CN1981855A - Self-emusified composition containing diamond vine extract - Google Patents
Self-emusified composition containing diamond vine extract Download PDFInfo
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- CN1981855A CN1981855A CN 200510111423 CN200510111423A CN1981855A CN 1981855 A CN1981855 A CN 1981855A CN 200510111423 CN200510111423 CN 200510111423 CN 200510111423 A CN200510111423 A CN 200510111423A CN 1981855 A CN1981855 A CN 1981855A
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- rhizoma smilacis
- smilacis bockii
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- surfactant
- extract
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Abstract
A self-emulsifying composition in the form of softgel with high dissolving speed and biologic utilization rate contains the extract of bock greenbrier rhizome (20-60 Wt%), surfactant (10-80) and emulsifying aid (0-70).
Description
Technical field
The present invention relates to a kind of compositions that contains Rhizoma Smilacis Bockii extract.
Background technology
Rhizoma Smilacis Bockii is a liliaceous plant Rhizoma Smilacis Chinensis rhizome, effect with heat-clearing and toxic substances removing, dispersing swelling and dissipating binds, be mainly used in the yellow disease such as thick of hypogastralgia due to treatment adnexitis, the multiple inflammation of inflammatory masses of ovarian appendages and gynecological, lumbago, menoxenia, dysmenorrhea, leucorrhea clinically, also be used for the treatment of rheumatic arthritis, traumatic injury, cellulitis, gastroenteritis etc.
But formulation products in the market is mainly syrup, and tablet, capsule etc. are also arranged, because the active ingredient dissolution rate slowly and not exclusively, does not cause absorption difference, curative effect remarkable etc.
Summary of the invention
The objective of the invention is to disclose a kind of self-emulsifying composition that contains Rhizoma Smilacis Bockii extract, to overcome the above-mentioned defective that prior art exists.
Component and the weight content that contains the self-emulsifying composition of Rhizoma Smilacis Bockii extract of the present invention comprises:
Rhizoma Smilacis Bockii extract 20～60%
Surfactant 10～80%
Co-emulsifier 0～70%
Preferred ingredients and weight content:
Rhizoma Smilacis Bockii extract 30～50%
Surfactant 20～60%
Co-emulsifier 10～50%
Said Rhizoma Smilacis Bockii extract can make by known method, is prepared as disclosed methods such as CN03114644.9 patents.
Said surfactant is good with the lower nonionic surfactant of toxicity, is selected from polysorbate 20, polyoxyethylene sorbitan monoleate, Sorbitan Oleate, polyoxyethylene castor oil, polyoxyethylene hydrogenated Oleum Ricini, Brij30, polyoxyethylene hexadecanol ether, Vinlub 73 or the capric acid glyceryl laurate ester one or more; Preferred polyoxyethylene hydrogenated Oleum Ricini or polysorbate 20;
The main effect of surfactant is the hydrophilic that increases Rhizoma Smilacis Bockii extract, promotes its absorption in vivo, and HLB VALUE OF SURFACTANTS HLB value is big more, and its hydrophilic is also big more, and effect is also just stronger.
So surfactant can increase the dissolubility of insoluble drug in water, be commonly considered as because surfactant forms the result of micelle (micelle) in water.Micelle is inwardly to form a minimum oil droplet (nonpolar center) by the lipophilic group of surfactant, hydrophilic group then outside (hydrophilic group of nonionic then from oil droplets as wavy to around stretch into aqueous phase) form spheroid.Think that now micelle can insert solubilizate in the oil droplet in the micelle with the nonpolar part of its molecule with polar molecule slightly, its polarity part then stretches between the hydrophilic group of the surfactant in the water and produces solubilization.
Surfactant has the effect of lipin dissolving when low concentration, can dissolve the phospholipid of gastrointestinal mucosal and change epithelial permeability, reduces the barrier action of intestinal mucosa lipoid.So many medicines that originally were difficult to absorb, add surfactant and make to absorb and increase by passive diffusion.Therefore the agent of HLB value higher surface activity can increase the dissolubility of extract in water, can reduce the barrier action of intestinal mucosa lipoid again and increases its absorption in vivo.
Said co-emulsifier is selected from one or more in PEG400, Macrogol 600, ethanol, propylene glycol, the glycerol; Preferably glycerine, PEG400 or Macrogol 600.The adding of co-emulsifier can further promote the dissolving of medicine, reduces interfacial tension, increases the flowability of interfacial film, regulates the HLB value.
The preparation method that contains the self-emulsifying composition of Rhizoma Smilacis Bockii extract of the present invention is foolproof, can adopt the conventional blended method of physical agitation, and Rhizoma Smilacis Bockii extract, surfactant and co-emulsifier are mixed, and gets final product.
The invention still further relates to the treatment effective dose, the above-mentioned self-emulsifying composition that contains Rhizoma Smilacis Bockii extract is the soft gelatin capsule preparation of content;
Soft gelatin capsule preparation of the present invention is preparation like this: each component is quantitatively mixed according to the above ratio, it is clear and bright to be stirred to solution at a certain temperature, can make with colloid mill or high pressure dispersing emulsification machine etc. that preparation is easier to be carried out, the degassing, use then revolving die formula soft gelatin capsule maker with the medicinal liquid filling in gelatin rubber, also available liquid capsule filling machine fills in the hard capsule and seals.
Rhizoma Smilacis Bockii self-emulsifying composition of the present invention, can be used for the treatment of the yellow disease such as thick of hypogastralgia due to the multiple inflammation of adnexitis, inflammatory masses of ovarian appendages and gynecological, lumbago, menoxenia, dysmenorrhea, leucorrhea, also be used for the treatment of diseases such as rheumatic arthritis, traumatic injury, cellulitis, gastroenteritis.
The present invention is under the situation of gentle agitation or gastrointestinal peristalsis, because the existence of surfactant, spontaneous emulsification forms emulsion droplet, and outward appearance is clear and bright.
Dissolution method by the Chinese Pharmacopoeia regulation is tested, HCL with distilled water and 0.1mol/L is a medium respectively, the solubility property of Rhizoma Smilacis Bockii soft gelatin capsule more of the present invention and commercially available syrup, the result shows that Rhizoma Smilacis Bockii capsule dissolving out capability of the present invention is good, the relative commercially available syrup with degree of dissolution rate all is significantly increased, and indicates that it has the characteristics fast, that bioavailability is high that absorb in vivo.Accelerated test result shows that Rhizoma Smilacis Bockii soft gelatin capsule of the present invention meets the pharmacopeia requirement disintegration.
The specific embodiment
Embodiment 1
The preparation of Rhizoma Smilacis Bockii extract:
Rhizoma Smilacis Bockii is added 75% soak with ethanol 24h of 5 times of amounts, heating and refluxing extraction 3 times, each 1h, merge extractive liquid, filters, and filtrate concentrates the final vacuum drying, is ground into fine powder, promptly.
Embodiment 2
With Rhizoma Smilacis Bockii extract 100 grams, PEG400 200 grams, glycerol 50 grams, polyoxyethylene hydrogenated Oleum Ricini 150 grams mix, and 65 ℃ of heating are with 500 rev/mins rotating speed, it is clear and bright to be stirred to solution, the degassing is pressed into 1000 of soft gelatin capsules with revolving die formula soft gelatin capsule maker, and Rhizoma Smilacis Bockii extract content is 0.1 gram/grain.
Embodiment 4
With Rhizoma Smilacis Bockii extract 200 grams, capric acid glyceryl laurate ester 200 grams, PEG400 300 grams mix, it is clear and bright to be ground to solution with colloid mill after stirring, the degassing is pressed into 1000 of soft gelatin capsules with revolving die formula soft gelatin capsule maker, and Rhizoma Smilacis Bockii extract content is 0.2 gram/grain.
Embodiment 5
With Rhizoma Smilacis Bockii extract 300 grams, polysorbate 20 200 grams, capric acid glyceryl laurate ester 150, glycerol 100 grams mix, and it is clear and bright that the back that stirs is ground to solution with colloid mill, the degassing, be pressed into 1000 of soft gelatin capsules with revolving die formula soft gelatin capsule maker, Rhizoma Smilacis Bockii extract content is 0.3 gram/grain.
Embodiment 6
External bacteriostasis
The pastille culture medium for preparing a series of concentration (0.25,0.5,1.0,2.0,3.0,4.0,5.0,10.0,15.0%), staphylococcus aureus and escherichia coli are used nutrient agar, gonorrhea diplococcus is used the gonorrhea diplococcus culture medium, Candida albicans rose-bengal agar culture medium.With commercially available syrup is relatively fungistatic effect of matched group and capsule of the present invention, inoculates not the pastille flat board simultaneously and makes growth control.The result shows, the dull and stereotyped bacterial growth of pastille is not good, the Rhizoma Smilacis Bockii syrup agent is 1.0% to the minimal inhibitory concentration (MIC) of staphylococcus aureus, to colibacillary MIC is 3.0%, to gonococcal MIC is 4.0%, bacteriostasis to candida albicans is not obvious, and MIC is greater than 15.0%; Rhizoma Smilacis Bockii soft gelatin capsule content of the present invention is 0.5% to the minimal inhibitory concentration (MIC) of staphylococcus aureus, is 1.0% to colibacillary MIC, is 3.0% to gonococcal MIC, is 15.0% to the MIC of candida albicans.Therefore the capsular bacteriostasis of Rhizoma Smilacis Bockii of the present invention is than eager to excel in whatever one does many of commercially available Rhizoma Smilacis Bockii granule.
Embodiment 7
Antiinflammatory action
What 1, xylol caused mice ear influences 50 of mices, and male and female half and half are divided into 5 groups at random: normal saline group (negative control group); The Rhizoma Smilacis Bockii syrup group, 60g (crude drug)/kg; The large, medium and small dosage group of Rhizoma Smilacis Bockii soft gelatin capsule, 60g (crude drug)/kg, 40g/kg, 20g/kg.Every group of gastric infusion three days, 1h after the last administration smears every mice left side ear with 100% dimethylbenzene (0.02mL/), put to death after 15 minutes, cut left and right sides ear, lay round auricle at same position respectively with card punch, weigh, two auricle weight differences are the swelling degree.Result such as following table, Rhizoma Smilacis Bockii soft gelatin capsule of the present invention will obviously be better than the syrup group to the inhibitory action of mice ear.
Table 1 'Jingangteng ' is to the influence of mice ear
| Group | Dosage (g/kg) | Swelling degree (mg) |
| Contrast | / | ?2.1±3.0 |
| Rhizoma Smilacis Bockii syrup | 60 | ?3.4±2.5 |
| The Rhizoma Smilacis Bockii soft gelatin capsule | 60 | ?3.0±1.9 |
| 40 | ?5.3±2.7 | |
| 20 | ?6.1±1.2 |
What 2, on Carrageenan caused rat paw edema influences 50 of SD rats, and male and female half and half are divided 5 groups: normal saline group (negative control group) at random; The Rhizoma Smilacis Bockii syrup group, 60g (crude drug)/kg; The large, medium and small dosage group of Rhizoma Smilacis Bockii soft gelatin capsule, 60g (crude drug)/kg, 40g/kg, 20g/kg.The syrup group gavages 2 times every day, 2mL/100g, and all the other are respectively organized and gavage every day once, 1.2mL/100g, successive administration three days.1h after the last administration, give every right back sufficient subcutaneous injection 1% carrageenin of rat (0.1mL/ only), with volumetric method measure before the administration and behind the injection carrageenin 30,60, the right back sufficient volume of 120min rat, obtain swelling degree (after the administration before volume one administration volume).Result such as following table, Rhizoma Smilacis Bockii soft gelatin capsule of the present invention will obviously be better than the syrup group to the inhibitory action of rat paw edema.
Table 2 'Jingangteng ' on Carrageenan causes the influence of rat paw edema
| Group | Dosage (g/kg) | ?30min | ?60min | ?120min |
| Contrast | / | ?0.45±0.12 | ?0.54±0.21 | ?0.75±0.27 |
| Rhizoma Smilacis Bockii syrup | 60 | ?0.25±0.09 | ?0.31±0.05 | ?0.48±0.13 |
| The Rhizoma Smilacis Bockii soft gelatin capsule | 60 | ?0.20±0.15 | ?0.27±0.06 | ?0.45±0.11 |
| 40 | ?0.26±0.06 | ?0.31±0.15 | ?0.50±0.24 | |
| 20 | ?0.30±0.14 | ?0.35±0.08 | ?0.52±0.18 |
Embodiment 8
Analgesic activity
100 of mices, male and female half and half are divided 5 groups at random, 20 every group: normal saline group (negative control group); The Rhizoma Smilacis Bockii syrup group, 60g (crude drug)/kg; The large, medium and small dosage group of Rhizoma Smilacis Bockii capsule, 60g (crude drug)/kg, 40g/kg, 20g/kg.Gavage every day once, totally three days, 1h only injected 0.6% glacial acetic acid solution 0.2mL/ to each group mouse peritoneal after the last perfusion, observes mouse writhing response situation in the 20min.Result such as following table, visible Rhizoma Smilacis Bockii capsule of the present invention is more much better than than the analgesic activity of syrup.
The analgesic activity of table 3 'Jingangteng '
| Group | Dosage (g/kg) | Number of animals (only) | Writhing response number (only) | Analgesia percentage rate (%) |
| Matched group | / | ?20 | ?20 | ?0 |
| Rhizoma Smilacis Bockii syrup | 60 | ?20 | ?8 | ?60 |
| The Rhizoma Smilacis Bockii capsule | 60 | ?20 | ?4 | ?80 |
| 40 | ?20 | ?9 | ?55 | |
| 20 | ?20 | ?14 | ?30 |
Claims (4)
1. a self-emulsifying composition that contains Rhizoma Smilacis Bockii extract is characterized in that, component and weight content comprise:
Rhizoma Smilacis Bockii extract 20～60%
Surfactant 10～80%
Co-emulsifier 0～70%
Said surfactant is selected from one or more in polysorbate 20, polyoxyethylene sorbitan monoleate, Sorbitan Oleate, polyoxyethylene castor oil, polyoxyethylene hydrogenated Oleum Ricini, Brij30, polyoxyethylene hexadecanol ether, Vinlub 73 or the capric acid glyceryl laurate ester; Preferred polyoxyethylene hydrogenated Oleum Ricini or polysorbate 20;
Said co-emulsifier is selected from one or more in PEG400, Macrogol 600, ethanol, propylene glycol or the glycerol.
2. the self-emulsifying composition that contains Rhizoma Smilacis Bockii extract according to claim 1 is characterized in that said surfactant is selected from glycerol, PEG400 or Macrogol 600.
3. the self-emulsifying composition that contains Rhizoma Smilacis Bockii extract according to claim 1 and 2 is characterized in that, component and weight content are:
Rhizoma Smilacis Bockii extract 30～50%
Surfactant 20～60%
Co-emulsifier 10～50%.
One kind with the treatment soft gelatin capsule preparation effective dose, that each described self-emulsifying composition that contains Rhizoma Smilacis Bockii extract of claim 1～3 is a content.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510111423 CN1981855A (en) | 2005-12-13 | 2005-12-13 | Self-emusified composition containing diamond vine extract |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510111423 CN1981855A (en) | 2005-12-13 | 2005-12-13 | Self-emusified composition containing diamond vine extract |
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| Publication Number | Publication Date |
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| CN1981855A true CN1981855A (en) | 2007-06-20 |
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| CN 200510111423 Pending CN1981855A (en) | 2005-12-13 | 2005-12-13 | Self-emusified composition containing diamond vine extract |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101912447A (en) * | 2010-07-30 | 2010-12-15 | 马宏达 | Rhizoma corydalis total alkaloids self-emulsifying drug delivery system and preparation method and application thereof |
-
2005
- 2005-12-13 CN CN 200510111423 patent/CN1981855A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101912447A (en) * | 2010-07-30 | 2010-12-15 | 马宏达 | Rhizoma corydalis total alkaloids self-emulsifying drug delivery system and preparation method and application thereof |
| CN101912447B (en) * | 2010-07-30 | 2013-01-30 | 马宏达 | Rhizoma corydalis total alkaloids self-emulsifying drug delivery system and preparation method and application thereof |
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Open date: 20070620 |