CN102641311A - Kiwi fruit seed oil liposome oral liquid and preparation method thereof - Google Patents
Kiwi fruit seed oil liposome oral liquid and preparation method thereof Download PDFInfo
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Abstract
The invention discloses a kiwi fruit seed oil liposome oral liquid and a preparation method thereof. The method comprises the following steps: (1) adding a phosphate buffer solution with pH of 6.8 in a constant temperature oscillator, heating in a water bath to 60 DEG C and keeping constant temperature; (2) based on anhydrous ethanol as a solvent, preparing a mixed solution containing15-25mg/ml of lecithin, 5-20mg/ml of cholesterol and 5-20mg/ml of kiwi fruit seed oil; and (3) injecting the mixed solution in the step (2) into the phosphate buffer solution in the step (1), placing in the constant-temperature water bath at the temperature of 60 DEG C, then performing ultrasonic treatment, adding distilled water to a certain volume, sealing and sterilizing to obtain the kiwi fruit seed oil liposome oral liquid. According to the kiwi fruit seed oil liposome oral liquid prepared by the method disclosed by the invention, kiwi fruit seed oil has high stability and safety, unsaturated fatty acid in the kiwi fruit seed oil can be prevented from being oxidized, and the purposes of convenience in transportation and long-term preservation can be further achieved.
Description
Technical field
The invention belongs to the health-care preparation field, be specifically related to a kind of Chinese gooseberry seed oil liposome oral fluid and preparation method thereof.
Background technology
Fructus actinidiae chinensis (
Actinidia chinensis) having another name called carambola, Fructus actinidiae chinensis, XIANTAO, Radix Fici Hirtae etc., New Zealand Mi base dimension fruit (kiwifruit) is a kind of liana, is one of precious fruit of China's special product.Along with the development of Fructus actinidiae chinensis processing industry, the fruit level of residue increases.Mainly fruit crude fibre and seed in the Fructus actinidiae chinensis residue.These factories produce a large amount of marcs in the processing process, wherein contain a large amount of Fructus actinidiae chinensis seed seeds.According to yellow notable big grade (Huang Zhuowei, Yi Minghua. Chinese gooseberry seed refines the research [J] of high-quality edible oil. oil and foodstuffs science and technology, 1992, (4): 11 ~ 12) report, more than 250 at least of the seed in each Fructus actinidiae chinensis wild fruit, grain surplus in the of 800 nearly, average about 500.Through measuring, oil content is 28.85% in the seed, in the Chinese gooseberry seed oil unsaturated fatty acid content up to 90.37%, wherein linoleic acid, Caulis et Folium Lini
Acid content accounts for 74.83%; The zoopery result shows that Chinese gooseberry seed oil has tangible effect for reducing blood fat, oral safety non-toxic.Yao Maojun (Yao Maojun, Li Jiaxing, Zhang Yongkang. [J] inquired in the development and use of Chinese gooseberry seed oil. food and fermentation industries; 2001,27 (12): 28 ~ 30 ,] Yao Maojun; Li Jiaxing, Zhang Yongkang. Chinese gooseberry seed oil physicochemical property and fatty acid are formed [J]. Wuxi Light Industry Univ.'s journal, 2002; 2 (3): 307 ~ 309), Zhang Yongkang (Zhang Yongkang, Jiang Jianbo, Chen Lihua. the mensuration of kiwifruit nut fatty acid oil and utilization thereof [J]. University Of Jishou's journal (natural science edition); 37 ~ 38,82) etc. 2001,22 (4): the seed of having studied the western Hunan, Hunan " Mi Liangyi number " Fructus actinidiae chinensis; Find that oil content is 23.5%, the gas Chromatographic Determination fatty acid is formed, and the a-linolenic acid content is up to 63.99%.Therefore Chinese gooseberry seed oil can be used as the oily resource of important health care of replenishing unsaturated fatty acid and develops.
Containing linolenic acid and linoleic acid in the monkey peach seed oil, is the highest crude vegetal of finding at present of linolenic acid content except that Fructus Perillae oil.Linoleic acid plus linolenic acid is two kinds of essential fatty acid to the health particular importance, can only be from external world picked-up and can not be synthetic voluntarily in human body.Alpha-linolenic acid is the precursor substance of EPA and DHA, thereby Chinese gooseberry seed oil has blood fat reducing, cholesterol and blood pressure, and angiocardiopathy preventing suppresses platelet aggregation, prevents thrombosis, prevents that cancer from multiple effects such as antioxidation and slow down aging taking place.So Chinese gooseberry seed oil is the raw material of a kind of fine functional food, medicine and cosmetics.
But content has brought problem for greasy preservation up to 90% unsaturated fatty acid in the Chinese gooseberry seed oil.Monounsaturated fatty acid molecule contains a plurality of pairs of keys, thus to oxygen, light and thermoae be responsive, oxidation deterioration very easily.Greasy oxidation not only makes it lose due health protection function, but also can produce some harmful materials.
Liposome (liposome) is a kind of a kind of lipoid spherula that is made up of phospholipid that Bangham found in nineteen sixty-five.It is the miniature spheroid (Bangham ad.difusion of univalent ions aeross the lamellae of swollen Phosphlipids [J] .Mol. Biol, 1965 13:238 ~ 252.) that drug encapsulation is processed in the thin film that lipid (phospholipid and cholesterol) bilayer forms.Seal fat-soluble and water soluble drug inside and outside the bilayer respectively, its physicochemical property and similar cell membrane are called artificial membrane again.Liposome receives much concern as a kind of functional component preparation of novelty, and in recent years, Liposomal formulation research obtains very great development with application.The effect characteristics of Liposomal formulation mainly contain (Lu Bin. novel pharmaceutical formulation and new technique [M]. second edition. Beijing: People's Health Publisher, 2005.5):
(l) the defencive function composition improves stability
Some unsettled functional components can be received the protection of liposome duplicature by after liposomal encapsulated: the functional component that is wrapped is not destroyed by enzyme and immune system in vivo in the transport process.
(2) reduce functional component toxicity
Liposome itself is to human non-toxic, and the functional component back cumulant specific ionization functional component in the heart, kidney that is wrapped is low, the heart, the virose functional component of kidney are sealed liposome after, can obviously reduce toxicity.
(3) slow releasing function
The rate of release of control functional component reaches long-acting slow-release.
(4) targeting property
By reticuloendothelial system phagocytic, functional component is mainly accumulated in histoorgans such as liver, spleen, lung and bone marrow after getting in the body, realized the passive target administration.
Liposome is used ripe in pharmaceuticals industry, but still belongs to the starting stage at field of food.Liposome through the coating of phospholipid, both can improve the stability of embedding substance as a good carrier, made it have the target same sex again, can improve the bioavailability of functional component.At present, the method for preparing of liposome and example thereof are following:
1. mechanical dispersion method (mechanical dispersion) normally is dissolved in lipid in the organic solvent earlier; The decompression rotary evaporation makes it to form uniform lipid film at the inwall of glass container, adds aqueous media then and lipid is disperseed and the formation liposome through jolting.For example silybin oil lipidosome preparation: recipe quantity lecithin, cholesterol, Herba Silybi mariani oil are dissolved in the 5ml chloroform; Evaporated under reduced pressure organic solvent on Rotary Evaporators; After reaching colloidal state, add the PBS (PBS) of an amount of volume, in 35 ℃ of extremely complete aquations of constant temperature water bath vibration; With 0.45 μ m filtering with microporous membrane 3 times, promptly get.It is comparatively general to adopt the method to prepare liposome, but organic reagents such as employing chloroform, toxicity is big, is not suitable for field of food.
2. solvent dispersion method
Solvent dispersion method (solvent dispersion) is earlier lipid to be dissolved in the organic solvent, joins the aqueous phase that contains the medicine that is wrapped again, and phospholipid is arranged with monolayer (being the half the of liposome bimolecular tunic) on organic facies and water interface.
The for example preparation of tea tree oil liposome: take by weighing the lecithin, cholesterol, tea tree oil, VE, sodium deoxycholate, tween 80 of recipe quantity etc., ultrasonic even to wherein adding an amount of dehydrated alcohol to suspension, the lipoid suspension; Hydration medium places on the constant temperature blender with magnetic force to keep the temperature and the mixing speed of regulation.The lipoid suspension is slowly splashed in the hydration medium, get liposome suspension (wherein alcoholic acid volume fraction is 10%) just, this first suspension is placed ultrasonic 20 min of water-bath type Ultrasound Instrument, promptly get the tea tree oil liposome suspension.The mass concentration of lecithin is 10 gL
-1, lecithin and cholesterol mass ratio be that the mass concentration of 5:1, tea tree oil is 1.0 gL
-1, VE mass concentration be 1.0 gL
-1, sodium deoxycholate mass concentration be 0.5 gL
-1, tween 80 mass concentration be 4.0 gL
-1, aqueous media is that pH value is 6.8 PBS buffer solution.It is less to take the method to prepare the case of liposome, mainly be because technological parameter must be controlled accurately, otherwise the liposome that makes is unstable.
To the characteristics of the easy oxidation of Chinese gooseberry seed oil, employing spray drying methods such as Feng Weihua carry out Research of Microencapsulation (research of Chinese gooseberry seed oil microencapsulation technology, EI, 2004,20 (1) 234 ~ 236) to Chinese gooseberry seed oil.Yao Maojun etc. have prepared Soft Capsules of Kiwifruit Seed Oil (research of kiwifruit oil soft capsule, fermentation and food industry, 29 (12): 2003,58 ~ 61).Spray drying method still needs higher temperature (180 ℃ of air inlets, 80 ℃ of air outlets), therefore Chinese gooseberry seed oil is had loss.The public reported that preparation Chinese gooseberry seed oil lipidosome is not arranged at present as yet.
Summary of the invention
Technical problem to be solved by this invention provides a kind of Chinese gooseberry seed oil liposome oral fluid and preparation method thereof; The Chinese gooseberry seed oil liposome oral fluid for preparing with the inventive method; Chinese gooseberry seed oil stability high; Safety has avoided the unsaturated fatty acid in the Chinese gooseberry seed oil oxidized, thereby reaches the purpose of convenient transportation and long-term preservation.
Technical scheme provided by the invention is: a kind of method for preparing of Chinese gooseberry seed oil liposome oral fluid, this method comprises the steps:
(1) measure phosphate buffer and place constant temperature oscillator, heating in water bath is to 55-65 ℃, and maintenance constant temperature;
(2) with the dehydrated alcohol be solvent, compound concentration is the lecithin of 15-25 mg/ml, the cholesterol of 5 ~ 20mg/ml, the Chinese gooseberry seed oil mixed solution of 5 ~ 20mg/ml respectively;
(3) with being injected in the phosphate buffer in the step (1) behind three kinds of solution mix homogeneously described in the step (2); In water bath with thermostatic control 20-40min; Remove residual ethanol, carry out supersound process 20-40min, adding distil water standardize solution then; Sealing promptly gets Chinese gooseberry seed oil lipidosome oral administration solution after the sterilization.
Described method for preparing, preferably, in the step (1), the phosphate buffer of measuring pH6.8 places constant temperature oscillator, heating in water bath to 60 ℃, and under the 150r/min rotating speed, keep constant temperature; In the step (3),, remove residual ethanol, carry out supersound process 30min (ultrasonic power 80W) then in 60 ℃ of water bath with thermostatic control 30min, the adding distil water standardize solution, sealing promptly gets Chinese gooseberry seed oil lipidosome oral administration solution after the sterilization.
Described method for preparing, preferably, in the step (1), preparation lecithin soln concentration is 20mg/ml; After three kinds of solution mixed in the step (3), the lecithin wherein and the mass ratio of cholesterol were 2:1, and the mass ratio of lecithin and Chinese gooseberry seed oil is 4:1.。
Described method for preparing, preferably, in the step (3), 60 ℃ of water bath with thermostatic control 30min, most residual ethanol is waved in evaporation, carries out supersound process then, and 30min, ultrasonic power are 80W.
Method of the present invention preferably adopts Hunan Laodie Agricultural Technology Development Co., Ltd. that Chinese gooseberry seed oil is provided, and for example batch number is 20111230.
The present invention also provides the Chinese gooseberry seed oil that is prepared by above-mentioned method for preparing liposome oral fluid.
The present invention has following beneficial effect:
Chinese gooseberry seed oil is the important component that the Chinese gooseberry seed used always utilizes; Because its contained linolenic health-care effect; Improve the stability of Chinese gooseberry seed oil, realize linolenic targeted in the Chinese gooseberry seed oil, improve its absorption and utilize the focus that has become domestic and international research.Macaque seed oil is insoluble in water, and oral administration biaavailability is low, has limited its clinical efficacy greatly; Because linolenic the containing up to more than 60% in the Chinese gooseberry seed oil, oxidized extremely easily, the present invention combines the targeting property and the slow-releasing of liposome; Chinese gooseberry seed oil is prepared into the liposome oral administration solution; Can improve Chinese gooseberry seed oil stability, safety avoids the unsaturated fatty acid in the Chinese gooseberry seed oil oxidized; And can realize the targeting transportation of Chinese gooseberry seed oil, reach the effect that improves the Chinese gooseberry seed oil absorption rate.Thereby reach the purpose of convenient transportation and long-term preservation, promoted the commercial value of Chinese gooseberry seed oil liposome technology.The present invention takes lower temperature, has overcome the higher shortcoming of spray drying temperature in the microencapsulation process, and simultaneously rate of release is slow than soft capsule, can be further as the raw material of slow releasing preparation.
The specific embodiment
Come further to illustrate the present invention through the detailed description of the specific embodiment below, but be not limitation of the present invention, only make example description.
Embodiment 1
1, the mensuration of Chinese gooseberry seed oil liposome encapsulation
Adopt the content of dialysis-determined by ultraviolet spectrophotometry Chinese gooseberry seed oil.Pipette 20ml Chinese gooseberry seed oil lipidosome and put into bag filter, behind the dialysis 17h, pour solution in the bag into the 100ml volumetric flask; Selecting ethanol for use is demulsifier, in conjunction with ultrasonic, adds Petroleum ether extraction; Mixed solution carried out centrifugal (3000r/min 3min), gets the 10ml supernatant in the 25ml volumetric flask; Use the petroleum ether standardize solution, measure its absorbance A at the 233nm place
1; Measure the blank liposome absorbance A with method
0, calculate △ A, obtain the content of the Chinese gooseberry seed oil of sealing by standard curve.
Envelop rate %=△ A*100/A
1
2, prescription and optimal process
The key problem in technology of liposome oral administration solution is the preparation of liposome.With the envelop rate is index, and the mass ratio (L:O) of the mass ratio (L:C) of lecithin and cholesterol, lecithin and oil, water-bath time (t), heating-up temperature four factors such as (T) are to sealing the influence of effect in the investigation prescription.According to the single factor experiment result, select L9 (4 for use
3) orthogonal table carries out liposome prescription Orthogonal Experiment and Design.
Table 1 orthogonal design factor table
Table 2 orthogonal array and L (9) 3 as a result
4
| Divide into groups | L:C(w/w) | L:O(w/w) | The water-bath time (min) | T(℃) | Envelop rate (%) |
| 1 | 1 | 1 | 1 | 1 | 36.34 |
| 2 | 1 | 2 | 2 | 2 | 38.54 |
| 3 | 1 | 3 | 3 | 3 | 45.67 |
| 4 | 2 | 1 | 2 | 3 | 74.45 |
| 5 | 2 | 2 | 3 | 1 | 65.35 |
| 6 | 2 | 3 | 1 | 2 | 66.36 |
| 7 | 3 | 1 | 3 | 2 | 50.56 |
| 8 | 3 | 2 | 1 | 3 | 45.57 |
| 9 | 3 | 3 | 2 | 1 | 55.20 |
| K1 | 40.183 | 50.783 | 49.423 | 52.297 | ? |
| K2 | 68.720 | 49.820 | 56.063 | 51.820 | ? |
| K3 | 50.443 | 55.743 | 53.860 | 55.230 | ? |
| Optimal level | 2 | 3 | 2 | 3 | ? |
| R | 28.537 | 5.923 | 6.640 | 3.410 | ? |
| Significance | *(p<0.05) | ? | ? | ? | ? |
Through intuitive analysis, can know best prescription and process conditions for therefore, the best preparation technology of Chinese gooseberry seed oil lipidosome is: 60 ℃ of the mass ratio of lecithin and cholesterol (2:1), lecithin and oily mass ratio (4:1), water-bath time 30min, heating-up temperatures.The ratio of lecithin and cholesterol has the greatest impact to what liposome formed in the prescription.
Embodiment 2
The constant-temperature shaking actuator temperature is set to 60 ℃, preheating.The phosphate buffer of accurately measuring 100mlpH6.8 places constant temperature oscillator, heating in water bath to 60 ℃, and under the 150r/min rotating speed, keep constant temperature.With the dehydrated alcohol is solvent, and preparing lecithin (LC) concentration respectively is 20mg/ml, and cholesterol (CH) concentration is 10mg/ml, and Chinese gooseberry seed oil (KFO) concentration is 15mg/ml, purity 99.0%.With evenly being injected in the phosphate buffer in the constant temperature oscillator with syringe behind each solution mix homogeneously.60 ℃ of water bath with thermostatic control 30min remove residual ethanol, supersound process 30min (ultrasonic power 80W), and adding distil water is settled to 250ml, and sealing promptly gets Chinese gooseberry seed oil lipidosome oral administration solution behind the irradiation sterilization.
Method of the present invention preferably adopts Hunan Laodie Agricultural Technology Development Co., Ltd. that Chinese gooseberry seed oil is provided, and the used batch number of present embodiment is 20111230.
Embodiment 3
Preparing lecithin (LC) concentration with ethanol respectively as solvent is 16mg/ml, and cholesterol (CH) concentration is 12mg/ml, and Chinese gooseberry seed oil (KFO) concentration is 10mg/ml, and method for preparing is with embodiment 2.
Embodiment 4
Preparing lecithin (LC) concentration with ethanol respectively as solvent is 20mg/ml, and cholesterol (CH) concentration is 20mg/ml, and Chinese gooseberry seed oil (KFO) concentration is 5mg/ml, and method for preparing is with embodiment 2.
Embodiment 5
Preparing lecithin (LC) concentration with ethanol respectively as solvent is 23mg/ml, and cholesterol (CH) concentration is 6mg/ml, and Chinese gooseberry seed oil (KFO) concentration is 18mg/ml, and method for preparing is with embodiment 2.
Claims (5)
1. the method for preparing of a Chinese gooseberry seed oil liposome oral fluid is characterized in that this method comprises the steps:
(1) measure phosphate buffer and place constant temperature oscillator, heating in water bath is to 55-65 ℃, and maintenance constant temperature;
(2) with the dehydrated alcohol be solvent, compound concentration is the lecithin soln of 15 ~ 25 mg/ml, and concentration is the cholesterol of 5 ~ 20mg/ml, and concentration is the Chinese gooseberry seed oil mixed solution of 5 ~ 20mg/ml;
(3) with being injected in the phosphate buffer in the step (1) behind three kinds of solution mix homogeneously described in the step (2); In water bath with thermostatic control 20-40min, remove residual ethanol, carry out supersound process 20-40min then; Supersound process (ultrasonic power 80W); The adding distil water standardize solution, sealing promptly gets Chinese gooseberry seed oil lipidosome oral administration solution after the sterilization.
2. method for preparing according to claim 1 is characterized in that: in the step (1), the phosphate buffer of measuring pH6.8 places constant temperature oscillator, heating in water bath to 60 ℃, and under the 150r/min rotating speed, keep constant temperature; In the step (3), in 60 ℃ of water bath with thermostatic control 30min, remove residual ethanol, carry out supersound process 30min then, ultrasonic power is 80W, the adding distil water standardize solution, and sealing promptly gets Chinese gooseberry seed oil lipidosome oral administration solution after the sterilization.
3. method for preparing according to claim 1 is characterized in that: in the step (2), preparation lecithin soln concentration is 20mg/ml.
4. according to each described method for preparing of claim 1 to 3, it is characterized in that: after three kinds of solution mixed in the step (3), the lecithin wherein and the mass ratio of cholesterol were 2:1, and the mass ratio of lecithin and Chinese gooseberry seed oil is 4:1.
5. Chinese gooseberry seed oil liposome oral fluid, it is characterized in that: it is prepared by each described method for preparing of claim 1 to 4.
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103053906A (en) * | 2013-01-20 | 2013-04-24 | 湖南奇异生物科技有限公司 | Preparation method of kiwi fruit seed oil oral emulsion |
| CN103202810A (en) * | 2013-04-01 | 2013-07-17 | 浙江中医药大学 | Chinese actinidia root polysaccharide lipidosome and preparation method thereof |
| CN107951031A (en) * | 2018-01-01 | 2018-04-24 | 王艳萍 | A kind of preparation method of pine nut oral liquid |
| CN111638188A (en) * | 2020-05-27 | 2020-09-08 | 东北农业大学 | Method for measuring entrapment rate of lipid liposome |
-
2012
- 2012-05-21 CN CN 201210157277 patent/CN102641311B/en not_active Expired - Fee Related
Non-Patent Citations (3)
| Title |
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| 冯祚臻等: "冬虫夏草多糖脂质体口服液制备工艺优选", 《中国药业》 * |
| 吴瑾瑾等: "猕猴桃根多糖脂质体包封率测定方法研究", 《中国实验方剂学杂志》 * |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103053906A (en) * | 2013-01-20 | 2013-04-24 | 湖南奇异生物科技有限公司 | Preparation method of kiwi fruit seed oil oral emulsion |
| CN103202810A (en) * | 2013-04-01 | 2013-07-17 | 浙江中医药大学 | Chinese actinidia root polysaccharide lipidosome and preparation method thereof |
| CN107951031A (en) * | 2018-01-01 | 2018-04-24 | 王艳萍 | A kind of preparation method of pine nut oral liquid |
| CN111638188A (en) * | 2020-05-27 | 2020-09-08 | 东北农业大学 | Method for measuring entrapment rate of lipid liposome |
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