CN1714796A - Medicine for treating cardiocerebral vascular diseases - Google Patents
Medicine for treating cardiocerebral vascular diseases Download PDFInfo
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- CN1714796A CN1714796A CN 200410019851 CN200410019851A CN1714796A CN 1714796 A CN1714796 A CN 1714796A CN 200410019851 CN200410019851 CN 200410019851 CN 200410019851 A CN200410019851 A CN 200410019851A CN 1714796 A CN1714796 A CN 1714796A
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- adjuvant
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Abstract
The present invention provides a kind of medicine prepared with breviscapine and proper amount of supplementary material for treating cardiac and cerebral vascular diseases. Compared with available similar medicines, the medicine of the present invention has high safety, lower toxic side effect and good taste.
Description
Technical field
The present invention relates to field of medicaments, particularly, relating to Chinese medicine is the pharmaceutical preparation of the treatment cardiovascular and cerebrovascular disease made of raw material.
Background technology
Cardiovascular and cerebrovascular disease is listed as first of each big disease, serious harm human body health, and the sequela that is caused is also brought very big misery to patient and family members, becomes the social problem of a worth extensive concern.Countries in the world medicine worker constantly studies, develops the prevention and the rehabilitation medicine of medicine, the especially cardiovascular and cerebrovascular disease of cardiovascular and cerebrovascular disease, and the cardiovascular and cerebrovascular disease patient can effectively be treated.Therefore, the development of cardiovascular and cerebrovascular diseases medicine is not only being healed the wounded and rescue the dying, is being had extremely important social meaning aspect the rehabilitation, but also has remarkable economic efficiency.
Breviscapine (Brceviscapini), be yellow powder, dissolve in aqueous alkali, be slightly soluble in methanol, water insoluble, chloroform etc., have and more obviously improve the brain blood circulation, increase cerebrovascular flow, reduce the effect of vascular resistance and anti-platelet aggregation, evidence: better to paralysis and the paralysis of the sequela due to cerebral hemorrhage curative effect due to the obliterated cerebral vascular disease, make the breviscapine dispersible tablet with breviscapine at present, erigeron breviscapus powder injection, erigeron breviscapus slow release capsule, Erigreron breviscapus extract controlled releasing tablet, erigeron breviscopus element soft capsule, dosage form such as breviscapine infusion preparation and breviscapine drop pills.
The synthetic chemical substance commonly used as modern medicine spreaded all over each corner of human lives, chemical synthetic drug becomes the main flow of medicine, yet, appearance along with multiple difficult serious symptom miscellaneous diseases, western medical treatment presents imperfect, the human lives and the healthy reality and the up-to-date successes achieved in research have all proposed query to this situation, particularly along with the continuous appearance of chemical drugs toxic and side effects, the change of spectrum of disease and conversion of medical, make modern medicine be subjected to unprecedented challenge, and people also place hope in the application and development of traditional medicine on gradually.Advocate back to nature, pay attention to plant amedica use, hanker after traditional remedies, the trend of advocating natural drug forms, making full use of natural materials is human best selections.
At present, in the world, natural drug all has certain market, along with people increasing and the aging of population to the health requirements level of understanding, sub-health stateization, people thirst for back to nature more, the problem of utilize the high Drug therapy of pure natural degree, preventing some chemical synthetic drugs cann't be solved, so the background that exceeds its original traditional national culture has been expanded in the application of natural plant.From natural drug, seek the little and inexpensive medicine of side effect and become the target that countries in the world pharmaceutical manufacturer is chased.The European Community has carried out unified legislation to medical herbs, state medical herbs status such as Canada and Australia have legalized, U.S. government has also drafted the plant amedica management method, the compound recipe mix preparation that begins to accept natural drug is as curative, and these provide good international environment for Chinese medicine enters international medical market as curative.On the other hand, along with the quickening of global economic integration progress, particularly China becomes a full member of WTO, and Chinese Medicine market incorporates the breadth and depth of international medical big market and will further aggravate.Face the enormous impact of Asian countries's traditional medicine product such as the keen competition of powerful transnational medical group and Japan, Korea S, India, Thailand and European countries' plant amedica such as Germany, France, numerous products that China's Chinese medicine produces are owing to still can not meet the standard of international medical market and requirement and being kept outside of the door.
Expansion and human back to nature requirement along with the market global range, use the low medicine of toxic and side effects, especially pure natural medical more and more becomes people's first-selection, dropping pill formulation be a kind of have efficient, quick-acting new medicine preparations, it has overcome the shortcoming and deficiency of Chinese medicine preparation in the past, but present dropping pill formulation generally faces following problem: 1, drop pill adjuvant pure natural degree is not high: at present, drop pill substrate adjuvant mostly is synthetic, natural degree is lower, the searching of new alternative substrate adjuvant, the searching of the alternative substrate adjuvant that particularly natural degree is high and preparation technology thereof determine, it is again very difficult thing, because the required preparation condition of at present common possible natural substrates adjuvant succedaneum is very harsh, it all is to influence the key that drop pill prepares molding that adjuvant temperature and drop pill thereof drip the system condition.The too high then viscosity of adjuvant melt temperature is low, and poor plasticity is though the adjuvant melt temperature is crossed lowplastcity by force, but drop pill has shortcomings such as easily sticking ball, distortion, therefore, seek pure natural degree height, and the adjuvant that is suitable for substituting existing drop pill substrate is a very job of hardships.2, the drop pill outlet encounters problems: along with expanding economy, more and more internationalize in market, China is also just making great efforts to adapt to this trend, present Chinese medicine dripping pills preparation as health food, successful export to many countries, but also face many problems at present, because different countries is different to the approval of the selected adjuvant of Chinese medicine dropping pill formulation, especially industrial flourishing Europe, more strict to food adjuvant and medical auxiliary materials, and as the selected chemosynthesis adjuvant (as Polyethylene Glycol) of the dropping pill formulation of health food outlet not in the catalogue of some national food additive, it is very unfavorable that this moves towards the international market to the Chinese medicine dropping pill formulation, becomes the stumbling-block that Chinese medicine enters the international market, therefore, seek the new of one or more, can be particularly important, also very urgent for the substrate adjuvant that the international market is accepted.3, the shortcoming of mouthfeel and onset speed: the mouthfeel of Chinese medicine and preparation thereof is relatively poor to be the big characteristics of one, people when taking some drugs to the frightened of disagreeable taste that medicine had even be better than fear far away to disease, What is more, some patients are because can not overcome the poor taste of Chinese medicine or its preparation or abnormal smells from the patient and abandon the treatment of Chinese medicine, though can improve mouthfeel as medicine being made capsule or sugar coated tablet, reducing stimulates, but disintegration rate prolongs, be unfavorable for the rapid onset of medicine, to some disease, particularly need the disease of the rapid onset of medicine inapplicable.4, the preparation process difficulty of drop pill suitability for industrialized production: in the replacement process of dropping pill formulation adjuvant, determining of the preparation process of its suitability for industrialized production is very difficult something, as the ratio of the melt temperature of substrate adjuvant, the proportioning of dripping system temperature, adjuvant and medicine, dropper bore, condensing agent etc. all are the factors that influence drop pill, therefore, the replacement of substrate and to be suitable for suitability for industrialized production be a job consuming time, as to expend substantial contribution.
In order to change drop pill substrate adjuvant for a long time based on the situation of chemosynthesis adjuvant, it is low to solve the pure natural degree that present drop pill substrate faced, and can not satisfy more and more that people require back to nature, take low toxicity, the problem of the pure natural medical that has no side effect; Also can solve some problems that Chinese medicine preparation, particularly dropping pill formulation are run in exit procedure, strengthen the competitiveness of international market; The present invention has invented the pure Chinese medicine dripping pills preparation that a kind of toxic and side effects is low, evident in efficacy, moderate, adapt to industrialized great production by a large amount of tests and the research of preparation process.
Summary of the invention
The medicine that the purpose of this invention is to provide a kind of treatment cardiovascular and cerebrovascular disease with new type natural substrate adjuvant preparation.
Another object of the present invention provides a kind of preparation method for the treatment of the cardiovascular and cerebrovascular diseases medicament preparation.
The present invention is the new pharmacological action that the qi-blood relationship theory learned according to Chinese traditional medicine and modern medicine are found various institutes of Chinese materia medica, according to the principle of " symptomatic treatment in acute condition, radical treatment in chronic case ", set upright based on reinforcing, " lead to " and just must not hinder, " benefit " must not be detained, treating both the principal and secondary aspects of a disease.The medicine of producing according to this method has late result again, and finally reaches the healing purpose the existing short term effect of the treatment of coronary heart disease, and generation without any side effects.The selected substrate adjuvant of the present invention is resulting by a large amount of tests, it is little to have molecular weight, soluble in water, and molten diffusing speed is faster, pure natural degree height, toxic and side effects is lower, and can reduce the medicine irritation abnormal smells from the patient, has the oral cavity of improvement acid-base value during the buccal of oral cavity, improve the characteristics of oral cavity smell, the used substrate adjuvant of the present invention is the agent of food sedan-chair flavor, takes that mouthfeel is good, the acceptant characteristics of patient, is the direction of following substrate adjuvant development.
The consumption of drug component of the present invention and the selection of adjuvant thereof also grope to sum up to draw through the inventor in a large number, each amounts of components all has curative effect preferably in following ranges: breviscapine, appropriate amount of auxiliary materials is made, wherein adjuvant comprises filler and plasticity substrate, said filler is selected from the natural adjuvant of following one or more plant origins: erythritol, sorbitol, fructose, D-ribonic acid-gamma lactone, arabitol, trehalose, D-ribose, low melting-point agarose, Lac, xylitol, Raffinose, glucose, malic acid, citric acid, isomalt, lactose, maltose etc., and they contain the water of crystallization chemical compound; Said plasticity substrate is selected from the natural adjuvant of following one or more plant origins: starch and derivant thereof, cellulose and derivant thereof, arabic gum, dextran, chitin, sesbania gum, carrageenan, Ficus elastica, Furcellaran, tragakanta, carrageenin, tamarind gum, pectin, xanthan gum, alginic acid and salt thereof, dextrin, cyclodextrin, agar, lactose; Described starch and derivant thereof such as pregelatinized Starch, modified starch, hydroxypropyl starch, carboxymethyl starch, described cellulose and derivant thereof such as methylcellulose, microcrystalline Cellulose, sodium carboxymethyl cellulose, hydroxypropyl emthylcellulose, cross-linking sodium carboxymethyl cellulose, hydroxyethylmethyl-cellulose, hydroxyethyl-cellulose, hydroxypropyl cellulose;
Preferred drug component consumption of the present invention and adjuvant thereof be chosen as 0.2～48 part of breviscapine, 4.8～60 parts of adjuvants are made, wherein adjuvant comprises filler and plasticity substrate, said filler is selected from natural adjuvant erythritol, sorbitol, fructose, D-ribonic acid-gamma lactone, arabitol, trehalose, D-ribose, low melting-point agarose, Lac, xylitol, Raffinose, glucose, malic acid, citric acid, isomalt, lactose, maltose of following one or more plant origins etc., and they contain the water of crystallization chemical compound; Said plasticity substrate is selected from the natural supplementary product starch of following one or more plant origins and derivant, cellulose and derivant thereof, arabic gum, dextran, chitin, sesbania gum, carrageenan, Ficus elastica, Furcellaran, tragakanta, carrageenin, tamarind gum, pectin, xanthan gum, alginic acid and salt thereof, dextrin, cyclodextrin, agar, lactose; Described starch and derivant thereof such as pregelatinized Starch, modified starch, hydroxypropyl starch, carboxymethyl starch, described cellulose and derivant thereof such as methylcellulose, microcrystalline Cellulose, sodium carboxymethyl cellulose, hydroxypropyl emthylcellulose, cross-linking sodium carboxymethyl cellulose, hydroxyethylmethyl-cellulose, hydroxyethyl-cellulose, hydroxypropyl cellulose;
Further preferred drug component consumption of the present invention and adjuvant thereof be chosen as 0.6～1.5 part of breviscapine, 2.0～20 parts of adjuvants are made, filler adjuvant wherein is selected from following one or more the natural adjuvant sorbitol of plant origin, xylitol, lactose, maltose, and they contain the water of crystallization chemical compound; Plasticity substrate wherein is selected from following one or more the natural adjuvant pregelatinized Starch of plant origin, carboxymethyl starch, methylcellulose, sodium carboxymethyl cellulose, hydroxypropyl emthylcellulose, arabic gum, alginic acid, dextrin, cyclodextrin, agar, lactose;
Further preferred drug component consumption of the present invention and adjuvant thereof be chosen as 0.8～1.2 part of breviscapine, 2.3～15 parts of adjuvants are made, filler adjuvant wherein is selected from following one or more the natural adjuvant sorbitol of plant origin, xylitol, lactose, maltose, and they contain the water of crystallization chemical compound; Plasticity substrate wherein is selected from following one or more the natural adjuvant pregelatinized Starch of plant origin, carboxymethyl starch, methylcellulose, sodium carboxymethyl cellulose, hydroxypropyl emthylcellulose, arabic gum, alginic acid, dextrin, cyclodextrin, agar, lactose;
Further preferred drug component consumption of the present invention and adjuvant thereof be chosen as 1 part of breviscapine, 3～10 parts of adjuvants are made, filler adjuvant wherein is selected from following one or more the natural adjuvant sorbitol of plant origin, xylitol, lactose, maltose, and they contain the water of crystallization chemical compound; Plasticity substrate wherein is selected from following one or more the natural adjuvant pregelatinized Starch of plant origin, carboxymethyl starch, methylcellulose, sodium carboxymethyl cellulose, hydroxypropyl emthylcellulose, arabic gum, alginic acid, dextrin, cyclodextrin, agar, lactose;
Best drug component consumption of the present invention and adjuvant thereof be chosen as 1 part of breviscapine, 3～10 parts of adjuvants are made, filler adjuvant wherein is selected from following one or more the natural adjuvant xylitol of plant origin, lactose; Plasticity substrate wherein is selected from following one or more the natural supplementary product starch of plant origin, arabic gum.
Can also contain chemosynthesis adjuvant and animal origin adjuvant in the above-mentioned adjuvant, wherein filler comprises phenylglycol, hexadecanol, octadecanol, sodium stearate, tristerin, tripalmitin, carbamide, polyoxyethylene monostearate, polyoxyethylene alkyl ether; Wherein plasticity substrate comprises polyvinylpyrrolidone, crospolyvinylpyrrolidone, carbomer, polyvinyl alcohol, acrylic resin, poloxamer, gelatin.
At ratio of adjuvant molding is found in the sex research, in the combination of xylitol and starch, lactose and starch, xylitol and arabic gum, low melting point substrate adjuvant is 1: 0～1: 1.5 with the ratio of the weight of plasticity substrate adjuvant, be preferably 1: 0.1～1: 0.9, the best is 1: 0.1～1: 0.5.Low melting point substrate adjuvant of being formed within this scope and plasticity substrate adjuvant, the drug matrices fused solution all can ooze, and can condensation.Specific to each combination, xylitol is preferably 1: 0.2 with the ratio of the weight of starch～1: 0.3, and lactose is preferably 1: 0.2 with the ratio of the weight of starch～1: 0.3, and the ratio of the weight of xylitol and arabic gum is preferably 1: 0.2～and 1: 0.4.Find that in the research of temperature temperature is big especially to the influence of drop pill mouldability to the influence of drop pill mouldability, when temperature is too low, owing to the too big effect that oozes that influences drop pill of viscosity of substrate, when temperature is too high, not condensation of drop pill.Find that mixing time can have influence on the mouldability of drop pill in mixing time in to the sex research of drop pill molding, mixing time is too short, and mobile poor, influence oozes, and mixing time is oversize, influences the condensation of drop pill.Dripping under the system temperature, mixing time in 1～120 minute all can, suitable mixing time was at 10～30 minutes.Consider that mixing time can not be too short in the suitability for industrialized production, adopt the method that low temperature stirs for a long time, high temperature drips system.Find that in the research of dropper bore to the influence of drop pill particle diameter the dropper bore influences the size of drop pill and the flowability of fusion substrate, the system effect is dripped in influence.Drop pill diminishes and diminishes along with bore, but after 1.4 millimeters, along with the bore change of size that diminishes is not obvious, but the matrix flow reduction, system is dripped in influence.
So in the preparation method of preparation, medicine mixes mixing time with the substrate adjuvant be 10～30 minutes; The mixed heating and melting temperature of medicine and substrate adjuvant is 45～115 ℃, dripping the system temperature is 45～95 ℃, and liquid coolant is liquid paraffin, methyl-silicone oil or vegetable oil (Oleum Glycines, Semen Ricini wet goods), and the temperature of liquid coolant is-20～25 ℃, dropper mouth internal diameter is 1.0～4.0 millimeters; Preferred heating and melting temperature is 60～85 ℃, and dripping a system temperature is 60～85 ℃, and condensing agent is liquid paraffin, methyl-silicone oil, and the condensing agent temperature is 0～18 ℃, and the dropper bore is 1.1～3.5 millimeters, and the difference of dropper mouth external diameter and internal diameter is less for well; Best heating and melting temperature is that to make temperature be that 64 ℃, dropper bore are that 1.2～2.5 millimeters, condensing agent are 0 ℃ methyl-silicone oil to 64 ℃, droplet.
The substrate adjuvant of the best of the present invention is xylitol and starch, and xylitol is 1: 0.2～1: 0.3 with the ratio of the weight of starch; Or be lactose and starch, lactose is 1: 0.2～1: 0.3 with the ratio of the weight of starch; Or be xylitol and arabic gum, the ratio of the weight of xylitol and arabic gum is 1: 0.2～1: 0.4.
Xylitol is a kind of natural plant sweetening agent, approve through World Health Organization (WHO), xylitol is a kind of safest sweeting agent, countries in the world are extensive use of in fields such as food and oral-cavity articles, xylitol enters the help that need not insulin in the cell, when sugar utilizes obstacle, can not cause blood sugar increasing yet, can improve diabetics symptom, have the ketoplastic effect of powerful inhibition, can promote the generation of liver glycogen, directly infiltrate the Developmental and Metabolic Disorder that tissue is participated in metabolism, can be corrected protein, fat and steroid; Xylose is the internal metabolism intermediate product, and body has higher toleration to it.Clinical practice proves: the highest oral dosis tolerata can reach 220g every day, and intravenous drip every day can reach 100g.The oral 25700mg/Kg of median lethal dose(LD 50) (LD50) mice, quiet notes 6400mg/Kg, the quiet notes of rat 6200mg/Kg.
Medicine mesostroma adjuvant of the present invention and amount of drug are than can being the scope that allows on the galenic pharmacy, medicine described here can be that crude drug also can be the effective ingredient extract, in order to adapt to industrialized great production, used medicine material is a breviscapine among the present invention.
Medicine of the present invention can adopt the preparation of Chinese medicine preparation conventional method, but in order to make each crude drug of this medicine better bring into play drug effect, the present invention adopts preparation method as follows, but this can not limit protection scope of the present invention.
The preparation method of medicine of the present invention is as follows:
(a) by proportioning take by weighing each crude drug breviscapine, appropriate amount of auxiliary materials is standby;
(b) in appropriate amount of auxiliary materials, add breviscapine, fully mix, be prepared into the oral formulations that allows on the pharmaceutics according to the pharmaceutics preparation method, promptly.
Preferred manufacturing procedure comprises the following steps:
(a) by proportioning take by weighing 0.2～48 part of breviscapine of each crude drug, 4.8～60 parts of adjuvants are standby;
(b) in appropriate amount of auxiliary materials, add breviscapine, fully mix, mixture is at 45～115 ℃ of heating and meltings, stir, mixing time is 1～120 minute, insulation, at 45～95 ℃ of temperature following system, dropper bore is 1.0～4.0 millimeters, splash in-20～25 ℃ liquid paraffin, methyl-silicone oil or the vegetable oil, drip and make ball, promptly.
Further preferred manufacturing procedure comprises the following steps:
(a) by proportioning take by weighing 0.6～1.5 part of breviscapine of each crude drug, 2.0～20 parts of adjuvants are standby;
(b) in adjuvant, add the said extracted thing, fully mix, mixture stirs at 60～85 ℃ of heating and meltings, mixing time is 10～30 minutes, insulation is 1.1～3.5 millimeters at 60～85 ℃ of temperature following system, dropper bore, splashes in 0～18 ℃ the liquid paraffin, methyl-silicone oil, drip and make ball, liquid coolant is use up and wiped to the drop pill drop that forms, back packing to be dried, promptly.
Further preferred manufacturing procedure comprises the following steps:
(a) by proportioning take by weighing 0.8～1.2 part of breviscapine of each crude drug, 2.3～15 parts of adjuvants are standby;
(b) in adjuvant, add the said extracted thing, fully mix, mixture stirs at 60～85 ℃ of heating and meltings, mixing time is 10～30 minutes, insulation is 1.1～3.5 millimeters at 60～85 ℃ of temperature following system, dropper bore, splashes in 0～18 ℃ the liquid paraffin, methyl-silicone oil, drip and make ball, liquid coolant is use up and wiped to the drop pill drop that forms, back packing to be dried, promptly.
Best preparation method comprises the following steps:
(a) by proportioning take by weighing 1 part of breviscapine of each crude drug, 3～10 parts of adjuvants are standby;
(b) get appropriate amount of auxiliary materials, add the active component of method for preparing, fully mix, mixture is at 64 ℃ of heating and meltings, stir, mixing time is 10～30 minutes, insulation, at 64 ℃ of temperature following system, dropper bore is 1.2～2.5 millimeters, splash in 0 ℃ the methyl-silicone oil, drip and make ball, to the greatest extent and wipe liquid coolant the drop pill drop that forms, back packing to be dried, promptly.
The best preparation method of medicine of the present invention is:
(a) by proportioning take by weighing 1 part of breviscapine of each crude drug, 3～10 parts of adjuvants are standby;
(b) get 3～10 parts of xylitol and starch, xylitol is 1: 0.2～1: 0.3 with the ratio of the weight of starch; Or 3～10 parts of lactose and starch, lactose is 1: 0.2～1: 0.3 with the ratio of the weight of starch; Or 3～10 parts of xylitol and arabic gum, the ratio of the weight of xylitol and arabic gum is 1: 0.2～1: 0.4 a adjuvant, adds the active component of method for preparing, fully mix, mixture stirs at 64 ℃ of heating and meltings, mixing time is 10～30 minutes, insulation is 1.2～2.5 millimeters at 64 ℃ of temperature following system, dropper bore, splashes in 0 ℃ the methyl-silicone oil, drip and make ball, liquid coolant is use up and wiped to the drop pill drop that forms, back packing to be dried, promptly.
More than form when producing and to increase or to reduce according to corresponding ratio, as large-scale production can be unit with kilogram or with the ton, small-scale production can be unit with the gram also, and weight can increase or reduce, but the crude drug material weight proportion constant rate between each composition.
Medicine of the present invention can be determined usage and dosage according to patient's situation in use, but every day 1-3 time, and every day, each crude drug consumption was as the criterion with the state-promulgated pharmacopoeia dosage, was no more than the pharmacopeia ormal weight.
The drop pill that the present invention is prepared, conventional drop pill advantage is simple as preparing except having, steady quality, can make liquid medicine solidification, convenient drug administration, efficient, quick-acting, its biggest advantage is:
1, the selected adjuvant pure natural of the present invention degree height: the substrate adjuvant that employed substrate adjuvant derives from natural plants or originates based on natural plants among the present invention, selected substrate adjuvant is xylitol and starch or lactose and starch or xylitol and arabic gum, this substrate adjuvant has pure natural degree height, toxic and side effects is low, mouthfeel is good, dissolve scattered time limit is short, rapid-action, it is a kind of new medium adjuvant, can be used for substituting present chemosynthesis adjuvant, the drop pill made from this kind adjuvant, it is low to solve the pure natural degree that present drop pill substrate faced, and more and more can not satisfy people and require back to nature, take low toxicity, the problem of the pure natural medical that has no side effect.
2, some problems in the outlet of solution Chinese medicine: medicine of the present invention also can solve Chinese medicine preparation, some problems of in exit procedure, being run into of dropping pill formulation particularly, solve because different countries, especially the European countries of industry prosperity are to the difference identification of the selected adjuvant of Chinese medicine dropping pill formulation, overcome as the selected adjuvant Polyethylene Glycol of the dropping pill formulation of the health food outlet defective in some national food additive catalogue not, improve the Chinese medicine dripping pills preparation and move towards the international market, strengthen the competitiveness of international market.
3, solve the relatively poor problem of dropping pill formulation taste and further improve drug effect speed (dissolve scattered time limit): the medicinal dropping ball made from this kind substrate adjuvant of the present invention, can improve Chinese medicine preparation, the particularly present not good shortcoming of dropping pill formulation taste, improve mouthfeel, more easy for patients to accept, and the drop pill that adopts the selected adjuvant of medicine of the present invention to make has shorter dissolve scattered time limit, making drug effect faster, is the medicine that coronary heart disease, angina pectoris, myocardial ischemia are treated in a kind of onset faster.
4, higher safety and solve some problems in the drop pill storage process: the selected substrate of the present invention is not only additive, nutrient commonly used in the food industry, and can do medicinal, but do not see that it uses as the drug matrices adjuvant, therefore, with regard to substrate, be perfectly safe, have no side effect, a large amount of evidences, the drop pill made from this adjuvant can reduce effective ingredient separating out in storage process, the sticking ball of drop pill, easy shortcomings such as moisture absorption deliquescing, but the big production of suitability for industrialized.
The present invention is under instruction of Chinese Medicine theory, preparation technology's test that process is a large amount of and pharmacology, the resulting preparation of pharmacodynamics test.The present invention is evident in efficacy, has the effect of expelling cold and relieving exterior syndrome, expelling wind and removing dampness, activating blood circulation to dissipate blood stasis, dredge the meridian passage, anti-inflammatory analgetic.Herba Erigerontis is mainly used in the treatment of ischemic cerebrocardiac disease clinically at present, has the curative effect of highly significant for cerebral infarction especially.Reasonable recipe of the present invention, poisonous side effect of medicine is low, overcome that western medicine coronary heart disease toxic and side effects is big, expense is high, the Chinese medicine curative effect is low, flavour of a drug are many, the shortcoming of incompatibility large-scale production, is the medicine of the definite treatment coronary heart disease of a kind of economy, material benefit, curative effect.
In order to understand the present invention better, below with test explanation advantages of the present invention such as the present invention's's (following the present invention is called breviscapine drop pills) dissolve scattered time limit, weight differential, drop pill soft durometer, the sticking balls of drop pill.
Test example 1: dissolve scattered time limit, weight differential contrast experiment's example
In vitro tests
The present invention be that the breviscapine drop pills that adjuvant is made compares with the Polyethylene Glycol, by measuring dissolve scattered time limit, investigate its good releasing effect; By measuring indexs such as the ball method of double differences is different, investigate whether it ripe in preparation technology, whether be fit to suitability for industrialized production.
1. test medication: the new substrate breviscapine drop pills of the present invention (newly), Tianjin Tasly Pharmaceutical Co., Ltd provides, and is the breviscapine drop pills (old) that adjuvant is made with the Polyethylene Glycol.
2. method and result:
Dissolve scattered time limit: by " method is measured under this item of Chinese pharmacopoeia; The ball method of double differences is different: by " method is measured under this item of Chinese pharmacopoeia.Result of the test sees Table 1.
Three batches of breviscapine drop pills made from the new medium adjuvant of table 1 (newly) with Polyethylene Glycol be breviscapine drop pills (old) dissolve scattered time limit made of main adjuvant, weight differential relatively
| 0 month | January | February | March | June | December | 18 months | ||
| 1 batch | Criterion | The result | ||||||
| Weight differential (± 15%) | All in 10% | All in 10% | All in 10% | All in 10% | All in 10% | All in 10% | All in 10% | |
| Dissolve scattered time limit (newly) (30 minutes) (old) | 2′10″ 5′19″ | 2′14″ 5′17″ | 2′15″ 5′14″ | 2′14″ 5′27″ | 2′18″ 5′31″ | 2′18″ 5′30″ | 2′20″ 5′35″ | |
| 2 batches | Weight differential (± 15%) | All in 10% | All in 10% | All in 10% | All in 10% | All in 10% | All in 10% | All in 10% |
| Dissolve scattered time limit (newly) (30 minutes) (old) | 2′9″ 5′18″ | 2′15″ 5′20″ | 2′17″ 5′21″ | 2′18″ 5′23″ | 2′18″ 5′30″ | 2′19″ 5′30″ | 2′21″ 5′32″ | |
| 3 batches | Weight differential (± 15%) | All in 10% | All in 10% | All in 10% | All in 10% | All in 10% | All in 10% | All in 10% |
| Dissolve scattered time limit (newly) (30 minutes) (old) | 2′11″ 5′17″ | 2′14″ 5′16″ | 2′14″ 5′18″ | 2′15″ 5′23″ | 2′17″ 5′24″ | 2′19″ 5′30″ | 2′22″ 5′35″ |
Test data shows, the dissolve scattered time limit of new substrate breviscapine drop pills is lacking of the breviscapine drop pills made of main adjuvant with Polyethylene Glycol, and the ball method of double differences of the breviscapine drop pills that new and old substrate is made is different all to be controlled in the pharmacopeia prescribed limit.Result of the test explanation, the molten diffusing speed of the breviscapine drop pills made from novel adjuvant is faster, is more conducive to medicine and plays a role in the shortest time; The ball method of double differences is different all to be controlled in the pharmacopeia prescribed limit, difference not statistically significant, the alternative present chemosynthesis adjuvant of this natural substrates adjuvant, but suitability for industrialized production.
Test example 2: the present invention with Polyethylene Glycol be the sticking ball comparative observation of the breviscapine drop pills soft durometer made of main adjuvant adjuvant, drop pill
1. test medication: the new substrate breviscapine drop pills of the present invention (newly) is the breviscapine drop pills (old) that main adjuvant is made with Polyethylene Glycol.
2. method and result: three batches of the things of getting it filled are loaded in the porcelain vase respectively, and use the bottle stopper good seal.Putting it into the bottom has in the exsiccator of saturated Nacl (humidity 75%) solution, exsiccator is put into 40 ℃ of drying baker of constant temperature again, and timing sampling is observed situations such as drop pill soft durometer, the sticking ball of drop pill, the results are shown in Table 2.1, table 2.2.
Three batches in table 2.1 is that the breviscapine drop pills reserved sample observing that main adjuvant is made compares with Polyethylene Glycol
| 0 month | January | February | March | June | December | 18 months | ||
| 1 batch | Criterion | The result | ||||||
| Sticking ball | Not sticking | Not sticking | Not sticking | Not sticking | Not sticking | Sticking slightly | Sticking slightly | |
| Soft durometer | Firmly | Firmly | Firmly | Firmly | Firmly | Harder | Harder | |
| 2 batches | Sticking ball | Not sticking | Not sticking | Not sticking | Not sticking | Not sticking | Not sticking | Sticking slightly |
| Soft durometer | Firmly | Firmly | Firmly | Firmly | Firmly | Harder | Harder | |
| 3 batches | Sticking ball | Not sticking | Not sticking | Not sticking | Not sticking | Not sticking | Sticking slightly | Sticking slightly |
| Soft durometer | Firmly | Firmly | Firmly | Firmly | Firmly | Harder | Harder | |
Table 2.2: three batches of breviscapine drop pills made from the new medium adjuvant (newly) with Polyethylene Glycol be breviscapine drop pills (old) character observation made of main adjuvant relatively
| 0 month | January | February | March | June | December | 18 months |
| Criterion | The result | |||||||
| 1 batch | Sticking ball | Sticking (old) do not glue (newly) | Sticking (old) do not glue (newly) | Sticking (old) do not glue (newly) | Sticking (old) do not glue (newly) | Sticking (old) do not glue (newly) slightly | Sticking (old) glues (newly) slightly slightly | Sticking (old) be sticking (newly) slightly |
| Soft durometer | (old) hard (newly) firmly | (old) hard (newly) firmly | (old) hard (newly) firmly | (old) hard (newly) firmly | Hard (old) hard (newly) | Hard slightly (old) hard (newly) | Hard slightly (old) be hard (newly) slightly | |
| 2 batches | Sticking ball | Sticking (old) do not glue (newly) | Sticking (old) do not glue (newly) | Sticking (old) do not glue (newly) | Sticking (old) do not glue (newly) | Sticking (old) do not glue (newly) | Sticking (old) do not glue (newly) slightly | Sticking (old) glues (newly) slightly slightly |
| Soft durometer | (old) hard (newly) firmly | (old) hard (newly) firmly | (old) hard (newly) firmly | (old) hard (newly) firmly | Hard (old) hard (newly) | Hard slightly (old) hard (newly) | Hard slightly (old) be hard (newly) slightly | |
| 3 batches | Sticking ball | Sticking (old) do not glue (newly) | Sticking (old) do not glue (newly) | Sticking (old) do not glue (newly) | Sticking (old) do not glue (newly) | Sticking (old) do not glue (newly) slightly | Sticking (old) do not glue (newly) slightly | Sticking (old) be sticking (newly) slightly |
| Soft durometer | (old) hard (newly) firmly | (old) hard (newly) firmly | (old) hard (newly) firmly | (old) hard (newly) firmly | (old) hard (newly) firmly | Hard slightly (old) hard (newly) | Hard slightly (old) be hard (newly) slightly | |
Result of the test shows, the soft durometer of new substrate breviscapine drop pills changes and be that the breviscapine drop pills made of main adjuvant is similar, strong slightly with Polyethylene Glycol; The sticking ball variation of the drop pill of new substrate breviscapine drop pills, firmness change and be that the breviscapine drop pills made of main adjuvant is similar with Polyethylene Glycol.Presentation of results, the sticking ball of the breviscapine drop pills that new, old substrate adjuvant is made changes, firmness change is similar, and the alternative present chemosynthesis adjuvant of this natural substrates adjuvant is described, but suitability for industrialized production.
The specific embodiment
Embodiment 1
(a) get each crude drug breviscapine 0.2g, xylitol 4g, starch 0.8g is standby;
(b) in xylitol and starch mixture, add breviscapine, fully mix, mixture is at 85～115 ℃ of heating and meltings, stir, mixing time is 1～12 minute, insulation, at 45～65 ℃ of temperature following system, dropper bore is 1.40～4.0 millimeters, splash in-20～25 ℃ the methyl-silicone oil, make 1000 drop pill, promptly.
Dissolve scattered time limit sees Table 1.
Embodiment 2
(a) get each crude drug breviscapine 48g, xylitol 50g, starch 10g is standby;
(b) in xylitol and starch mixture, add breviscapine, fully mix, mixture is at 85～115 ℃ of heating and meltings, stir, mixing time is 1～12 minute, insulation, at 50～65 ℃ of temperature following system, dropper bore is 1.40～4.0 millimeters, splash in-20～25 ℃ the liquid paraffin, make 5000 drop pill, promptly.
The sticking ball comparative observation of drop pill soft durometer, drop pill sees Table 2.1, table 2.2
Embodiment 3
(a) get each crude drug breviscapine 4.8g, sorbitol 18.5g, xanthan gum 9.g is standby;
(b) in sorbitol and xanthan gum mixtures, add breviscapine, fully mix, mixture is at 65～85 ℃ of heating and meltings, stir, mixing time is 10～15 minutes, insulation, at 55～68 ℃ of temperature following system, dropper bore is 1.70～3.5 millimeters, splash in 5～15 ℃ the liquid paraffin, make 1000 drop pill, promptly.
Embodiment 4
(a) get each crude drug breviscapine 3g, xylitol 25g, methylcellulose 5g is standby;
(b) in xylitol and methylcellulose mixture, add breviscapine, fully mix, mixture is at 65～85 ℃ of heating and meltings, stir, mixing time is 10 minutes, insulation, at 45～75 ℃ of temperature following system, dropper bore is 1.30～3.0 millimeters, splash in 8～10 ℃ the vegetable oil, make 1000 drop pill, promptly.
Embodiment 5
(a) get each crude drug breviscapine 10g, lactose 17.9g, starch 7.1g is standby;
(b) in lactose and starch mixture, add breviscapine, fully mix, mixture stirs at 60～85 ℃ of heating and meltings, mixing time is 10～30 minutes, insulation is 1.1～3.5 millimeters at 60～85 ℃ of temperature following system, dropper bore, splashes in 2 ℃ the methyl-silicone oil, make 1000 drop pill, liquid coolant is use up and wiped to the drop pill drop that forms, back packing to be dried, promptly.
Embodiment 6
(a) get each crude drug breviscapine 0.6g, xylitol 26.5g, starch 3.g is standby;
(b) in xylitol and starch mixture, add breviscapine, fully mix, mixture stirs at 80～85 ℃ of heating and meltings, mixing time is 10～30 minutes, insulation is 1.21～3.5 millimeters at 60～65 ℃ of temperature following system, dropper bore, splashes in 5 ℃ the liquid paraffin, make 1000 drop pill, liquid coolant is use up and wiped to the drop pill drop that forms, back packing to be dried, promptly.
Embodiment 7
(a) get each crude drug breviscapine 1.5g, xylitol 21.5g, cyclodextrin 6.5g is standby;
(b) in xylitol and cyclodextrin mixt, add breviscapine, fully mix, mixture stirs at 60～85 ℃ of heating and meltings, mixing time is 10～30 minutes, insulation is 1.21～3.5 millimeters at 60～85 ℃ of temperature following system, dropper bore, splashes in 5～15 ℃ the methyl-silicone oil, make 1000 drop pill, liquid coolant is use up and wiped to the drop pill drop that forms, back packing to be dried, promptly.
Embodiment 8
(a) get each crude drug breviscapine 1.5g, xylitol 17g, arabic gum 3g is standby;
(b) in xylitol and arabic gum mixture, add breviscapine, fully mix, mixture stirs at 60～85 ℃ of heating and meltings, mixing time is 10～12 minutes, insulation is 1.6～3.5 millimeters at 60～65 ℃ of temperature following system, dropper bore, splashes in 0～8 ℃ the liquid paraffin, make 1000 drop pill, liquid coolant is use up and wiped to the drop pill drop that forms, back packing to be dried, promptly.
Embodiment 9
(a) get each crude drug breviscapine 0.8g, xylitol 13.3g, starch 2.7g is standby;
(b) get xylitol and starch mix homogeneously, add breviscapine, fully mix, mixture is at 64 ℃ of heating and meltings, stir, mixing time is 10～30 minutes, insulation, at 64 ℃ of temperature following system, dropper bore is 1.2～2.5 millimeters, splash in 0 ℃ the methyl-silicone oil, make 1000 drop pill, to the greatest extent and wipe liquid coolant the drop pill drop that forms, back packing to be dried, promptly.
Embodiment 10
(a) get each crude drug breviscapine 6g, lactose 12g, starch 6g is standby;
(b) get lactose and starch and mix evenly, add breviscapine, fully mix, mixture is at 64 ℃ of heating and meltings, stir, mixing time is 10～30 minutes, insulation, at 64 ℃ of temperature following system, dropper bore is 1.2～2.5 millimeters, splash in 0 ℃ the methyl-silicone oil, make 1000 drop pill, to the greatest extent and wipe liquid coolant the drop pill drop that forms, back packing to be dried, promptly.
Embodiment 11
(a) get each crude drug breviscapine 2g, xylitol 18g, arabic gum 2g is standby;
(b) get xylitol and arabic gum and mix evenly, add breviscapine, fully mix, mixture is at 64 ℃ of heating and meltings, stir, mixing time is 10～30 minutes, insulation, at 64 ℃ of temperature following system, dropper bore is 1.2～2.5 millimeters, splash in 0 ℃ the methyl-silicone oil, make 1000 drop pill, to the greatest extent and wipe liquid coolant the drop pill drop that forms, back packing to be dried, promptly.
Embodiment 12
(a) get each crude drug breviscapine 1.2g, xylitol 12.5g, starch 2.5g is standby;
(b) get above-mentioned xylitol and starch and mix, add breviscapine, fully mix, mixture is at 60～69 ℃ of heating and meltings, stir, mixing time is 10～30 minutes, insulation, at 60～69 ℃ of temperature following system, dropper bore is 1.2～2.5 millimeters, splash in 0 ℃ the methyl-silicone oil, make 1000 drop pill, to the greatest extent and wipe liquid coolant the drop pill drop that forms, back packing to be dried, promptly.
Embodiment 13
(a) get each crude drug breviscapine 12g, xylitol 13.5g, Furcellaran 5.2g is standby;
(b) get xylitol and Furcellaran and mix evenly, add breviscapine, fully mix, mixture is at 55～70 ℃ of heating and meltings, stir, mixing time is 10～30 minutes, insulation, at 58～69 ℃ of temperature following system, dropper bore is 1.21～2.5 millimeters, splash in 0 ℃ the methyl-silicone oil, make 1000 drop pill, to the greatest extent and wipe liquid coolant the drop pill drop that forms, back packing to be dried, promptly.
Embodiment 14
(a) it is standby to get each crude drug breviscapine 0.2g, D-ribonic acid-gamma lactone 5g, agar 0.7g;
(b) in D-ribonic acid-gamma lactone and agar mixture, add breviscapine, fully mix, mixture is at 85～115 ℃ of heating and meltings, stir, mixing time is 10～12 minutes, insulation, at 45～65 ℃ of temperature following system, dropper bore is 1.40～4.0 millimeters, splash in-5～5 ℃ the methyl-silicone oil, make 1000 drop pill, promptly.
Embodiment 15
(a) get each crude drug breviscapine 45g, fructose 48g, pectin 12g is standby;
(b) in fructose and pectin mixture, add breviscapine, fully mix, mixture is at 85～115 ℃ of heating and meltings, stir, mixing time is 10～12 minutes, insulation, at 50～65 ℃ of temperature following system, dropper bore is 1.40～4.0 millimeters, splash in-2～5 ℃ the liquid paraffin, make 5000 drop pill, promptly.
Embodiment 16
(a) get each crude drug breviscapine 4.8g, low melting-point agarose 18.4g, microcrystalline Cellulose 9.1g is standby;
(b) in low melting-point agarose and microcrystalline cellulose mixt, add breviscapine, fully mix, mixture is at 65～85 ℃ of heating and meltings, stir, mixing time is 10～15 minutes, insulation, at 55～68 ℃ of temperature following system, dropper bore is 1.70～3.5 millimeters, splash in 5～15 ℃ the liquid paraffin, make 1000 drop pill, promptly.
Embodiment 17
(a) get each crude drug breviscapine 3g, Raffinose 27g, cross-linking sodium carboxymethyl cellulose 4g is standby;
(b) in Raffinose and cross-linking sodium carboxymethyl cellulose mixture, add breviscapine, fully mix, mixture is at 65～85 ℃ of heating and meltings, stir, mixing time is 10 minutes, insulation, at 45～75 ℃ of temperature following system, dropper bore is 1.30～3.0 millimeters, splash in 8～10 ℃ the vegetable oil, make 1000 drop pill, promptly.
Embodiment 18
(a) get each crude drug breviscapine 9g, malic acid 17.9g, hydroxypropyl cellulose 7.8g is standby;
(b) in malic acid and hydroxypropyl cellulose mixture, add breviscapine, fully mix, mixture stirs at 60～85 ℃ of heating and meltings, mixing time is 10～30 minutes, insulation is 1.1～3.5 millimeters at 60～85 ℃ of temperature following system, dropper bore, splashes in 2 ℃ the methyl-silicone oil, make 1000 drop pill, liquid coolant is use up and wiped to the drop pill drop that forms, back packing to be dried, promptly.
Embodiment 19
(a) get each crude drug breviscapine 0.6g, isomalt 25.5g, microcrystalline Cellulose 3.4g is standby;
(b) in isomalt and microcrystalline cellulose mixt, add breviscapine, fully mix, mixture stirs at 80～85 ℃ of heating and meltings, mixing time is 10～30 minutes, insulation is 1.21～3.5 millimeters at 60～65 ℃ of temperature following system, dropper bore, splashes in 5 ℃ the liquid paraffin, make 1000 drop pill, liquid coolant is use up and wiped to the drop pill drop that forms, back packing to be dried, promptly.
Embodiment 20
(a) get each crude drug breviscapine 1.5g, glucose 21.5g, sesbania gum 6.5g is standby;
(b) in glucose and sesbania gum mixture, add breviscapine, fully mix, mixture stirs at 60～85 ℃ of heating and meltings, mixing time is 10～30 minutes, insulation is 1.21～3.5 millimeters at 60～85 ℃ of temperature following system, dropper bore, splashes in 10～15 ℃ the methyl-silicone oil, make 1000 drop pill, liquid coolant is use up and wiped to the drop pill drop that forms, back packing to be dried, promptly.
Embodiment 21
(a) get each crude drug breviscapine 1.5g, Furcellaran 20g, dextran 2g is standby;
(b) in Furcellaran and dextran mixture, add breviscapine, fully mix, mixture stirs at 60～85 ℃ of heating and meltings, mixing time is 10～12 minutes, insulation is 1.6～3.5 millimeters at 60～65 ℃ of temperature following system, dropper bore, splashes in 0～8 ℃ the liquid paraffin, make 1000 drop pill, liquid coolant is use up and wiped to the drop pill drop that forms, back packing to be dried, promptly.
Embodiment 22
(a) get each crude drug breviscapine 0.8g, maltose 13.3g, agar 2.7g is standby;
(b) get maltose and agar mix homogeneously, add breviscapine, fully mix, mixture is at 63 ℃ of heating and meltings, stir, mixing time is 10～30 minutes, insulation, at 64 ℃ of temperature following system, dropper bore is 1.2～2.5 millimeters, splash in 0 ℃ the methyl-silicone oil, make 1000 drop pill, to the greatest extent and wipe liquid coolant the drop pill drop that forms, back packing to be dried, promptly.
Embodiment 23
(a) get each crude drug breviscapine 6g, sesbania gum 12g, dextran 6g is standby;
(b) get sesbania gum and dextran and mix evenly, add breviscapine, fully mix, mixture is at 64 ℃ of heating and meltings, stir, mixing time is 10～30 minutes, insulation, at 64 ℃ of temperature following system, dropper bore is 1.2～2.5 millimeters, splash in 0 ℃ the methyl-silicone oil, make 1000 drop pill, to the greatest extent and wipe liquid coolant the drop pill drop that forms, back packing to be dried, promptly.
Embodiment 24
(a) get each crude drug breviscapine 2g, low melting-point agarose 18g, pregelatinized Starch 2g is standby;
(b) get low melting-point agarose and pregelatinized Starch and mix evenly, add breviscapine, fully mix, mixture is at 65 ℃ of heating and meltings, stir, mixing time is 10～30 minutes, insulation, at 65 ℃ of temperature following system, dropper bore is 1.2～2.5 millimeters, splash in 2 ℃ the methyl-silicone oil, make 1000 drop pill, to the greatest extent and wipe liquid coolant the drop pill drop that forms, back packing to be dried, promptly.
Claims (15)
1, a kind of medicine for the treatment of cardiovascular disease, it is characterized in that it is to be made by breviscapine, appropriate amount of auxiliary materials, wherein adjuvant comprises filler and plasticity substrate, said filler is selected from natural adjuvant erythritol, sorbitol, fructose, D-ribonic acid-gamma lactone, arabitol, trehalose, D-ribose, low melting-point agarose, Lac, xylitol, Raffinose, glucose, malic acid, citric acid, isomalt, lactose, maltose of following one or more plant origins etc., and they contain the water of crystallization chemical compound; Said plasticity substrate is selected from the natural supplementary product starch of following one or more plant origins and derivant, cellulose and derivant thereof, arabic gum, dextran, chitin, sesbania gum, carrageenan, Ficus elastica, Furcellaran, tragakanta, carrageenin, tamarind gum, pectin, xanthan gum, alginic acid and salt thereof, dextrin, cyclodextrin, agar, lactose; Described starch and derivant thereof such as pregelatinized Starch, modified starch, hydroxypropyl starch, carboxymethyl starch, described cellulose and derivant thereof such as methylcellulose, microcrystalline Cellulose, sodium carboxymethyl cellulose, hydroxypropyl emthylcellulose, cross-linking sodium carboxymethyl cellulose, hydroxyethylmethyl-cellulose, hydroxyethyl-cellulose, hydroxypropyl cellulose.
2, the medicine of treatment cardiovascular disease as claimed in claim 1, it is characterized in that it is by 0.2～48 part of breviscapine, 4.8～60 parts of adjuvants are made, wherein adjuvant comprises filler and plasticity substrate, said filler is selected from the natural adjuvant erythritol of following one or more plant origins, sorbitol, fructose, D-ribonic acid-gamma lactone, arabitol, trehalose, D-ribose, low melting-point agarose, Lac, xylitol, Raffinose, glucose, malic acid, citric acid, isomalt, lactose, maltose etc., and they contain the water of crystallization chemical compound; Said plasticity substrate is selected from the natural supplementary product starch of following one or more plant origins and derivant, cellulose and derivant thereof, arabic gum, dextran, chitin, sesbania gum, carrageenan, Ficus elastica, Furcellaran, tragakanta, carrageenin, tamarind gum, pectin, xanthan gum, alginic acid and salt thereof, dextrin, cyclodextrin, agar, lactose; Described starch and derivant thereof such as pregelatinized Starch, modified starch, hydroxypropyl starch, carboxymethyl starch, described cellulose and derivant thereof such as methylcellulose, microcrystalline Cellulose, sodium carboxymethyl cellulose, hydroxypropyl emthylcellulose, cross-linking sodium carboxymethyl cellulose, hydroxyethylmethyl-cellulose, hydroxyethyl-cellulose, hydroxypropyl cellulose.
3, the medicine of treatment cardiovascular disease as claimed in claim 2, it is characterized in that it is to be made by 0.6～1.5 part of breviscapine, 2.0～20 parts of adjuvants, filler adjuvant wherein is selected from following one or more the natural adjuvant sorbitol of plant origin, xylitol, lactose, maltose, and they contain the water of crystallization chemical compound; Plasticity substrate wherein is selected from following one or more the natural adjuvant pregelatinized Starch of plant origin, carboxymethyl starch, methylcellulose, sodium carboxymethyl cellulose, hydroxypropyl emthylcellulose, arabic gum, alginic acid, dextrin, cyclodextrin, agar, lactose.
4, the medicine of treatment cardiovascular disease as claimed in claim 3, it is characterized in that it is to be made by 0.8～1.2 part of breviscapine, 2.3～15 parts of adjuvants, filler adjuvant wherein is selected from following one or more the natural adjuvant sorbitol of plant origin, xylitol, lactose, maltose, and they contain the water of crystallization chemical compound; Plasticity substrate wherein is selected from following one or more the natural adjuvant pregelatinized Starch of plant origin, carboxymethyl starch, methylcellulose, sodium carboxymethyl cellulose, hydroxypropyl emthylcellulose, arabic gum, alginic acid, dextrin, cyclodextrin, agar, lactose.
5, the medicine of treatment cardiovascular disease as claimed in claim 4, it is characterized in that it is to be made by 1 part of breviscapine, 3～10 parts of adjuvants, filler adjuvant wherein is selected from following one or more the natural adjuvant sorbitol of plant origin, xylitol, lactose, maltose, and they contain the water of crystallization chemical compound; Plasticity substrate wherein is selected from following one or more the natural adjuvant pregelatinized Starch of plant origin, carboxymethyl starch, methylcellulose, sodium carboxymethyl cellulose, hydroxypropyl emthylcellulose, arabic gum, alginic acid, dextrin, cyclodextrin, agar, lactose.
6, the medicine of treatment cardiovascular disease as claimed in claim 5,1 part of breviscapine, 3～10 parts of adjuvants are made, and filler adjuvant wherein is selected from following one or more the natural adjuvant xylitol of plant origin, lactose; Plasticity substrate wherein is selected from following one or more the natural supplementary product starch of plant origin, arabic gum.
7, as the medicine of the arbitrary described treatment cardiovascular disease of claim 1～6, it is characterized in that it can also contain chemosynthesis adjuvant and animal origin adjuvant in above-mentioned dressing, wherein filler comprises phenylglycol, hexadecanol, octadecanol, sodium stearate, tristerin, tripalmitin, carbamide, polyoxyethylene monostearate, polyoxyethylene alkyl ether; Wherein plasticity substrate comprises polyvinylpyrrolidone, crospolyvinylpyrrolidone, carbomer, polyvinyl alcohol, acrylic resin, poloxamer, gelatin.
8, the medicine of treatment cardiovascular disease as claimed in claim 6 is characterized in that described adjuvant is xylitol and starch, and xylitol is 1: 0.2～1: 0.3 with the ratio of the weight of starch.
9, the medicine of treatment cardiovascular disease as claimed in claim 6 is characterized in that described adjuvant is lactose and starch, and lactose is 1: 0.2～1: 0.3 with the ratio of the weight of starch.
10, the medicine of treatment cardiovascular disease as claimed in claim 6 is characterized in that described adjuvant is xylitol and arabic gum, and the ratio of the weight of xylitol and arabic gum is 1: 0.2～1: 0.4.
11,, it is characterized in that this method comprises the steps: as the preparation method of the arbitrary described treatment cardiovascular disease medicine of claim 1～6
(a) by proportioning take by weighing each crude drug breviscapine, appropriate amount of auxiliary materials is standby;
(b) in appropriate amount of auxiliary materials, add breviscapine, fully mix, be prepared into the oral formulations that allows on the pharmaceutics according to the pharmaceutics preparation method, promptly.
12, the preparation method of treatment cardiovascular disease medicine as claimed in claim 11 is characterized in that this method comprises the steps:
(a) by proportioning take by weighing 0.2～48 part of breviscapine of each crude drug, 4.8～60 parts of adjuvants are standby;
(b) in appropriate amount of auxiliary materials, add breviscapine, fully mix, mixture is at 45～115 ℃ of heating and meltings, stir, mixing time is 1～120 minute, insulation, at 45～95 ℃ of temperature following system, dropper bore is 1.0～4.0 millimeters, splash in-20～25 ℃ liquid paraffin, methyl-silicone oil or the vegetable oil, drip and make ball, promptly.
13, the preparation method of treatment cardiovascular disease medicine as claimed in claim 12 is characterized in that this method comprises the steps:
(a) by proportioning take by weighing 0.6～1.5 part of breviscapine of each crude drug, 2.0～20 parts of adjuvants are standby;
(b) in adjuvant, add the said extracted thing, fully mix, mixture stirs at 60～85 ℃ of heating and meltings, mixing time is 10～30 minutes, insulation is 1.1～3.5 millimeters at 60～85 ℃ of temperature following system, dropper bore, splashes in 0～18 ℃ the liquid paraffin, methyl-silicone oil, drip and make ball, liquid coolant is use up and wiped to the drop pill drop that forms, back packing to be dried, promptly.
14, the preparation method of treatment cardiovascular disease medicine as claimed in claim 13 is characterized in that this method comprises the steps:
(a) by proportioning take by weighing 0.8～1.2 part of breviscapine of each crude drug, 2.3～15 parts of adjuvants are standby;
(b) in adjuvant, add the said extracted thing, fully mix, mixture stirs at 60～85 ℃ of heating and meltings, mixing time is 10～30 minutes, insulation is 1.1～3.5 millimeters at 60～85 ℃ of temperature following system, dropper bore, splashes in 0～18 ℃ the liquid paraffin, methyl-silicone oil, drip and make ball, liquid coolant is use up and wiped to the drop pill drop that forms, back packing to be dried, promptly.
15, the preparation method of treatment cardiovascular disease medicine as claimed in claim 14 is characterized in that this method comprises the steps:
(a) by proportioning take by weighing 1 part of breviscapine of each crude drug, 3～10 parts of adjuvants are standby;
(b) get appropriate amount of auxiliary materials, add the active component of method for preparing, fully mix, mixture is at 64 ℃ of heating and meltings, stir, mixing time is 10～30 minutes, insulation, at 64 ℃ of temperature following system, dropper bore is 1.2～2.5 millimeters, splash in 0 ℃ the methyl-silicone oil, drip and make ball, to the greatest extent and wipe liquid coolant the drop pill drop that forms, back packing to be dried, promptly.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100198517A CN100548307C (en) | 2004-06-30 | 2004-06-30 | A kind of medicine for the treatment of cardiovascular and cerebrovascular disease |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100198517A CN100548307C (en) | 2004-06-30 | 2004-06-30 | A kind of medicine for the treatment of cardiovascular and cerebrovascular disease |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1714796A true CN1714796A (en) | 2006-01-04 |
| CN100548307C CN100548307C (en) | 2009-10-14 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB2004100198517A Expired - Fee Related CN100548307C (en) | 2004-06-30 | 2004-06-30 | A kind of medicine for the treatment of cardiovascular and cerebrovascular disease |
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| Country | Link |
|---|---|
| CN (1) | CN100548307C (en) |
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| CN100548307C (en) | 2009-10-14 |
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Inventor after: Li Yongqiang Inventor after: Wei Feng Inventor after: Chen Jianming Inventor after: Zhu Guoguang Inventor after: Zheng Yongfeng Inventor after: Zhu Yonghong Inventor after: Li Xu Inventor after: Zhang Shunnan Inventor after: Liu Jinping Inventor after: Ye Zhengliang Inventor before: Li Yongqiang Inventor before: Wei Feng Inventor before: Chen Jianming Inventor before: Zhu Guoguang Inventor before: Zheng Yongfeng Inventor before: Zhu Yonghong Inventor before: Li Xu Inventor before: Zhang Shunnan Inventor before: Liu Jinping Inventor before: Ye Zhengliang |
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