CN101829186B - Solid dispersant for improving dissolution of Tibet medicinal halenia extract - Google Patents
Solid dispersant for improving dissolution of Tibet medicinal halenia extract Download PDFInfo
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- CN101829186B CN101829186B CN2010101659060A CN201010165906A CN101829186B CN 101829186 B CN101829186 B CN 101829186B CN 2010101659060 A CN2010101659060 A CN 2010101659060A CN 201010165906 A CN201010165906 A CN 201010165906A CN 101829186 B CN101829186 B CN 101829186B
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Abstract
The invention relates to a solid dispersant for improving dissolution of Tibet medicinal halenia extract. The solid dispersant is prepared from water-soluble carrier and Tibet medicinal halenia extract by a conventional method. Polyethylene glycol, poloxamer, polyvidones and microcrystalline cellulose serving as carriers of the halenia extract effectively improve the dissolution (solubility) of anti-hepatitis active ingredients and demethoxyhaleniaside of the halenia extract in water and human gastric juice, so the solubility of the effective substances in the human gastric juice is improved to 85 to 90 percent from the initial about 20 percent, and the bioavailability of the anti-hepatitis active ingredients in the human body can be effectively improved.
Description
Technical field
The present invention relates to a kind of solid dispersion that improves the plant extract dissolution, relate in particular to a kind of solid dispersion that improves Tibetan medicine corniculate spurgentian herb extract dissolution.
Background technology
Solid dispersion (SD) is meant a kind of disperse system that exists with solid form that the medicine high degree of dispersion is formed in solid carrier.The particle diameter of medicine in carrier is between 0.001～0.1 millimeter, is mainly used in the stripping of quickening and increasing insoluble drug, improves its bioavailability.That the SD carrier should have is nontoxic, non-carcinogenesis, not with medicine generation chemical change, the curative effect that does not influence medicine and content detection, can make medicine obtain optimum dispersion state or slow release effect, condition such as cheap and easy to get.SD carrier commonly used can be divided into three types of water solublity, slightly solubility and enteric solubilities, and these three types of carriers can single or Combined application.Wherein water-solubility carrier comprise Polyethylene Glycol (macrogol, polyethylene glycol, PEG), poloxamer (Poloxamer), polyvidone class (PVP-k15 ,-k30) and microcrystalline Cellulose (MCC).
Oval leaf Herba Haleniae Corniculatae (Halenia elliptica D.Don) is Gentianaceae (Gentianaceae) Herba Haleniae Corniculatae platymiscium; The annual herb plant; Be a kind of in " ZANGYINCHEN " type medicinal plants, main product is distributed in China North China, northwest, each provinces and regions, southwest in the Qinghai-Tibet Platean.Herb or aerial parts are used as medicine, and its bitter in the mouth is cold in nature, has clearing heat and expelling damp, effects such as depressed liver-energy dispersing and function of gallbladder promoting, " Tibetan medicine will " record Herba Haleniae Corniculatae " heat-clearing and toxic substances removing, cooling blood for hemostasis.Treating the liver is scorching, vasculitis, trauma infection contamination fever, traumatic hemorrhage ", be usually used in treating diseases such as acute icterohepatitis, cholecystitis, dizzy headache, be one of China Tibetan, Qiang's medical herbs commonly used among the people.
The main chemical compositions of Herba Haleniae Corniculatae platymiscium is mouthful diphenylene ketone oxide (Xanthone) and mouthful diphenylene ketone oxide glycoside (Xanthoneglycosides), secoiridoid class (Secoiridoid), triterpenes (Triterpenes), flavonoid (Flavone) and some alkaloid compounds (Alkaloids) etc., from the Halenia comiculata plant extract isolation identification 15 kinds of mouth diphenylene ketone oxide and flavones ingredient.Modern pharmacology research shows that the effective ingredient of anti-hepatitis in the Herba Haleniae Corniculatae is a mouthful xanthone glycosides constituents (especially so that wherein Haleniaside (Haleniaside) and de-methoxy Haleniaside (Demethoxyhaleniaside) are main).The mouth diphenylene ketone oxide is again benzene a pair of horses going side by side chromone, and aglycon is fat-soluble to be main, behind the one-tenth glycosides; Though water solublity has improvement; But total mouth xanthone glycosides water solublity still less (dissolubility: every ml water dissolves 0.26 milligram of corniculate spurgentian herb extract, less than the prescribed limit of every milliliter of milligram), drug absorption is poor; In clinical practice, receive very big restriction, influenced the good performance and the application of medicine.
Summary of the invention
Technical problem to be solved by this invention provides that a kind of drug absorption is good, the solid dispersion of the raising Tibetan medicine corniculate spurgentian herb extract dissolution that is easy to clinical practice.
For addressing the above problem, a kind of solid dispersion that improves Tibetan medicine corniculate spurgentian herb extract dissolution of the present invention is characterized in that: this solid dispersion is processed by conventional method by water-solubility carrier and Tibetan medicine corniculate spurgentian herb extract.
Said Tibetan medicine corniculate spurgentian herb extract is meant the Tibetan medicine Halenia comiculata plant through solvent extraction, concentrated, and the Herba Haleniae Corniculatae total glycosides content that obtains after the remove impurity is 5～100% extract.
Said water-solubility carrier is a Polyethylene Glycol; The mass ratio of said Tibetan medicine corniculate spurgentian herb extract and said Polyethylene Glycol is 1: 1～6.
Said water-solubility carrier is a poloxamer; The mass ratio of said Tibetan medicine corniculate spurgentian herb extract and said poloxamer is 9～19: 1.
Said water-solubility carrier is polyvidone class and microcrystalline Cellulose; The mass ratio of said Tibetan medicine corniculate spurgentian herb extract and said polyvidone class and microcrystalline Cellulose is 95～85: 5: 0～15.
The present invention compared with prior art has the following advantages:
Because the present invention prepares the solid dispersion of corniculate spurgentian herb extract as the carrier of corniculate spurgentian herb extract with Polyethylene Glycol (PEG), poloxamer and polyvidone class (PVP), microcrystalline Cellulose (MCC); And these water-solubility carriers itself have safety non-toxic; Be easy in the human gastrointestinal tract absorb; The content analysis of interference medicament not; Can increase the dissolution rate of medicine significantly; Improve the characteristic of bioavailability of medicament, therefore, (mouth xanthone glycosides constituents---Haleniaside (Haleniaside) and de-methoxy Haleniaside (Demethoxyhaleniaside) are at the dissolution (dissolubility) of water and human gastric juice can effectively to improve anti-hepatitis effective ingredient in the corniculate spurgentian herb extract; Make the dissolubility of effective substance in simulated gastric fluid bring up to 85～90% from initial about 20%, thereby can effectively improve the bioavailability of anti-hepatitis effective ingredient at human body.
The specific embodiment
1 one kinds of solid dispersions that improve Tibetan medicine corniculate spurgentian herb extract dissolution of embodiment are made up of water-solubility carrier and Tibetan medicine corniculate spurgentian herb extract.Wherein water-solubility carrier is a Polyethylene Glycol; The Tibetan medicine corniculate spurgentian herb extract is meant the Tibetan medicine Halenia comiculata plant through solvent extraction, concentrated, and the Herba Haleniae Corniculatae total glycosides content that obtains after the remove impurity is 35% extract (method for distilling is referring to the patent No. 200410083088 " a kind of method of from Halenia comiculata plant, extracting anti-hepatitis effective ingredient "); The mass ratio of Tibetan medicine corniculate spurgentian herb extract and Polyethylene Glycol is 1: 1.
The method for preparing of this solid dispersion: at first, take by weighing Polyethylene Glycol (PEG4000) 500mg, put in the container heating and melting under 70～90 ℃ of temperature; Then, add corniculate spurgentian herb extract 500mg, after mixing, stirring, cooling rapidly, and take out behind the freezing 2h to-20 ℃ of conditions; At last, through natural drying and after grinding 80 mesh sieves, promptly obtain corniculate spurgentian herb extract--the solid dispersion of Polyethylene Glycol (PEG4000).Through test, corniculate spurgentian herb extract brings up to 65～68% at the dissolubility of simulated gastric fluid.
2 one kinds of solid dispersions that improve Tibetan medicine corniculate spurgentian herb extract dissolution of embodiment are made up of water-solubility carrier and Tibetan medicine corniculate spurgentian herb extract.Wherein water-solubility carrier is a Polyethylene Glycol, and the Herba Haleniae Corniculatae total glycosides content of Tibetan medicine corniculate spurgentian herb extract is 15% extract; The mass ratio of Tibetan medicine corniculate spurgentian herb extract and Polyethylene Glycol is 1: 6.
The method for preparing of this solid dispersion: at first, take by weighing Polyethylene Glycol (PEG4000) 3000mg, put in the container heating and melting under 70～90 ℃ of temperature; Then, add corniculate spurgentian herb extract 500mg, after mixing, stirring, cooling rapidly, and take out behind the freezing 2h to-20 ℃ of conditions; At last, through natural drying and after grinding 80 mesh sieves, promptly obtain corniculate spurgentian herb extract--the solid dispersion of Polyethylene Glycol (PEG4000).Through test, corniculate spurgentian herb extract brings up to 85～95% at the dissolubility of simulated gastric fluid.
3 one kinds of solid dispersions that improve Tibetan medicine corniculate spurgentian herb extract dissolution of embodiment are made up of water-solubility carrier and Tibetan medicine corniculate spurgentian herb extract.Wherein water-solubility carrier is a Polyethylene Glycol, and the Herba Haleniae Corniculatae total glycosides content of Tibetan medicine corniculate spurgentian herb extract is 50% extract; The mass ratio of Tibetan medicine corniculate spurgentian herb extract and Polyethylene Glycol is 1: 4.
The method for preparing of this solid dispersion: at first, take by weighing Polyethylene Glycol (PEG4000) 800mg, put in the container heating and melting under 70～90 ℃ of temperature; Then, add corniculate spurgentian herb extract 200mg, after mixing, stirring, cooling rapidly, and take out behind the freezing 2h to-20 ℃ of conditions; At last, through natural drying and after grinding 80 mesh sieves, promptly obtain corniculate spurgentian herb extract--the solid dispersion of Polyethylene Glycol (PEG4000).Through test, corniculate spurgentian herb extract brings up to 75～85% at the dissolubility of simulated gastric fluid.
4 one kinds of solid dispersions that improve Tibetan medicine corniculate spurgentian herb extract dissolution of embodiment are made up of water-solubility carrier and Tibetan medicine corniculate spurgentian herb extract.Wherein water-solubility carrier is a poloxamer, and the Herba Haleniae Corniculatae total glycosides content of Tibetan medicine corniculate spurgentian herb extract is 100% extract; The mass ratio of Tibetan medicine corniculate spurgentian herb extract and poloxamer is 9: 1.
The method for preparing of this solid dispersion: at first, take by weighing poloxamer (188) 100mg, poloxamer is dissolved in the dehydrated alcohol, then, add corniculate spurgentian herb extract 900mg, mix homogeneously; Secondly, under 70～90 ℃ of temperature, boil off dehydrated alcohol, after the natural cooling drying, promptly obtain Haleniaside--the solid dispersion of poloxamer.Through test, corniculate spurgentian herb extract brings up to 35～45% at the dissolubility of simulated gastric fluid.
5 one kinds of solid dispersions that improve Tibetan medicine corniculate spurgentian herb extract dissolution of embodiment are made up of water-solubility carrier and Tibetan medicine corniculate spurgentian herb extract.Wherein water-solubility carrier is a poloxamer, and the Herba Haleniae Corniculatae total glycosides content of Tibetan medicine corniculate spurgentian herb extract is 5% extract; The mass ratio of Tibetan medicine corniculate spurgentian herb extract and poloxamer is 19: 1.
The method for preparing of this solid dispersion: at first, take by weighing poloxamer (188) 50mg, poloxamer is dissolved in the dehydrated alcohol, then, add corniculate spurgentian herb extract 950mg, mix homogeneously; Secondly, under 70～90 ℃ of temperature, boil off dehydrated alcohol, after the natural cooling drying, promptly obtain Haleniaside--the solid dispersion of poloxamer.Through test, corniculate spurgentian herb extract brings up to 90～97% at the dissolubility of simulated gastric fluid.
6 one kinds of solid dispersions that improve Tibetan medicine corniculate spurgentian herb extract dissolution of embodiment are made up of water-solubility carrier and Tibetan medicine corniculate spurgentian herb extract.Wherein water-solubility carrier is a poloxamer, and the Herba Haleniae Corniculatae total glycosides content of Tibetan medicine corniculate spurgentian herb extract is 58% extract; The mass ratio of Tibetan medicine corniculate spurgentian herb extract and poloxamer is 14: 1.
The method for preparing of this solid dispersion: at first, take by weighing poloxamer (188) 100mg, poloxamer is dissolved in the dehydrated alcohol, then, add corniculate spurgentian herb extract 1400mg, mix homogeneously; Secondly, under 70～90 ℃ of temperature, boil off dehydrated alcohol, after the natural cooling drying, promptly obtain Haleniaside--the solid dispersion of poloxamer.Through test, corniculate spurgentian herb extract brings up to 45～55% at the dissolubility of simulated gastric fluid.
7 one kinds of solid dispersions that improve Tibetan medicine corniculate spurgentian herb extract dissolution of embodiment are made up of water-solubility carrier and Tibetan medicine corniculate spurgentian herb extract.Wherein water-solubility carrier is polyvidone class and microcrystalline Cellulose, and the Herba Haleniae Corniculatae total glycosides content of Tibetan medicine corniculate spurgentian herb extract is 70% extract; The mass ratio of Tibetan medicine corniculate spurgentian herb extract and polyvidone class and microcrystalline Cellulose is 80: 5: 15.
The method for preparing of this solid dispersion: take by weighing corniculate spurgentian herb extract 800mg, polyvidone class (PVP-k30) 50mg, microcrystalline Cellulose (MCC) 150mg; With grinding 30min to mix homogeneously in three kinds of materials adding mortars; Cross 80 mesh sieves, promptly obtain corniculate spurgentian herb extract--the solid dispersion of polyvidone class (PVP-k30), microcrystalline Cellulose (MCC).Through test, corniculate spurgentian herb extract brings up to 40～53% at the dissolubility of simulated gastric fluid.
8 one kinds of solid dispersions that improve Tibetan medicine corniculate spurgentian herb extract dissolution of embodiment are made up of water-solubility carrier and Tibetan medicine corniculate spurgentian herb extract.Wherein water-solubility carrier is the polyvidone class, and the Herba Haleniae Corniculatae total glycosides content of Tibetan medicine corniculate spurgentian herb extract is 80% extract; The mass ratio of Tibetan medicine corniculate spurgentian herb extract and polyvidone class is 95: 5.
The method for preparing of this solid dispersion: take by weighing corniculate spurgentian herb extract 950mg, polyvidone class (PVP-k30) 50mg; With grinding 30min to mix homogeneously in three kinds of materials adding mortars; Cross 80 mesh sieves, promptly obtain corniculate spurgentian herb extract--the solid dispersion of polyvidone class (PVP-k30), microcrystalline Cellulose (MCC).Through test, corniculate spurgentian herb extract brings up to 35～40% at the dissolubility of simulated gastric fluid.
9 one kinds of solid dispersions that improve Tibetan medicine corniculate spurgentian herb extract dissolution of embodiment are made up of water-solubility carrier and Tibetan medicine corniculate spurgentian herb extract.Wherein water-solubility carrier is polyvidone class and microcrystalline Cellulose, and the Herba Haleniae Corniculatae total glycosides content of Tibetan medicine corniculate spurgentian herb extract is 45% extract; The mass ratio of Tibetan medicine corniculate spurgentian herb extract and polyvidone class and microcrystalline Cellulose is 85: 5: 10.
The method for preparing of this solid dispersion: take by weighing corniculate spurgentian herb extract 850mg, polyvidone class (PVP-k30) 50mg, microcrystalline Cellulose (MCC) 100mg; With grinding 30min to mix homogeneously in three kinds of materials adding mortars; Cross 80 mesh sieves, promptly obtain corniculate spurgentian herb extract--the solid dispersion of polyvidone class (PVP-k30), microcrystalline Cellulose (MCC).Through test, corniculate spurgentian herb extract brings up to 48～55% at the dissolubility of simulated gastric fluid.
Claims (2)
1. solid dispersion that improves Tibetan medicine corniculate spurgentian herb extract dissolution, it is characterized in that: this solid dispersion is processed by conventional method by water-solubility carrier poloxamer and Tibetan medicine corniculate spurgentian herb extract; Or water-solubility carrier polyvidone class and microcrystalline Cellulose and Tibetan medicine corniculate spurgentian herb extract are processed by conventional method; The mass ratio of said Tibetan medicine corniculate spurgentian herb extract and said poloxamer is 9～19: 1; The mass ratio of said Tibetan medicine corniculate spurgentian herb extract and said polyvidone class and microcrystalline Cellulose is 95～85: 5: 0～15.
2. a kind of solid dispersion that improves Tibetan medicine corniculate spurgentian herb extract dissolution as claimed in claim 1; It is characterized in that: said Tibetan medicine corniculate spurgentian herb extract is meant the Tibetan medicine Halenia comiculata plant through solvent extraction, concentrated, and the Herba Haleniae Corniculatae total glycosides content that obtains after the remove impurity is 5～100% extract.
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| CN2010101659060A CN101829186B (en) | 2010-05-04 | 2010-05-04 | Solid dispersant for improving dissolution of Tibet medicinal halenia extract |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1739602A (en) * | 2004-08-26 | 2006-03-01 | 中国科学院西北高原生物研究所 | A kind of technology of from Halenia comiculata plant, extracting anti-hepatitis effective ingredient |
| CN101455674A (en) * | 2007-12-13 | 2009-06-17 | 中国科学院兰州化学物理研究所 | Halenia ellipitica D.Don. total di-phenylcumalin drop-pills for treating chronic hepatitis and preparation method thereof |
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1739602A (en) * | 2004-08-26 | 2006-03-01 | 中国科学院西北高原生物研究所 | A kind of technology of from Halenia comiculata plant, extracting anti-hepatitis effective ingredient |
| CN101455674A (en) * | 2007-12-13 | 2009-06-17 | 中国科学院兰州化学物理研究所 | Halenia ellipitica D.Don. total di-phenylcumalin drop-pills for treating chronic hepatitis and preparation method thereof |
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