CN101513393A - Silymarin soft capsule and method for preparing same - Google Patents
Silymarin soft capsule and method for preparing same Download PDFInfo
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- CN101513393A CN101513393A CNA2008100545597A CN200810054559A CN101513393A CN 101513393 A CN101513393 A CN 101513393A CN A2008100545597 A CNA2008100545597 A CN A2008100545597A CN 200810054559 A CN200810054559 A CN 200810054559A CN 101513393 A CN101513393 A CN 101513393A
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Abstract
The invention provides a silymarin soft capsule, a method for preparing the same, and application thereof. The liquid medicine of the soft capsule consists of silymarin, a filling agent and a latent solvent. The dissolution and the bioavailability of the silymarin soft capsule provided by the invention are improved remarkably.
Description
Technical field
The present invention relates to a kind of soft capsule and preparation method thereof, be specifically related to a kind of silymarin soft capsule and preparation method thereof.
Background technology
Silymarin is the active component that extracts from plant amedica Herba Silybi mariani Silybum marianum fruit, and Herba Silybi mariani is a kind of biennial draft feverfew, originates in Europe.Herba Silybi mariani is the fruit of feverfew Herba Silybi mariani, and at the end of the sixties, people such as the German pharmacy H.Wagner of man find that the Herba Silybi mariani fruit contains silymarin (silymarin), have the protection liver plasma membrane, improve effects such as liver function.Herba Silybi mariani has become international and has protected the liver plant at present, has been widely used in treating acute, chronic hepatitis and hepatitis interstitialis chronica etc. with its preparation as principal agent.By a large amount of pharmacological experiment studies, Herba Silybi mariani also has blood fat reducing simultaneously, protection cardiac muscle and diabetes effect.
The preparation that is made by silymarin is referred to as silybin in China.Its main component is a silibinin, contains Isosilybin, silidianin, Silychristin in addition, is flavone compound.Silymarin is a kind of liver plasma membrane stabilizing agent, and the function of protection and enhance hepatocyte mucosa is arranged, and can exempt because of being subjected to hazardous substances that liver function is degenerated.At present clinically be used for the treatment of hepatic injury, metabolism toxic liver injury, cholelithiasis and the spleen disease etc. that acute, chronic hepatitis, hepatitis interstitialis chronica, fatty liver, ethanol cause.Can directly remove active oxygen, suppress 5 '-lipoxygenase, the protection liver plasma membrane, promote to be damaged hepatocyte synthetic DNA and structural protein, pharmacological actions such as anti-hepatic fibrosis are closed in immunomodulating.In addition, it can also reduce the nephrotoxicity of cisplatin and not influence the latter's active anticancer.Can also prevent and treat diabetes, blood fat reducing, protection hepatocyte, anti-platelet aggregation, antioxidation etc.The toxic and side effects of silymarin is very low, can take for a long time, and application prospect is very wide.Herba Silybi mariani in Europe as the history in existing more than 100 year of hepatic, existing clinical acute and chronic hepatitis and chronic persistent hepatitis, hepatitis interstitialis chronica, fatty liver, the cholecystitis etc. of being used for the treatment of.
The oral formulations of the silymarin of listing has tablet, capsule etc. at present.Because silymarin is flavanolignan's compounds, almost insoluble in water, the dissolution rate of silymarin tablet is very low, sees (" Chinese patent medicine ", 1993 the 15th volume the 6th phase 2-4, Chen Dawei, Liu Limin etc.), has therefore influenced the therapeutic effect of silymarin.Zoopery shows; the silymarin intraperitoneal injection has stronger anti-cell poison, protection hepatocyte, transaminase lowering and effect for reducing blood fat, but behind the oral administration; effect is undesirable, even has the report oral administration invalid or need more heavy dose of administration just effectively.The clinical experiment result also similarly.Its main cause is the own poor solubility of silymarin (its water solublity, fat-soluble all bad), and oral difficult absorption causes bioavailability low, is difficult to arrive site of action.The dissolution of homemade silymarin tablet in simulated gastric fluid is low, and the release total amount was lower than 30% in 50 minutes, influenced the performance of silymarin clinical efficacy.
In recent years, people are made into clathrate, solid dispersion or complex and improve its dissolution rate, utilize the beta-cyclodextrin inclusion compound technology as Li Fanzhu etc., make silymarin and Benexate Hydrochloride, see (" time precious traditional Chinese medicines research ", 1996,7 (3): 146); The somebody sees (Eur J Drug MetabPharmaookinet, 1990,15 (4): 333) with silymarin and lecithin complexation; These methods all can significantly improve the dissolution and the bioavailability of silymarin, but above-mentioned preparation method complexity needs a large amount of organic solvents, and the cost height, are unfavorable for commercial production.Given this invention provides a kind of easy to prepare, cost is low, stripping is fast, bioavailability height, and the soft capsule of stable homogeneous.
Summary of the invention
The objective of the invention is to overcome deficiency of the prior art, a kind of silymarin soft capsule is provided.A kind of silymarin preparation of soft capsule method is provided simultaneously.
Silymarin soft capsule provided by the invention is made up of medicinal liquid and capsule material.Its herb liquid is by 10%～20% silymarin (silibinin and Isosilybin meter), 60%～80% filler substrate, and 0～20% cosolvent is formed.The preferred silymarin 13% of the prescription of medicinal liquid, filler substrate 82%, cosolvent 5%.
Filler is liquid PEG, and cosolvent is a tween; Filler matrix optimization PEG400, the preferred tween of cosolvent.
The medicinal liquid preparation method is: PEG400, tween mixing and stirring, add silymarin, and stir, both got medicinal liquid.With gelatin, glycerol, aquation glue liquid, the compacting capsule promptly gets soft capsule preparation.
Soft capsule provided by the invention, the capsule material comprises sizing material, plasticizer and water, and weight ratio is 1: 0.2～0.6; 0.7～1.4; Sizing material can be gelatin, arabic gum or its combination; Plasticizer is glycerol, sorbitol or other combinations.
Soft capsule provided by the invention, its herb liquid preparation method is: filler, cosolvent are mixed, add silymarin, continue heated and stirred, remain on 80～100 ℃, dissolve fully to silymarin, the water that adds recipe quantity again, stirring promptly gets medicinal liquid.Soft capsule can adopt conventional preparation technology to make.As manual die pressing, rotating mould platen press or dropping preparation method.Generally select pressing such as rotating mould platen press for use, use rotation automatically to press the capsule machine, temperature is controlled between 40～50 ℃, and every soft capsule content weight of preparation is between 0.1～0.8g, and preferred weight is 0.2-0.5g.The moisture silibin (in silibinin) that flies of the dosage unit of every soft capsule is preferably 38.5mg between 10.0-154mg.
The technology of the present invention content height is better than the silybin product of general dosage form in curative effect and safety, be mainly reflected in:
1, determined curative effect, mechanism are clear and definite.
Suppress 5 '-lipoxygenase, directly remove active oxygen.Immunomodulating, anti-hepatic fibrosis, promotion are damaged hepatocyte synthetic DNA and structural protein, protection liver plasma membrane.
2, rapid-action.
The one, absorb soon, increased compositions such as surfactant, short absorbent in the silybin soft capsule prescription, accelerated infiltration rate greatly.
The 2nd, the dissolution height; silybin effective ingredient-silymarin is a solid state in preparations such as tablet, capsule; in gastrointestinal medicine can't be fast, discharge completely, do not get a desired effect, such preparation is taken the liver-protective effect that do not have before wine.The silybin soft capsule makes the effective ingredient of silybin increase greatly in the degree that gastric discharges, and could guarantee that like this medicine plays due effect, could be real remove worry for hepatopath and alcohol user.
Fig. 1, Fig. 2, Fig. 3 are the Yiganling tablet and the dissolution contrast of the external Yiganling tablet of producing in different medium of silybin soft capsule and domestic production, and the stripping of silybin soft capsule is the highest the three from scheming as can be known.
3, the silybin soft capsule quality is more stable.The capsule shell of En Bipu Pharmaceutical production silybin soft capsule can be airtight fully with medicine, be hedged off from the outer world and avoid the oxidation of medicine, add the exclusive soft capsule production Technology of stone medicine group, thereby increased the quality stability of medicine, the drug safety coefficient is higher; Avoided the volatilization of middle pharmaceutically active ingredient simultaneously.
4, the silybin soft capsule is totally-enclosed dosage form, can't smell the abnormal smells from the patient of any Chinese medicine when taking, and has increased the compliance of patient's medication, has enlarged crowd's scope of medication, has embodied the superiority of the modernization of Chinese medicine from wider scope.
The present invention is through a large amount of experimental studies have found that, soft capsule provided by the invention is compared with existing silymarin preparation, the dissolution height, and bioavailability is good.
Description of drawings
Fig. 1 sample and reference substance (Yiganling tablet, the Legalon) dissolution in simulated gastric fluid
Fig. 2 sample and reference substance (Yiganling tablet, the Legalon) dissolution in simulated intestinal fluid
Fig. 3 sample and reference substance (Yiganling tablet, the Legalon) dissolution in distilled water
The specific embodiment
Preparation example 1: preparation soft capsule
Take by weighing PEG400 2800g (70%), glycerol 300g (7.5%) and tween 80 160g (4%), mix, add silymarin 620g (15.5%), continue heated and stirred, maintain the temperature at 85-90 ℃, dissolve fully until silymarin, add entry 120g (3%) again, stir, promptly get medicinal liquid.
Take by weighing 50 parts in gelatin, 50 parts in water, 20 parts of glycerol.Gelatin is added in the entry, allow the gelatin water absorption and swelling.Glycerol added be heated to 60-80 ℃ in the glue pot, add swollen gelatin, fusion stirs, and promptly gets glue.
With rotation mold pressing encapsulating machine, adjust every and contain content 0.31g, make the silymarin soft capsule.Record every silymarin content and count 38.85mg, record 30 minutes dissolutions 98.75% with silibinin.
Preparation example 2: preparation soft capsule
Take by weighing PEG400 2000g (50%), glycerol 400g (10%) and tween 80 200g (5%), mix, add silymarin 1200g (30%), continue heated and stirred, maintain the temperature at 95～100 ℃, dissolve fully until silymarin, add entry 200g (5%) again, stir, promptly get medicinal liquid.
Take by weighing 50 parts in gelatin, 50 parts in water, 15 parts of glycerol.Gelatin is added in the entry, allow the gelatin water absorption and swelling.Glycerol added be heated to 60-80 ℃ in the glue pot, add swollen gelatin, fusion stirs, and promptly gets glue.
With rotation mold pressing encapsulating machine, adjust every and contain content 0.2g, make the silymarin soft capsule.Record every silymarin content and count 42.33mg with silibinin, recording dissolution is 96.38% in the time of 30 minutes.
Preparation example 3: preparation soft capsule
Method by preparation example 1 changes PEG400 into Macrogol 600, and tween 80 changes tween 20 into, and other conditions are constant, adjust every and contain content 0.329, make the silymarin soft capsule.Record every silymarin content and count 40.22mg with silibinin, dissolution 97.62% in 30 minutes.
Preparation example 4: preparation soft capsule
Take by weighing PEG400 3600g (88%), glycerol 160g (4%) and tween 80 80g (2%), mix, add silymarin 120g (3%), continue heated and stirred, maintain the temperature at 85-90 ℃, dissolve fully until silymarin, add entry 120g (3%) again, stir, promptly get medicinal liquid.Other operations are with preparation example 1.
Make every of soft capsule and contain content 0.8g, record every silymarin content and count 16.80mg, record 30 minutes dissolutions 99.10% with silibinin.
Claims (8)
1. soft capsule that contains silymarin, it is characterized by: the medicinal liquid main component is a silymarin, is made by Chinese medicine Herba Silybi mariani extract or crude drug.
2. according to claim 1, the amount of medicinal liquid main component silymarin is calculated by the amount of silibinin after giving money as a gift and Isosilybin.
3. according to claim 1, medicinal liquid is by 10%～20% silymarin (silibinin and Isosilybin meter), 60%～80% filler substrate, and 0～30% cosolvent is formed.
4. according to claim 3, the preferred silymarin 13% of the prescription of medicinal liquid, filler substrate 82%, cosolvent 5%.
5. according to claim 3, filler matrix optimization PEG400, the preferred tween of cosolvent.
6. according to claim 3, the medicinal liquid preparation method is: PEG400, the tween mixing and stirring adds silymarin, stirs, and has both got medicinal liquid.With gelatin, glycerol, aquation glue liquid, the compacting capsule promptly gets soft capsule preparation.
7. according to claim 6, by the soft capsule of the prescription preparation of medicinal liquid, unit dose preferred (in silymarin) is 38.5mg.
8. according to claim 1, have the effect that improves liver function, protection liver plasma membrane by the soft capsule of the prescription preparation of medicinal liquid, be used for the treatment of acute and chronic hepatitis and chronic persistent hepatitis.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008100545597A CN101513393A (en) | 2008-02-22 | 2008-02-22 | Silymarin soft capsule and method for preparing same |
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| Application Number | Priority Date | Filing Date | Title |
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| CNA2008100545597A CN101513393A (en) | 2008-02-22 | 2008-02-22 | Silymarin soft capsule and method for preparing same |
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| CN101513393A true CN101513393A (en) | 2009-08-26 |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111728209A (en) * | 2019-03-25 | 2020-10-02 | 株式会社爱茉莉太平洋 | Composition for enhancing bioavailability of silymarin |
| CN115721640A (en) * | 2022-07-07 | 2023-03-03 | 中国科学院长春应用化学研究所 | Application of isosilybin in preparing medicament for treating osteosarcoma |
-
2008
- 2008-02-22 CN CNA2008100545597A patent/CN101513393A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111728209A (en) * | 2019-03-25 | 2020-10-02 | 株式会社爱茉莉太平洋 | Composition for enhancing bioavailability of silymarin |
| CN115721640A (en) * | 2022-07-07 | 2023-03-03 | 中国科学院长春应用化学研究所 | Application of isosilybin in preparing medicament for treating osteosarcoma |
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Open date: 20090826 |