Cause its period of guaranteeing the quality all shorter.Meanwhile the ingredient complicated as one, although the minimizing technology to impurity also constantly follows up,
The purity of extract is also higher and higher, but clinically the adverse reaction of total saposins injection is still unavoidable from.For commercially available
Notoginseng total saponin powder injection agent for, it is slow that there are solution rates, it is necessary to used after being dissolved with the special cosolvent of ethyl alcohol class,
It is used to limit part ethyl alcohol allergy sufferers, but also easily causes pollution.
Invention content
The object of the present invention is to provide a kind of 3beta,6alpha,12beta-Trihydroxydammar-20's preparation that can be used for being injected intravenously and preparation method, the works
Skill increases the solubility of saponin monomer in Saponin formulations, makes by adding NaCl and glucose and the preparation way for being aided with heating
All patients can use.
The technical solution adopted in the present invention is：
The preparation method for the 3beta,6alpha,12beta-Trihydroxydammar-20's preparation that can be used for being injected intravenously, it is characterised in that：
The preparation is 3beta,6alpha,12beta-Trihydroxydammar-20's injection, and preparation method includes the following steps：
（1）3beta,6alpha,12beta-Trihydroxydammar-20's monomer after purification is dissolved in NaCl aqueous solutions, ultrasound：2s/2s~5s/5s, 5~
10min makes its dissolving as a large amount of as possible；
（2）Continue to add glucose solution in this solution, temperature control is 60 DEG C~100 DEG C, ultrasound：2s/2s~5s/
5s, 10~15min so that 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside is completely dissolved；
（3）For dissolved solution through 0.22 μm of filtering with microporous membrane, cooling is filling, obtains 3beta,6alpha,12beta-Trihydroxydammar-20's injection.
In gained 3beta,6alpha,12beta-Trihydroxydammar-20's injection, the mass volume ratio of 3beta,6alpha,12beta-Trihydroxydammar-20's monomer and cosolvent is 1:50, it helps
Solvent is the summation of NaCl aqueous solutions and glucose solution.
In gained 3beta,6alpha,12beta-Trihydroxydammar-20's injection, the final concentration of 0.5%-2% of final concentration of 4%~6%, the NaCl of glucose.
The 3beta,6alpha,12beta-Trihydroxydammar-20's preparation that can be used for being injected intravenously made from preparation method as mentioned, it is characterised in that：
The preparation is injection.
The preparation method for the 3beta,6alpha,12beta-Trihydroxydammar-20's preparation that can be used for being injected intravenously, it is characterised in that：
The preparation is 3beta,6alpha,12beta-Trihydroxydammar-20's powder-injection, and preparation method includes the following steps：
（1）Beta-cyclodextrin aqueous solution, 85 DEG C of water-baths are configured, stirring makes beta-cyclodextrin aqueous solution be in uniform state, is kept stirring
State, add 3beta,6alpha,12beta-Trihydroxydammar-20's monomer after purification, stir 1~2h, it is cooling；
（2）With 0.22 μm of filtering with microporous membrane degerming, vacuum freeze drying freeze-drying is dispensed into cillin bottle, obtains ginseng soap
Glycosides Rk3 powder-injection.
The mass fraction of beta-cyclodextrin aqueous solution is 15%~25%.
In gained 3beta,6alpha,12beta-Trihydroxydammar-20's powder-injection, the mass volume ratio of 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside and beta-cyclodextrin is（1:25）~
（1:10）.
Physiological saline or glucose for injection dissolving, pH are adjusted to when gained 3beta,6alpha,12beta-Trihydroxydammar-20's powder-injection clinical application
5.5~6.0.
The 3beta,6alpha,12beta-Trihydroxydammar-20's preparation that can be used for being injected intravenously made from preparation method as mentioned, it is characterised in that：
The preparation is powder-injection.
The present invention has the following advantages：
3beta,6alpha,12beta-Trihydroxydammar-20's preparation of the present invention includes 3beta,6alpha,12beta-Trihydroxydammar-20's injection and 3beta,6alpha,12beta-Trihydroxydammar-20's freeze drying powder injection,
It can be used for being injected intravenously, improve the bioavilability and effect of 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside, not only solve existing saponin(e powder needle on the market
Agent improves soap in the injection and powder-injection due to drug effect difference caused by complicated component and shelf-life short problem
The solubility of glycosides, when use, no longer need to be dissolved with the special cosolvent such as ethyl alcohol, with the patient suitable for ethyl alcohol allergy.
Description of the drawings
Fig. 1 is 3beta,6alpha,12beta-Trihydroxydammar-20's solution solute effect of 3beta,6alpha,12beta-Trihydroxydammar-20's injection and common 0.9% NaCl dissolvings
Comparison diagram.
Fig. 2 be 3beta,6alpha,12beta-Trihydroxydammar-20's powder-injection and its with 0.9% NaCl dissolving under state.
Fig. 3 is influence of the 0.9% 3beta,6alpha,12beta-Trihydroxydammar-20's injection to NCI-H460 tumor bearing nude mices weight and tumor size.
Fig. 4 is shadow of the ginsenoside 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside powder-injection to NCI-H460 tumor bearing nude mices weight and tumor size
It rings.
Specific implementation mode
The present invention will be described in detail With reference to embodiment.
The present invention relates to can be used for be injected intravenously 3beta,6alpha,12beta-Trihydroxydammar-20's preparation preparation method, preparation include injection and
Powder-injection.
The preparation method of 3beta,6alpha,12beta-Trihydroxydammar-20's injection includes the following steps：
（1）3beta,6alpha,12beta-Trihydroxydammar-20's monomer after purification is dissolved in NaCl aqueous solutions, ultrasound：2s/2s~5s/5s, 5~
10min makes its dissolving as a large amount of as possible；
（2）Continue the glucose solution of addition high concentration in this solution, temperature control is 60 DEG C~100 DEG C, preferably 95 DEG C
~100 DEG C, ultrasound：2s/2s~5s/5s, 10~15min so that 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside is completely dissolved；
（3）For dissolved solution through 0.22 μm of filtering with microporous membrane, cooling is filling, obtains 3beta,6alpha,12beta-Trihydroxydammar-20's injection.
In gained 3beta,6alpha,12beta-Trihydroxydammar-20's injection, 3beta,6alpha,12beta-Trihydroxydammar-20's monomer and cosolvent（NaCl aqueous solutions and glucose water
The total amount of solution）Mass volume ratio be 1:50.
In gained 3beta,6alpha,12beta-Trihydroxydammar-20's injection, final concentration of the 4%~6% of glucose, preferably 5%, NaCl's is final concentration of
0.5%~2%.
Its water-soluble content calculation with 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside, assay method is sulfuric acid vanillin assay, by this legal system
The solubility of standby 3beta,6alpha,12beta-Trihydroxydammar-20's injection out is than directly using the molten of 3beta,6alpha,12beta-Trihydroxydammar-20's aqueous solution that 0.9% NaCl dissolves
Solution degree is 6 times high.
The preparation method of 3beta,6alpha,12beta-Trihydroxydammar-20's powder-injection includes the following steps：
（1）Beta-cyclodextrin aqueous solution, 85 DEG C of water-baths are configured, stirring makes beta-cyclodextrin aqueous solution be in uniform state, is kept stirring
State, add 3beta,6alpha,12beta-Trihydroxydammar-20's monomer after purification, stir 1~2h, it is cooling；
（2）With 0.22 μm of filtering with microporous membrane degerming, vacuum freeze drying freeze-drying is dispensed into cillin bottle, obtains ginseng soap
Glycosides Rk3 powder-injection.
The mass fraction of beta-cyclodextrin aqueous solution is 15%~25%, preferably 20%.
In gained 3beta,6alpha,12beta-Trihydroxydammar-20's powder-injection, the mass volume ratio of 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside and beta-cyclodextrin is（1:25）~
（1:10）.
Physiological saline or glucose for injection dissolving, pH are adjusted to when gained 3beta,6alpha,12beta-Trihydroxydammar-20's powder-injection clinical application
5.5~6.0.
The preparation of 1 3beta,6alpha,12beta-Trihydroxydammar-20's injection of embodiment
800mg 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranosides are dissolved in the NaCl aqueous solutions of 20mL 1.8%, and 2s/2s ultrasound 5min stand 20min, and sulfuric acid is fragrant
Oxalaldehyde colorimetric method surveys the concentration of 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside in supernatant；Continue the glucose solution of addition 20mL 20%, and temperature is heated to
60℃；2s/2s ultrasound 5min, stand 20min, and sulfuric acid vanillin assay surveys the concentration of 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside in supernatant.
800mg 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranosides are dissolved in the NaCl aqueous solutions of 20mL 1.8%, and 2s/2s ultrasound 5min stand 20min, sulphur
Sour vanillin assay surveys the concentration of 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside in supernatant；Continue the glucose solution of addition 20mL 5%, and temperature adds
Heat is to 80 DEG C；2s/2s ultrasound 5min, stand 20min, and sulfuric acid vanillin assay surveys the concentration of 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside in supernatant.
800mg 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranosides are dissolved in the NaCl aqueous solutions of 20mL 1.8%, and 2s/2s ultrasound 5min stand 20min, sulphur
Sour vanillin assay surveys the concentration of 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside in supernatant；Continue the glucose solution of addition 20mL 20%, and temperature adds
Heat is to 90 DEG C；2s/2s ultrasound 5min, stand 20min, and sulfuric acid vanillin assay surveys the concentration of 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside in supernatant.
800mg 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranosides are dissolved in the NaCl aqueous solutions of 20mL 1.8%, and 2s/2s ultrasound 5min stand 20min, sulphur
Sour vanillin assay surveys the concentration of 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside in supernatant；Continue the glucose solution of addition 20mL 20%, and temperature adds
Heat is to 100 DEG C；2s/2s ultrasound 5min, stand 20min, and sulfuric acid vanillin assay surveys the concentration of 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside in supernatant.
Influence of the temperature to Aqueous soluble ginseng's saponin(e Rk3 solubility is as shown in table 1：
For dissolved solution through 0.22 μm of filtering with microporous membrane, cooling is filling, obtains 3beta,6alpha,12beta-Trihydroxydammar-20's injection.
Attached drawing 1 is the ginseng soap of the 3beta,6alpha,12beta-Trihydroxydammar-20's injection and common 0.9% NaCl dissolvings that are obtained under condition optimizing
Glycosides Rk3.
The preparation of 2 3beta,6alpha,12beta-Trihydroxydammar-20's freeze drying powder injection of embodiment
The beta-cyclodextrin aqueous solution 100mL of configuration 10%, 85 DEG C of water-baths, stirring make it fully dissolve in uniform state, keep stirring
3beta,6alpha,12beta-Trihydroxydammar-20's monomer of 1g is added in the state mixed in this solution, stirs 1h, and it is 5.5~6.0 to adjust solution ph, cooling
The content of 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside in supernatant is surveyed after standing.
The beta-cyclodextrin aqueous solution 100ml of configuration 15%, 85 DEG C of water-baths, stirring make it fully dissolve in uniform state, protect
The state of stirring is held, 3beta,6alpha,12beta-Trihydroxydammar-20's monomer of 1g is added in this solution, stirs 1h, it is 5.5~6.0 to adjust solution ph,
The content of 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside in supernatant is surveyed after cooling and standings.
The beta-cyclodextrin aqueous solution 100ml of configuration 20%, 85 DEG C of water-baths, stirring make it fully dissolve in uniform state, protect
The state of stirring is held, 3beta,6alpha,12beta-Trihydroxydammar-20's monomer of 1g is added in this solution, stirs 1h, it is 5.5~6.0 to adjust solution ph,
The content of 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside in supernatant is surveyed after cooling and standings.
The beta-cyclodextrin aqueous solution 100ml of configuration 25%, 85 DEG C of water-baths, stirring make it fully dissolve in uniform state, protect
The state of stirring is held, 3beta,6alpha,12beta-Trihydroxydammar-20's monomer of 1g is added in this solution, stirs 1h, it is 5.5~6.0 to adjust solution ph,
The content of 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside in supernatant is surveyed after cooling and standings.
The results are shown in Table 2 for influence of the beta-cyclodextrin concentration to Aqueous soluble ginseng's saponin(e Rk3 solubility：
The beta-cyclodextrin prepared -3beta,6alpha,12beta-Trihydroxydammar-20's solution, with 0.22 μm of filtering with microporous membrane degerming, vacuum freeze drying
3beta,6alpha,12beta-Trihydroxydammar-20's freeze-dried powder is made in freeze-drying, is dispensed into cillin bottle, every bottle of 10mg, seals, obtains 3beta,6alpha,12beta-Trihydroxydammar-20's powder-injection.
Physiological saline or glucose for injection dissolving when clinical application.
Under attached drawing 2 is the beta-cyclodextrin -3beta,6alpha,12beta-Trihydroxydammar-20's powder-injection obtained under condition optimizing and its is dissolved with 0.9%NaCl
State：
Evaluating drug effect in 3 3beta,6alpha,12beta-Trihydroxydammar-20's injecting fluid of embodiment
By female BAl BIc/c nude inoculation NCI-H460 cells, every nude mice injection 3 × 106~4 × 106A cell.Inoculation 20
After it, it is observed that the left armpit of nude mice subcutaneously has tumor mass to grow, only grain of rice size.Continue to raise nude mice after 4 days, tumour
Size is probably more than 100mm3When, nude mice is grouped.3 groups are classified as according to tumor size (paying the utmost attention to) and nude mice weight,
Blank group and treatment group 1 and treatment group 2：Blank group is by 5% glucose of weight gavage, 0.9%NaCl mixed aqueous solutions；Treatment group 1,
2 by weight gavage a concentration of 20mg/kg/d containing 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside general ginsenosides Rk3-0.9% NaCl and prepare
Rk3 injections.Once a day, continuous 25 days.
From table 3 it will be seen that blank group and 1,2 nude mice weight for the treatment of group increase with the time, wherein：Treatment group
The trend of weight gain becomes apparent from, and the trend of 2 weight gain for the treatment of group is higher than treatment group 1 again.Table 4 can see, blank
The gross tumor volume of group and 1,2 nude mice for the treatment of group increases with the time, wherein：The increased trend of blank group is higher than treatment group,
And the gross tumor volume of 1 nude mice for the treatment of group increases is higher than treatment group 2 again.This explanation, the active ingredient of drug used in treatment group 2
Content is than 1 Chinese medicine higher for the treatment of group, and drug effect is also than merely using 3beta,6alpha,12beta-Trihydroxydammar-20's anticancer effect of 0.9% NaCl solvents dissolving
It is better.
25th day, the tumour inhibiting rate of 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside was up to 33.63% in treatment group 1；Ginsenoside ginseng soap in treatment group 2
The tumour inhibiting rate of glycosides Rk3 is up to 71.70%.From attached drawing 3, we can more intuitively observe two groups of nude mice weight and tumor size
Variation.
The internal evaluating drug effect of 4 3beta,6alpha,12beta-Trihydroxydammar-20's powder-injection of embodiment
By female BAl BIc/c nude inoculation NCI-H460 cells, every nude mice injection 3 × 106~4 × 106A cell.Inoculation 20
After it, it is observed that the left armpit of nude mice subcutaneously has tumor mass to grow, only grain of rice size.Continue to raise nude mice after 4 days, tumour
Size is probably more than 100mm3When, nude mice is grouped.3 groups are classified as according to tumor size (paying the utmost attention to) and nude mice weight,
Blank group and treatment group 3 and treatment group 4：Blank group presses 20% beta-cyclodextrin of weight gavage-aqueous solution；Treatment group 3,4 is filled by weight
The general ginsenosides Rk3-0.9% NaCl and dissolved Rk3 powder-injection of stomach a concentration of 20mg/kg/d containing 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside.
Once a day, continuous 25 days.
From table 5 it will be seen that blank group and 3,4 nude mice weight for the treatment of group increase with the time, wherein：Treatment group
The trend of weight gain becomes apparent from, and the trend of 4 weight gain for the treatment of group is higher than treatment group 3 again.This as can be seen from Table 6,
The gross tumor volume of 3,4 nude mice of blank group and treatment group increases with the time, wherein：The increased trend of blank group is higher than treatment
Group, and the gross tumor volume of 3 nude mice for the treatment of group increases higher than treatment group 4.This illustrates that drug used is effective in treatment group 4
Component content is than 3 Chinese medicine higher for the treatment of group, and drug effect is also than merely using 3beta,6alpha,12beta-Trihydroxydammar-20's anticancer of 0.9% NaCl solvents dissolving
Effect will be got well.
25th day, the tumour inhibiting rate of ginsenoside Rk1 was up to 26.47% in treatment group 3；3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside in treatment group 4
Tumour inhibiting rate is up to 73.97%.From attached drawing 4, we can more intuitively observe the variation of two groups of nude mice weight and tumor size.
Present disclosure is not limited to cited by embodiment, and those of ordinary skill in the art are by reading description of the invention
And to any equivalent transformation that technical solution of the present invention is taken, it is that claim of the invention is covered.
Claims (9)
1. the preparation method for the 3beta,6alpha,12beta-Trihydroxydammar-20's preparation that can be used for being injected intravenously, it is characterised in that：
The preparation is 3beta,6alpha,12beta-Trihydroxydammar-20's injection, and preparation method includes the following steps：
（1）3beta,6alpha,12beta-Trihydroxydammar-20's monomer after purification is dissolved in NaCl aqueous solutions, ultrasound：2s/2s~5s/5s, 5~
10min makes its dissolving as a large amount of as possible；
（2）Continue to add glucose solution in this solution, temperature control is 60 DEG C~100 DEG C, ultrasound：2s/2s~5s/
5s, 10~15min so that 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside is completely dissolved；
（3）For dissolved solution through 0.22 μm of filtering with microporous membrane, cooling is filling, obtains 3beta,6alpha,12beta-Trihydroxydammar-20's injection.
2. the preparation method of the 3beta,6alpha,12beta-Trihydroxydammar-20's preparation according to claim 1 that can be used for being injected intravenously, feature exist
In：
In gained 3beta,6alpha,12beta-Trihydroxydammar-20's injection, the mass volume ratio of 3beta,6alpha,12beta-Trihydroxydammar-20's monomer and cosolvent is 1:50, cosolvent
For the summation of NaCl aqueous solutions and glucose solution.
3. the preparation method of the 3beta,6alpha,12beta-Trihydroxydammar-20's preparation according to claim 1 that can be used for being injected intravenously, feature exist
In：
In gained 3beta,6alpha,12beta-Trihydroxydammar-20's injection, the final concentration of 0.5%-2% of final concentration of 4%~6%, the NaCl of glucose.
4. the 3beta,6alpha,12beta-Trihydroxydammar-20's preparation that can be used for being injected intravenously made from preparation method as described in claim 1, feature exist
In：
The preparation is injection.
5. the preparation method for the 3beta,6alpha,12beta-Trihydroxydammar-20's preparation that can be used for being injected intravenously, it is characterised in that：
The preparation is 3beta,6alpha,12beta-Trihydroxydammar-20's powder-injection, and preparation method includes the following steps：
（1）Beta-cyclodextrin aqueous solution, 85 DEG C of water-baths are configured, stirring makes beta-cyclodextrin aqueous solution be in uniform state, is kept stirring
State, add 3beta,6alpha,12beta-Trihydroxydammar-20's monomer after purification, stir 1~2h, it is cooling；
（2）With 0.22 μm of filtering with microporous membrane degerming, vacuum freeze drying freeze-drying is dispensed into cillin bottle, obtains ginseng soap
Glycosides Rk3 powder-injection.
6. the preparation method of the 3beta,6alpha,12beta-Trihydroxydammar-20's preparation according to claim 5 that can be used for being injected intravenously, feature exist
In：
The mass fraction of beta-cyclodextrin aqueous solution is 15%~25%.
7. the preparation method of the 3beta,6alpha,12beta-Trihydroxydammar-20's preparation according to claim 5 that can be used for being injected intravenously, feature exist
In：
In gained 3beta,6alpha,12beta-Trihydroxydammar-20's powder-injection, the mass volume ratio of 3beta,6alpha,12beta-Trihydroxydammar-20(21),24-diene-6-O-beta-D-glucopyranoside and beta-cyclodextrin is（1:25）~（1:
10）.
8. the preparation method of the 3beta,6alpha,12beta-Trihydroxydammar-20's preparation according to claim 5 that can be used for being injected intravenously, feature exist
In：
Physiological saline or glucose for injection dissolving when gained 3beta,6alpha,12beta-Trihydroxydammar-20's powder-injection clinical application, pH is adjusted to 5.5~
6.0。
9. the 3beta,6alpha,12beta-Trihydroxydammar-20's preparation that can be used for being injected intravenously made from preparation method as claimed in claim 5, feature exist
In：
The preparation is powder-injection.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN109394703A (en) * | 2018-07-05 | 2019-03-01 | 西安巨子生物基因技术股份有限公司 | 3beta,6alpha,12beta-Trihydroxydammar-20's intravenous formulations and preparation method |
| CN116023423A (en) * | 2023-03-29 | 2023-04-28 | 中国农业科学院特产研究所 | Ginsenoside Rk3 and preparation and application thereof in preparation of folliculitis medicines |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN109394703A (en) * | 2018-07-05 | 2019-03-01 | 西安巨子生物基因技术股份有限公司 | 3beta,6alpha,12beta-Trihydroxydammar-20's intravenous formulations and preparation method |
| CN116023423A (en) * | 2023-03-29 | 2023-04-28 | 中国农业科学院特产研究所 | Ginsenoside Rk3 and preparation and application thereof in preparation of folliculitis medicines |
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Application publication date: 20181016 |