CN102078349A - Cyclodextrin inclusion compound containing angelica volatile oil - Google Patents
Cyclodextrin inclusion compound containing angelica volatile oil Download PDFInfo
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- CN102078349A CN102078349A CN2009102018719A CN200910201871A CN102078349A CN 102078349 A CN102078349 A CN 102078349A CN 2009102018719 A CN2009102018719 A CN 2009102018719A CN 200910201871 A CN200910201871 A CN 200910201871A CN 102078349 A CN102078349 A CN 102078349A
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- cyclodextrin
- volatile oil
- radix angelicae
- angelicae sinensis
- sinensis volatile
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Abstract
The invention provides a cyclodextrin inclusion compound containing angelica volatile oil. The cyclodextrin inclusion compound comprises the angelica volatile oil and hydroxypropy-beta-cyclodextrin, wherein the angelica volatile oil is included in the hydroxypropy-beta-cyclodextrin so as to form the inclusion compound, and the weight percentage of angelica volatile oil and hydroxypropy-beta-cyclodextrin is 10%-20%. The cyclodextrin inclusion compound further comprises povidone K29/32, the dosage of cyclodextrin inclusion compound accounts for 10%-50% of the weight percentage of hydroxypropy-beta-cyclodextrin. The cyclodextrin inclusion compound containing the angelica volatile oil can be prepared into tablets, capsules, powders or injection powders and can be used for treatment of painful menstruation.
Description
Technical field
The invention belongs to biomedicine field, be specifically related to comprise the cyclodextrin clathrate of Radix Angelicae Sinensis volatile oil and this clathrate is treated emmenagogue object space face in preparation purposes.
Background technology
Clathrate is all or part ofly in a kind of space structure of molecule to wrap into another kind of molecule and form, and claims molecular capsule again.Cyclodextrin is because its structure has the particularity of " outer hydrophilic, interior hydrophobic " and nontoxic premium properties, can with multiple object inclusion, adopt the clathrate of proper method preparation that some character of object is improved.
The cyclodextrin molecular structure is formed by connecting by α-1,4 glycosidic bond by 6 above glucoses, is tubbiness.Form the hydrophobicity cavity in the bucket, can absorb the hydrophobic small molecules material or the group of a certain size and shape, form stable non-covalent complex.By six, seven, eight glucose monomers are α-CD by the cyclodextrin that α-1,4 glycosidic bond is formed by connecting, β-CD, γ-CD respectively.β-CD is one of best enclose material of known effect, is most widely used in three types.
(HP-β-CYD) not only chemical compound lot is had good envelope effect improves by the envelope Stability of Substance HP-, and it also has the water solublity height and improves by the rate of release of envelope medicine and bioavailability in vivo.HP-β-CYD hemolytic activity is low on the other hand, and show activity is low, to skin and muscle nonirritant, is a kind of good cosolvent.
When the dry root that is classified as Umbelliferae (Umbelliferae) plant Radix Angelicae Sinensis Angelica sinensis (Oliv.) Diels, when being included into liver, the heart, spleen channel, the property of medicine is sweet, hot, warm, having enriches blood invigorates blood circulation, blood stasis dispelling, menstruction regulating and pain relieving, the effect of moisturizing laxation are used for menoxenia, anemia, amenorrhea, dysmenorrhea, metrorrhagia etc.When being classified as one of the highest Chinese medicine of clinical frequency of utilization.Domestic and international many scholars have all carried out comparatively detailed research to chemical constituent, pharmacological action and the clinical practice of Radix Angelicae Sinensis, isolate multiple compositions such as phthalide-type, terpenoid, aromatic compound at present from this plant.Radix Angelicae Sinensis volatile oil is to rat normal unpregnancy uterus and in the isolated uterine experiment that oxytocin is handled, find that but Radix Angelicae Sinensis volatile oil dose dependent and time compliance ground suppress the contractile function of uterine smooth muscle, the dysmenorrhea effect is promptly treated in the effect of the significant anti-uterine smooth muscle spasm of prompting Radix Angelicae Sinensis volatile oil tool.
Volatile medicine is made cyclodextrin clathrate, except reducing volatilization, also has slow releasing function.Some are easy to oxidation Decomposition, rotten, and the clathrate that light, heat-labile spice be can be made into beta-schardinger dextrin-stores and uses, and so not only can keep original fragrance but also can prevent that it is rotten, and can prolong the resting period.
Summary of the invention
The purpose of this invention is to provide a kind of cyclodextrin clathrate that comprises Radix Angelicae Sinensis volatile oil.
The present invention also provides the method for the described clathrate of preparation, and the pharmaceutical dosage forms of described clathrate.
The present invention comprises the cyclodextrin clathrate of Radix Angelicae Sinensis volatile oil, contain Radix Angelicae Sinensis volatile oil, HYDROXYPROPYL BETA-CYCLODEXTRIN, the Radix Angelicae Sinensis volatile oil enclose forms clathrate in HYDROXYPROPYL BETA-CYCLODEXTRIN, wherein, the percentage by weight of Radix Angelicae Sinensis volatile oil and HYDROXYPROPYL BETA-CYCLODEXTRIN is 10%-20%, and the percentage by weight of preferred Radix Angelicae Sinensis volatile oil and HYDROXYPROPYL BETA-CYCLODEXTRIN thing is 12%-15%.
The present invention comprises the cyclodextrin clathrate of Radix Angelicae Sinensis volatile oil, further comprise 30 POVIDONE K 30 BP/USP 29/32, the percentage by weight that its consumption accounts for HYDROXYPROPYL BETA-CYCLODEXTRIN is that the percentage by weight that preferred 30 POVIDONE K 30 BP/USP 29/32 consumption of 10%-50% accounts for HYDROXYPROPYL BETA-CYCLODEXTRIN is 25%-30%.
The present invention also comprises the Pharmaceutical composition that comprises described cyclodextrin clathrate, and in described compositions, the percentage by weight that cyclodextrin clathrate accounts for compositions is 1%-10%.
Described Pharmaceutical composition can be tablet, capsule, powder or injection powder injection.
Described tablet, capsule, powder also comprise the excipient that pharmaceutically is suitable for, for example filler, disintegrating agent, wetting agent, binding agent, effervescent, surfactant, lubricant, fluidizer, correctives, the strong excipient of smelling the solid preparation of agent, coloring agent and other kinds.
Filler can be selected from one or more the combination of following material: calcium carbonate, magnesium carbonate, calcium phosphate, calcium sulfate, magnesium oxide, carboxymethylcellulose calcium, sodium carboxymethyl cellulose, sucrose, lactose, fructose, xylitol, mannitol, starch and derivant thereof, dextrin, microcrystalline Cellulose.
Disintegrating agent can be selected from one or more the combination of following material: starch, alginic acid, carboxymethylcellulose calcium, sodium carboxymethyl cellulose, cross-linking sodium carboxymethyl cellulose, crospolyvinylpyrrolidone, low substituted hydroxy-propyl methylcellulose, microcrystalline Cellulose, methylcellulose.
Effervescent can be selected from the combination of citric acid, tartaric acid, boric acid, maleic acid etc. and carbonate, or selects phosphatic combination for use, or selects succinic anhydrides for use, organic acid anhydride classes such as citron anhydride.
Surfactant can be selected from one or more combination of following material: sodium lauryl sulphate, poloxamer, Tweens, bromination hexadecane trimethylamine, sodium laurylsulfate, stearyl alcohol sodium sulfonate, polyoxyethylene high fatty alcohol, sucrose ester, sorbitol fatty ester, soybean phospholipid etc.
Wetting agent can be selected from one or more the combination of following material: distilled water, ethanol, starch slurry, dodecyl sodium sulfate, Tweens surfactant.
Binding agent can be selected from one or more the combination of following material: arabic gum, gelatin, Tragacanth, dextrin, polyvinylpyrrolidone, starch and derivant thereof, sodium alginate, sorbitol, syrup, hydroxypropyl emthylcellulose, methylcellulose, hydroxypropyl cellulose, hydroxyethyl-cellulose, ethyl cellulose, sodium carboxymethyl cellulose, carboxymethylcellulose calcium, glucose, polymethacrylates.
Lubricant can be selected from one or more the combination of following material: calcium stearate, glyceryl monostearate, glyceryl palmitostearate, magnesium stearate, microcrystalline Cellulose, sodium benzoate, sodium chloride, sodium lauryl sulphate, magnesium stearate, stearyl fumarate, Pulvis Talci, zinc stearate, Polyethylene Glycol.
Fluidizer can be selected from one or more the combination of following material: silica sol, Powderd cellulose, magnesium trisilicate, silicon dioxide and Pulvis Talci.
Correctives can be selected from aspartame, stevioside, fructose, glucose, syrup, Mel, xylitol, mannitol, lactose, sorbitol, maltose alcohol, glycyrrhizin, phyllodulcin and various essence, rectify and to smell agent and can select aromatic oil for use, the artificial or synthetic pigment of the optional usefulness of coloring agent.
Understand easily as those skilled in the art institute, for solid orally ingestible, above-mentioned substance enumerate the restriction that does not constitute technical scheme, the used excipient of the solid preparation of other that do not enumerate equally also goes for this programme, thereby is also included within this programme.
The present invention also comprises the Preparation methods of cyclodextrin inclusion complexes that comprises Radix Angelicae Sinensis volatile oil, comprises the steps:
(1) preparation HYDROXYPROPYL BETA-CYCLODEXTRIN aqueous solution;
(2) add 30 POVIDONE K 30 BP/USP 29/32, mix homogeneously;
(3) be heated to 30 ℃-50 ℃;
(3) under agitation add Radix Angelicae Sinensis volatile oil, the maintenance temperature also stirred 1-6 hour;
(4) lyophilization or rotary evaporation are removed organic solvent.
The cyclodextrin clathrate that the present invention comprises Radix Angelicae Sinensis volatile oil can be used for preparation treatment dysmenorrhea medicine.
The specific embodiment
The preparation of HYDROXYPROPYL BETA-CYCLODEXTRIN aqueous solution
The 50g HYDROXYPROPYL BETA-CYCLODEXTRIN is dissolved in the 50ml water, stirs, add 30 POVIDONE K 30 BP/USP 29/32, be diluted to 100ml. with water
The preparation of inclusion complex in solution
Under stirring fast, Radix Angelicae Sinensis volatile oil 10g is extremely transparent with the HYDROXYPROPYL BETA-CYCLODEXTRIN aqueous solution for preparing, be diluted to 200ml with water.
Freeze-drying prepares clathrate
The above-mentioned inclusion complex in solution for preparing is placed on is suitable for refrigerated and has in the ampoule of stopper, be positioned in the freezer dryer.
Claims (8)
1. the cyclodextrin clathrate that comprises Radix Angelicae Sinensis volatile oil, it is characterized in that contain Radix Angelicae Sinensis volatile oil, HYDROXYPROPYL BETA-CYCLODEXTRIN, the Radix Angelicae Sinensis volatile oil enclose forms clathrate in HYDROXYPROPYL BETA-CYCLODEXTRIN, wherein, the percentage by weight of Radix Angelicae Sinensis volatile oil and HYDROXYPROPYL BETA-CYCLODEXTRIN is 10%-20%.
2. the cyclodextrin clathrate that comprises Radix Angelicae Sinensis volatile oil as claimed in claim 1 is characterized in that, the percentage by weight of Radix Angelicae Sinensis volatile oil and HYDROXYPROPYL BETA-CYCLODEXTRIN thing is 12%-15%.
3. the cyclodextrin clathrate that comprises Radix Angelicae Sinensis volatile oil as claimed in claim 1 is characterized in that, further comprises 30 POVIDONE K 30 BP/USP 29/32, and the percentage by weight that its consumption accounts for HYDROXYPROPYL BETA-CYCLODEXTRIN is 10%-50%.
4. the cyclodextrin clathrate that comprises Radix Angelicae Sinensis volatile oil as claimed in claim 1 is characterized in that, the percentage by weight that 30 POVIDONE K 30 BP/USP 29/32 consumption accounts for HYDROXYPROPYL BETA-CYCLODEXTRIN is 25%-30%.
5. comprise as the arbitrary described Pharmaceutical composition that comprises the cyclodextrin clathrate of Radix Angelicae Sinensis volatile oil of claim 1 to 4, it is characterized in that, in described compositions, the percentage by weight that cyclodextrin clathrate accounts for compositions is 1%-10%.
6. Pharmaceutical composition as claimed in claim 5 is characterized in that, it is tablet, capsule, powder or injection powder injection.
7. as the arbitrary described Preparation methods of cyclodextrin inclusion complexes that comprises Radix Angelicae Sinensis volatile oil of claim 1 to 4, comprise the steps:
(1) preparation HYDROXYPROPYL BETA-CYCLODEXTRIN aqueous solution;
(2) add 30 POVIDONE K 30 BP/USP 29/32, mix homogeneously;
(3) be heated to 30 ℃-50 ℃;
(3) under agitation add Radix Angelicae Sinensis volatile oil, the maintenance temperature also stirred 1-6 hour;
(4) lyophilization or rotary evaporation are removed organic solvent.
8. be used to prepare the purposes of treatment dysmenorrhea medicine as the arbitrary described cyclodextrin clathrate that comprises Radix Angelicae Sinensis volatile oil of claim 1 to 4.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2009102018719A CN102078349A (en) | 2009-11-26 | 2009-11-26 | Cyclodextrin inclusion compound containing angelica volatile oil |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2009102018719A CN102078349A (en) | 2009-11-26 | 2009-11-26 | Cyclodextrin inclusion compound containing angelica volatile oil |
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| CN102078349A true CN102078349A (en) | 2011-06-01 |
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| CN2009102018719A Pending CN102078349A (en) | 2009-11-26 | 2009-11-26 | Cyclodextrin inclusion compound containing angelica volatile oil |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113289032A (en) * | 2021-06-02 | 2021-08-24 | 京津冀联创药物研究（北京）有限公司 | Cyclodextrin oil inclusion compound and preparation method thereof |
| CN113332451A (en) * | 2021-06-02 | 2021-09-03 | 京津冀联创药物研究（北京）有限公司 | Volatile oil cyclodextrin inclusion compound and preparation method thereof |
| CN113350523A (en) * | 2021-06-02 | 2021-09-07 | 京津冀联创药物研究（北京）有限公司 | Fat oil inclusion compound and preparation method thereof |
| CN113425687A (en) * | 2021-06-02 | 2021-09-24 | 京津冀联创药物研究（北京）有限公司 | Traditional Chinese medicine formula granule and preparation method thereof |
-
2009
- 2009-11-26 CN CN2009102018719A patent/CN102078349A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113289032A (en) * | 2021-06-02 | 2021-08-24 | 京津冀联创药物研究（北京）有限公司 | Cyclodextrin oil inclusion compound and preparation method thereof |
| CN113332451A (en) * | 2021-06-02 | 2021-09-03 | 京津冀联创药物研究（北京）有限公司 | Volatile oil cyclodextrin inclusion compound and preparation method thereof |
| CN113350523A (en) * | 2021-06-02 | 2021-09-07 | 京津冀联创药物研究（北京）有限公司 | Fat oil inclusion compound and preparation method thereof |
| CN113425687A (en) * | 2021-06-02 | 2021-09-24 | 京津冀联创药物研究（北京）有限公司 | Traditional Chinese medicine formula granule and preparation method thereof |
| CN113425687B (en) * | 2021-06-02 | 2022-09-16 | 京津冀联创药物研究（北京）有限公司 | Traditional Chinese medicine formula granule and preparation method thereof |
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Application publication date: 20110601 |