CN1430965A - Soft capsule of puerarin and preparing method thereof - Google Patents
Soft capsule of puerarin and preparing method thereof Download PDFInfo
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- CN1430965A CN1430965A CN 03111755 CN03111755A CN1430965A CN 1430965 A CN1430965 A CN 1430965A CN 03111755 CN03111755 CN 03111755 CN 03111755 A CN03111755 A CN 03111755A CN 1430965 A CN1430965 A CN 1430965A
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- puerarin
- soft capsule
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- gelatin
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Abstract
A kakonein softgel is composed of liquid medicine and soft shell. The said liquid medicine contains kakonein, diluent, antioxidizing agent, suspension aid, and emulsifier. The said soft shell contains gelatin and glycerine. Its preparing process includes dissolving gelatin in glycerine, colouring, vacuumizing, laying aside for further application, sequentially mixing others, preparing pills, shape fixation, drying and polishing. Its advantages are high dissolving speed, easy absorption, and high biological utilization rate.
Description
(1) technical field
The present invention relates to soft capsule oral medicine that contains the puerarin effective dose and preparation method thereof, belong to medical technical field.
(2) background technology
Puerarin is a kind of isoflavone monomer that extracts from the dry root of legume pueraria lobata, this medicine is a vasodilator, have the expansion coronary vasodilator, bring high blood pressure down and pharmacological actions such as myocardial oxygen consumption, arrhythmia and significant limitation acute myocardial infarction scope, be used for coronary heart disease, angina pectoris, myocardial infarction clinically, diseases such as retina artery and vein obstruction and sudden deafness have better curative effect.In recent years,, find that this product not only has good therapeutical effect to cardiovascular along with further investigation and clinical observation to the puerarin pharmacological action, and, cerebrovascular and some non-cardiovascular disease also there are desirable therapeutic.This product has beta-receptor blocking effect and energy cerebral blood flow increasing and the metabolic effect of brain.And puerarin causes focal cerebral ischemia to have protective effect to cerebral ischemia of rat acute imperfection and middle cerebral artery blocking-up.In recent years find also that Radix Puerariae have obvious functions of blood sugar, effect for reducing blood fat.From the puerarin pharmacokinetics, this medicine distributes extensively in vivo, absorb fast, be difficult for savings, mainly be distributed in kidney, blood plasma, other internal organs take second place, and can enter cerebral tissue by blood brain barrier, with plasma protein binding rate 24.6%.Quiet notes back is respectively 37%, 7%, 4% by urine, excrement, biliary excretion rate; Oral absorption is also fast.And to the heart, liver, kidney, lung, the harmless and toxic and side effects of spleen stomach function regulating function.
The puerarin application is more extensive clinically, but small-volume injection, transfusion and powder pin are only arranged at present, like this, and to having brought inconvenience in the clinical practice.Soft capsule compare with general formulation have the bioavailability height, good seal, content accurately, characteristic such as good looking appearance, very suitable for the hydrophobic drug of bioavailability difference, and the puerarin poorly water-soluble, gastrointestinal absorption is low and bioavailability is poor.The soft capsule so itself and macromolecule carrier are packed into after miscible can improve its bioavailability greatly.The puerarin soft capsule is a kind of anhydrous oily semi-fluid condition, oral back medicinal liquid adheres to the mucosa tissue surface, is beneficial to absorption of active agents, has improved the bioavailability of puerarin, also overcome simultaneously the injection puerarin and eliminated soon, kept short shortcoming of effective blood drug concentration time in the body.This dosage form than other puerarin dosage form have that the patient of convenience takes, steady quality, outstanding feature and application prospect such as be easy to carry about with one.
Crude drug puerarin and puerarin injection have recorded in Chinese Pharmacopoeia version (enlarged edition in 2002) in 2000.At present, solid preparation is not arranged clinically as yet.
(3) summary of the invention
The present invention is directed to the deficiencies in the prior art, a kind of puerarin soft capsule and preparation method thereof is provided, puerarin soft capsule route of administration is oral, is convenient to different patients and takes, carries, is beneficial to storage, transportation.
Puerarin soft capsule of the present invention comprises medicinal liquid and softgel shell, and medicinal liquid contains the puerarin and the pharmaceutic adjuvant of effective dosage, and pharmaceutic adjuvant comprises diluent, antioxidant, suspending agent, emulsifying agent, contains puerarin 0.01～0.5 gram by every herb liquid of normal capsules grain.
Above-mentioned diluent is one or more in vegetable oil, propylene glycol, Polyethylene Glycol (molecular weight 200～8000), the mineral oil.
Above-mentioned antioxidant is one or more in L cysteine hydrochloride, dithioglycollic acid, disodium EDTA, malic acid, glutathion, D-xylose, glycine, alpha-tocopherol, α-tocopheryl acetate, sodium sulfite, inositol, ascorbic acid, phytic acid, dibenzylatiooluene, sodium ascorbate, lecithin, hydroquinone, xylitol, glucono-, succinic acid, sodium pyrosulfite, the ethylenediaminetetraacetic acid.
Above-mentioned suspending agent is one or more in Carboxymethyl cellulose sodium, carbomer, polyvinyl alcohol, hydroxyethyl-cellulose, sodium alginate, chitin, chitose, hydroxypropyl emthylcellulose, ethyl cellulose, agar, hydroxyethylmethyl-cellulose, hyprolose, Cera Flava, xanthan gum, arabic gum, casein, the methylcellulose.
Mentioned emulsifier is one or more in methylcellulose, glyceryl monostearate, hydroxylated lecithin, acetylated monoglyceride, diethylene glycol distearate, orthoformic acid, casein, ethylene glycol monostearate, ethylhydroxyethylcellulose, diacetyl monoglyceride, acetic acid-fatty glyceride, Emulsifier LM-102, propylene glycol alginate, the two triglycerol monolaurates.
The content of each component can be by prior art on the basis of puerarin 0.01-0.5 gram/grain in the puerarin soft capsule medicinal liquid of the present invention.The invention provides following best proportioning:
Component weight (gram/grain)
Puerarin 0.01-0.5
Diluent 0.025-0.6
Antioxidant 0.0004-0.002
Suspending agent 0.002-0.05
Emulsifying agent 0.0031-0.05
Puerarin soft capsule shell component of the present invention comprises gelatin, glycerol and antiseptic.Gelatin is 10 parts in the softgel shell prescription, glycerol 3.1-3.40 part (weight portion).The component and the content of every softgel shell are as follows:
Gram/grain
Gelatin 0.03-0.31
The 3.10-3.40% of glycerin gelatine weight
Antiseptic 0.00001-0.00009
Foregoing preservatives be in sorbic acid, Sodium Methyl Hydroxybenzoate, benzoic acid, sorbic acid methyl ester, methyl parahydroxybenzoate, P-hydroxybenzoic acid phenyl ester, butyl p-hydroxybenzoate calcium, Oleum Caryophylli, benzyl alcohol, the Sodium Propyl Hydroxybenzoate one or more.
Gelatin, glycerol proportioning are held difficulty in the prescription of softgel shell.The amount of glycerol is too many, and softgel shell is softer, is easier to distortion after being squeezed, the amount of glycerol very little, softgel shell can hardening and crisp, influences the quality stability and the disintegration time of soft capsule.
Gelatin is added in the rustless steel glue pot, add the purified water of solubilized gelatin amount, airtight, 70～80 ℃ are incubated 3 hours, add the glycerol of test consumption more respectively, stir, vacuumize degassing 2 hours, put into 70～80 ℃ of insulations of gelatin heat-preserving container standing over night, second day, the moulding ball, drying at room temperature, keep sample and investigate six months, examination softgel shell outward appearance and physical property, see the following form:
Illustrate: the softgel shell prescription that is filtered out is applicable to the place of normal temperature, humidity.
Can reach a conclusion by above test and should contain 10 parts in gelatin, glycerol 3.18-3.37 part (weight ratio) in the softgel shell prescription.
Emulsifying agent, suspending agent are dissolved in the diluent, puerarin are added wherein again, add antioxidant afterwards and prevent that the medicinal liquid in the soft capsule from rotten (oxidation) taking place in storage process, the amount of every principal agent-puerarin of soft gelatin capsule is determined; Consider the size of economic factor and selected every ball easy to prepare, finally can determine the liquid formula of embodiment.
Puerarin preparation of soft capsule method may further comprise the steps, and the each component addition is all by noted earlier:
1. gelatin places the glue jar, adds the purified water of solubilized gelatin amount, and 70～80 ℃ of glue jar temperature after dissolving, add glycerol, antiseptic, with the cologne earth toning, stir, and are incubated set aside for use after the vacuumize degassing.
2. in proportion emulsifying agent, suspending agent are added in the diluent, take by weighing puerarin, mix with solution, treat to add antioxidant again behind the complete mixing, stir, room temperature leaves standstill.
3. the medicinal liquid for preparing is poured in the pellet processing machine, the hothouse drying is put in typing, scrapes promptly.
The puerarin soft capsule is compared with at present existing dosage form such as puerarin injection, and its superiority is steady quality, the accurate and effective composition stripping of content is fast, active substance easily absorbs, bioavailability height, visual appearance, carry, convenient drug administration.
Product of the present invention prepares as stated above, and its detailed component is provided by the following example, but protection scope of the present invention is not limited to this.
(4) specific embodiment
Embodiment 1.
Component weight (gram/grain)
Puerarin 0.5
Polyethylene Glycol (molecular weight 400) 0.6
Gelatin 0.3
Glycerol 0.01
Succinic acid 0.002
Cera Flava 0.05
Hydroxylated lecithin 0.05
Sorbic acid methyl ester 0.00009
Puerarin preparation of soft capsule method, step is as follows:
(1) take by weighing gelatin and add 100L gelatin retort, under stirring, add the purified water of solubilized gelatin amount, airtight, treat that gelatin dissolves fully after, add glycerol again, add antiseptic sorbic acid methyl ester, stir vacuumize degassing 2 hours, put into the gelatin heat-preserving container, insulation is left standstill, and is stand-by.
(2) under room temperature emulsifying agent hydroxylated lecithin, suspending agent Cera Flava are added in the diluent Polyethylene Glycol, take by weighing puerarin, pulverize, sieve, join in the above-mentioned solution, treat to add the antioxidant succinic acid again behind the complete mixing, stir, room temperature leaves standstill.
(3) medicinal liquid for preparing is poured in the medicinal liquid bucket, change mould and begin to press soft capsule, adjust the soft capsule loading amount to scope of design, drying at room temperature two days, reject the soft gelatin capsule of presentation quality difference, with soft gelatin capsule washing (removing lubricating oil in the pelleting process), again in 24 ℃ of dryings two days, puerarin soft capsule semi-finished product, the packing of the qualified back of quality testing, labeling, packing, promptly get puerarin soft capsule finished product.
Embodiment 2.
Component weight (gram/grain)
Puerarin 0.055
Semen Maydis oil 0.077
Gelatin 0.068
Glycerol 0.002
Ascorbic acid 0.0006
Hydroxyethyl-cellulose 0.008
Casein 0.0072
Butyl p-hydroxybenzoate calcium 0.000018
Embodiment 3.
Component weight (gram/grain)
Puerarin 0.4
Oleum Helianthi 0.5
Gelatin 0.21
Glycerol 0.007
Sodium sulphite 0.0018
Chitose 0.021
Diacetyl monoglyceride 0.04
Benzyl alcohol 0.000075
Embodiment 4.
Component weight (gram/grain)
Puerarin 0.15
Oleum Sesami 0.18
Gelatin 0.06
Glycerol 0.002
Glutathion 0.001
Sodium alginate 0.016
Methylcellulose 0.0015
Benzyl alcohol 0.00003
Embodiment 5.
Component weight (gram/grain)
Puerarin 0.30
Soybean oil 0.35
Gelatin 0.15
Glycerol 0.005
L cysteine hydrochloride 0.0016
Carbomer 0.028
Acetylated monoglyceride 0.03
Methyl parahydroxybenzoate 0.00006
Embodiment 6.
Component weight (gram/grain)
Puerarin 0.25
Oleum Ricini 0.3
Gelatin 0.12
Glycerol 0.004
Dibenzylatiooluene 0.0014
Polyvinyl alcohol 0.02
Diethylene glycol distearate 0.024
P-hydroxybenzoic acid phenyl ester 0.00005
Embodiment 7.
Component weight (gram/grain)
Puerarin 0.01
Hydrogenated vegetable oil 0.027
Gelatin 0.04
Glycerol 0.001
Sodium sulfite 0.0004
Chitin 0.0004
Ethylhydroxyethylcellulose 0.0032
Oleum Caryophylli 0.00001
Embodiment 8.
Component weight (gram/grain)
Puerarin 0.35
Oleum Gossypii semen 0.4
Gelatin 0.18
Glycerol 0.006
Alpha-tocopherol 0.0017
Carboxymethyl cellulose sodium 0.03
Orthoformic acid 0.035
Benzoic acid 0.00007
Embodiment 9.
Component weight (gram/grain)
Puerarin 0.2
Oleum Arachidis hypogaeae semen 0.23
Gelatin 0.09
Glycerol 0.003
Dithioglycollic acid 0.0012
Arabic gum 0.02
Ethylene glycol monostearate 0.02
Butyl p-hydroxybenzoate calcium 0.000038
Embodiment 10.
Component weight (gram/grain)
Puerarin 0.1
Rapeseed oil 0.13
Gelatin 0.03
Glycerol 0.0001
Ethylenediaminetetraacetic acid 0.0008
Hydroxypropyl emthylcellulose 0.012
Glyceryl monostearate 0.011
Benzoic acid 0.00002
Embodiment 11.
Component weight (gram/grain)
Puerarin 0.45
Propylene glycol 0.55
Gelatin 0.25
Glycerol 0.008
Dibutyl first hydroxy toluene 0.0019
Sodium alginate 0.04
Propylene glycol alginate 0.045
Oleum Caryophylli 0.00008
Claims (10)
1. puerarin soft capsule, comprise medicinal liquid and softgel shell, it is characterized in that medicinal liquid contains the puerarin and the pharmaceutic adjuvant of effective dosage, pharmaceutic adjuvant comprises diluent, antioxidant, suspending agent, emulsifying agent, contains puerarin 0.01～0.5 gram by every herb liquid of normal capsules grain.
2. puerarin soft capsule as claimed in claim 1 is characterized in that, described diluent is one or more in vegetable oil, propylene glycol, molecular weight polyethylene glycol 200-8000, the mineral oil.
3. puerarin soft capsule as claimed in claim 1, it is characterized in that described antioxidant is one or more in L-cysteine hydrochloride, dithioglycollic acid, disodium EDTA, malic acid, glutathion, D-xylose, glycine, alpha-tocopherol, α-tocopheryl acetate, sodium sulfite, inositol, ascorbic acid, phytic acid, dibenzylatiooluene, sodium ascorbate, lecithin, hydroquinone, xylitol, glucono-, succinic acid, sodium pyrosulfite, the ethylenediaminetetraacetic acid.
4. puerarin soft capsule as claimed in claim 1, it is characterized in that described suspending agent is one or more in Carboxymethyl cellulose sodium, carbomer, polyvinyl alcohol, hydroxyethyl-cellulose, sodium alginate, chitin, chitose, hydroxypropyl emthylcellulose, ethyl cellulose, agar, hydroxyethylmethyl-cellulose, hyprolose, Cera Flava, xanthan gum, arabic gum, casein, the methylcellulose.
5. puerarin soft capsule as claimed in claim 1; it is characterized in that described emulsifying agent is one or more in methylcellulose, glyceryl monostearate, hydroxylated lecithin, acetylated monoglyceride, diethylene glycol distearate, orthoformic acid, casein, ethylene glycol monostearate, ethylhydroxyethylcellulose, diacetyl monoglyceride, acetic acid-fatty glyceride, Emulsifier LM-102, propylene glycol alginate, the two triglycerol monolaurates.
6. puerarin soft capsule as claimed in claim 1 is characterized in that, the content of each component in the described medicinal liquid:
Component gram/grain
Puerarin 0.01-0.5
Diluent 0.025-0.6
Antioxidant 0.0004-0.002
Suspending agent 0.002-0.05
Emulsifying agent 0.0031-0.05.
7. puerarin soft capsule as claimed in claim 1 is characterized in that, described capsule softgel shell contains 10 parts in gelatin, glycerol 3.1-3.40 part, weight portion.
8. puerarin soft capsule as claimed in claim 1 is characterized in that, the component and the content of every softgel shell of described capsule softgel shell are as follows:
Gram/grain
Gelatin 0.03-0.31
The 3.10-3.40% of glycerin gelatine amount
Antiseptic 0.00001-0.00009.
9. puerarin soft capsule as claimed in claim 8, it is characterized in that, described antiseptic be in sorbic acid, Sodium Methyl Hydroxybenzoate, benzoic acid, sorbic acid methyl ester, methyl parahydroxybenzoate, P-hydroxybenzoic acid phenyl ester, butyl p-hydroxybenzoate calcium, Oleum Caryophylli, benzyl alcohol, the Sodium Propyl Hydroxybenzoate one or more.
10. the described puerarin preparation of soft capsule of claim 1 method may further comprise the steps:
(1) gelatin places the glue jar, adds the purified water of solubilized gelatin amount, and 70～80 ℃ of glue jar temperature after dissolving, add glycerol, antiseptic, with the cologne earth toning, stir, and are incubated set aside for use after the vacuumize degassing;
(2) emulsifying agent, suspending agent are added in the diluent, add puerarin, treat to add antioxidant again behind the complete mixing, stir, room temperature leaves standstill;
(3) medicinal liquid for preparing is poured in the pellet processing machine, the hothouse drying is put in typing, scrapes promptly.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03111755 CN1430965A (en) | 2003-01-23 | 2003-01-23 | Soft capsule of puerarin and preparing method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03111755 CN1430965A (en) | 2003-01-23 | 2003-01-23 | Soft capsule of puerarin and preparing method thereof |
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| CN1430965A true CN1430965A (en) | 2003-07-23 |
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| CN 03111755 Pending CN1430965A (en) | 2003-01-23 | 2003-01-23 | Soft capsule of puerarin and preparing method thereof |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101804045A (en) * | 2010-04-09 | 2010-08-18 | 上海新康制药厂 | Application of puerarin |
| CN109528679A (en) * | 2019-01-15 | 2019-03-29 | 南宁富莱欣生物科技有限公司 | One kind includes multivitamin soft capsule and its production method |
| CN109662953A (en) * | 2019-02-18 | 2019-04-23 | 威海金思力生物科技股份有限公司 | A kind of vitamin D soft capsule and preparation method thereof |
-
2003
- 2003-01-23 CN CN 03111755 patent/CN1430965A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101804045A (en) * | 2010-04-09 | 2010-08-18 | 上海新康制药厂 | Application of puerarin |
| CN109528679A (en) * | 2019-01-15 | 2019-03-29 | 南宁富莱欣生物科技有限公司 | One kind includes multivitamin soft capsule and its production method |
| CN109662953A (en) * | 2019-02-18 | 2019-04-23 | 威海金思力生物科技股份有限公司 | A kind of vitamin D soft capsule and preparation method thereof |
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