CN1739545A - Pueraria flavone micro pill prepn and its prepn process - Google Patents
Pueraria flavone micro pill prepn and its prepn process Download PDFInfo
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- CN1739545A CN1739545A CN 200510094163 CN200510094163A CN1739545A CN 1739545 A CN1739545 A CN 1739545A CN 200510094163 CN200510094163 CN 200510094163 CN 200510094163 A CN200510094163 A CN 200510094163A CN 1739545 A CN1739545 A CN 1739545A
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Abstract
The present invention belongs to the field of medicine technology, and discloses pueraria flavone micro pill preparation as one new preparation form of pueraria flavone and its preparation process. The pueraria flavone micro pill preparation has raised pueraria flavone bioavailability, relatively low production cost, and simple preparation process. The pueraria flavone micro pill preparation is compounded with pueraria flavone, supplementary material, wetter or adhesive, and has micro pill diameter smaller than 2.5 mm. The preparation process includes the steps of: 60-120 mesh sieving pueraria flavone and supplementary material, mixing, adding wetter or adhesive and mixing, pelletizing and drying.
Description
Technical field
The invention belongs to field of medicaments, relate to a kind of Chinese medicine pellet preparation and preparation method thereof, exactly relate to a kind of novel drugs dosage form of Radix Puerariae flavone---pueraria flavone micro pill preparation and preparation method thereof.
Background technology
Radix Puerariae flavone is refining through extraction from Chinese medicine Herba Gelsemii Elegantis Pueraria lobata (Willd.) Ohwi and pale brown toner end that get, and its main component is puerarin (puerarin).Radix Puerariae flavone has significant reduction myocardial oxygen consumption, and dilating coronary blood vessel increases arteria coronaria and brain vessel blood amount, arrhythmia, and antioxidation, enhancing human body immunity power, blood sugar lowering waits pharmacological action.Puerarin is owing to its determined curative effect, wide, the low widely use clinically of toxicity of safety range.Radix Puerariae flavone class preparation is mainly used in diseases such as treatment coronary heart disease, angina pectoris, nervous headache, hypertension, cerebral arteriosclerosis and early sudden deafness clinically.
Radix Puerariae flavone (puerarin) preparation is mainly dosage forms such as injection, tablet, drop pill at present.Because puerarin injection is made troubles to the patient; And Yufengningxin drop pill bioavailability is not high, yufeng ningxin tablets, yufeng ningxin pian is lower, China Patent No.: 03135459 has announced the patent of invention of a kind of " preparation method of Yufengningxin micropill " by name, but the micropill disintegrate at short notice that should invent, release is very unstable, can not satisfy the clinical application demand; This invention method for making is manual general system, can not satisfy Chinese medicine preparation modernization requirement.Therefore be necessary to research and develop a kind of taking convenience, oral administration biaavailability height, be suitable for novel form---the pueraria flavone micro pill that modernization industry is produced, micropill is meant all kinds of pills of diameter less than 2.5mm, can make slow release or controlled release preparation according to different needs, pueraria flavone micro pill can improve oral administration biaavailability, can satisfy the requirement of extensive patients again.
Summary of the invention
The present invention seeks to solve above-mentioned the deficiencies in the prior art and problem, a kind of pueraria flavone micro pill preparation is provided, it can improve the bioavailability of Radix Puerariae flavone, and production cost is lower again, cheap.
Another object of the present invention provides a kind of preparation method of pueraria flavone micro pill preparation simultaneously, and preparation method is simple and convenient.
Purpose of the present invention realizes by following technical solution:
A kind of pueraria flavone micro pill preparation, it is formulated by Radix Puerariae flavone, adjuvant, wetting agent or binding agent, the micropill diameter of making is less than 2.5mm, wherein Radix Puerariae flavone and adjuvant quality proportioning are 1: 0.5～10, preferred 1: 0.5～5, wetting agent or adhesive consumption be---the ratio that the volume and the Radix Puerariae flavone of wetting agent or binding agent add adjuvant quality sum is 1: 0.2～5, and preferred 1: 0.5～5, the volume unit of wetting agent or binding agent is mL, and Radix Puerariae flavone and adjuvant mass unit are g.
Contain puerarin 10%～90% in the described Radix Puerariae flavone; Described adjuvant is one or more the mixture in microcrystalline Cellulose, lactose, micropowder silica gel, dextrin, starch, the mannitol; Described wetting agent or binding agent are one or more the mixture in water, ethanol, Gonak, the carboxymethylcellulose sodium solution.
The preparation method of pueraria flavone micro pill preparation of the present invention, step is as follows:
Get Radix Puerariae flavone and adjuvant, mixing behind mistake 60～120 mesh sieves adds wetting agent or binding agent mixing then respectively, through the pelletize after drying, makes pellet preparations of the present invention.
Wherein said Radix Puerariae flavone and adjuvant quality proportioning are 1: 0.5～10, preferred 1: 0.5～5, wetting agent or adhesive consumption be---the ratio that the volume and the Radix Puerariae flavone of wetting agent or binding agent add adjuvant quality sum is 1: 0.2～5, preferred 1: 0.5～5, the volume unit of wetting agent or binding agent is mL, and Radix Puerariae flavone and adjuvant mass unit are g.
Contain puerarin 10%～90% in the described Radix Puerariae flavone; Described adjuvant is one or more the mixture in microcrystalline Cellulose, lactose, micropowder silica gel, dextrin, starch, the mannitol; Described wetting agent or binding agent are one or more the mixture in water, ethanol, Gonak, the carboxymethylcellulose sodium solution.
Process for granulating described in the preparation method of the present invention is for extruding round as a ball comminution granulation, centrifugal fluidization comminution granulation, the general method for making of coating pan, fluid bed pill method, laminated type pill method, spraying and congeal pill method or spray drying pill method; Described drying means is atmosphere pressure desiccation, hypobaric drying method, boulton process or fluid-bed drying.
Beneficial effect of the present invention is as follows:
1, seldom be subjected to digestive tract to carry the influence of the food rhythm and pace of moving things (especially pylorus keying); 2, micropill is bigger at the area of gastrointestinal tract surface distributed, thereby improves bioavailability, reduces or eliminates local excitation; 3, can make slow release, controlled release preparation according to clinical needs; 4, good looking appearance, good fluidity; 5, content of dispersion is big, and advantage such as taking dose is little; 6, in the drug release process, the micropill surface can inwardly not subside, and release is stable, controlled.
The bioavailability height of pueraria flavone micro pill preparation of the present invention in addition, cost is low, low price, patient's taking convenience, preparation technology is simple simultaneously, can satisfy the demand of extensive patients.
Description of drawings
Fig. 1 is the releasing curve diagram of pueraria flavone micro pill preparation in normal saline.
Curve chart when Fig. 2 is the medicine of oral pueraria flavone micro pill preparation of domesticated dog and Yufengningxin drop pill.
The specific embodiment
Below by specific embodiment explanation the present invention, but the present invention not merely is defined in these embodiment.
Embodiment 1
Pueraria flavone micro pill preparation and preparation method
Prescription is formed:
Radix Puerariae flavone 12.5g
Microcrystalline Cellulose 30g
Micropowder silica gel 7.5g
50% ethanol 31mL
Preparation method:
Get Radix Puerariae flavone, microcrystalline Cellulose and micropowder silica gel by said ratio, cross mixing behind 60 mesh sieves respectively, add 50% pure 31mL mixing then, reuse is extruded round as a ball comminution granulation, and to make diameter down dry in 60 ℃ of normal pressures after less than the microgranule of 2.5mm, makes pellet preparations of the present invention.It is 95% that the result records yield, and the micropill roundness is good, and release is stable.
Pueraria flavone micro pill preparation and preparation method
Prescription is formed:
Radix Puerariae flavone 12.5g
Microcrystalline Cellulose 32.5g
Lactose 5g
Water 32.5mL
Preparation method:
Get Radix Puerariae flavone, microcrystalline Cellulose and lactose by said ratio, cross mixing behind 120 mesh sieves respectively, add entry 32.5mL mixing then, reuse fluid bed pill method make diameter less than the microgranule of 2.5mm after in 50 ℃ of drying under reduced pressure, make pellet preparations of the present invention.It is 92% that the result records yield, and the micropill roundness is good, and release is stable.
Embodiment 3
Pueraria flavone micro pill preparation and preparation method
Prescription is formed:
Radix Puerariae flavone 22.5g
Starch 30.5g
Lactose 7.5g
Water 30.5mL
Preparation method:
Get Radix Puerariae flavone, starch and lactose by said ratio, cross mixing behind 120 mesh sieves respectively, add entry 30.5mL mixing then, reuse laminated type pill method make diameter less than the microgranule of 2.5mm after in 50 ℃ of drying under reduced pressure, make pellet preparations of the present invention.It is 94% that the result records yield, and the micropill roundness is good, and release is stable.
Embodiment 4
Pueraria flavone micro pill preparation and preparation method
Prescription is formed:
Radix Puerariae flavone 17.5g
Microcrystalline Cellulose 25g
Dextrin 12.5g
Water 32mL
Preparation method:
Get Radix Puerariae flavone, microcrystalline Cellulose and dextrin by said ratio, cross mixing behind 120 mesh sieves respectively, add entry 32mL mixing then, the reuse spraying congeal the pill method make diameter less than the microgranule of 2.5mm after in 50 ℃ of drying under reduced pressure, make pellet preparations of the present invention.It is 90% that the result records yield, and the micropill roundness is good, and release is stable.
Pueraria flavone micro pill preparation and preparation method
Prescription is formed:
Radix Puerariae flavone 20g
Starch 32.5g
Mannitol 5g
5％HPMC 35mL
Preparation method:
Get Radix Puerariae flavone, starch and mannitol by said ratio, cross mixing behind 120 mesh sieves respectively, add 5% hydroxypropyl emthylcellulose (HPMC) solution 35mL mixing then, reuse spray drying pill method make diameter less than the microgranule of 2.5mm after in 50 ℃ of drying under reduced pressure, make pellet preparations of the present invention.It is 88% that the result records yield, and the micropill roundness is good, and release is stable.
Below further set forth the beneficial effect and the curative effect of pueraria flavone micro pill preparation of the present invention by Comparative Examples and test example.
Comparative Examples 1: the release effect of different pueraria flavone micro pill preparations of the present invention
Get embodiment 1,2,4 samples, according to dissolution method (two appendix XC of Chinese Pharmacopoeia version in 2005), dissolution medium is a normal saline, rotating speed 100rmin
-1Temperature is to carry out dissolution in vitro under 37 ± 0.5 ℃ of conditions to investigate, press ultraviolet spectrophotometry and measure trap in 250nm wavelength place, the standard curve equation is c=0.0259A-0.0045 (r=0.9995 n=6), calculate micropill in the external relatively stripping percentage rate of different time according to standard curve, the results are shown in Figure 1.
As seen from Figure 1, the external release of micropill made under the different embodiment is stable, and release is complete in 2 hours.
Comparative Examples 2: the bioavailability of the relative Yufengningxin drop pill of pueraria flavone micro pill preparation of the present invention
6 of healthy domesticated dogs, body weight (11.8 ± 2.3) kg, male and female half and half are provided by the Jiangsu Prov. Research Inst. Traditional Chinese Medical Experimental Animal Center.Fasting is 12 hours before the administration, the unified feed of test back 4h.Fasting contains soy food product in the whole process.Single dose gives Radix Puerariae total flavones micropill and commercially available Yufengningxin drop pill, and dosage (by puerarin) is 50mgkg
-1, week back intersection administration.In 0,0.33,0.67,1.0,1.5,2.0,3.0,4.0,6.0,8.0,12.0,24.0h gets blood 3mL from the forelimb vein after the administration.The blood sample anticoagulant heparin, the centrifugal 10min of 4000rpm, separated plasma is measured the puerarin concentration in blood drug level and the blood plasma, the results are shown in Figure 2.
By Fig. 2 result as seen, pueraria flavone micro pill preparation area under curve of the present invention (AUC) is 8459ngh/mL, and Yufengningxin drop pill area under curve (AUC) is 5601ngh/mL, and relative bioavailability is 151%.
The test example: the pueraria flavone micro pill preparation of the inventive method preparation is to the clinical observation of treatment cardiovascular and cerebrovascular disease
1. physical data
20 routine outpatient services and partial hospitalization patient, among the patient, male's 13 examples, women's 7 examples, 24～75 years old age, hypertension 12 examples wherein, coronary heart disease 6 examples, arrhythmia 2 examples.
2. Therapeutic Method
Above-mentioned 20 routine cardiovascular and cerebrovascular disease patients are awarded pueraria flavone micro pill treat, every day 3 times, each (by puerarin) 100mg, 7 is a course of treatment.
3. therapeutic evaluation standard
Three kinds of cases are improved as the therapeutic evaluation index with blood pressure drops, arteria coronaria vasodilation, the rhythm of the heart respectively.
4. result
20 patients received treatment after 4 courses of treatment, effective 17 examples, and produce effects 8 examples wherein, invalid 3 examples, total effective rate reaches 85%.
Claims (10)
1, a kind of pueraria flavone micro pill preparation, it is characterized in that it being formulated by Radix Puerariae flavone, adjuvant, wetting agent or binding agent, the micropill diameter of making is less than 2.5mm, wherein Radix Puerariae flavone and adjuvant quality proportioning are 1: 0.5～10, wetting agent or adhesive consumption be---the ratio that the volume and the Radix Puerariae flavone of wetting agent or binding agent add adjuvant quality sum is 1: 0.2～5, the volume unit of wetting agent or binding agent is mL, and Radix Puerariae flavone and adjuvant mass unit are g.
2, pueraria flavone micro pill preparation according to claim 1, it is characterized in that described Radix Puerariae flavone and adjuvant quality proportioning are 1: 0.5～5, wetting agent or adhesive consumption be---the ratio that the volume and the Radix Puerariae flavone of wetting agent or binding agent add adjuvant quality sum is 1: 0.5～5, the volume unit of wetting agent or binding agent is mL, and Radix Puerariae flavone and adjuvant mass unit are g.
3, pueraria flavone micro pill preparation according to claim 1 and 2 is characterized in that containing in the described Radix Puerariae flavone puerarin 10%～90%.
4, pueraria flavone micro pill preparation according to claim 1 and 2 is characterized in that described adjuvant is one or more the mixture in microcrystalline Cellulose, lactose, micropowder silica gel, dextrin, starch, the mannitol.
5, pueraria flavone micro pill preparation according to claim 1 and 2 is characterized in that described wetting agent or binding agent are one or more the mixture in water, ethanol, Gonak, the carboxymethylcellulose sodium solution.
6, according to the described pueraria flavone micro pill preparation of claim 1～5, its preparation method, step is as follows:
Get Radix Puerariae flavone and adjuvant, mixing behind mistake 60～120 mesh sieves adds wetting agent or binding agent mixing then respectively, through the pelletize after drying, makes pellet preparations of the present invention.
7, preparation method according to claim 6 is characterized in that described process for granulating is for extruding round as a ball comminution granulation, centrifugal fluidization comminution granulation, the general method for making of coating pan, fluid bed pill method, laminated type pill method, spraying and congeal pill method or spray drying pill method.
8, preparation method according to claim 6 is characterized in that described drying means is atmosphere pressure desiccation, hypobaric drying method, boulton process or fluid-bed drying.
9, pueraria flavone micro pill preparation according to claim 1 is characterized in that being made by the material of following proportioning:
Radix Puerariae flavone 12.5g
Microcrystalline Cellulose 30g
Micropowder silica gel 7.5g
50% ethanol 31mL
10, preparation method according to claim 6 is characterized in that step is as follows:
Get Radix Puerariae flavone 22.5g, starch 30.5g and lactose 7.5g, cross mixing behind 120 mesh sieves respectively, add entry 30.5mL mixing then, reuse laminated type pill method make diameter less than the microgranule of 2.5mm after in 50 ℃ of drying under reduced pressure, promptly get pellet preparations of the present invention.
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| CNB2005100941631A CN100335064C (en) | 2005-08-31 | 2005-08-31 | Pueraria flavone micro pill prepn and its prepn process |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102783647A (en) * | 2012-08-28 | 2012-11-21 | 句容茅宝葛业有限公司 | Preparation method of kudzu root isoflavone powder |
| CN103800428A (en) * | 2012-11-15 | 2014-05-21 | 吉林吉春制药股份有限公司 | Medicine for treating yin deficiency and yang excess syndrome of hypertension and coronary heart disease and preparation method thereof |
| CN105994798A (en) * | 2016-05-18 | 2016-10-12 | 江苏茅宝葛业有限公司 | Method for preparing soluble tea pills from wild pueraria flavonoid extract |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1569068A (en) * | 2003-07-22 | 2005-01-26 | 周美华 | Preparation method of |
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2005
- 2005-08-31 CN CNB2005100941631A patent/CN100335064C/en not_active Expired - Fee Related
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102783647A (en) * | 2012-08-28 | 2012-11-21 | 句容茅宝葛业有限公司 | Preparation method of kudzu root isoflavone powder |
| CN103800428A (en) * | 2012-11-15 | 2014-05-21 | 吉林吉春制药股份有限公司 | Medicine for treating yin deficiency and yang excess syndrome of hypertension and coronary heart disease and preparation method thereof |
| CN105994798A (en) * | 2016-05-18 | 2016-10-12 | 江苏茅宝葛业有限公司 | Method for preparing soluble tea pills from wild pueraria flavonoid extract |
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| CN100335064C (en) | 2007-09-05 |
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Granted publication date: 20070905 Termination date: 20120831 |