CN101204392A - Self-emulsifying microemulsion daidzein oral liquid preparation composite and preparation method thereof - Google Patents
Self-emulsifying microemulsion daidzein oral liquid preparation composite and preparation method thereof Download PDFInfo
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- CN101204392A CN101204392A CNA2007101721604A CN200710172160A CN101204392A CN 101204392 A CN101204392 A CN 101204392A CN A2007101721604 A CNA2007101721604 A CN A2007101721604A CN 200710172160 A CN200710172160 A CN 200710172160A CN 101204392 A CN101204392 A CN 101204392A
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Abstract
The invention discloses an oral preparation composition of a self-emulsified daidzein and a preparation method. The composition is made up of 0.5 through 5 percent daidzein, 30 through 60 percent emulsifier, 10 through 40 percent auxiliary emulsifier and 10 through 30 percent grease. The preparation method is as follows: the daidzein is dissolved in cosurfactant under the temperature ranging from 10 DEG C to 80 DEG C, after being cooled, the daidzein is added with an oil phase and the emulsifier then is stirred uniformly. The invention has the advantages of simple operation and easy preservation. The oral preparation composition of the self-emulsified daidzein in the invention can absorb the water in human gastrointestinal tract after being taken orally, with uniform grain diameter ranging from 10nm to 100nm.
Description
Technical field
The present invention relates to self-emulsifying microemulsion oral formulations of a kind of technical field of pharmaceuticals and preparation method thereof, particularly a kind of daidzein self-emulsifying microemulsion oral formulations and preparation method thereof.
Technical background
Daidzein (daidzein) has another name called daidzein, is leguminous plant effective ingredient such as Chinese medicine Radix Puerariae and Semen Glycines, can be by chemosynthesis or Chinese medicine extraction and isolation technics preparation.Daidzein has expansion hat tremulous pulse, cerebral arteries, peripheral blood vessel and blood capillary; Increase arteria coronaria blood vessel, cerebrovascular, peripheral blood vessel, blood capillary blood flow and circulation; Anticoagulant is removed vasospasm, and cholesterol reducing and blood viscosity weaken vascular resistance; Increase myocardium shrinkage function, improve heart rate, reduce myocardial oxygen consumption, increase blood supply of cardiac muscle; β-adrenoreceptor retardance; Antioxidation, enhancing body resistance are improved the climacteric syndrome, strengthen effects such as calcareous absorption.It is mainly used in treatment hypertension, coronary heart disease and cranial nerve disease, also can be used for preventing and treating sudden deafness, treatment climacteric syndrome, prevention angina pectoris, myocardial infarction, the senile dementia of formation cerebral thrombosis, diseases such as osteoporosis.Daidzein toxicity is lower, is fit to long-term prescription.Daidzein belongs to the isoflavone structure, and poorly water-soluble is fat-soluble also undesirable, commercially available daidzein medicament only limits to oral tablet and capsule at present, absorbs slowly in the body, and bioavailability is very low, thereby influenced the curative effect performance of daidzein, limited its extensively practicality.So be necessary to adopt a kind of novel daidzein oral formulations, make things convenient for the patient.
Through the literature search of prior art is found, people such as Zhao Peng " Chinese Journal of New Drugs " (2007, delivered paper " spray drying method solidifies the research of daidzein solid lipid nanoparticle " on 16:955-958).Adopt nanotechnology that daidzein is made in this article and be used for oral solid lipid nanoparticle with the holdup time in the body that prolongs daidzein; help the raising of interior absorption of daidzein body and curative effect; and the solid lipid nanoparticle suspension is cured as redispersible drying nano grain by spray drying method, improve stability.But the shortcoming that its technology exists is that aerosol apparatus blocks easily.Spray-drying process easily produces wall sticking phenomenon.The result of sticking wall can make medicine for a long time attached to the high-temperature part of equipment, causes coking or fusion, and production can't be carried out, and causes the serious gathering of solid lipid nanoparticle simultaneously.
Summary of the invention
The present invention is directed to the deficiencies in the prior art, daidzein oral preparation composition of a kind of self-microemulsion and preparation method thereof is provided, makes it overcome the above-mentioned defective that background technology exists, the preparation of self-emulsifying microemulsion oral administration system does not need special equipment, simple to operate, and be easy to preserve.
The present invention is achieved by the following technical solutions:
The daidzein oral preparation composition of self-microemulsion involved in the present invention, its component and mass percentage content thereof are:
Daidzein 0.5%-5%
Emulsifying agent 30%-60%
Co-emulsifier 10%-40%
Oils and fats 10%-30%
Described emulsifying agent is selected from a kind of or its mixture in polyethylene glycol glycerol three esters, polyoxyethylene castor oil, polyoxyethylene hydrogenated Oleum Ricini, phospholipid, Tween 80 or the polysorbas20.
Described co-emulsifier is selected from a kind of or its mixture in ethanol, propylene glycol or the Polyethylene Glycol.
Described oils and fats is selected from a kind of or its mixture in ethyl oleate, Ethyl linoleate, Oleum Ricini, Oleum Arachidis hypogaeae semen, hydrogenated corn oil, MCT Oil or the isopropyl myristate.
The preparation method of the daidzein oral preparation composition of self-emulsifying microemulsion involved in the present invention is concrete: under 10-80 ℃ of condition temperature, according to mass percent, daidzein is dissolved in co-emulsifier earlier, after cooling, add oils and fats and emulsifying agent, stirring gets final product.The inventive method is very simple, is easy to preserve.
Take for the ease of the patient, the daidzein oral preparation composition of self-emulsifying microemulsion of the present invention can be adopted method well known in the art canned in capsule, obtain capsule; Or, adopt method well known in the art to be prepared as tablet, capsule, soft capsule, oral liquid, oral administration mixed suspension, oral gel or granule etc. with the daidzein oral preparation composition of self-emulsifying microemulsion of the present invention and medically acceptable carrier.
Described carrier is meant the pharmaceutical carrier of pharmaceutical field routine, as diluent, excipient such as water etc., filler, as starch, sucrose etc., binding agent, as cellulose derivative gelatin, polyethylene pyrrole alkane ketone etc., lubricant is as Pulvis Talci etc.
The daidzein oral preparation composition of self-microemulsion of the present invention can be applied to treat in the aspect medicines such as hypertension, coronary heart disease, angina pectoris, myocardial infarction, cerebral thrombosis, arrhythmia, cranial nerve disease, sudden deafness, osteoporosis, climacteric syndrome.
Compared with prior art, the daidzein oral preparation composition of self-emulsifying microemulsion of the present invention, after oral, absorb the interior moisture of gastrointestinal tract and carry out self-emulsifying microemulsion, formed microemulsion is a kind of transparent, low viscous, each homogeny and thermodynamically stable profit hybrid system, its particle diameter is even, is distributed between 10～100nm.The preparation of self-emulsifying microemulsion oral administration system does not need special equipment, simple to operate, and be easy to preserve, as a kind of novel medicament carrier, the present invention possesses low viscosity, stable, absorb rapidly, characteristics such as target administration, and improve the oral absorption of medicine, bioavailability of medicament is brought up to 2.5 times of contrast suspension, reduces toxic and side effects.
Description of drawings
Fig. 1 is the particle size distribution figure of daidzein microemulsion of the present invention.
Fig. 2 curve chart during for the medicine of the light water suspension of rat of the present invention oral daidzein self-emulsifying microemulsion capsule and daidzein.
The specific embodiment
Below in conjunction with accompanying drawing embodiments of the invention are elaborated: present embodiment is being to implement under the prerequisite with the technical solution of the present invention, provided detailed embodiment and concrete operating process, but protection scope of the present invention is not limited to following embodiment.
The component of the self-emulsifying composition of present embodiment and percentage by weight thereof are: daidzein 1%, emulsifying agent 60%, co-emulsifier 20%, oils and fats 19%.
Described emulsifying agent is a polyoxyethylene hydrogenated Oleum Ricini.
Described co-emulsifier is a PEG400.
Described oils and fats is an ethyl oleate.
The preparation technology of the self-emulsifying composition in the present embodiment is: under 10-80 ℃ of condition temperature, daidzein is dissolved in the PEG400 of recipe quantity earlier, after cooling, press recipe quantity and add polyoxyethylene hydrogenated Oleum Ricini and ethyl oleate, both stir can.
The beneficial effect of present embodiment is: after (1) becomes self-emulsifying composition with medication preparation, be dissolution medium with 0.1M HCl, daidzein self-emulsifying composition 30 minutes can stripping more than 80%.(2) with after 100 times of the self-emulsifying composition dilutions of preparation, the mensuration mean diameter is 21.6nm.Particle size distribution is seen accompanying drawing 1.By accompanying drawing 1 as seen, the particle diameter of this microemulsion system overwhelming majority except that the minority granule meets in the pharmaceutics requirement to microemulsion formulation at 10-100nm.(3) because particle diameter is little, medicine degree of scatter height, thus the degree of absorption of increase medicine improves bioavailability.
Embodiment 2
The component of the self-emulsifying composition of present embodiment and percentage by weight thereof are: daidzein 0.5%, emulsifying agent 55%, co-emulsifier 24.5%, oils and fats 10%.
Described emulsifying agent is a polyoxyethylene castor oil.
Described co-emulsifier is a PEG400.
Described oils and fats is an isopropyl myristate.
The preparation technology of the self-emulsifying composition in the present embodiment is: under 10-80 ℃ of condition temperature, daidzein is dissolved in the PEG400 of recipe quantity earlier, after cooling, press recipe quantity and add polyoxyethylene castor oil and isopropyl myristate, both stir can.
The beneficial effect of present embodiment is: after (1) becomes self-emulsifying composition with medication preparation, be dissolution medium with 0.1M HCl, daidzein self-emulsifying composition 30 minutes can stripping more than 80%.(2) with after 100 times of the self-emulsifying composition dilutions of preparation, particle diameter is less than 100nm.(3) because particle diameter is little, medicine degree of scatter height, thus the degree of absorption of increase medicine improves bioavailability.
Embodiment 3
The component of the self-emulsifying composition of present embodiment and percentage by weight thereof are: daidzein 0.5%, emulsifying agent 60%, co-emulsifier 20%, oils and fats 19.5%.
Described emulsifying agent is a polyoxyethylene castor oil.
Described co-emulsifier is a propylene glycol.
Described oils and fats is an isopropyl myristate.
The preparation technology of the self-emulsifying composition in the present embodiment is: under 10-80 ℃ of condition temperature, daidzein is dissolved in the propylene glycol of recipe quantity earlier, after cooling, presses recipe quantity and add polyoxyethylene castor oil and isopropyl myristate, both stir can.
The beneficial effect of present embodiment is: after (1) becomes self-emulsifying composition with medication preparation, be dissolution medium with 0.1M HCl, daidzein self-emulsifying composition 30 minutes can stripping more than 80%.(2) with after 100 times of the self-emulsifying composition dilutions of preparation, particle diameter is less than 100nm.(3) because particle diameter is little, medicine degree of scatter height, thus the degree of absorption of increase medicine improves bioavailability.
Embodiment 4
The component of the self-emulsifying composition of present embodiment and percentage by weight thereof are: daidzein 3%, emulsifying agent 40%, co-emulsifier 40%, oils and fats 17%.
Described emulsifying agent is a Tween 80.
Described co-emulsifier is a PEG400.
Described oils and fats is an ethyl oleate.
The preparation technology of the self-emulsifying composition in the present embodiment is: under 10-80 ℃ of condition temperature, daidzein is dissolved in the PEG400 of recipe quantity earlier, after cooling, presses recipe quantity and add Tween 80 and ethyl oleate, both stir can.
The beneficial effect of present embodiment is: after (1) becomes self-emulsifying composition with medication preparation, be dissolution medium with 0.1M HCl, daidzein self-emulsifying composition 30 minutes can stripping more than 80%.(2) with after 100 times of the self-emulsifying composition dilutions of preparation, particle diameter is less than 100nm.(3) because particle diameter is little, medicine degree of scatter height, thus the degree of absorption of increase medicine improves bioavailability.
The component of the self-emulsifying composition of present embodiment and percentage by weight thereof are: daidzein 5%, emulsifying agent 35%, co-emulsifier 30%, oils and fats 30%.
Described emulsifying agent is a polyoxyethylene hydrogenated Oleum Ricini.
Described co-emulsifier is a propylene glycol.
Described oils and fats is a MCT Oil.
The preparation technology of the self-emulsifying composition in the present embodiment is: under 10-80 ℃ of condition temperature, daidzein is dissolved in the propylene glycol of recipe quantity earlier, after cooling, press recipe quantity and add polyoxyethylene hydrogenated Oleum Ricini and MCT Oil, both stir can.
The beneficial effect of present embodiment is: after (1) becomes self-emulsifying composition with medication preparation, be dissolution medium with 0.1M HCl, daidzein self-emulsifying composition 30 minutes can stripping more than 80%.(2) with after 100 times of the self-emulsifying composition dilutions of preparation, particle diameter is less than 100nm.(3) because particle diameter is little, medicine degree of scatter height, thus the degree of absorption of increase medicine improves bioavailability.
Embodiment 6
Canned with the compositions daidzein oral preparation composition of embodiment 1 in No. 0 capsule.Measure capsular dissolution with reference to two appendix XC of Pharmacopoeia of the People's Republic of China version in 2005 three therapeutic methods of traditional Chinese medicine.Be dissolution medium with 900mL0.1M HCl or pH6.8PBS respectively, rotating speed is 50rpm, respectively at 5,10,15,30,45,60,90, the 120min timing sampling, and 0.45 μ m filtering with microporous membrane, ultraviolet spectrophotometer is measured daidzein concentration.
The release kilsyth basalt of daidzein self-emulsifying microemulsion capsule of the present invention in different medium sees the following form.As can be seen from the above results, the release there was no significant difference of daidzein self-emulsifying microemulsion capsule in different medium.
| Time (min) | 5 | 10 | 15 | 30 | 45 | 60 | 90 | 120 |
| ?0.1mol/L?HCl ?PH6.8?PBS | 11.08％ 5.42％ | 38.50％ 35.17％ | 52.10％ 56.80％ | 80.28％ 79.12％ | 89.48％ 85.80％ | 92.65％ 88.48％ | 93.62％ 93.40％ | 94.22％ 95.75％ |
Embodiment 7
The capsular bioavailability of daidzein self-emulsifying microemulsion of inventing in order to check has been studied the relative bioavailability of the light water suspension of rat oral daidzein self-emulsifying microemulsion capsule and daidzein, the results are shown in accompanying drawing 2.
The capsular AUC of the oral daidzein self-emulsifying microemulsion of rat is 381.17ng.hour/mL, and the AUC of the light water suspension of daidzein is 955.18ng.hour/mL, and relative bioavailability is 250.6%.This self-microemulsion is compared with common suspension as seen from Figure 3, and the Cmax of self-microemulsion is higher, and it is close with peak time that medicine is eliminated time MRT.
Claims (6)
1. the daidzein oral preparation composition of a self-microemulsion is characterized in that, component and mass percentage content thereof are:
Daidzein 0.5%-5%
Emulsifying agent 30%-60%
Co-emulsifier 10%-40%
Oils and fats 10%-30%.
2. the daidzein oral preparation composition of self-microemulsion according to claim 1, it is characterized in that described emulsifying agent is selected from a kind of or its mixture in polyethylene glycol glycerol three esters, polyoxyethylene castor oil, polyoxyethylene hydrogenated Oleum Ricini, phospholipid, Tween 80 or the polysorbas20.
3. the daidzein oral preparation composition of self-microemulsion according to claim 1 is characterized in that, described co-emulsifier is selected from a kind of or its mixture in ethanol, propylene glycol or the Polyethylene Glycol.
4. the daidzein oral preparation composition of self-microemulsion according to claim 1, it is characterized in that described oils and fats is selected from a kind of or its mixture in ethyl oleate, Ethyl linoleate, Oleum Ricini, Oleum Arachidis hypogaeae semen, hydrogenated corn oil, MCT Oil or the isopropyl myristate.
5. the daidzein oral preparation composition of self-microemulsion according to claim 1 is characterized in that, described compositions, and its particle diameter is even, is distributed between 10～100nm.
6. the preparation method of the daidzein oral preparation composition of a self-microemulsion as claimed in claim 1 is characterized in that, under 10-80 ℃ of condition temperature, by mass percentage, daidzein is dissolved in co-emulsifier earlier, after cooling, add oils and fats and emulsifying agent, stir.
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| CNA2007101721604A CN101204392A (en) | 2007-12-13 | 2007-12-13 | Self-emulsifying microemulsion daidzein oral liquid preparation composite and preparation method thereof |
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Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101632650A (en) * | 2009-07-07 | 2010-01-27 | 沈阳药科大学 | Self-microemulsifying semisolid skeleton capsule of daidzein and preparation method thereof |
| CN102008454A (en) * | 2010-12-03 | 2011-04-13 | 上海交通大学 | Daidzein-entrapped PLGA nanoparticles and preparation method thereof |
| CN102258475A (en) * | 2010-05-28 | 2011-11-30 | 中国科学院上海药物研究所 | Daidzein solid lipid nanoparticles and preparation method thereof |
| CN102475700A (en) * | 2010-11-25 | 2012-05-30 | 四川科伦药物研究有限公司 | Daidzein concentrated solution and special diluent agent thereof |
| CN102114245B (en) * | 2009-12-31 | 2012-11-07 | 四川科伦药物研究有限公司 | Special solvent for daidzein pre-emulsified injection and preparation method and purpose thereof |
| CN102114012B (en) * | 2009-12-31 | 2013-10-16 | 四川科伦药物研究有限公司 | Medicinal composition for treating heart cerebrovascular diseases as well as preparation method and application thereof |
| CN104784158A (en) * | 2015-04-03 | 2015-07-22 | 上海交通大学 | PLGA (poly (lactic-co-(glycolic) acid) electrospinning fiber loaded with daidzein NLCs (nanostructure lipid carriers) as well as preparation method |
-
2007
- 2007-12-13 CN CNA2007101721604A patent/CN101204392A/en active Pending
Cited By (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101632650A (en) * | 2009-07-07 | 2010-01-27 | 沈阳药科大学 | Self-microemulsifying semisolid skeleton capsule of daidzein and preparation method thereof |
| CN101632650B (en) * | 2009-07-07 | 2013-11-27 | 沈阳药科大学 | Self-microemulsifying semisolid skeleton capsule of daidzein and preparation method thereof |
| CN102114245B (en) * | 2009-12-31 | 2012-11-07 | 四川科伦药物研究有限公司 | Special solvent for daidzein pre-emulsified injection and preparation method and purpose thereof |
| CN102114012B (en) * | 2009-12-31 | 2013-10-16 | 四川科伦药物研究有限公司 | Medicinal composition for treating heart cerebrovascular diseases as well as preparation method and application thereof |
| CN102258475A (en) * | 2010-05-28 | 2011-11-30 | 中国科学院上海药物研究所 | Daidzein solid lipid nanoparticles and preparation method thereof |
| CN102258475B (en) * | 2010-05-28 | 2013-05-22 | 中国科学院上海药物研究所 | Daidzein solid lipid nanoparticles and preparation method thereof |
| CN102475700A (en) * | 2010-11-25 | 2012-05-30 | 四川科伦药物研究有限公司 | Daidzein concentrated solution and special diluent agent thereof |
| CN102008454A (en) * | 2010-12-03 | 2011-04-13 | 上海交通大学 | Daidzein-entrapped PLGA nanoparticles and preparation method thereof |
| CN102008454B (en) * | 2010-12-03 | 2012-07-04 | 上海交通大学 | Daidzein-entrapped PLGA nanoparticles and preparation method thereof |
| CN104784158A (en) * | 2015-04-03 | 2015-07-22 | 上海交通大学 | PLGA (poly (lactic-co-(glycolic) acid) electrospinning fiber loaded with daidzein NLCs (nanostructure lipid carriers) as well as preparation method |
| CN104784158B (en) * | 2015-04-03 | 2017-10-31 | 上海交通大学 | The PLGA Electrospuns and preparation method of Daidzein nano structured lipid carrier |
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