CN1698591A - Ginger phenols extract microcapsule and preparation method thereof - Google Patents
Ginger phenols extract microcapsule and preparation method thereof Download PDFInfo
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- CN1698591A CN1698591A CN 200510078463 CN200510078463A CN1698591A CN 1698591 A CN1698591 A CN 1698591A CN 200510078463 CN200510078463 CN 200510078463 CN 200510078463 A CN200510078463 A CN 200510078463A CN 1698591 A CN1698591 A CN 1698591A
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Abstract
Disclosed is a ginger phenols extract microcapsule wherein the gingerol extract is bundled in a microcapsule, the microcapsule makes the semi-liquid state gingerol extract exist in the state of solid particles, and increases the constancy of the gingerol extract. The invention also provides the process for preparing the gingerol extract microcapsule.
Description
Technical field
The present invention relates to biomedicine field, particularly a kind of ginger phenols extract microcapsule and preparation method thereof.
Background technology
Rhizoma Zingiberis Recens is China's Chinese medicine, also is China's seasoning good merchantable brand commonly used, and the effect of the cold expelling that induces sweat, warming middle-JIAO to arrest vomiting, preventing phlegm from forming and stopping coughing is arranged.The medicinal ingredient of Rhizoma Zingiberis Recens can prepare by vapor distillation or solvent extraction (comprising supercritical extraction) (Yu Zhen etc. the pungency component analysis of Rhizoma Zingiberis Recens. unming Medical College's journal, 2001, (4): 57-60; Wang Fasong etc. the molecular distillation purification and the chemical composition analysis of oil of ginger. Chinese Journal of Pharmaceuticals, 2003,34 (3): 125-127; Zhou Xiaodong. supercritical CO
2The research of extraction Rhizoma Zingiberis Recens characteristic component oil of ginger. meticulous and specialty chemicals, 2004,12 (9): 13-15.).Ginger phenols extract refer to contain phenols component and with phenols component as medicinal Rhizoma Zingiberis Recens extract, it is to separate the effective site composition that obtains from the bright rhizome of Rhizoma Zingiberis Recens, have anti-kinetosis (motion sickness) effects such as stronger resisting swooned, emesis, can be prepared into Chinese medicinal soft capsule after it is dissolved in an amount of vegetable oil, carry out the new drug registration in national drug administration section at present.The ginger phenols extract ingredient is complicated, wherein to contain the 6-gingerol and the 6-shogaol is more.Can extract with modern supercritical extraction technique and to obtain the ginger phenols extract that phenols component accounts for more than 20% even accounts for (wherein based on gingerol compounds such as 6-gingerols) more than 50%, its outward appearance is brown or the sepia semiliquid, viscosity is bigger, the fragrance that Rhizoma Zingiberis Recens is arranged, acrid in the mouth is peppery, very easily is dissolved in ethanol, ethyl acetate, ether, and is water insoluble, need be airtight, the moistureproof storage.Its general leaching process is to pulverize after getting the Rhizoma Zingiberis Recens chip drying, and CO packs into
2In the supercritical extraction unit, under appropraite condition, extract, obtain the ginger phenols extract of semi liquid state.
Because ginger phenols extract is semi liquid state, wherein volatile ingredient is more volatile again, so its dosage form has only been selected soft capsule at present, is after ginger phenols extract is in harmonious proportion with an amount of vegetable oil dissolving, to prepare soft capsule with gelatin.Ginger phenols extract is prepared into soft capsule dosage form has following defective: (1) ginger phenols extract raw material is volatile and rotten, therefore in storage, transportation and the preparation of raw material are produced, must be noted that environment, prevents its rotten and volatilization; (2) the soft capsule volume is big slightly, takies than large space; (3) soft capsule easily squeezes and breaks, and gives and transports, preserves, carries and take certain problem of bringing; (4) after soft capsule is taken, discharge than heavy wool and ginger phenols extract in stomach, certain zest is arranged; (5) can only orally use.Therefore need to consider to change the dosage form of present ginger phenols extract.
Microcapsule (Microcapsule) is to adopt filmogen (common name capsule material) that solid, liquid or gas isoreactivity material (the common name capsule heart) are wrapped synthetic fine particle.The particle diameter of microcapsule is generally at micrometer range, and is bigger in the millimeter scope, less in nanometer range (claiming nanocapsule this moment).After the medicament microcapsuleization (Microcapsulation), generally form flowable powder, can further be made into dosage forms such as powder, tablet, granule, capsule and injection.The advantage of medicament microcapsuleization comprises: (1) improves stability of drug, and the factors such as air, moisture, light that prevent cause the variation of medicine; (2) cover the bad smell and the taste of medicine; (3) prevent medicine inactivation under the effect of gastric acid, reduce the stimulation of medicine simultaneously stomach; (4) it is solid-state liquid drug to be changed into, is convenient to store, transports and uses; (5) interaction of minimizing compound medicine and compatibility change; (6) give medicament slow release, controlled release and Targeting Performance (Bi Dianzhou. pharmaceutics. the 4th edition. Beijing: the People's Health Publisher, 1999,121-140).
Yet there are no product or report that the bigger semi liquid state medication preparation of viscosity becomes microcapsule.
The capsule material of microcapsule is the important materials of preparation microcapsule.The capsule material should possess stable in properties, suitable rate of releasing drug is arranged, nontoxic nonirritant, can with conditions such as compatibility of drugs.The capsule material mostly is natural, semi-synthetic or synthesized polymer material.According to solubility property, the capsule material can also be divided into water solublity capsule material, water-insoluble capsule material and enteric solubility capsule material etc.The method of making microcapsule is a lot, generally decides according to the granularity and the Release Performance of pharmaceutical properties and required microcapsule.At present the microencapsulation method can be divided into three major types by its preparation principle, i.e. chemical method, physical-chemical process and physical mechanical method also have some microcapsule process may relate to two or more methods or certainly between two methods.Microcapsule can be spheroidal, similar round or irregular shape (Tu Xide etc. pharmaceutics. the third edition. Beijing: the People's Health Publisher, 2002,1025-1051).
Microcapsule can further be prepared into various dosage forms according to its material difference and instructions for use, comprise powder, tablet (He Wen etc. the development of vitamin E microcapsule sheet and quality investigation thereof. the Chinese Hospitals pharmaceutical journal, 2002,22 (11): 669-672), capsule (Tang Huaqin etc. the development of fish oil microcapsule capsule. the Chinese Hospitals pharmaceutical journal, 1998,18 (1): 25-27), suspensoid, dry suspension (cold sun etc. the exploitation of pesticide encapsulated form and present situation. pesticide science and management, 2003,24 (3): 34-37), injection (Lou Yuefen etc. the preparation Chinese Journal of Pharmaceuticals of Oleum Curcumae microcapsule suppository, 2003,34 (8): 391-392; Liu's plinth, Lu Bin. the research of Norgestrel Compound slow-releasing microcapsule injection. Chinese Journal of Pharmaceuticals, 1994,25 (11): 494-497), ointment (in west congruence. the research that the preparation of gentamycin sulfate microcapsule cream and transdermal test in vitro absorb. the pharmacy practice magazine, 1998,16 (4): 216-218), suppository (Liu Dong etc. the pharmacokinetics of ciclosporin A microcapsule suppository in the rabbit body. Chinese Hospitals pharmaceutical journal, 2003,23 (2): 87-89), gel etc.
Summary of the invention
The invention provides a kind of ginger phenols extract microcapsule, feature is that ginger phenols extract is wrapped in the microcapsule.It has the unexistent many advantages of its soft capsule dosage form in the past, as the semi liquid state ginger phenols extract solid powdering that viscosity is bigger, helps storing, transports and further be prepared into various dosage forms; Increased the stability of ginger phenols extract; Minimizing ginger phenols extract etc. stimulates gastrointestinal; Dosage is more even; The inside and outside of selecting to control ginger phenols extract behind the suitable capsule material discharges.This microcapsule makes the ginger phenols extract of semi liquid state exist with the solid particle state, and has increased the stability of ginger phenols extract.
Be used to prepare the ginger phenols extract raw material of ginger phenols extract microcapsule among the present invention, be meant that containing phenols component accounts for the above ginger phenols extract of 20% weight ratio, preferably phenols component accounts for the above ginger phenols extract of 50% weight ratio.Ginger phenols extract can extract from Rhizoma Zingiberis Recens by tradition or modernism and obtain, as steam distillation, solvent extraction.Be easier to extract with the supercritical extraction technique in modern times and obtain the higher ginger phenols extract of phenols component content.
The capsule material component of the ginger phenols extract microcapsule among the present invention mainly is made up of macromolecular material.Macromolecular material can be selected from one or more of natural macromolecular material, semi-synthetic macromolecular material, synthesized polymer material.Optional from gelatin, arabic gum, pectin, tara gum, elsinan, alginate, zein (zein), chitosan and derivant thereof, Pullulan, hetastarch, carboxymethyl starch, maleic acid esterification starch acrylamide acid copolymer, Lac one or more of natural macromolecular material are preferably from one or more of gelatin, arabic gum, chitosan, Pullulan.Semi-synthetic macromolecular material can be selected from one or more of carboxymethyl cellulose salt, cellulose acetate butyrate, cellulose acetate phthalate ester (cellulose acetate phthalate), celluloid, methylcellulose, ethyl cellulose, hypromellose, hypromellose phthalate ester (Hydroxypropyl methyl cellulose phtalate), Hydroxypropyl Methyl Cellulose Phthalate, preferably from one or more of cellulose acetate phthalate ester, methylcellulose, ethyl cellulose, hypromellose phthalate ester, Hydroxypropyl Methyl Cellulose Phthalate.The optional autohemagglutination carbon of synthesized polymer material ester, polyamino acid, polylactic acid, polyacrylic resin, polymethyl methacrylate, poly hydroxy ethyl acrylate, paracyanogen base alkyl acrylate, Vicryl Rapide, polyvinyl alcohol, polyvinylpyrrolidone, polyamide, PLEG, caprolactone and lactide block copolymer, one or more of polymeric anhydride and Sensor Chip CM 5 are preferably from polyamino acid, polylactic acid, polyacrylic resin, polymethyl methacrylate, poly hydroxy ethyl acrylate, paracyanogen base alkyl acrylate, Vicryl Rapide, polyvinyl alcohol, one or more of polymeric anhydride.
For improving the character of ginger phenols extract microcapsule, can also in the capsule material, add various additives.Additive can be selected from one or more of paraffin, Brazil wax, spermaceti, Cera Flava, stearic acid, octadecanol, hexadecanol, tristerin, Pulvis Talci, magnesium stearate, titanium dioxide, silica gel, surfactant.
The general step of ginger phenols extract microcapsule preparation method is that ginger phenols extract is dissolved in an amount of solvent, and then adopts conventional method to prepare ginger phenols extract microcapsule.Solvent can be selected from one or more in ethanol, acetone, ethylene glycol, propylene glycol, glycerol, ether, dichloromethane, liquid paraffin, the vegetable oil, preferably ethanol, acetone, vegetable oil.Above-mentioned conventional method comprises chemical method, physical-chemical process and physical mechanical method, also can be with two or more methods in conjunction with enforcement.Chemical method can be selected from interfacial polymerization, interface composite algorithm, chemical radiation.Optional self-coagulation method of physical-chemical process and intra-liquid desiccation method.The physical mechanical method comprises spray drying method, congealing spray, air suspension coating, electrostatic deposition, vacuum coating method and porous centrifuging.In the said method, can adopt as long as be fit to the method for ginger phenols extract microcapsule preparation, concrete grammar requires to design according to capsule wood property matter and microcapsule.If obtain microcapsule is the pastel that wets, and can adopt that room temperature is dried, heat drying, drying under reduced pressure or lyophilization, obtains powdered granule at last.
Ginger phenols extract microcapsule preparation method based on above-mentioned preparation method all belongs to scope of the present invention.
Ginger phenols extract microcapsule among the present invention, its particle diameter are less than 2 millimeters, preferably less than 0.5 millimeter, more preferably less than 0.05 millimeter.
Ginger phenols extract microcapsule among the present invention can further be prepared into powder, tablet, capsule, suspensoid, dry suspension, injection, ointment, suppository, and concrete preparation prescription and technology can be with reference to the pharmaceutics professional books.
Description of drawings
Fig. 1 ginger phenols extract gelatin microcapsule microphotograph (* 400 times)
Fig. 2 ginger phenols extract hypromellose phthalate ester microcapsule microphotograph (* 400 times)
The specific embodiment
Embodiment 1. ginger phenols extract gelatin microcapsules
At first prepare ginger phenols extract.Pulverize after getting 50 kilograms of clean Rhizoma Zingiberis Recens chip dryings, CO packs into
2In the supercritical extraction unit, extract under appropraite condition, obtain the bigger semi liquid state ginger phenols extract of viscosity, total phenols weight ratio wherein accounts for more than 58%, and 6-gingerol weight ratio accounts for more than 16%.
Get ginger phenols extract 0.2g and add Semen Maydis oil 0.5g dissolving, add 10% gelatin 10ml then, homogenate becomes Emulsion, adds the dilution of 20ml water, regulates pH to 3.5 with 10% acetum, puts into 50 ℃ of stirred in water bath.30% metabisulfite solution 25ml of 0 ℃ of Dropwise 5 in the Emulsion that is stirring, stir about 30min, the 75ml water that adds 50 ℃ again, be cooled to 15 ℃ then, the 21.5% metabisulfite solution 100ml that adds 15 ℃, stir, produce a large amount of floccules, add 2.5ml formaldehyde, after stirring 10min, NaOH solution with 1mol/l is regulated pH to 8.0, continues to stir 30min, filters, water, acetone, water washs in proper order, the semi liquid state pastel that obtains carries out vacuum drying, or carries out lyophilization after adding an amount of mannitol solution, and obtaining pale yellow powder shape solid at last promptly is the ginger phenols extract gelatin microcapsule.
After getting above-mentioned ginger phenols extract gelatin microcapsule and disperseing with low amounts of water, examine under a microscope, find that microcapsule becomes spheroidal, most of particle diameter is below 50 microns (0.05 millimeters), and its microphotograph is seen Fig. 1.
Fig. 1 ginger phenols extract gelatin microcapsule microphotograph (* 400 times)
Embodiment 2. ginger phenols extract hypromellose phthalate ester microcapsules
Get ginger phenols extract 0.2g and add ethanol 1ml dissolving.Get 0.4g Na
2HPO
4.12H
2O is dissolved in the 10ml water, adds 0.5g hypromellose phthalate ester (HP55), and stirring makes molten entirely.In HP55 solution, add the 0.1g polysorbas20, under agitation add above-mentioned ginger phenols extract alcoholic solution then, stir into breast, add 6ml 20% metabisulfite solution, in stirred in water bath, and the bath temperature to 50 ℃ of raising gradually, produce yellow floccule, behind the stirring 10min, leave standstill a moment, make the floccule precipitation, inclining supernatant.The residue precipitation is divided three washings with 30ml 8.5% metabisulfite solution (50 ℃), adding 10ml 5% acetum stirring 10min in the last precipitation again solidifies microcapsule, reuse 30ml dilute acetic acid solution washing three times, filter, washing, the semi liquid state pastel that obtains carries out vacuum drying, or carries out lyophilization after adding an amount of mannitol solution, and obtaining pale yellow powder shape solid at last promptly is ginger phenols extract hypromellose phthalate ester microcapsule.
After getting above-mentioned ginger phenols extract hypromellose phthalate ester microcapsule and disperseing with low amounts of water, examine under a microscope, find that microcapsule becomes spheroidal, most of particle diameter is below 50 microns (0.05 millimeters), and its microphotograph is seen Fig. 2.
This microcapsule does not dissolve in simulated gastric fluid, does not discharge ginger phenols extract, but microcapsule dissolving in simulated intestinal fluid discharges ginger phenols extract.
Fig. 2 ginger phenols extract hypromellose phthalate ester microcapsule microphotograph (* 400 times)
Embodiment 3. ginger phenols extract microcapsule sheets
The ginger phenols extract microcapsule tablet recipe
Component content
Ginger phenols extract gelatin microcapsule 5g
Microcrystalline Cellulose 40g
Magnesium stearate 1g
Preparation technology: ginger phenols extract gelatin microcapsule and the microcrystalline Cellulose got among the embodiment 1 mix, and cross 30 mesh sieve mixings, again with Pulvis Talci and magnesium stearate mixing, use the 11mm stamping, unilateral bright and clean, the about 2～4kg of hardness, every contains the about 50mg of ginger phenols extract gelatin microcapsule.
Embodiment 4. ginger phenols extract microcapsule capsules
Ginger phenols extract microcapsule capsule prescription
Component content
Ginger phenols extract hypromellose phthalate ester microcapsule 10g
Starch 15g
Sucrose 5g
Hypromellose is an amount of
Magnesium stearate 1g
Preparation technology: get starch and cane sugar powder and be prepared into 40 order granules with 2% hypromellose aqueous solution, and granule mixed with ginger phenols extract hypromellose phthalate ester microcapsule among the embodiment 2, cross 30 mesh sieve mixings, again with the magnesium stearate mixing, the filling hard capsule, every capsules contains ginger phenols extract hypromellose phthalate ester microcapsule 100mg approximately.
Claims (10)
1. a ginger phenols extract microcapsule is characterized in that ginger phenols extract is wrapped in the microcapsule.
2. ginger phenols extract microcapsule as claimed in claim 1 is characterized in that the phenols component weight ratio in the ginger phenols extract raw material accounts for more than 20%.
3. ginger phenols extract microcapsule as claimed in claim 1 is characterized in that the phenols component weight ratio in the ginger phenols extract raw material accounts for more than 50%.
4. ginger phenols extract microcapsule as claimed in claim 1 is characterized in that the capsule material component is selected from one or more in natural macromolecular material, semi-synthetic macromolecular material, the synthesized polymer material.
5. ginger phenols extract microcapsule as claimed in claim 1, the natural macromolecular material that it is characterized in that the capsule material component is selected from one or more in gelatin, arabic gum, chitosan, the Pullulan.
6. ginger phenols extract microcapsule as claimed in claim 1, the semi-synthetic macromolecular material that it is characterized in that the capsule material component is selected from one or more in cellulose acetate phthalate ester, methylcellulose, ethyl cellulose, hypromellose phthalate ester, the Hydroxypropyl Methyl Cellulose Phthalate.
7. ginger phenols extract microcapsule as claimed in claim 1, the synthesized polymer material that it is characterized in that the capsule material component is selected from one or more in polyamino acid, polylactic acid, polyacrylic resin, polymethyl methacrylate, poly hydroxy ethyl acrylate, paracyanogen base alkyl acrylate, Vicryl Rapide, polyvinyl alcohol, the polymeric anhydride.
8. ginger phenols extract microcapsule as claimed in claim 1 is with its powder that is prepared into, tablet, capsule, suspensoid, dry suspension, injection, ointment, suppository.
9. the preparation method of the described ginger phenols extract microcapsule of claim 1 is characterized in that ginger phenols extract is dissolved in an amount of solvent, and then adopts conventional method to prepare ginger phenols extract microcapsule.
10. ginger phenols extract microcapsule preparation method as claimed in claim 9 is characterized in that the solvent that adopts is selected from one or more in ethanol, acetone, ethylene glycol, propylene glycol, glycerol, ether, dichloromethane, liquid paraffin, the vegetable oil.
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102489229A (en) * | 2011-12-06 | 2012-06-13 | 刘�东 | Core-shell nano particle for covering plant extractive and preparation method thereof |
| CN102680637A (en) * | 2012-06-08 | 2012-09-19 | 桂林三金药业股份有限公司 | Quality detection method of gingerol type extract |
| CN103405400A (en) * | 2013-08-30 | 2013-11-27 | 孙威 | Levosulpiride injection and preparation method thereof |
| CN105326803A (en) * | 2015-12-05 | 2016-02-17 | 翔宇药业股份有限公司 | Difenidol hydrochloride tablets for treating motion sickness and preparation method thereof |
| CN111990513A (en) * | 2020-09-08 | 2020-11-27 | 桂林丰润莱生物科技股份有限公司 | Sweet tea suitable for diabetics to drink |
-
2005
- 2005-06-20 CN CN 200510078463 patent/CN1698591A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102489229A (en) * | 2011-12-06 | 2012-06-13 | 刘�东 | Core-shell nano particle for covering plant extractive and preparation method thereof |
| CN102489229B (en) * | 2011-12-06 | 2014-02-12 | 刘�东 | Core-shell nano particle for covering plant extractive and preparation method thereof |
| CN102680637A (en) * | 2012-06-08 | 2012-09-19 | 桂林三金药业股份有限公司 | Quality detection method of gingerol type extract |
| CN103405400A (en) * | 2013-08-30 | 2013-11-27 | 孙威 | Levosulpiride injection and preparation method thereof |
| CN105326803A (en) * | 2015-12-05 | 2016-02-17 | 翔宇药业股份有限公司 | Difenidol hydrochloride tablets for treating motion sickness and preparation method thereof |
| CN111990513A (en) * | 2020-09-08 | 2020-11-27 | 桂林丰润莱生物科技股份有限公司 | Sweet tea suitable for diabetics to drink |
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