CN104147223A - Application of freeze-dried rehmannia glutinosa in preparation of drug - Google Patents
Application of freeze-dried rehmannia glutinosa in preparation of drug Download PDFInfo
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- CN104147223A CN104147223A CN201410418839.7A CN201410418839A CN104147223A CN 104147223 A CN104147223 A CN 104147223A CN 201410418839 A CN201410418839 A CN 201410418839A CN 104147223 A CN104147223 A CN 104147223A
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- radix rehmanniae
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Abstract
The invention relates to an application of freeze-dried rehmannia glutinosa in preparation of drugs and the application in preparation of a drug in which an effective ingredient catalpol is high in bioavailability. The freeze-dried rehmannia glutinosa has better effects on diseases such as diabetes, cardiovascular and cerebrovascular diseases, hypertension, hepatitis, constipation and the like.
Description
Invention field
The present invention relates to medicine method for making, particularly lyophilizing Radix Rehmanniae, in the application of preparing in medicine, belongs to medical technical field.
Background technology
Radix Rehmanniae is the fresh or dried root of scrophulariaceae rehmannia glutinosa plant Rehmannia glutinosa Li-bosch..Excavate autumn, except removing LU, fibrous root and silt, using fresh herb, practises and claim " Radix Rehmanniae ".It is slowly cured to eighty per cant dry, practise and claim " Radix Rehmanniae ".Get Radix Rehmanniae and stew to wine exhaustion according to stewed with wine method (" Chinese Pharmacopoeia " version appendix II D in 2010), take out, when dry in the sun is slightly dry to crust mucus; Or according to extremely black profit of steaming method (" Chinese Pharmacopoeia " version appendix II D in 2010) steaming, take out, shine while doing to approximately eighty per cant, cut sheet or piece, dry, obtain " Radix Rehmanniae Preparata ".The pharmacodynamic feature of these 3 kinds of Radix Rehmanniae is different, and Radix Rehmanniae has effect of clearing away heat and promoting production of body fluid, removing heat from blood, hemostasis; Radix Rehmanniae has the effect of clearing away heat and cooling blood, YIN nourishing and the production of body fluid promoting; Radix Rehmanniae Preparata has the function that nourishing YIN and supplementing blood, beneficial essence are filled out marrow.
The pharmacological research of Radix Rehmanniae has been subject to paying close attention to widely in recent years, and is widely used in clinical.For hemostasis, for diabetes, for cardiovascular and cerebrovascular disease, for hypertension, for nephritis, for dull-witted, for urinary system, for oral ulcer etc.
The main effective ingredient of Radix Rehmanniae is glycoside, and wherein taking iridoid glycosides as main, catalpol is one of its main active, there is diuresis, relax rush down under, the biological activity such as blood sugar lowering, neuroprotective.Improve content and the bioavailability of the main effective ingredient catalpol of Radix Rehmanniae, and then improve curative effect, very necessary.
Summary of the invention
The object of this invention is to provide lyophilizing Radix Rehmanniae in the application of preparing in medicine, be specifically related to the application of lyophilizing Radix Rehmanniae in the high medicine of the bioavailability of preparing effective ingredient catalpol.
The object of the present invention is achieved like this:
Lyophilizing Radix Rehmanniae is in the application of preparing in medicine, the application in the high medicine of the bioavailability of preparing effective ingredient catalpol.
Described lyophilizing Radix Rehmanniae is in the application of preparing in medicine, and the method for lyophilizing Radix Rehmanniae is: Radix Rehmanniae is put in freeze dryer, is refrigerated to below-10 DEG C, is evacuated to below drying chamber pressure 30Pa subliming by heating; The temperature of distillation should be controlled at below 40 DEG C, and the temperature of resolution phase is controlled at below 45 DEG C, to dry.
Described lyophilizing Radix Rehmanniae is in the application of preparing in medicine, is that lyophilizing Radix Rehmanniae is made powder and adds in prepared medicine.
Described lyophilizing Radix Rehmanniae is in the application of preparing in medicine, is that lyophilizing Radix Rehmanniae is made powder and makes powder.
So far completed the present invention, it provides the new purposes of a kind of lyophilizing Radix Rehmanniae, and lyophilizing Radix Rehmanniae is in the application of preparing in medicine, the application in the high medicine of the bioavailability of preparing effective ingredient catalpol.
Catalpol is one of main active of Radix Rehmanniae, under having diuresis, protecting the liver, rush down, the biological activity such as blood sugar lowering, neuroprotective.The bioavailability of the medicine catalpol of preparation is high, and then known, is used for the treatment of diabetes, cardiovascular and cerebrovascular disease, hypertension, hepatitis, constipation and other diseases better effects if.
Below by test example, usefulness of the present invention is described.
The Radix Rehmanniae of being gathered in same plot simultaneously, process respectively by the following method:
1) Radix Rehmanniae: new Radix Rehmanniae soil buries, plastic bag sealing moisturizing;
2) Radix Rehmanniae: get Radix Rehmanniae, be cut into sheet, 60 DEG C are slowly cured to eighty per cant dry;
3) lyophilizing Radix Rehmanniae, gets Radix Rehmanniae, is cut into sheet, puts in freeze dryer, and solidification point is controlled between-28～-32 DEG C; Reach and control after temperature, be evacuated to immediately below drying chamber pressure 50Pa, then subliming by heating, the temperature of distillation is controlled at below 40 DEG C, and resolution temperature is controlled at below 45 DEG C, to dry, takes out, and to obtain final product.
Two, catalpol content comparison in different dry drying method Radix Rehmanniae
Instrument: Shimadzu LC-3A chromatograph, chromatographic condition: chromatographic column YWG-C18,10 μ m, 25cm × 4.6mm.Mobile phase: 0.6% acetonitrile-water.Flow velocity: 1.0mLmin
-1, measure wavelength 210 nm.40 DEG C of column temperatures.
The preparation of sample solution: Radix Rehmanniae is rubbed, Radix Rehmanniae was pulverized 40 mesh sieves, the Radix Rehmanniae 2.5g(drying of accurately weighed rubbing test 5g Radix Rehmanniae obtains 1g lyophilizing Radix Rehmanniae respectively), Radix Rehmanniae, the each 0.5g of lyophilizing Radix Rehmanniae, add methanol 25mL, weighs, supersound process 20min, let cool, mend and weigh, filter.Get subsequent filtrate as need testing solution.
The preparation of reference substance solution: accurately weighed catalpol reference substance 2.87mg, put in 10 mL measuring bottles, add mobile phase and dissolve and be diluted to scale, shake up product solution in contrast.
The accurate reference substance solution 3 μ L that draw respectively, need testing solution 6 μ L, inject hplc determination.In dry product, the results are shown in Table 1.
Catalpol content in table 1 different dry drying method Radix Rehmanniae
| ? | Catalpol content (%) |
| Radix Rehmanniae | 6.25 |
| Radix Rehmanniae | 0.54 |
| Lyophilizing Radix Rehmanniae | 6.18 |
Table 1 result is known, and lyophilizing Radix Rehmanniae of the present invention and lyophilizing rehmannia catalpol content are basic identical, and lyophilizing rehmannia catalpol content is slightly lower than Radix Rehmanniae, all apparently higher than Radix Rehmanniae.
Two, lyophilizing Radix Rehmanniae powder and the comparison of Radix Rehmanniae bioavailability
Instrument: Shimadzu LC-3A chromatograph, chromatographic condition: chromatographic column YWG-C18,10 μ m, 25cm × 4.6mm.Mobile phase: 0.6% acetonitrile-water.Flow velocity: 1.0mLmin-1, measures wavelength 210 nm.40 DEG C of column temperatures.
The preparation of reference substance solution: with test one.
The preparation of sample solution: Radix Rehmanniae is rubbed; Lyophilizing Radix Rehmanniae was pulverized 40 mesh sieves, made lyophilizing Radix Rehmanniae powder, and distilled water adds to 5 times of amounts (drying test 5g Radix Rehmanniae obtains 1g lyophilizing Radix Rehmanniae).
The preparation of rat blood serum after administration: by 30 of Wistar rats, be divided at random 3 groups, blank group, lyophilizing Radix Rehmanniae powder group, Radix Rehmanniae group.Administration group dosage is 1.5mL/100g, gavage, and blank group gives same volume distilled water.Fasting 12h before experiment, freely drinks water.After administration 2h, intramuscular injection 10% chloral hydrate (0.3mL/100g) anesthesia, abdominal aortic blood.Blood leaves standstill 1h, and the centrifugal 10min of 3000r/min draws supernatant, puts in-20 DEG C of refrigerators and saves backup.
The processing of serum: the accurate serum 2mL that draws, adds methanol 8mL, vortex vibration 2min, the centrifugal 20min of 3000r/min, get supernatant, it is dry that nitrogen dries up instrument, and mobile phase is dissolved, be settled in 2mL volumetric flask, 0.45 μ m filtering with microporous membrane, for efficient liquid phase chromatographic analysis.
The high performance liquid chromatogram collection of illustrative plates contrast of each serum: high activity radix rehmanniae group and the more blank serum group of Radix Rehmanniae group serum, have more a new chromatographic peak, new chromatographic peak in identical position, illustrates that new chromatographic peak is the characteristic peak of catalpol with catalpol chromatographic peak.
The relatively peak area of catalpol in lyophilizing Radix Rehmanniae powder group and Radix Rehmanniae group serum, result, lyophilizing Radix Rehmanniae powder group peak area is 1.31 times of Radix Rehmanniae group serum peak area.The bioavailability that effective ingredient catalpol prepared by lyophilizing Radix Rehmanniae is described is high.
Detailed description of the invention
Lyophilizing Radix Rehmanniae is in the application of preparing in medicine, the application in the high medicine of the bioavailability of preparing effective ingredient catalpol.
Described lyophilizing Radix Rehmanniae is in the application of preparing in medicine, and the method for lyophilizing Radix Rehmanniae is: Radix Rehmanniae is put in freeze dryer, is refrigerated to below-10 DEG C, is evacuated to below drying chamber pressure 30Pa subliming by heating; The temperature of distillation is controlled at below 40 DEG C, and the temperature of resolution phase is controlled at below 45 DEG C, to dry.
Described lyophilizing Radix Rehmanniae is in the application of preparing in medicine, is that lyophilizing Radix Rehmanniae is made powder and adds in prepared medicine.
Described lyophilizing Radix Rehmanniae is in the application of preparing in medicine, is that lyophilizing Radix Rehmanniae is made powder and makes powder.
embodiment 1
Radix Rehmanniae is put in freeze dryer, is refrigerated to-10 DEG C, is evacuated to drying chamber pressure 30Pa, subliming by heating; The temperature of distillation is controlled at 40 DEG C, and the temperature of resolution phase is controlled at 45 DEG C, to dry.Take out, make powder.
embodiment 2
Radix Rehmanniae is put in freeze dryer, is refrigerated to-20 DEG C, is evacuated to drying chamber pressure 35Pa, subliming by heating; The temperature of distillation is controlled at 45 DEG C, and the temperature of resolution phase is controlled at 50 DEG C, to dry.Take out, make the watered pill.
embodiment 3
Radix Rehmanniae is put in freeze dryer, is refrigerated to-20 DEG C, is evacuated to drying chamber pressure 35Pa, subliming by heating; The temperature of distillation is controlled at 45 DEG C, and the temperature of resolution phase is controlled at 50 DEG C, to dry.Take out, make the watered pill.
embodiment 4
Radix Rehmanniae is put in freeze dryer, is refrigerated to-30 DEG C, is evacuated to drying chamber pressure 40Pa, subliming by heating; The temperature of distillation is controlled at 50 DEG C, and the temperature of resolution phase is controlled at 50 DEG C, to dry.Take out, make capsule.
embodiment 5
Get lyophilizing Radix Rehmanniae 160g, Fructus Corni 80g, Cortex Moutan 60g, Rhizoma Dioscoreae 80g, Poria 60g, Rhizoma Alismatis 60g, be ground into fine powder, sieve, mix.Every 100g powder adds refined honey 35～50g and appropriate water, and general ball is dry, makes water-honeyed pill.
embodiment 6
Get Cortex Cinnamomi 20g, Radix Aconiti Lateralis Preparata (system) 20g, lyophilizing Radix Rehmanniae 160g, Cortex Moutan 60g, Fructus Corni (system) 80g, Rhizoma Dioscoreae 80g, Poria 60g, Rhizoma Alismatis 60g.
Above eight tastes, Cortex Cinnamomi, Radix Aconiti Lateralis Preparata, Cortex Moutan, Fructus Corni (system), Rhizoma Dioscoreae, Poria, Rhizoma Alismatis, be ground into coarse powder, decoct with water secondary, 3 hours for the first time, 2 hours for the second time, merging filtrate, filters, and filtrate is condensed into the clear paste that relative density is 1.30～1.35 (20 DEG C); Lyophilizing Radix Rehmanniae is ground into fine powder, mixes with clear paste, makes ball, and dry, polishing, to obtain final product.
Claims (4)
1. lyophilizing Radix Rehmanniae, in the application of preparing in medicine, is characterized in that: prepare the application in the medicine that the bioavailability of effective ingredient catalpol is high.
According to the lyophilizing Radix Rehmanniae of claim 1 in the application of preparing in medicine, it is characterized in that: the method for lyophilizing Radix Rehmanniae is: Radix Rehmanniae is put in freeze dryer, be refrigerated to below-10 DEG C, be evacuated to below drying chamber pressure 30Pa subliming by heating; The temperature of distillation should be controlled at below 40 DEG C, and the temperature of resolution phase is controlled at below 45 DEG C, to dry.
According to the lyophilizing Radix Rehmanniae of claim 1 in the application of preparing in medicine, be that lyophilizing Radix Rehmanniae is made powder and adds in prepared medicine.
According to the lyophilizing Radix Rehmanniae of claim 1 or claim 3 in the application of preparing in medicine, be that lyophilizing Radix Rehmanniae is made powder and makes powder.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201410418839.7A CN104147223A (en) | 2014-08-25 | 2014-08-25 | Application of freeze-dried rehmannia glutinosa in preparation of drug |
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| CN201410418839.7A CN104147223A (en) | 2014-08-25 | 2014-08-25 | Application of freeze-dried rehmannia glutinosa in preparation of drug |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103055017A (en) * | 2013-01-10 | 2013-04-24 | 济南康众医药科技开发有限公司 | Freeze-dried rehmannia for treating diabetes mellitus |
| CN103055022A (en) * | 2013-01-10 | 2013-04-24 | 济南康众医药科技开发有限公司 | Method for processing rehmannia and application for rehmannia in preparation for medicine |
| CN103055019A (en) * | 2013-01-10 | 2013-04-24 | 济南康众医药科技开发有限公司 | Freeze-dried radix rehmanniae recens for treating cerebral thrombus |
-
2014
- 2014-08-25 CN CN201410418839.7A patent/CN104147223A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103055017A (en) * | 2013-01-10 | 2013-04-24 | 济南康众医药科技开发有限公司 | Freeze-dried rehmannia for treating diabetes mellitus |
| CN103055022A (en) * | 2013-01-10 | 2013-04-24 | 济南康众医药科技开发有限公司 | Method for processing rehmannia and application for rehmannia in preparation for medicine |
| CN103055019A (en) * | 2013-01-10 | 2013-04-24 | 济南康众医药科技开发有限公司 | Freeze-dried radix rehmanniae recens for treating cerebral thrombus |
Non-Patent Citations (1)
| Title |
|---|
| 赵应征: "《生物药物制剂学》", 30 June 2011, 浙江大学出版社 * |
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Application publication date: 20141119 |
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