CN100353936C - Ferulaic acid sodium transfusion and prescription and preparation thereof - Google Patents
Ferulaic acid sodium transfusion and prescription and preparation thereof Download PDFInfo
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- CN100353936C CN100353936C CNB03153242XA CN03153242A CN100353936C CN 100353936 C CN100353936 C CN 100353936C CN B03153242X A CNB03153242X A CN B03153242XA CN 03153242 A CN03153242 A CN 03153242A CN 100353936 C CN100353936 C CN 100353936C
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- sodium ferulate
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Abstract
The present invention relates to a medicinal preparation, particularly to a large capacity injection prepared from sodium ferulate. Every 1 ml of physic liquor in the injection contains 0.1 mg to 6.0 mg of sodium ferulate; the physic liquor is filled into an infusion bottle and can be directly administered for intravenous injection; the physic liquor can be a water solution of sodium ferulate; or furthermore, isotonic agents, antioxidants, etc. can be added to the physic liquor. The preparation method of the large capacity sodium ferulate injection comprises: weighing and taking a definite quantity of sodium ferulate and selectively added isotonic agents, antioxidants, etc.; adding water or other proper solvents to prepare physic liquor, wherein every 1 ml of the physic liquor contains 0.1 mg to 6.0 mg of sodium ferulate; regulating the pH value of the prepared physic liquor; filtering the physic liquor through a 0.45 mum to 0.22 mum microporous filtering film until the physic liquor is clear; filling the physic liquor into bottles and introducing nitrogen (N2); rolling covers and hot pressing for sterilization for a predetermined period of time; obtaining finished products of sodium ferulate large capacity injections. The sodium ferulate large capacity injection of the present invention has the advantages of safe and convenient use; the present invention is especially suitable for the first aid for patients with acute and severe diseases and meets the requirement of medical treatment.
Description
Technical field
The present invention relates to a kind of pharmaceutical preparation, particularly relate to the bulk capacity injection made from sodium ferulate, and prescription and preparation technology.
Background technology
Sodium ferulate has another name called angelicin, Rhizoma Chuanxiong element, and chemical name is 3-methoxyl group-4-Hydroxycinnamic Acid sodium salt dihydrate.It is the active ingredient of blood-activating and stasis-removing Radix Angelicae Sinensis and Rhizoma Chuanxiong, now existing synthetic.
Cardiovascular and cerebrovascular disease is one of principal disease that threatens human health.Pharmacological research shows that sodium ferulate is non-peptide-like endothelin receptor antagonist, but the vasoconstriction that the antagonism Endothelin causes, boosts and vascular smooth muscle cell proliferation, alleviates vascular endothelial injury; Increase the synthetic of NO, lax vascular smooth muscle; Anticoagulant, anticoagulation, improve hemorheology and learn feature.Sodium ferulate also can suppress the synthetic of cholesterol, and blood fat reducing is removed free radical, the control lipid peroxidation injury; Influence complement, the enhance immunity function, and have certain analgesia, spasmolysis.
Sodium ferulate has now been made tablet, powder, injectable powder, aqueous injection.In order to solve that the oral formulations drug effect is slow, bioavailability is low and injection problems such as complex operation, drug contamination when using, the present inventor has made bulk capacity injection with sodium ferulate, direct intravenous administration, safety, convenient is particularly useful for endangering, weighing disease patient's urgent rescue.As a kind of novel form, the sodium ferulate transfusion has its unique advantage.
Summary of the invention
One object of the present invention is to provide a kind of sodium ferulate novel form, i.e. sodium ferulate high-capacity injection.In the medicinal liquid of this injection, every 1ml medicinal liquid contains sodium ferulate 0.1mg～6.0mg, and fill is in the 100ml infusion bottle.Satisfying under the condition of intravenous drip, can carry out various variations as required, such as the variation of infusion bottle specification.These variations comprise within the scope of the present invention.In one embodiment, this medicinal liquid is the aqueous solution of sodium ferulate.Furthermore, can add compositions such as isotonic agent, antioxidant in the medicinal liquid of the present invention.
Another object of the present invention provides a kind of method that prevents sodium ferulate variable color in aqueous solution.
For achieving the above object, the present invention takes following technical scheme:
(1) a certain amount of sodium ferulate is dissolved in an amount of distilled water, is made into the solution of 0.1mg/ml～6.0mg/ml.
(2) solution that obtains in the above-mentioned steps is divided into two parts, a copy of it adds antioxidant, and another part does not add antioxidant, filters respectively, and fill is led to nitrogen N in infusion bottle
2, epiphragma is jumped a queue, and rolls lid.
(3) 110 ℃ of autoclavings 30 minutes, sample.
(4) color and luster of sample for reference, and adopt high-efficient liquid phase technique to check related substance.
A further object of the present invention provides a kind of method for preparing the sodium ferulate transfusion.
For achieving the above object, the present invention takes following technical scheme, promptly adopts following prescription or component amount:
Sodium ferulate (pure) 0.1g～6.0g
Isotonic agent is an amount of
Antioxidant is an amount of
Active carbon is an amount of
Water for injection (adding to) 1000ml
Said preparation method or technology comprise:
(1) take by weighing the isotonic agent of above-mentioned component amount, add an amount of water for injection dissolving, add proper amount of active carbon, boiled after stirring evenly 30 minutes, carbon removal is filtered in cooling, filtrate for later use.
(2) take by weighing the sodium ferulate of recipe quantity, add in the filtrate of gained, stirring and dissolving adds an amount of antioxidant again, stirring and dissolving, moisturizing is regulated the medicinal liquid pH value to 1000ml, the microporous filter membrane of crossing 0.45 μ m and 0.22 μ m is clear and bright to medicinal liquid, fill in infusion bottle, logical N
2, roll lid, behind the pressure sterilizing certain hour, check that packing gets product.
Medicine of the present invention is to be the prevention of active ingredient and the medicine of treatment cardiovascular and cerebrovascular disease with the sodium ferulate, contain sodium ferulate 0.1mg～6.0mg in every 1ml medicinal liquid, the isotonic agent in the prescription can be pharmaceutically acceptable materials such as sodium chloride, glucose, sorbitol; Antioxidant can be glycine, L-cysteine, N-acetylcystein (and its esters), citric acid (and its esters), ethylenediaminetetraacetic acid pharmaceutically acceptable materials such as (and its esters); Solvent can be water or other polar solvent.
Medicine of the present invention can be directly used in intravenous administration, and its consumption can be adjusted according to the order of severity of patient's age, body weight, disease, general each 100mg～300mg, and 1 time on the one, 10 days is a course of treatment, intravenous drip.
The present invention has carried out system, the comprehensive analysis to sodium ferulate, especially the research that the stability of sodium ferulate in aqueous solution is carried out, and taked effective method, particularly add suitable antioxidation measures such as antioxidant, and injection is adjusted to suitable pH value, guaranteed the stable of injection.PH value is between 4.0-7.0, and preferred range is between 5.3-5.7.This method is convenient, simple, very with practical value.
Compare with existing 2ml, 5ml small-volume injection, on technology, the former is the injection production technology, and the latter is the transfusion production technology, is diverse.The important bulk capacity injection that is has satisfied needing of medical treatment as a kind of novel form, and directly intravenous administration safely, conveniently, has been eliminated the medicine pollution in the transfusion process for preparation, is particularly useful for endangering, weighing disease patient's urgent rescue.
Be further introduced below in conjunction with accompanying drawing:
Description of drawings
Fig. 1 is the process chart of preparation sodium ferulate transfusion;
Fig. 2 criticizes the HPLC collection of illustrative plates of sodium ferulate transfusion for 030606A;
Fig. 3 criticizes the HPLC collection of illustrative plates of sodium ferulate transfusion for 030606B;
Fig. 4 is the HPLC collection of illustrative plates of 030607 batch of sodium ferulate transfusion;
Fig. 5 is the HPLC collection of illustrative plates of blank solution.
The code name that uses in the presents, such as 030606A criticize, 030606B criticizes, 030607 batch etc., all be the code name of regulation voluntarily in the research, there is no the actual product listing.
Invention embodiment
The preparation of embodiment 1. sodium ferulate transfusion
(1) takes by weighing sodium chloride 27.0g, add water 270ml dissolving, add the 1.5g active carbon and stir evenly, boiled 30 minutes, take out, put coldly, filter carbon removal.
(2) above-mentioned solution adds 3.0g sodium ferulate, 0.15g glycine and 0.3g disodiumedetate, stirring and dissolving, and moisturizing is surveyed pH=5.8 to 3000ml.
(3) cross 0.45 μ m and 0.22 μ m microporous filter membrane, fill is filled N in the 100ml infusion bottle
2, roll lid.
(4) 110 ℃ of autoclavings 30 minutes.
Adopt embodiment 1 described method, only change the sodium ferulate consumption that is added in the step (2), be respectively 6.0g, 9.0g, 12.0g, 15.0g and 18.0g.Having prepared concentration is 2mg/ml, 3mg/ml, 4mg/ml, the sodium ferulate transfusion of 5mg/ml and 6mg/ml.
Embodiment 2: the preparation of sodium ferulate sodium chloride injection
(1) takes by weighing sodium chloride 27.0g, add water 270ml dissolving, add the 1.5g active carbon, stir evenly, boiled 30 minutes, take out, put coldly, filter carbon removal.
(2) above-mentioned solution adds 1.5g sodium ferulate, 0.15g glycine and 0.3g disodiumedetate, stirring and dissolving, and moisturizing is surveyed pH=5.8 to 3000ml.
(3) cross 0.45 μ m and 0.22 μ m microporous filter membrane, fill is filled N in the infusion bottle of 100ml
2, roll lid.
(4) 110 ℃ of autoclavings 30 minutes.
According to the method for embodiment 2, adjust for the amount of the sodium ferulate that adds in the step (2), be adjusted into 1.2g respectively, 0.9g, 0.75g, 0.6g and 0.3g.Prepared concentration and be respectively 0.4mg/ml, 0.3mg/ml, 0.25mg/ml, the sodium ferulate sodium chloride injection of 0.2mg/ml and 0.1mg/ml.
The effect of embodiment 3. antioxidant glycine
(1) takes by weighing sodium chloride 18.0g, add water 180ml dissolving, add the 2.0g active carbon and stir evenly, boiled 30 minutes, take out, put coldly, filter carbon removal.
(2) above-mentioned solution adds the 2.0g sodium ferulate, stirring and dissolving, and moisturizing is surveyed pH=6.3 to 2000ml.Solution is divided into two parts, every part of 1000ml, a copy of it (being designated as 030601A criticizes) adjust pH is 5.6; Another part (being designated as 030601B criticizes) adds glycine 0.5g, and stirring and dissolving transfers to pH=5.6.
(3) cross 0.45 μ m and 0.22 μ m microporous filter membrane respectively, fill is filled N in the 100ml infusion bottle
2, roll lid.
(4) 110 ℃ of autoclavings 30 minutes.
The gained sample is checked color and luster, and wherein 030601A criticizes and do not add antioxidant, is colourless before the sterilization, and is No. 4 colors after the sterilization; 030601B criticizes and is added with antioxidant, is colourless before and after the sterilization.The result shows, the sodium ferulate transfusion adds suitable antioxidant, and the color and luster of injection is had significant improvement.
(1) take by weighing sodium chloride 1.8g, add water 18ml dissolving, add the 2.4g sodium ferulate, moisturizing is to 200ml.Medicinal liquid is divided into two parts, and every part of 100ml, a copy of it (being designated as 030606A) add the dissolving of 0.5g sodium metabisulfite, survey pH=5.5.Another part (being designated as 030606B) adds the 0.1g disodiumedetate, and stirring and dissolving is surveyed pH=5.68.
(3) cross 0.45 μ m and 0.22 μ m microporous filter membrane respectively, fill is filled N in the 100ml infusion bottle
2, roll lid.
(4) 110 ℃ of autoclavings 30 minutes.
The gained sample is checked related substance, sees Fig. 2, Fig. 3.030606A criticizes to adding the sample of antioxidant sodium metabisulfite, as shown in Figure 2, locates in about 4 minutes in retention time, and an impurity peaks is arranged; And 030606B except that main peak, does not occur other impurity peaks (locating to be the blank solvent peak in about 3 minutes in retention time) for adding the sample of disodiumedetate.
Results suggest, the sulphite kind antioxidant may interact with sodium ferulate, produces other impurity.030607 batch of sample for adding antioxidant glycine and disodiumedetate as seen from Figure 4, except that main peak and solvent peak, other impurity peaks do not occur.
The clinical practice of embodiment 5. sodium ferulate intravenously administrables
Quiet sodium ferulate treatment migraine 8 routine curative effects are summed up
The positive tawny daylily arrangement in Xuanwu Hospital, Capital Medical College Neurology Department Shen.
From year October in February, 1984 to 1985, quiet treatment of injectable powder that we are provided with medical courses in general institute medicine 8 routine migraineurs now is summarized as follows curative effect:
1. case is selected:
Selected 8 examples, male 2 examples, women 6 examples, 25～50 years old age, 37 years old mean age.8 examples are the classical migraine patient, medical history more than 4～30 year, and headache degree in the recent period increases the weight of, and outbreak is frequent, once uses multiple analgesic drug product poor effect, and before the sodium ferulate treatment, all cases are all through electroencephalogram and department of neurology physical examination.Indivedual cases also are CT and waist is worn inspection, with except encephalopathy etc. other cause the department of neurology illness of headache.
2. method:
The 100mg sodium ferulate be dissolved in 5% Glucose Liquid quiet 1 time/day, 30 days is a course of treatment.Write down headache degree, frequency and major-minor effect every day in the observation process.Other analgesic drug product of forbidding during the treatment.8 routine patient's 5 examples are in hospital quiet, quiet of 3 routine outpatient services.
3. result:
8 routine patients are all effective with quiet treatment of sodium ferulate, and wherein 6 examples are cured or produce effects, and 2 examples effectively.None example has any side effect in the therapeutic process.
Quiet sodium ferulate treated 4 routine migraine observation of curative effect
Tang of Beijing Friendship Hospital ten thousand instrument, period-luminosity prolongs and Li Zhimin puts in order.
Sodium ferulate is the active ingredient of controlling blood blood stasis dispelling Chinese medicine angelica and Rhizoma Chuanxiong.Confirmed that Radix Angelicae Sinensis has the anticoagulant effect and suppresses platelet release reaction, its mechanism of action generates relevant with inhibition platelet T XA2.Migraineur's platelet aggregation increases.We select 4 routine migraineurs all to have outbreak frequently, and oral excessively I number or II medicine.Purpose is observed the effect (clinical data sees the following form) of different approaches and dosage dispensing.
Method: sodium ferulate 200mg adds dead point in 5% glucose saline, once a day, and logotype 6 days.Dead point before and after look platelet aggregation.
The result:
| Sequence number | Name | Sex | Age | Outbreak frequency | Oral curative effect | The sodium ferulate dead point | Platelet aggregation rate | ||||
| Dosage | Number of times | Effect | Before the injection | After the |
|||||||
| 1 | Marquis * * | The woman | 32 | In | II number | 200mg | 6 | Control fully | 86％ | 45％ | |
| 2 | Lee * * | The woman | In | I, II number | 200mg | 6 | Degree alleviates | 90％ | 79％ | ||
| 3 | The * * of the Qin | The woman | In | I number invalid, the II produce effects | 200mg | 1 | Control fully | 50％ | |||
| 4 | Marquis * * | The |
25 | Heavy | I number | 200mg | 6 | Degree is alleviated | 82％ | ||
Annotate: looked in 15th after the drug withdrawal.
Sodium ferulate can be used as quick treatment one means.Example 1 outbreak is frequent, and example 3 pain outbreak in just suitable menstrual period is vomitted serious unbearably.Behind dead point, all can take effect immediately.Example 3 for some reason only dead point once, but headache control is more satisfactory, continues a not outbreak in month, the oral II medicine of this example is a produce effects, may be to the sense of this susceptibility.The dead point effect is obvious.
Claims (7)
1. a sodium ferulate high-capacity injection is characterized in that this injection liquid includes a kind of solvent and antioxidant glycine, contains sodium ferulate 0.1mg～6.0mg in every 1ml medicinal liquid, directly intravenous administration.
2. sodium ferulate high-capacity injection as claimed in claim 1 is characterized in that the solvent in the described medicinal liquid is a water.
3. sodium ferulate high-capacity injection as claimed in claim 1 is characterized in that this injection liquid further comprises isotonic agent and other antioxidant.
4. sodium ferulate high-capacity injection as claimed in claim 3 is characterized in that described isotonic agent is selected from sodium chloride, glucose, sorbitol or its combination.
5. sodium ferulate high-capacity injection as claimed in claim 3 is characterized in that described other antioxidant are selected from L-cysteine and its esters, N-acetylcystein, citric acid and its esters, ethylenediaminetetraacetic acid and its esters or their combination.
6. method for preparing sodium ferulate high-capacity injection as claimed in claim 1, it is characterized in that comprising the following steps: to take by weighing a certain amount of sodium ferulate and glycine, it is added water be mixed with certain density solution, moisturizing is regulated gained medicinal liquid pH value to 1000ml, microporous filter membrane through 0.45 μ m and 0.22 μ m is clear and bright to medicinal liquid, fill feeds nitrogen in bottle, roll lid, pressure sterilizing obtains the finished product sodium ferulate high-capacity injection after one scheduled time.
7. method as claimed in claim 6, its feature also is: after taking by weighing a certain amount of sodium ferulate, further the isotonic agent of weighing Sq and other antioxidant are allocated in the solution.
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| Application Number | Priority Date | Filing Date | Title |
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| CNB03153242XA CN100353936C (en) | 2003-08-07 | 2003-08-07 | Ferulaic acid sodium transfusion and prescription and preparation thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB03153242XA CN100353936C (en) | 2003-08-07 | 2003-08-07 | Ferulaic acid sodium transfusion and prescription and preparation thereof |
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| CN1543939A CN1543939A (en) | 2004-11-10 |
| CN100353936C true CN100353936C (en) | 2007-12-12 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN101756894B (en) * | 2008-12-23 | 2011-07-06 | 上海华中药业有限公司 | Method for filtering sodium ferulate high-capacity injection |
| CN107669643A (en) * | 2017-11-24 | 2018-02-09 | 海南通用康力制药有限公司 | Nicergoline for injection freeze drying powder injection and preparation method thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1050869A (en) * | 1990-11-28 | 1991-04-24 | 四川省劳动卫生职业病防治研究所 | α, the synthetic method of beta-unsaturated acid |
| CN1347316A (en) * | 1999-04-13 | 2002-05-01 | 科技基因有限公司 | Composition for preventing or treating dementia comprising hydroxycinnamic acid deriv. or extract of plant of genus angelicae contg. same |
-
2003
- 2003-08-07 CN CNB03153242XA patent/CN100353936C/en not_active Expired - Lifetime
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1050869A (en) * | 1990-11-28 | 1991-04-24 | 四川省劳动卫生职业病防治研究所 | α, the synthetic method of beta-unsaturated acid |
| CN1347316A (en) * | 1999-04-13 | 2002-05-01 | 科技基因有限公司 | Composition for preventing or treating dementia comprising hydroxycinnamic acid deriv. or extract of plant of genus angelicae contg. same |
Non-Patent Citations (1)
| Title |
|---|
| 药剂学 卷号:版本号: 1998.08.01 * |
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