CN1491661A - Total penoniforn preparation and its use - Google Patents
Total penoniforn preparation and its use Download PDFInfo
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- CN1491661A CN1491661A CNA031534961A CN03153496A CN1491661A CN 1491661 A CN1491661 A CN 1491661A CN A031534961 A CNA031534961 A CN A031534961A CN 03153496 A CN03153496 A CN 03153496A CN 1491661 A CN1491661 A CN 1491661A
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- radix paeoniae
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Abstract
The present invention discloses a kind of total penoniforin preparation with thrombolysis activity and used as medicine for treating cardiac and cerebral vascular diseases. The preparation contains total penoniforin in 50-99 % of solid matter weight. Pharmacodynamical experiment shows that the preparation has obvious thrombolytic and thrombosis resisting effect.
Description
Affiliated field
The present invention relates to a kind of cardiovascular medicament Radix Paeoniae general glycoside preparation and preparation method thereof, belong to medical pharmaceutical field, particularly belong to Chinese medicine antithrombotic reagent pharmaceutical technology field with thrombolytic and antithrombotic acitivity.
Background technology
Radix Paeoniae (Paeonia Lactflora Pall) is divided into two kinds of the Radix Paeoniae Alba and Radix Paeoniae Rubra, starts from Song's Holy Benevolent Prescriptions.Its main effective ingredient is paeoniflorin (Paeoniforin), peony lactone glycoside (Albiforin), and hydroxypaeoniflorin (Oxypaeoniflorin), benzoylpaeoniflorin monoterpene glycoside compounds such as (Benzoyl paeoniflorin) is called for short the Radix Paeoniae general glycoside.The modern plants chemistry thinks that Radix Paeoniae Alba total glycosides is the active component in the Radix Paeoniae, mainly is present in the root bark portion of Radix Paeoniae.Traditional medicine thinks, Radix Paeoniae Rubra can clearing away heat and cooling blood, and eliminating stasis to stop pain clinically, is diseases such as monarch drug prescription therapeutic ischemic angiocardiopathy and cerebrovascular with Radix Paeoniae Rubra or with Radix Paeoniae Rubra.
Retrieve in the relevant patent and data of literatures of having applied for Radix Paeoniae, do not mention that also with content be the pharmaceutical preparation that the Radix Paeoniae general glycoside of 50-99% is made, effect experiment proves, injection, injectable powder, infusion solution and the lipomul made of the Radix Paeoniae general glycoside of content has significant thrombolytic and antithrombotic effect thus.
Summary of the invention
The invention discloses a kind of cardiovascular medicament Radix Paeoniae general glycoside preparation with thrombolytic and antithrombotic acitivity and preparation method thereof, the Radix Paeoniae general glycoside accounts for the 50-99% of total solid in the preparation of making.Its dosage form is injection, injectable powder, infusion solution and lipomul.
The solid constituent of Radix Paeoniae total glycoside injection is made up of Radix Paeoniae general glycoside and pharmaceutic adjuvant, and wherein the total salidroside content of Radix Paeoniae is 50%-99%.
The Radix Paeoniae total glycoside injection mainly contains injection, injectable powder, infusion solution and lipomul.Its preparation method is different according to different dosage forms.
The Radix Paeoniae general glycoside is dissolved with water for injection, after the injection of adding metering dissolved with the water solublity pharmaceutic adjuvant, regulator solution PH to 6.0-7.0 was after the microporous filter membrane ultrafiltration, add the injection water and add to ormal weight, carry out packing or carry out dried according to the dosage form needs again.
Preparation Radix Paeoniae general glycoside injection, the content of the interior Radix Paeoniae general glycoside of injection is 10-100mg/ml before the packing, be sub-packed in the ampoule bottle, every 2ml, the sealing by fusing sterilization, after the assay was approved, packing is promptly.
Preparation Radix Paeoniae general glycoside infusion solution, the content of Radix Paeoniae general glycoside is 1-10mg/ml in the preceding injection of packing, is packed as 100ml, 150ml, 200ml in corresponding infusion bottle, rolls lid, after the assay was approved, packing is promptly.
Preparation Radix Paeoniae general glycoside injectable powder, after the Radix Paeoniae general glycoside doubly measured water for injection dissolving with 5-10, after the injection of adding metering fully dissolves with the water solublity pharmaceutic adjuvant, transfer PH to 6.0-7.0, filter, in 40 ℃ of following vacuum dryings, aseptic subpackaged in the 5ml cillin bottle, every bottle contains Radix Paeoniae general glycoside 100-250mg, rolls lid, after the assay was approved, packing promptly.
Preparation Radix Paeoniae general glycoside lyophilized injectable powder, with the Radix Paeoniae general glycoside after refining, doubly measure the water for injection dissolving with 5-10 after, the injection water solublity pharmaceutic adjuvant that adds metering, transfer PH to 5.0-7.0, filter, be diluted to every milliliter with water for injection and contain Radix Paeoniae general glycoside 10-20mg, be sub-packed in the ampoule, every 10ml, after lyophilization, sealing by fusing, after the assay was approved, packing promptly.
Below by embodiment cardiovascular medicament total paeony glycoside preparation with thrombolytic and antithrombotic acitivity of the present invention and preparation method thereof is described further.
Embodiment 1:
Preparation Radix Paeoniae general glycoside aqueous injection.
1kg is dissolved in the 100L water for injection with the Radix Paeoniae general glycoside, is made into 10mg/ml, regulates PH to 6.0.After the microporous filter membrane ultrafiltration, replenish water for injection to ormal weight, fill is in ampoule bottle, and the sealing by fusing sterilization through after the assay was approved, is packed promptly.
Embodiment 2
Preparation Radix Paeoniae general glycoside injectable powder.
Radix Paeoniae general glycoside 1kg is dissolved in an amount of 100L water for injection, the pharmaceutic adjuvant that adds metering, regulate PH to 6.0, after the microporous filter membrane ultrafiltration, vacuum drying gets Radix Paeoniae general glycoside aseptic powder, and aseptic powder is sub-packed in the cillin bottle, make every bottle and contain Radix Paeoniae general glycoside aseptic powder 100mg, three specifications of 150mg, 200mg, roll lid, through after the assay was approved, packing promptly.
Embodiment 3
Preparation Radix Paeoniae general glycoside lyophilized injectable powder
With Radix Paeoniae general glycoside 1kg, after the dissolving of 5 times of amount water for injection, add the injection water solublity pharmaceutic adjuvant of metering, regulate PH to 6.0, filter, be loaded in the ampoule bottle, every 10ml, after lyophilization, sealing by fusing, after the assay was approved, packing is promptly.
Embodiment 4
Preparation Radix Paeoniae general glycoside lipomul.
With Radix Paeoniae general glycoside 1kg, be dissolved in the 100L injection fat solvent (forming) by water for injection and emulsifying agent, be made into the solution of 10mg/ml, regulate PH to 6.0.After the microporous filter membrane ultrafiltration, be sub-packed in 2ml, the 5ml ampoule, after the assay was approved, packing is promptly.
The pharmacological effect experiment
Experiment 1, Radix Paeoniae general glycoside are to the thrombotic influence of rats in vitro
Experiment material
1. medicine: Radix Paeoniae general glycoside powder pin: 50mg/ props up; The injection XUESHUANTONG: 50mg/ props up.
2. animal: 40 of healthy male Wistar rats, body weight 210.72 ± 9.0g.
Experimental technique
40 rats are divided into 4 groups (10 every group) at random: 1. matched group (0.9% sodium chloride injection, 5.0ml/kg), 2. Radix Paeoniae general glycoside powder pin 20mg/kg dosage group, 3. Radix Paeoniae general glycoside powder pin 10mg/kg dosage group, 4. injection XUESHUANTONG 20mg/kg dosage group.Each treated animal by described dosage with the injection volume of 5.0ml/kg through the tail vein injection administration, once a day, successive administration 3 days, 30min after the last administration with pentobarbital sodium (30.0mg/kg) anesthesia, is used for external thrombus from abdominal aortic blood 2ml and forms and measure.
External thrombus forms to be measured: according to the Chandler in vitro method, at once blood is injected in the rotating ring, the blood volume of injection is full of rotating ring below 1/2, rapidly sealing, put on the thrombosis instrument, rotation 10min, inclining thrombosis, the normal saline washing, measure length, the weighing weight in wet base is put 80 ℃ of baking oven 3h with the thrombosis bar, claims its dry weight after the constant weight.
Experimental result:
Table 1. Radix Paeoniae general glycoside is to the thrombotic influence of rats in vitro (X ± SD)
| Group | Dosage (/kg) | Number of animals | Thrombosis | ||
| Length (mm) | Weight in wet base (mg) | Dry weight (mg) | |||
| Matched group | ????10 | ??23.1±1.2 | ??154.4±12.0 | ??27.2±1.5 | |
| The injection XUESHUANTONG | ??20mg | ????10 | ??16.7±2.0 | ??132.6±20.3 | ??19.4±4.3 |
| Radix Paeoniae general glycoside powder pin | ??10mg | ????10 | ??20.9±1.3 | ??130.7±13.8 | ??24.7±5.2 |
| Radix Paeoniae general glycoside powder pin | ??20mg | ????10 | ??16.9±2.7 | ??131.0±21.8 | ??20.3±4.0 |
Annotate: compare P＜0.01 with matched group
By table 1 as seen, compare with matched group, the thrombosis length of Radix Paeoniae general glycoside powder pin 20mg/kg and 10mg/kg dosage group all obviously shortens (P＜0.01), and wet weight of thrombus and dry weight all obviously alleviate (P＜0.01), and the thrombosis dry weight has the trend of alleviating; The thrombosis dry weight of injection XUESHUANTONG group obviously alleviates (P＜0.05), and thrombosis length has shortening trend, and wet weight of thrombus has the trend of alleviating.Show that Radix Paeoniae general glycoside powder needle set has the effect that suppresses thrombosis, blood viscosity lowering, to compare drug effect suitable with XUESHUANTONG.
Experiment 2: the Radix Paeoniae general glycoside is to the influence of clotting time of mice
50 of kunming mices are divided into 5 groups at random, each treated animal by described dosage with the injection volume of 5.0ml/kg through the tail vein injection administration, once a day, successive administration 3 days, behind the 1h, abdominal aortic blood is used the determination of tube method clotting time after the last administration.The result: three kinds of dosage all obviously prolong the clotting time of mice.
Experimental result:
Table 2 Radix Paeoniae general glycoside is to the influence of clotting time of mice (n=10, x ± s)
Group dosage (mg/kg) clotting time (s)
Capacity such as normal saline 55.1 ± 10.8
Total paeony glycoside (greatly) 20 70.8 ± 12.0
Total paeony glycoside (in) 10 64.5 ± 12.2
Total paeony glycoside (little) 5 57.6 ± 9.7
Aspirin 10 67.0 ± 10.6
Compare P＜0.01 with the normal saline group
Claims (7)
1. cardiovascular medicament Radix Paeoniae general glycoside preparation with thrombolytic and antithrombotic acitivity is characterized in that the total salidroside content of Radix Paeoniae in the preparation accounts for the 50%-99% of total solid.Its dosage form is injection, injectable powder, infusion solution and lipomul.
2,, form as active component and pharmaceutic adjuvant by the Radix Paeoniae general glycoside according to the injection in the claim 1.
3, according to the aqueous injection in the claim 1, form by Radix Paeoniae general glycoside and water for injection and water soluble adjuvant, it is characterized in that: the Radix Paeoniae general glycoside is dissolved in an amount of water for injection, adds the injection water soluble adjuvant of metering, regulate PH to 5.0-7.0, after the microporous filter membrane ultrafiltration, replenish water for injection to ormal weight, fill is in ampoule bottle or in the infusion bottle, sealing by fusing/roll lid, through after the assay was approved, packing promptly.The total salidroside content of Radix Paeoniae is 3.0-30.0mg/ml in the injection, and specification is 2ml, 5ml.Infusion solution contains Radix Paeoniae general glycoside 2.0-30.0mg/ml, and specification is 50ml, 100ml, 150ml and 200ml.
4, according to the injectable powder in the claim 1, form by Radix Paeoniae general glycoside and water for injection dissolubility pharmaceutic adjuvant, it is characterized in that: the Radix Paeoniae general glycoside is dissolved in an amount of water for injection, adds the pharmaceutic adjuvant of metering, adjusting PH is 5.0-7.0, after the microporous filter membrane ultrafiltration, low-temperature vacuum drying, aseptic subpackaged in cillin bottle, every bottle contains Radix Paeoniae general glycoside 10-200mg, roll lid, through after the assay was approved, packing promptly.
5, according to the lyophilized injectable powder in the claim 1, form by Radix Paeoniae general glycoside and water for injection dissolubility pharmaceutic adjuvant, it is characterized in that: the Radix Paeoniae general glycoside is dissolved in an amount of water for injection, adds the pharmaceutic adjuvant of metering, adjusting PH is 5.0-7.0, after the microporous filter membrane ultrafiltration, be sub-packed in the ampoule bottle, the total salidroside content of Radix Paeoniae is 10-200mg in the per ampoule bottle, sealing by fusing after lyophilization, after the assay was approved, packing promptly.
6, according to the lipomul in the claim 1, be the Radix Paeoniae general glycoside to be dissolved in the injection fat solvent (comprise water for injection, emulsifying agent and pharmaceutic adjuvant), be sub-packed in behind the mix homogeneously in the ampoule bottle, the total salidroside content of Radix Paeoniae is 3.0-30.0mg/ml in the per ampoule bottle, and specification is 2ml, 5ml.
7, extract from the plant amedica Radix Paeoniae Rubra or the Radix Paeoniae Alba according to the Radix Paeoniae general glycoside in the claim 1.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA031534961A CN1491661A (en) | 2003-08-15 | 2003-08-15 | Total penoniforn preparation and its use |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA031534961A CN1491661A (en) | 2003-08-15 | 2003-08-15 | Total penoniforn preparation and its use |
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| Publication Number | Publication Date |
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| CN1491661A true CN1491661A (en) | 2004-04-28 |
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| CNA031534961A Pending CN1491661A (en) | 2003-08-15 | 2003-08-15 | Total penoniforn preparation and its use |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1767210A4 (en) * | 2004-07-02 | 2010-09-08 | Shanghai Inst Materia Medica | The medical use of paeoniflorin |
| CN1706397B (en) * | 2005-02-04 | 2011-11-16 | 沈阳药科大学 | Composition of paeoniflorin and peony lactone glycoside with function of increasing leukocyte |
-
2003
- 2003-08-15 CN CNA031534961A patent/CN1491661A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1767210A4 (en) * | 2004-07-02 | 2010-09-08 | Shanghai Inst Materia Medica | The medical use of paeoniflorin |
| CN1706397B (en) * | 2005-02-04 | 2011-11-16 | 沈阳药科大学 | Composition of paeoniflorin and peony lactone glycoside with function of increasing leukocyte |
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