CN106822843A - A kind of Xinshenghua side's active component, active ingredient composition and preparation method thereof - Google Patents

A kind of Xinshenghua side's active component, active ingredient composition and preparation method thereof Download PDF

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CN106822843A
CN106822843A CN201710128514.9A CN201710128514A CN106822843A CN 106822843 A CN106822843 A CN 106822843A CN 201710128514 A CN201710128514 A CN 201710128514A CN 106822843 A CN106822843 A CN 106822843A
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parts
xinshenghua
active ingredient
active component
total
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黄胜良
彭国平
辛小娜
李存玉
吴建雄
孙大正
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JIANGSU RENSHOU PHARMACEUTICAL CO Ltd
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JIANGSU RENSHOU PHARMACEUTICAL CO Ltd
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    • A61K2236/55Liquid-liquid separation; Phase separation

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Abstract

The invention discloses a kind of Xinshenghua side's active component, active ingredient composition extremely preparation method, said composition is prepared from by the raw material of following weight:20 40 parts of motherwort total alkaloid, 10 20 parts of safflower total flavone, 5 10 parts of ligustrazine, 10 20 parts of forulic acid, 5 10 parts of amarogentin, 15 parts of glycyrrhizic acid, 15 parts of Chinese angelica volatile oil, 10 20 parts of the total phenol of rhizoma zingiberis, 15 parts of liquiritin.The present invention provide Chinese medicine composition there is good promoting blood circulation, menstruction regulating and pain relieving effect, flavour of a drug to simplify after ensure good effects while, clinical application amount is less.The Chinese medicine composition preparation method that the present invention is provided, to effectively prevent and cause active component, active ingredient precipitation loss because soda acid composition forms compound during Traditional Chinese medicine decocting, realizes that natural resources of Chinese medicinal materials is rationally utilized while curative effect of medication is ensured.

Description

A kind of Xinshenghua side's active component, active ingredient composition and preparation method thereof
Technical field
The invention belongs to field of medicaments, it is related to a kind of Chinese medicine composition with promoting blood circulation, menstruction regulating and pain relieving, and in particular to A kind of Xinshenghua side's active component, composition of active ingredient and preparation method thereof.
Background technology
Dysmenorrhoea is one of most common symptom of gynaecology, and the women that there are about 75% occurs dysmenorrhoea.Dysmenorrhoea be divided into primary and after Two major classes of hair property, between primary dysmenorrhea refers to month paramenstrum, lower abdomen and waist spasmic pain, with evil when serious The heart, vomiting, limb are cold, are especially more common in Unmarried women.Chinese medicine gynecological disease has long history, with the dialectical differentiation of disease With reference to, traditional Chinese medicine manifests the treatment advantage of its uniqueness further, but at present more than the compound medicine for the treatment of dysmenorrhoea in the presence of formula flavour of a drug group Cheng Duo, dosage are big, indefinite using inconvenience, complicated component, active component, and the material base that curative effect is played in compound is unclear, And there are problems that certain, therefore necessary removed crudely and store essence under the guidance of traditional Chinese medical theory, preferably go out one Kind of drug ratio is simplified, determined curative effect, Small side effects, convenient to take, for promoting blood circulation, the medicine of menstruction regulating and pain relieving.
The content of the invention
In view of the shortcomings of the prior art, it is an object of the invention to provide a kind of Xinshenghua side's active component, active ingredient Composition, said composition drug ratio is simplified, dosage is few, good effect, side effect are smaller, convenient to take, and with work The effect of blood and dissolving stasis, menstruction regulating and pain relieving;Preparation method another object of the present invention is to provide said composition.
The present invention is achieved by the following technical solutions:
A kind of Xinshenghua side's active component, active ingredient composition, are prepared from by the raw material of following weight:
Motherwort total alkaloid 20-40 parts, safflower total flavone 10-20 parts, ligustrazine 5-10 parts, forulic acid 10-20 parts, semen armeniacae amarae Glycosides 5-10 parts, glycyrrhizic acid 1-5 parts, Chinese angelica volatile oil 1-5 parts, total phenol 10-20 parts, liquiritin 1-5 parts of rhizoma zingiberis.
There is choosing, the parts by weight of raw materials proportioning is motherwort total alkaloid 25-35 parts, safflower total flavone 12-18 parts, river 6-8 parts of rhizome of chuanxiong piperazine, forulic acid 12-18 parts, amarogentin 6-8 parts, glycyrrhizic acid 2-4 parts, Chinese angelica volatile oil 2-4 parts, the total phenol 12- of rhizoma zingiberis 18 parts, liquiritin 2-4 parts.
Further improvement of the present invention scheme is:
A kind of Xinshenghua side's active component, the preparation method of active ingredient composition, comprise the following steps:
Step one, each raw material is weighed according to described weight;
Step 2, takes Chinese angelica volatile oil and uses beta-cyclodextrin inclusion compound, beta-schardinger dextrin to be dissolved in purified water, and addition ethanol dissolves Chinese angelica volatile oil solution, included using high speed disperser, inclusion solution is super using the Da molecular cut offs of 5000-30 000 Filter membrane is separated, and collects ultrafiltrate, and ultrafiltrate is concentrated using the NF membrane of 100-800 Da molecular cut offs, and concentrate is dry through spraying It is dry to process to obtain Ligustilide spray powder;
Step 3, by motherwort total alkaloid, safflower total flavone, ligustrazine, forulic acid, amarogentin, glycyrrhizic acid, the total phenol of rhizoma zingiberis Fine powder is ground into liquiritin, after being mixed with Ligustilide spray powder, and pharmaceutically acceptable carrier, such as brown sugar, medicinal shallow lake Powder, sucrose, are prepared into the clinically receptible formulation of institute.
The weight ratio of Chinese angelica volatile oil and beta-schardinger dextrin is 1 in the step 2:5-20.
The receptible formulation of the clinically institute is water decoction, capsule, tablet, granule, syrup, suppository, injection Agent or encapsulated form.
Further improvement project of the invention is:
Water decoction, capsule, tablet, the particle being made of a kind of described Xinshenghua side's active component, active ingredient composition Agent, syrup, suppository, injection or microcapsules.
Each raw material is extracted by the following method:Motherwort total alkaloid is extracted by motherwort water, and extract solution adjusts pH Prepared using cationic ion-exchange resin enrichment after to 3-4;Safflower total flavone is extracted by safflower water, and extract solution adjusts pH to 2- Prepared using polyamide enrichment after 3;Ligustrazine is to adjust pH value of solution to 2-3, ethanol alcohol after Ligusticum wallichii water is extracted It is heavy, and then obtained by the enrichment of C18 preparative chromatographies;Forulic acid is to adjust pH value of solution to 7-8, ethanol alcohol after Ligusticum wallichii water is extracted It is heavy, and then obtained by the enrichment of C18 preparative chromatographies;Amarogentin is extracted for bitter almond water, and extract solution uses poly- after adjusting pH to 2-3 Amide resin enrichment is prepared;The preparation method of glycyrrhizic acid and liquiritin is rich using macroreticular resin after liquorice beverage is extracted Collection, and then using different concentration ethanol wash-out, segmentation, obtain glycyrrhizic acid and liquiritin;Chinese angelica volatile oil passes through Radix Angelicae Sinensis vapor Distillation is prepared;, the total phenol of rhizoma zingiberis preparation method be ginger ale extract, extract solution adjust pH to 2-3 after use polyamide Enrichment is prepared.In addition, above-mentioned each raw material can be bought from market.
The present invention is screened in early stage to treating dysmenorrhoea prescription at all times, under the guidance of traditional Chinese medical theory, diagnosis and treatment based on an overall analysis of the illness and the patient's condition, With reference to the pathogenesis and disease symptom of dysmenorrhoea, with it is promoting blood circulation and removing blood stasis be treatment according to screening prescription is carried out, it is determined that with motherwort total The total phenol of alkaloid, safflower total flavone, ligustrazine, forulic acid, amarogentin, glycyrrhizic acid, rhizoma zingiberis, liquiritin and Chinese angelica volatile oil group Into Chinese medicine composition.
The present invention based on tcm treatment according to syndrome differentiation combination modern pharmacology research, motherwort total is biological have anti-inflammatory, analgesia and Anti- dysmenorrhoea effectiveness, safflower total flavone realizes promoting blood circulation and removing blood stasis, ligustrazine antithrombus formation by platelet aggregation-against, and forulic acid can be with Platelet aggregation-against and thrombus, anti-inflammatory, strengthen immunity, amarogentin anti-inflammatory, glycyrrhizic acid can be antiviral with liver protection, the total phenol of rhizoma zingiberis Platelet cyclooxygenase generation can be suppressed, suppress thrombokinase generation, platelet aggregation, liquiritin is promoting blood circulation and removing blood stasis, improves Blood vessel microcirculation, Chinese angelica volatile oil can raise uterus NO levels, so as to there is preferable effect to primary dysmenorrhea.The present invention exists Removed crudely and store essence under the guidance that Chinese herb decoction is treated, simplify composition of prescription.Shown according to pharmacological screening result, Chinese medicine composition is lived Promoting blood circulation, menstruction regulating and pain relieving effect are strong, and dosage is less, and adverse reaction is lower.
Beneficial effects of the present invention are:
(1)The present invention is screened in early stage to treating dysmenorrhoea prescription at all times, under the guidance of traditional Chinese medical theory, diagnosis and treatment based on an overall analysis of the illness and the patient's condition, With reference to the pathogenesis and disease symptom of dysmenorrhoea, with it is promoting blood circulation and removing blood stasis be treatment according to the screening for carrying out drug ratio, remove crudely and store essence, Flavour of a drug are simplified, it is determined that total with motherwort total alkaloid, safflower total flavone, ligustrazine, forulic acid, amarogentin, glycyrrhizic acid, rhizoma zingiberis Phenol and liquiritin and Chinese angelica volatile oil are combined, and optimize the weight proportion of extract, test result indicate that, the present invention is provided Chinese medicine composition there is good promoting blood circulation, menstruction regulating and pain relieving effect, flavour of a drug to simplify after ensure good effects while, face Bed dosage is less.
(2)The Chinese medicine composition preparation method that the present invention is provided, effectively prevent during Traditional Chinese medicine decocting due to acid Alkali composition forms compound causes active component, active ingredient precipitation loss, realizes that Chinese medicine is provided while curative effect of medication is ensured Source rationally utilizes.
Specific embodiment
Xinshenghua side's active component, active ingredient are bought by market used by following embodiment.
Embodiment 1:The preparation of Chinese medicine composition
Take motherwort total alkaloid 300g, safflower total flavone 150g, ligustrazine 60g, forulic acid 150g, amarogentin 60g, Radix Glycyrrhizae Sour 30g, rhizoma zingiberis total phenol 150g, liquiritin 30g, the mL of Chinese angelica volatile oil 35.Take Chinese angelica volatile oil and use beta-cyclodextrin inclusion compound, weight Amount compares 1:10, beta-schardinger dextrin is dissolved in purified water, the Chinese angelica volatile oil solution dissolved with ethanol is slowly added to, using high speed point Device inclusion is dissipated, inclusion solution collects ultrafiltrate using the Ultra filtration membrane of 10 000 Da molecular cut offs, and ultrafiltrate uses 100 The NF membrane concentration of Da molecular cut offs, concentrate is spray-dried to process to obtain Ligustilide spray powder;Motherwort total alkaloid, The total phenol of safflower total flavone, ligustrazine, forulic acid, amarogentin, glycyrrhizic acid, rhizoma zingiberis and liquiritin are ground into fine powder and Ligustilide Spray powder is mixed, and adds 800g brown sugar to be well mixed, and is added water and is made softwood, crosses the granulation of 20 mesh sieves, is dried, and is made particle, is packed, Obtain final product granule.
Embodiment 2:The preparation of Chinese medicine composition
Take motherwort total alkaloid 200g, safflower total flavone 100g, ligustrazine 50g, forulic acid 100g, amarogentin 50g, Radix Glycyrrhizae Sour 10g, rhizoma zingiberis total phenol 100g, liquiritin 10g, the mL of Chinese angelica volatile oil 10.Take Chinese angelica volatile oil and use beta-cyclodextrin inclusion compound, weight Amount compares 1:5, beta-schardinger dextrin is dissolved in purified water, the Chinese angelica volatile oil solution dissolved with ethanol is slowly added to, using high speed point Device inclusion is dissipated, inclusion solution collects ultrafiltrate using the Ultra filtration membrane of 20000 Da molecular cut offs, and ultrafiltrate uses 300 The NF membrane concentration of Da molecular cut offs, concentrate is spray-dried to process to obtain Ligustilide spray powder;Motherwort total alkaloid, The total phenol of safflower total flavone, ligustrazine, forulic acid, amarogentin, glycyrrhizic acid, rhizoma zingiberis and liquiritin are ground into fine powder and Ligustilide Spray powder is mixed, and adds medical starch 1000g to be well mixed, and is added water and is made softwood, crosses the granulation of 20 mesh sieves, is dried, and is made particle Load capsule, every 0.3g.
Embodiment 3:The preparation of Chinese medicine composition
Take motherwort total alkaloid 400g, safflower total flavone 200g, ligustrazine 100g, forulic acid 200g, amarogentin 100g is sweet Oxalic acid 50g, rhizoma zingiberis total phenol 200g, liquiritin 50g, the mL of Chinese angelica volatile oil 50.Take Chinese angelica volatile oil and use beta-cyclodextrin inclusion compound, Weight compares 1:20, beta-schardinger dextrin is dissolved in purified water, the Chinese angelica volatile oil solution dissolved with ethanol is slowly added to, using at a high speed Disperser is included, and inclusion solution collects ultrafiltrate using the Ultra filtration membrane of 10000 Da molecular cut offs, and ultrafiltrate is used The NF membrane concentration of 100 Da molecular cut offs, concentrate is spray-dried to process to obtain Ligustilide spray powder;Motherwort total is given birth to The total phenol of alkaloids, safflower total flavone, ligustrazine, forulic acid, amarogentin, glycyrrhizic acid, rhizoma zingiberis and liquiritin are ground into fine powder and ligusticumic This lactone spray powder is mixed, and adds sucrose 600g, is well mixed, 2000 mL water dissolves, 0.22 μm of filtering with microporous membrane, bag Dress, obtains final product syrup.
Embodiment 4
After method according to embodiment 1 mixes each raw material, conventionally, water decoction, tablet, suppository, injection are made Or microcapsules.
Embodiment 5:The influence shunk to the mouse isolated uterine caused by oxytocin
Experimental technique:Take unpregnancy female mice, 18~22g of body weight;Intraperitoneal injection oestradiol benzoate for three days on end before experiment 1mg·kg-1·d-1, to synchronize uterus and increase sensitiveness of the uterus to oxytocin.De- cervical vertebra is put to death when testing within 4th, Cut open the belly and take uterus, stripping is attached to connective tissue and fat in uterine wall, be placed in Locke ' s solution and clean, with fine rule point Cervix end and both sides ovary end are not tied, and bath bottom is fixed in one end, and the other end is connected on tonotransducer.It is placed in In 20ml Locke ' s liquid thermostatic baths, temperature is (37 ± 0.1) DEG C, continues oxygen supply, pH 7.3, by adjusting nut plus 1g Load (10mN), balances 40min, treats uterine contractile stabilization, after spontaneous rhythm recovers, proceeds by experiment.
Pre-recorded 5-10min normal contractions curve, after oxytocin injection 10 μ L, final concentration of 5 μ L/L is added, acts on Chinese medicine composition is added after 15min(Embodiment 1, embodiment 2 and embodiment 3 are obtained), Siwu Tang be test medicine, it is each tested The initial concentration that medicine is added is 1g test medicines/mL, the final concentration of 10mg test medicines/mL of test medicine in bath, Observation medicine causes the inhibitory action that hysterotrismus is shunk to oxytocin.
After sample stabilization, record normal activity curve is used as control.By in each test medicine addition nutrient canal, question response reaches To after peak value, rinsed 3-5 times with fresh nutrient solution, it is reusable after stabilization.
The average Muscle tensility in uterus after preceding and administration is administered using T methods of inspection statistics, calculates and suppresses uterotonic hundred Divide rate (IR%).:Parameter × 100, specific experiment result such as table 1 before IR (%)=(parameter after parameter-administration before administration)/administration It is shown.
The influence (n=10) that each medicine of table 1 shrinks to the mouse isolated uterine caused by oxytocin
The influence result that the mouse isolated uterine caused by oxytocin shrinks is shown by each medicine of table 1, the Chinese medicine that the present invention is provided Composition have than Siwu Tang have preferably suppress uterotonic effect, therefore, experimental result further demonstrates that the present invention The Chinese medicine composition of offer, by after rational proportion, playing good synergistic function, clinically strong drug action, consumption it is few, peace Entirely, it is easy to take.
Embodiment 6:On the experimental study of the external thrombin time of blood plasma of rabbit (TT) influence
Experimental technique:NZw is taken, male, after fasting 8h, is anaesthetized with yellow Jackets by 6, and arteria carotis takes blood, uses (blood is 9 with anti-coagulants volume ratio to 3.8% sodium citrate:1) anti-freezing is collected in plastic centrifuge tube, with 3000rmin-1Centrifugation 10min, draws upper solution, is prepared into test plasma, using distilled water as blank, 10 is added in each road of test cup μ L Chinese medicine compositions (embodiment 1, embodiment 2 and embodiment 3 are obtained), Siwu Tang, then respectively plus test plasma 50 μ L, 37 DEG C After pre-temperature 3min, 0.1molL is added-1The 15UmL of pH 7.4Tris-HCl buffer solutions dilution-1The μ L of thrombin solution 50. With the external clotting time of LG-PABER-I type platelet aggregation each medicine groups of clotting factor analysis-e/or determining, and with [(administration group Clotting time-control group clotting time)/control group the clotting time] × 100% cruor time extending the rate for calculating each medicine group. Specific experiment result is as shown in table 2.
Influence of each medicine of table 2 to the external thrombin time of blood plasma of rabbit
Note:* compare with blank control group, *P< 0.05, * *P< 0.01
By table 2 test result indicate that, compared with Siwu Tang, the present invention provide Chinese traditional medicine composition being capable of more significantly extension rabbit External thrombin time of blood plasma, with statistical significance, illustrates by after scientific matching, playing a part of Synergistic, anti-freezing Blood effect enhancing, the Chinese medicine composition composition that the present invention is provided more is simplified, and dosage is less, and multi-flavor medicine can be avoided to bring not Good reaction.

Claims (6)

1. a kind of Xinshenghua side's active component, active ingredient composition, it is characterised in that by the raw material system of following weight It is standby to form:
Motherwort total alkaloid 20-40 parts, safflower total flavone 10-20 parts, ligustrazine 5-10 parts, forulic acid 10-20 parts, semen armeniacae amarae Glycosides 5-10 parts, glycyrrhizic acid 1-5 parts, Chinese angelica volatile oil 1-5 parts, total phenol 10-20 parts, liquiritin 1-5 parts of rhizoma zingiberis.
2. a kind of Xinshenghua side's active component according to claim 1, active ingredient composition, it is characterised in that:It is described Parts by weight of raw materials proportioning is motherwort total alkaloid 25-35 parts, safflower total flavone 12-18 parts, ligustrazine 6-8 parts, forulic acid 12- 18 parts, amarogentin 6-8 parts, glycyrrhizic acid 2-4 parts, Chinese angelica volatile oil 2-4 parts, total phenol 12-18 parts, liquiritin 2-4 parts of rhizoma zingiberis.
3. a kind of Xinshenghua side's active component, the method for active ingredient composition described in claim 1 are prepared, it is characterised in that Comprise the following steps:Weight described in claim 1 or 2:
Step one, uses beta-cyclodextrin inclusion compound, beta-schardinger dextrin to be dissolved in purified water Chinese angelica volatile oil, and addition ethanol dissolves Chinese angelica volatile oil solution, included using high speed disperser, inclusion solution is super using the Da molecular cut offs of 5000-30 000 Filter membrane is separated, and collects ultrafiltrate, and ultrafiltrate is concentrated using the NF membrane of 100-800 Da molecular cut offs, and concentrate is dry through spraying It is dry to process to obtain Ligustilide spray powder;
Step 2, by motherwort total alkaloid, safflower total flavone, ligustrazine, forulic acid, amarogentin, glycyrrhizic acid, the total phenol of rhizoma zingiberis Fine powder is ground into liquiritin, after being mixed with Ligustilide spray powder, and pharmaceutically acceptable carrier is prepared into clinically institute Receptible formulation.
4. a kind of Xinshenghua side's active component according to claim 3, the preparation method of active ingredient composition, its feature It is:The weight ratio of Chinese angelica volatile oil and beta-schardinger dextrin is 1 in the step 2:5-20.
5. a kind of Xinshenghua side's active component according to claim 3, the preparation method of active ingredient composition, its feature It is:The formulation is water decoction, capsule, tablet, granule, syrup, suppository, injection or encapsulated form.
6. water decoction, the capsule being made of a kind of Xinshenghua side's active component described in claim 1, active ingredient composition Agent, tablet, granule, syrup, suppository, injection or microcapsules.
CN201710128514.9A 2017-03-06 2017-03-06 A kind of Xinshenghua side's active component, active ingredient composition and preparation method thereof Pending CN106822843A (en)

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Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105362975A (en) * 2014-08-29 2016-03-02 江苏仁寿药业有限公司 Traditional Chinese medicine granule for treating postpartum lochiorrhea and lesser-abdominal pain and preparation method thereof

Patent Citations (1)

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Publication number Priority date Publication date Assignee Title
CN105362975A (en) * 2014-08-29 2016-03-02 江苏仁寿药业有限公司 Traditional Chinese medicine granule for treating postpartum lochiorrhea and lesser-abdominal pain and preparation method thereof

Non-Patent Citations (1)

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HANQING PANG ET AL: "Comparative analysis of the main bioactive components of Xin-Sheng-Hua granule and its single herbs by ultrahigh performance liquid chromatography with tandem mass spectrometry", 《JOURNAL OF SEPARATION SCIENCE》 *

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Application publication date: 20170613