CN100336505C - Soybean aglycone soft capsule and its preparing method - Google Patents
Soybean aglycone soft capsule and its preparing method Download PDFInfo
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- CN100336505C CN100336505C CNB2004100237418A CN200410023741A CN100336505C CN 100336505 C CN100336505 C CN 100336505C CN B2004100237418 A CNB2004100237418 A CN B2004100237418A CN 200410023741 A CN200410023741 A CN 200410023741A CN 100336505 C CN100336505 C CN 100336505C
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- daidzein
- soft capsule
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Abstract
The present invention relates to a daidzein soft capsule and a preparation process thereof, which belongs to the technical field of medicines. The daidzein soft capsule comprises physic liquor and a capsule shell, wherein the physic liquor comprises daidzin as a main medicine and pharmaceutic adjuvants comprising cosolvents, diluting agents, emulsifying agents and disintegrating agents; the capsule shell comprises the following components: 10 portions by weight of gelatin, 3.00 to 4.60 portions by weight of glycerol, opacifiers and preservative agents; the physic liquor of each capsule granule contains 0.01 to 0.5 gram of daidzein by standard. The daidzein soft capsule improves the water solubility and the dispersivity of daidzein, the permeability of gastrointestinal mucous membranes can be improved when medicines enter bodies, and oral taking absorption can be improved; accordingly, the bioavailability of oral taking can be obviously improved. The daidzein soft capsule is oral-taken and is convenient for different patients to take and carry, and the daidzein soft capsule can be conveniently stored and transported.
Description
(1) technical field
The present invention relates to soft capsule oral medicine that contains the daidzein effective dose and preparation method thereof, belong to medical technical field.
(2) background technology:
Daidzein is one of main active of Radix Puerariae, has coronary artery dilator, removes vasospasm, improve normal ischemic myocardium metabolism, slowly reduce heart rate, reduce myocardial oxygen consumption, improve myocardial function, reduce TXA2/PGI2, reduce blood viscosity, the antagonism isoproterenol, reduce the blood capillary spasm, the effect of microcirculation improvement, and these product also have the estrogenic effect of class, can obviously improve and eliminate the symptom of Women.The oral cardiovascular and cerebrovascular disease that is applicable to comprises hypertension and symptomatic hypertension, coronary heart disease, and angina pectoris, myocardial infarction, cerebral thrombosis, arrhythmia, vertigo, sudden deafness also can be used for climacteric syndrome etc.Find that in the metabolism research of daidzein 1.2h reclaims dosage and is respectively 54.95% and 36.67% of total amount after the administration, visible aglycon is very fast at the mice internal metabolism.Medicine menses and tissue slice temperature are incubated back mensuration yield, and aglycon is more obvious by hepatic metabolism as a result, hardly by the metabolism of blood institute.It distributes wide in vivo and is fast, eliminates also soon, is difficult for putting aside, and characteristics such as no metabolism saturated phenomenon are for data for clinical drug use provides important evidence.
Its oral formulations only has tablet and capsule clinically at present, since the awkward soluble substance of these product, the both water insoluble fat material that also is insoluble to, and therefore, common tablet and capsule are difficult to change the relatively poor problem of its bioavailability.Soft capsule is that medicine is dispersed in the substrate, be wrapped in the soft capsule solution is airtight by pressing, medicine is hedged off from the outer world, promptly covered the uncomfortable taste of medicine, improved stability of formulation again, the soft capsule that makes is exquisite appearance not only, taking convenience and medicament contg are accurate, the precision height, it is fast to prove effective, the bioavailability height.The daidzein soft capsule is the anhydrous oily semi-fluid substance of making through a kind of special process, the soft capsule that repressed method forms, prove by external dissolution test, the average dissolution of this product can reach 90%, the oral back of this dosage form medicinal liquid adheres to stomach, intestinal submucosa tissue surface, be beneficial to absorption of active agents, thus the raising bioavailability of medicament.And have the patient of convenience and use, outstanding feature and application prospect such as evident in efficacy, toxic and side effects is little, and cost is low.
(3) summary of the invention
The present invention is directed to the deficiencies in the prior art, a kind of daidzein soft capsule and preparation method thereof is provided.
Daidzein soft capsule of the present invention comprises medicinal liquid and softgel shell, and medicinal liquid comprises principal agent daidzein and pharmaceutic adjuvant, and pharmaceutic adjuvant comprises cosolvent, diluent, emulsifying agent and disintegrating agent.Contain daidzein 0.01～0.5 gram by every herb liquid of normal capsules grain.
Above-mentioned cosolvent is glycerol, polyvidone, cyclodextrin, propylene glycol, isopropyl alcohol, ethylenediamine, ethylene glycol amine, sodium lauryl sulphate, dodecylbenzene sodium sulfonate, lactic acid, Polyethylene Glycol
400-6000, among the polysorbate fat 20-85, polypropylene glycol, Oleum Ricini one or more.
Above-mentioned diluent is vegetable oil, linoleic acid, ethanol, propylene glycol, Polyethylene Glycol
200-8000, in the microcrystalline Cellulose, carboxymethylcellulose calcium, polyvinylpolypyrrolidone, sorbitol, starch, dextrin, mineral oil one or more.
Mentioned emulsifier is one or more in ethylhydroxyethylcellulose, sodium lauryl sulphate, dodecylbenzene sodium sulfonate, Stepanol MG, sodium tetradecyl sulfate, methylcellulose, glyceryl monostearate, lecithin, emulsifing wax, hydroxypropyl methylcellulose, hydroxylation ethyl cellulose, Cera Flava, casein, ethylene glycol monostearate, polysorbate 20-85, the Oleum Ricini.
Above-mentioned disintegrating agent is polysorbate 20-80, Polyethylene Glycol
400-6000, in the glycerol, potassium carbonate, sodium lauryl sulphate, Stepanol MG, methylcellulose, silicon dioxide, cross-linking sodium carboxymethyl cellulose, polyvinylpolypyrrolidone, polypropylene glycol, hydroxyethyl-cellulose, starch, microcrystalline Cellulose, carboxymethylcellulose calcium, polyoxyethylene one or more.
Each components contents is preferably as follows proportioning in the daidzein soft capsule medicinal liquid of the present invention on the basis of daidzein 0.01～0.5 gram/grain:
Group component (gram/grain)
Daidzein 0.01～0.5
Cosolvent 0.05～4.5
Diluent 0.099～4.95
Emulsifying agent 0.01～0.5
Disintegrating agent 0.004～0.5
Daidzein soft capsule shell component is by prior art among the present invention.The preferred ingredient of every softgel shell is as follows:
Group component (gram/grain)
Gelatin 0.05～0.5
Glycerol 0.015～0.23
Antiseptic 0.00005～0.0005
Opacifier 0.00022～0.0065
Water 0.0536～0.53570
Wherein, water drying in preparation process is removed.
Foregoing preservatives is one or more in sorbic acid, Sodium Methyl Hydroxybenzoate, benzoic acid, sorbic acid methyl ester, methyl parahydroxybenzoate, P-hydroxybenzoic acid phenyl formate, Sodium Propyl Hydroxybenzoate, ethyl hydroxybenzoate, Oleum Caryophylli, the benzyl alcohol.
Above-mentioned opacifier is one or more in red ferric oxide, titanium dioxide, barium sulfate, the precipitated calcium carbonate.
The proportioning of gelatin, glycerol is 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 purified water, airtight, 75 ℃, be incubated 3 hours, add the glycerol of test consumption more respectively, stir, vacuumize degassing 2 hours, put into 75 ℃ of insulations of gelatin heat-preserving container standing over night, second day, drying at room temperature, keep sample and investigate six months, investigate softgel shell outward appearance and physical property.
Principal agent daidzein of the present invention is the slightly solubility material, add suitable pharmaceutic adjuvant through test of many times, can improve the water solublity and the dispersibility of daidzein greatly, and can increase the permeability of gastrointestinal mucosa when making medicine enter in the body, improve oral absorption, therefore, can significantly improve oral bioavailability.
The principal agent daidzein is added an amount of cosolvent, emulsifying agent, disintegrating agent, be dissolved in the proper amount of diluting, the amount of every principal agent-daidzein 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.
Daidzein soft capsule route of administration is oral, is convenient to different patients and takes, carries, and is beneficial to storage, transportation.
Daidzein preparation of soft capsule method may further comprise the steps:
(1) gelatin, glycerol place the glue jar to add purified water, and 70～80 ℃ of glue jar temperature after dissolving, add opacifier, antiseptic, stir, and are incubated set aside for use after the vacuumize degassing.
(2) principal agent daidzein adding cosolvent, emulsifying agent, disintegrating agent are dissolved in the diluent, stir, room temperature leaves standstill.
(3) medicinal liquid for preparing is poured in the pellet processing machine, typing is put the hothouse drying, promptly.
The daidzein soft capsule is compared with at present existing dosage form such as daidzein sheet, and its superiority is steady quality, and content is accurate, and the effective ingredient stripping is fast, and active substance easily absorbs, the bioavailability height, and visual appearance is carried, 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.
Group component (gram/grain)
Daidzein 0.4
Polyvidone 2
Propylene glycol 3.96
Methylcellulose 0.034
Polysorbate 60 0.096
Preparation method is as follows:
(1) principal agent daidzein adding cosolvent, emulsifying agent, disintegrating agent are dissolved in the diluent, stir, room temperature leaves standstill.
(2) medicinal liquid for preparing is poured in the pellet processing machine, the hothouse drying is put in typing, scrapes promptly.
Embodiment 2.
Group component (gram/grain)
Daidzein 0.25
Polyethylene Glycol
80001.35
Cera Flava 0.035
Polypropylene glycol 0.012
Embodiment 3.
Group component (gram/grain)
Daidzein 0.045
Polysorbate 40 0.225
Mineral oil 0.4455
Orthoformic acid 0.0045
Alginic acid 0.0028
Embodiment 4.
Group component (gram/grain)
Daidzein 0.057
Polyvinylpolypyrrolidone 0.289
Soybean oil 0.063
Orthoformic acid 0.0046
Sodium lauryl sulphate 0.00278
Embodiment 5.
Group component (gram/grain)
Daidzein 0.28
Cyclodextrin 1.28
Propylene glycol 1.56
Sunflower oil 1.013
Emulsifier LM-102 0.038
Microwax 0.0122
Embodiment 6.
Group component (gram/grain)
Daidzein 0.18
Polysorbate 40 0.97
Semen Maydis oil 1.787
Methylcellulose 0.018
Polyethylene Glycol
60000.0082
Embodiment 7.
Group component (gram/grain)
Daidzein 0.045
Isopropyl alcohol 0.205
Semen Maydis oil 0.4465
Orthoformic acid 0.0055
Methylcellulose 0.0028
Embodiment 8.
Group component (gram/grain)
Daidzein 0.025
Cyclodextrin 0.175
Soybean oil 0.2673
Cera Flava 0.0027
Polyoxyethylene sorbitan monoleate 0.01
Embodiment 9.
Group component (gram/grain)
Daidzein 0.38
Polyethylene Glycol
40001.76
Propylene glycol 3.862
Methylcellulose 0.0378
Potassium carbonate 0.0152
Embodiment 10.
Group component (gram/grain)
Daidzein 0.07
Polysorbate 60 3.869
Soybean oil 2.98
Casein 0.0067
Stepanol MG 0.0034
Embodiment 11.
Group component (gram/grain)
Daidzein 0.01
Isobutanol 0.046
Propylene glycol 0.098
Orthoformic acid 0.0009
Methylcellulose 0.0039
Embodiment 12.
Group component (gram/grain)
Daidzein 0.5
Polypropylene glycol 2.59
Soybean oil 4.74
Propylene glycol alginate 0.054
Starch 0.021
Claims (2)
1, daidzein soft capsule, comprise medicinal liquid and softgel shell, it is characterized in that medicinal liquid comprises principal agent daidzein and pharmaceutic adjuvant, pharmaceutic adjuvant comprises cosolvent, diluent, emulsifying agent and disintegrating agent, contains daidzein 0.01～0.5 gram by every herb liquid of normal capsules grain;
Described cosolvent is a Polyethylene Glycol
4000, Polyethylene Glycol
6000, in the polypropylene glycol, polyvidone, sodium lauryl sulphate, cyclodextrin, polysorbate 60 one or more;
Described diluent is vegetable oil, mineral oil, propylene glycol, Polyethylene Glycol
8000, in the starch one or more;
Described emulsifying agent is one or more in Cera Flava, methylcellulose, the casein;
Described disintegrating agent is one or more in polysorbate 40, polysorbate 60, polyvinylpolypyrrolidone, potassium carbonate, the Stepanol MG.
2, daidzein soft capsule as claimed in claim 1 is characterized in that component is as follows:
Group component (gram/grain)
Daidzein 0.01～0.5
Cosolvent 0.05～4.5
Diluent 0.099～4.95
Emulsifying agent 0.01～0.5
Disintegrating agent 0.004～0.5.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100237418A CN100336505C (en) | 2004-03-16 | 2004-03-16 | Soybean aglycone soft capsule and its preparing method |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100237418A CN100336505C (en) | 2004-03-16 | 2004-03-16 | Soybean aglycone soft capsule and its preparing method |
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| Publication Number | Publication Date |
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| CN1561989A CN1561989A (en) | 2005-01-12 |
| CN100336505C true CN100336505C (en) | 2007-09-12 |
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| CNB2004100237418A Expired - Fee Related CN100336505C (en) | 2004-03-16 | 2004-03-16 | Soybean aglycone soft capsule and its preparing method |
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Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100413498C (en) * | 2006-04-25 | 2008-08-27 | 邵爱霞 | Drop pills of soybean aglycone, and preparation method |
| CN113694037A (en) * | 2021-08-25 | 2021-11-26 | 南宁富莱欣生物科技有限公司 | Soft capsule with high calcium content and preparation key technology |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1442148A (en) * | 2003-03-26 | 2003-09-17 | 耿燕 | Daidzein drip pill and its preparation method |
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1442148A (en) * | 2003-03-26 | 2003-09-17 | 耿燕 | Daidzein drip pill and its preparation method |
Non-Patent Citations (2)
| Title |
|---|
| 提高黄豆苷元片溶出度的工艺研究 杨敏，江亦川，广东药学院学报，第19卷第2期 2003 * |
| 葛根黄豆苷元分散片的制备及其溶出度测定 黄绮红，胡容融，广东药学院学报，第17卷第2期 2001 * |
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| CN1561989A (en) | 2005-01-12 |
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Effective date of registration: 20090508 Address after: No. 530 telecommunication Road, Fushan District, Shandong, Yantai Patentee after: Yantai Dayang Pharmaceutical Co., Ltd. Address before: No. 109, Dongguan East Street, Lixia District, Shandong, Ji'nan Patentee before: Shao Aixia |
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Address after: 250100 innovation building, No. 509, Hualong Road, Licheng District, Shandong, Ji'nan 202 Patentee after: Shao Aixia Address before: 250013 No. 109 East Street, Lixia District, Shandong, Ji'nan Patentee before: Shao Aixia |
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Granted publication date: 20070912 Termination date: 20130316 |