CN1415301A - Compound recipe formula containing kurarinone prostaglandin E1 and aspirin, its preparation method and application - Google Patents
Compound recipe formula containing kurarinone prostaglandin E1 and aspirin, its preparation method and application Download PDFInfo
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- CN1415301A CN1415301A CN 02146488 CN02146488A CN1415301A CN 1415301 A CN1415301 A CN 1415301A CN 02146488 CN02146488 CN 02146488 CN 02146488 A CN02146488 A CN 02146488A CN 1415301 A CN1415301 A CN 1415301A
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- prostaglandin
- kurarinone
- aspirin
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Abstract
A compound medicine containing kurarinol, prostaglandic E1 and aspirin is prepared through including the kurarinol and prostaglandin E1 by 6-0-malto-beta-cyclodextrin, mixing, adding others, and preparing the freeze dried powder injection. It can be used for treating cancers, cardiovascular and cerebrovascular diseases and hepatitis. Its advantages are sure curative effect, and no toxic by-effect.
Description
Technical field:
The present invention relates to a kind of medicine and its production and use, particularly a kind of kurarinone, prostaglandin E of containing
1With compound preparation of aspirin and its production and use.
Background technology:
Known kurarinone is extraction from Chinese crude drug Radix Sophorae Flavescentis or Radix Sophorae Tonkinensis, purification, the refining and monomer effective ingredient that obtains.Effects such as that pharmacology and clinical trial certificate, kurarinone have is anticancer, leukocyte increasing, anti-hepatitis virus, protection hepatocyte, but its anticancer mechanism only is an anticancer, and also the effect of this inhibition is significantly only not close with cyclophosphamide.Simultaneously, patient's feels pain when the Matrine Injection that uses uses at present is difficult to accept.
Known, prostaglandin E
1Has anticancer, promote the effect that cancerous cell transforms to normal cell, have simultaneously regulate human immune system, blood vessel dilating, inhibition platelet aggregation and, improve the function of microcirculation in human body, have radiation-resistant function simultaneously, regulate immunity, blood circulation promoting and blood stasis dispelling and prevent that the damage that radiotherapy brings has positive clinical effect for cancer patient.
Because prostaglandin E
1Also have expansion liver blood vessel function, can improve the hepatitis liver microcirculation, remove immune complex in liver and the blood, suppress the hepatic necrosis factor and discharge, the protection hepatocyte, and can promote hepatic cell growth, can be used for treating first, second, hepatitis C.It is still good cardiovascular and cerebrovascular disease medication simultaneously, is the wide spectrum endogenous substance of new generation of generally acknowledging, but has the directly side effect of anti-hepatitis virus and injection pain, makes application be restricted.
Known aspirin is good analgesic medicine, but can suppress PGI in the human body
2Synthetic, life-time service or consumption conference aggravation cardiovascular and cerebrovascular disease slightly take place or the aggravation disease.
Summary of the invention:
The objective of the invention is to utilize the mechanism of curing the disease of said medicine, a kind of have kurarinone, prostaglandin E are provided
1With the aspirin compound preparation, by the synergism of medicine, improve curative effect, and alleviate side effect human body.
Another object of the present invention provides the preparation method of this compound preparation.
A further object of the present invention is that the compound preparation that will provide is used for the treatment of cancer, cardiovascular and cerebrovascular disease and hepatitis.
Above-mentioned purpose of the present invention can realize by following technological means.
The component of this compound preparation is as follows:
The composition weight proportioning
Kurarinone 0.5-1.0g
Prostaglandin E
1100-400 μ g
2-6 times of prostaglandin E of 6-0-malt sugar group-beta-cyclodextrin
1Molal quantity
Aspirin or aspisol 0.25-0.9g
Sterilized water for injection or normal saline 0.6-2.2g
Low molecular dextran-40 2-10%
The preparation method of this compound preparation is as follows:
The kurarinone feed purification becomes to contain oxymatrine 99-102%; Prostaglandin E
1Being refined into purity is 99.5%, matrine and prostaglandin E
1Comprise with the 6-0-malt sugar group-beta-cyclodextrin respectively, aspirin or aspisol are dissolved in sterile water for injection or normal saline, the low molecular dextran-40 that is incorporated as gross weight 2-10% is as excipient, the adjustment pH value is 6.0-7.0, after using 0.22 μ m membrane filtration to remove antibacterial, measuring bacterial endotoxin, clarity, pH value, each constituent content of intermediate products carries out fill, false add plug after all qualified, carries out lyophilization in-45-30 ℃ under the vacuum of 2-15Pa, make water content≤2-3%, tamponade, roll lid, after the assay was approved encapsulation.
The present invention has following advantage:
1. prescription is novel unique, and each component is replenished mutually, makes therapeutic effect definite, treats widely, nontoxic, and side effect is slight.
(1) kurarinone has the anticancer function, but effect is not remarkable, prostaglandin E
1Use with kurarinone is collaborative, can significantly improve the function of anticancer, can break up cancerous cell simultaneously and transform prostaglandin E to normal cell
1Adjusting human immune system effect and blood circulation promoting and blood stasis dispelling and prevent that the damage that radiotherapy brings has positive clinical effect, the function of promoting blood circulation to disperse blood clots of aspirin is favourable to cancer patient treatment and rehabilitation, especially its good analgesic effect;
(2) prostaglandin E
1With aspirin or aspisol coupling, can remedy aspirin or aspisol to the synthetic PGI of human body
2The side effect that suppresses, prostaglandin E
1Can strengthen the human body complex functionality, itself also have and PGI simultaneously
2Identical physiological effect, thus overcome the untoward reaction of aspirin or aspisol to human body;
(3) analgesic activity of aspirin or aspisol can reduce kurarinone and prostaglandin E
1Injection pain;
(4) prostaglandin E
1With kurarinone Synergistic treatment hepatitis, can enlarge kurarinone and only treat hepatitis B and can treat first, second, the third three type hepatitis to this compound preparation.
2. the lyophilized injectable powder that compound preparation of the present invention is made makes medicine under aseptic apyrogeneity state, has both guaranteed that patient did not produce hazards of medication, also guarantee medicine produce and use in physicochemical property and physiological action do not change.
3. in the production technology of the present invention, adopt the 6-0-malt sugar group-beta-cyclodextrin to comprise kurarinone and prostaglandin E respectively first
1Both are carried out insulation blocking, guarantee not react between them or respond, thereby guarantee both effectiveness, reduce side effect with aspirin (or aspisol).
4. compound preparation of the present invention is of many uses, can treat cancer, cardiovascular and cerebrovascular disease and hepatitis.
The specific embodiment:
In conjunction with the embodiments the present invention is further detailed now.
The following example does not limit protection scope of the present invention.
Embodiment 1:
Prescription:
It is 99.5% prostaglandin E that the composition weight proportioning contains oxymatrine 99-102% kurarinone 500-700g purity
12-2.5 times of prostaglandin E of 100-250mg 6-0-malt sugar group-beta-cyclodextrin
1Molal quantity purity is 98% aspirin 250-300g
Purity is 98% or aspisol 450-550g
Sterilized water for injection 1500ml
Low molecular dextran-40 2-10%
Kurarinone is dissolved into makes saturated solution in the sterilized water for injection, the 6-0-malt sugar group-beta-cyclodextrin is dissolved into makes saturated solution in the sterilized water for injection, under agitation the kurarinone saturated solution is added drop-wise in the 6-0-malt sugar group-beta-cyclodextrin saturated solution, up to dissolving fully.
With prostaglandin E
1Become saturated solution with anhydrous alcohol solution, the 6-0-malt sugar group-beta-cyclodextrin is dissolved into makes saturated solution in the sterilized water for injection, under agitation with prostaglandin E
1The dehydrated alcohol saturated solution be added drop-wise in the 6-0-malt sugar group-beta-cyclodextrin saturated solution, up to fully the dissolving.
With kurarinone/6-0-malt sugar group-beta-cyclodextrin mixed solution and prostaglandin E
1/ 6-0-malt sugar group-beta-cyclodextrin mixed solution mixing and stirring, add a certain amount of sterilized water for injection again, make overall solution volume reach 1500ml, add aspirin or aspisol, stirring is dissolved it fully, adjust pH value to 6.0-7.0, remove antibacterial and remove undissolved particle through 0.22 μ m membrane filtration, measure the bacterial endotoxin of intermediate products, clarity, pH value, after each constituent content is all qualified, with 1000 of 3ml cillin bottle packing, every 1.5ml fill amount, under the vacuum of 2-15Pa, carry out lyophilization in-45-30 ℃, make water content≤2-3%, the moulding plug, roll aluminium-plastic cap, after the assay was approved encapsulation.
Embodiment 2:
Prescription: composition weight proportioning
Contain oxymatrine 99-102% kurarinone 800-1000g
Purity is 99.5% prostaglandin E
1300-400mg
5.5-6 times of prostaglandin E of 6-0-malt sugar group-beta-cyclodextrin
1Molal quantity
Purity is 98% aspirin 400-500g
Purity is 98% or aspisol 800-900g
Sterilized water for injection 1500ml
Low molecular dextran-40 2-10%
Concrete preparation method is identical with embodiment 1.
Claims (8)
1. one kind contains kurarinone, prostaglandin E
1Compound preparation with aspirin is characterized in that, the prescription below adopting:
The composition weight proportioning
Kurarinone 0.5-1.0g
Prostaglandin E
1100-400 μ g
2-6 times of prostaglandin E of 6-0-malt sugar group-beta-cyclodextrin
1Molal quantity
Aspirin or aspisol 0.25-0.9g
Sterilized water for injection or normal saline 0.6-2.2g
Low molecular dextran-40 2-10%
2. a kind of kurarinone, prostaglandin E of containing according to claim 1
1With the compound preparation of aspirin, oxymatrine concentration is 99-102% in the kurarinone during its feature also is to fill a prescription, and the weight proportion of kurarinone is 0.6-0.8g.
3. a kind of kurarinone, prostaglandin E of containing according to claim 1
1With the compound preparation of aspirin, its feature also is: the prostaglandin E in the prescription
1Purity is 99.5%, and weight proportion is 100-200 μ g.
4. one kind contains kurarinone, prostaglandin E
1Preparation method with the compound preparation of aspirin is characterized in that:
(1) adopt following prescription:
The composition weight proportioning
Kurarinone 0.5-1.0g
Prostaglandin E
1100-400 μ g
2-6 times of prostaglandin E of 6-0-malt sugar group-beta-cyclodextrin
1Molal quantity
Aspirin or aspisol 0.25-0.9g
Sterilized water for injection or normal saline 0.6-2.2g
Low molecular dextran-40 2-10%
(2) adopt following steps:
A. the kurarinone feed purification becomes to contain oxymatrine 99-102%, comprises with the 6-0-malt sugar group-beta-cyclodextrin;
B. prostaglandin E
1Being refined into purity is 99.5%, comprises with the 6-0-malt sugar group-beta-cyclodextrin;
C. to kurarinone and prostaglandin E
1Mixed solution in add sterile water for injection or normal saline, add aspirin or aspisol again, adjust pH value, after using 0.22 μ m membrane filtration to remove antibacterial, carry out fill, false add plug, tamponade after the lyophilization after bacterial endotoxin, clarity, pH value, each constituent content of mensuration intermediate products is all qualified, roll lid, after the assay was approved packing.
5. a kind of kurarinone, prostaglandin E of containing according to claim 4
1With the preparation method of the compound preparation of aspirin, its feature also is: the pH value among the step c is 6.0-7.0.
6. a kind of kurarinone, prostaglandin E of containing according to claim 4
1With the preparation method of the compound preparation of aspirin, its feature also is: the lyophilization among the step c is under the vacuum of 2-15Pa, carries out in-45-30 ℃, makes water content≤2-3%.
7. a kind of kurarinone, prostaglandin E of containing according to claim 4
1With the preparation method of the compound preparation of aspirin, its feature also is: adopt the fill of 3ml cillin bottle among the step c, supporting plug and aluminium-plastic cap.
8. one kind contains kurarinone, prostaglandin E
1Purposes with the compound preparation of aspirin is characterized in that: be used for the treatment of cancer, cardiovascular and cerebrovascular disease and hepatitis.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02146488 CN1415301A (en) | 2002-11-12 | 2002-11-12 | Compound recipe formula containing kurarinone prostaglandin E1 and aspirin, its preparation method and application |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02146488 CN1415301A (en) | 2002-11-12 | 2002-11-12 | Compound recipe formula containing kurarinone prostaglandin E1 and aspirin, its preparation method and application |
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|---|---|
| CN1415301A true CN1415301A (en) | 2003-05-07 |
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| CN 02146488 Pending CN1415301A (en) | 2002-11-12 | 2002-11-12 | Compound recipe formula containing kurarinone prostaglandin E1 and aspirin, its preparation method and application |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005091937A2 (en) * | 2004-03-04 | 2005-10-06 | The Regents Of The University Of California | Compositions useful for the treatment of microbial infections |
| CN101019872B (en) * | 2007-03-08 | 2010-12-01 | 蔡海德 | Nanometer antiviral liposome medicine and its preparation |
| US7846895B2 (en) | 2006-09-06 | 2010-12-07 | The Regents Of The University Of California | Selectively targeted antimicrobial peptides and the use thereof |
| CN102335179A (en) * | 2011-06-03 | 2012-02-01 | 蔡海德 | Alprostadil composite medicine, preparation method thereof, quality controlling method thereof, and purpose thereof |
| CN103816529A (en) * | 2014-03-20 | 2014-05-28 | 蔡欣 | Pharmaceutical composition for treating various serious diseases and preparation and use thereof |
-
2002
- 2002-11-12 CN CN 02146488 patent/CN1415301A/en active Pending
Cited By (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005091937A2 (en) * | 2004-03-04 | 2005-10-06 | The Regents Of The University Of California | Compositions useful for the treatment of microbial infections |
| WO2005091937A3 (en) * | 2004-03-04 | 2006-03-30 | Univ California | Compositions useful for the treatment of microbial infections |
| US7875598B2 (en) | 2004-03-04 | 2011-01-25 | The Regents Of The University Of California | Compositions useful for the treatment of microbial infections |
| US7846895B2 (en) | 2006-09-06 | 2010-12-07 | The Regents Of The University Of California | Selectively targeted antimicrobial peptides and the use thereof |
| US8680058B2 (en) | 2006-09-06 | 2014-03-25 | The Regents Of The University Of California | Selectively targeted antimicrobial peptides and the use thereof |
| US9351490B2 (en) | 2006-09-06 | 2016-05-31 | The Regents Of The University Of California | Selectively targeted antimicrobial peptides and the use thereof |
| US10111926B2 (en) | 2006-09-06 | 2018-10-30 | The Regents Of The University Of California | Selectively targeted antimicrobial peptides and the use thereof |
| CN101019872B (en) * | 2007-03-08 | 2010-12-01 | 蔡海德 | Nanometer antiviral liposome medicine and its preparation |
| CN102335179A (en) * | 2011-06-03 | 2012-02-01 | 蔡海德 | Alprostadil composite medicine, preparation method thereof, quality controlling method thereof, and purpose thereof |
| CN103816529A (en) * | 2014-03-20 | 2014-05-28 | 蔡欣 | Pharmaceutical composition for treating various serious diseases and preparation and use thereof |
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