CN1233318C - Hepadestal soft capsule and its preparing method - Google Patents
Hepadestal soft capsule and its preparing method Download PDFInfo
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- CN1233318C CN1233318C CN 200410052608 CN200410052608A CN1233318C CN 1233318 C CN1233318 C CN 1233318C CN 200410052608 CN200410052608 CN 200410052608 CN 200410052608 A CN200410052608 A CN 200410052608A CN 1233318 C CN1233318 C CN 1233318C
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- silymarin
- soft capsule
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- soybean
- vegetable oil
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Abstract
The present invention relates to a silymarin soft capsule for the medicine technical field and a preparation method. Silymarin and soybean phosphatide are taken and are mixed with a substrate, the silymarin is from 4 to 40 wt %, soybean ovolecithin is from 4 to 50 wt%, and the substrate is composed of 30 to 95 wt% of polyethyleneglycol 400, 0 to 5 wt% of polyethyleneglycol 6000, 5 to 40 wt % of glycerol or 30 to 95 wt % of vegetable oil, and 1 to 10 wt% of beeswax; the mixture is heated at 50 to 100 DEG C and is dissolved, or the silymarin and the soybean phosphatide are firstly heated in solvent, are in the phosphatide and are added with the substrate for uniform mixture; glutin is used as capsule skin, a soft capsule is pressed, and a finished product is obtained by packaging. The present invention avoids toxic solvent such as dioxane, petroleum ether, etc., and simplifies the operation; the prepared soft capsule has the characteristics of high biologic utilization, little side effect and high medicine effect, and can be used for treating diseases such as acute hepatitis, chronic hepatitis, transferring hepatitis, early liver cirrhosis, hyperlipemia, etc.
Description
Technical field
The present invention relates to be used for medical technical field, relate to a kind of silymarin soft capsule for the treatment of hepatitis, early stage liver cirrhosis and hyperlipidemia and preparation method thereof.
Background technology
Herba Silybi mariani is a kind of biennial draft feverfew, originates in Europe.Be rich in flavonolignan---silymarin in the seed, main chemical compositions is silibinin, silidianin and Silychristin, and China introduces a fine variety Herba Silybi mariani since the seventies, in Liaoning, ground such as Shaanxi, Jiangsu, Heilungkiang plants in a large number.Its extract one silymarin of clinical usefulness is made into tablet (trade name: Silibinin), be used to protect the liver and the treatment of chronic hepatitis, early stage liver cirrhosis.Also there is imported product (trade name: Legalon, Germany's production) on China market, to sell now.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.
Find by literature search, 1988, Bruno Gabetta etc. at first reported silymarin combined with soybean phospholipid and formed the oral administration biaavailability that complex can improve silymarin, to capsule, tablet and the suspension application of this complex United States Patent (USP) [US Patent 4764508,1988], this patent is on preparation technology, employing mixes silymarin with phospholipid, heat in organic solvent, then, steam solvent, add petroleum ether again complex curing is leached.Make various preparations at last according to a conventional method.Operate more numerous and diversely, and used bigger dioxane of toxicity and petroleum ether to do solvent and firming agent.Have not yet to see the bibliographical information and the listing product that utilize the phospholipid technology to prepare the silymarin soft capsule.
Summary of the invention
The objective of the invention is to overcome deficiency of the prior art, a kind of phospholipid silymarin soft capsule and preparation method thereof is provided, promptly directly with after silymarin and phospholipid and other substrate Hybrid Heating, seal and make, will in solvent, not solidify taking-up by the silymarin phosphatide complexes, avoid using toxic solvents such as dioxane, petroleum ether, and simplified operation.Prepared soft capsule has bioavailability height, side effect is little, drug effect is high characteristics.Can be used for treating diseases such as acute hepatitis, chronic hepatitis, chronic persistent hepatitis, early stage liver cirrhosis and hyperlipidemia.
The present invention is achieved by the following technical solutions, and the present invention is become with soybean phospholipid and other matrix group by silymarin, and the shared percentage by weight of silymarin is 4%-40%, soybean lecithin 4%-50%.The percentage by weight of described other each component of substrate is: PEG400 is: 30%-95%, polyethylene glycol 6000 are: 0%-5%, glycerol 5%-40%, or vegetable oil 30%-95%, Cera Flava 1%-10%.
Being further defined to of weight percentages of components of the present invention: silymarin 5%-20%, soybean lecithin 5%-25%, described other substrate is: PEG400: 50%-80%, polyethylene glycol 6000: 0%-3%, glycerol 10%-20%, or vegetable oil 50%-80%, Cera Flava 2%-5%.
Vegetable oil of the present invention is one or several of soybean oil, Oleum Cocois, Oleum Camelliae, vegetable oil, Oleum Ricini.
Silibin and soybean phospholipid and substrate are mixed in 50-100 ℃ of heating for dissolving to silymarin soft capsule preparation method of the present invention or elder generation heats silymarin and soybean phospholipid in solvent for water intaking flies, after the phospholipidization, add above-mentioned substrate mix homogeneously again, with the gelatin is the capsule skin, be pressed into soft capsule, packing obtains finished product.
Described solvent is meant to be further defined to a kind of in methanol, ethanol, the acetone: ethanol.
The present invention has following advantage: (1) the present invention becomes liposome with medicine with phospholipids incorporate, increases the fat-soluble of insoluble drug silymarin, and medicine is easily absorbed, the bioavailability behind the increase drug oral, and the drug effect performance is rapid, and toxic and side effects is little.(2) the fat-soluble substrate and the medicine intermiscibility of the present invention's use are good, have increased stability of drug; (3) technology of the present invention is simple, avoids using deleterious organic solvent, easy operating and industrial-scale production; (4) good, the safety of product hermeticity, dosage is accurate, dosage form is stable, and is aesthetic in appearance, carry with easy to use.
The specific embodiment
Provide following examples in conjunction with content of the present invention:
Embodiment one:
Prescription is formed: in the silymarin soft capsule, the shared percentage by weight of silymarin is 5%, and soybean lecithin 5%, PEG400 are: 80%, polyethylene glycol 6000 is: 2%, glycerol 18%.
Preparation method: silymarin 0.5kg (5%), add soybean lecithin 0.5kg (5%), PEG400 is: 8.0kg (80%), polyethylene glycol 6000 are: 0.2kg (2%), glycerol 1.8kg (18%), in stirring following 50 ℃ of heating 5 hours, put cold, thick solution, with the gelatin is the capsule skin, be pressed into soft capsule on HSR-800 type capsule machine, packing obtains 20000 of finished products.The result: smooth surface, mellow and full, Dissolve things inside is stable, even, not stratified, good fluidity.
Embodiment two:
Prescription is formed: in the silymarin soft capsule, the shared percentage by weight of silymarin is 5%, and soybean lecithin 12%, PEG400 are: 70%, polyethylene glycol 6000 is: 3%, glycerol 10%.
Preparation method: silymarin 0.5kg (5%), add soybean lecithin 1.2kg (12%), PEG400 is: 7.0kg (70%), polyethylene glycol 6000 are: 0.3kg (3%), glycerol 1.0kg (10%), in stirring following 75 ℃ of heating 5 hours, put cold, thick solution, with the gelatin is the capsule skin, be pressed into soft capsule on HSR-800 type capsule machine, packing obtains 20000 of finished products.The result: smooth surface, mellow and full, Dissolve things inside is stable, even, not stratified, good fluidity.
Embodiment three:
Prescription is formed: in the silymarin soft capsule, the shared percentage by weight of silymarin is 10%, and soybean lecithin 10%, PEG400 are: 65%, glycerol 15%.
Preparation method: silymarin 1.0kg (10%), add soybean lecithin 1.0kg (10%), PEG400 is: 6.5kg (65%), glycerol 1.5kg (15%), in stirring following 100 ℃ of heating 5 hours, put cold, thick solution, with the gelatin is the capsule skin, be pressed into soft capsule on HSR-800 type capsule machine, packing obtains 20000 of finished products.The result: smooth surface, mellow and full, Dissolve things inside is stable, even, not stratified, good fluidity.
Embodiment four:
Prescription is formed: in the silymarin soft capsule, the shared percentage by weight of silymarin is 20%, and the percentage by weight of each component of substrate is: soybean lecithin 24%, vegetable oil 53%, Cera Flava 3%.
Preparation method: silymarin 2.0kg (20%), add soybean lecithin 2.4kg (24%), ethanol 2L, reflux 2 hours steams ethanol under the decompression, add vegetable oil 5.3kg (53%), Cera Flava 0.3kg (3%), mixed grinding is even, is the capsule skin with the gelatin, is pressed into soft capsule on HSR-800 type capsule machine, packing obtains 20000 of finished products.The result: smooth surface, mellow and full, Dissolve things inside is stable, even, not stratified, good fluidity.
Embodiment five:
Prescription is formed: in the silymarin soft capsule, the shared percentage by weight of silymarin is 10%, soybean lecithin 24%, vegetable oil 64%, Cera Flava 2%.
Preparation method: silymarin 1.0kg (10%), add soybean lecithin 2.4kg (24%), ethanol 1.5L, reflux 2 hours steams ethanol under the decompression, add vegetable oil 6.4kg (64%), Cera Flava 0.2kg (2%), mixed grinding is even, is the capsule skin with the gelatin, is pressed into soft capsule on HSR-800 type capsule machine, packing obtains 20000 of finished products.The result: smooth surface, mellow and full, Dissolve things inside is stable, even, not stratified, good fluidity.
Embodiment six:
Prescription is formed: in the silymarin soft capsule, the shared percentage by weight of silymarin is 10%, soybean lecithin 5%, vegetable oil 80%, Cera Flava 5%.
Preparation method: silymarin 1.0kg (10%), add soybean lecithin 0.5kg (5%), ethanol 1L, reflux 2 hours steams ethanol under the decompression, add vegetable oil 8kg (80%), Cera Flava 0.5kg (5%), mixed grinding is even, is the capsule skin with the gelatin, is pressed into soft capsule on HSR-800 type capsule machine, packing obtains 20000 of finished products.The result: smooth surface, mellow and full, Dissolve things inside is stable, even, not stratified, good fluidity.
Claims (4)
1, a kind of silymarin soft capsule, it is characterized in that, become with soybean phospholipid and other matrix group by silymarin, the shared percentage by weight of silymarin is 4%-40%, soybean lecithin 4%-50%, the percentage by weight of described other each component of substrate is: PEG400 is: 30%-95%, polyethylene glycol 6000 are: 0%-5%, glycerol 5%-40%, or vegetable oil 30%-95%, Cera Flava 1%-10%, more than each composition weight satisfy 100%.
2, silymarin soft capsule according to claim 1, it is characterized in that, below being further defined to each weight percentages of components: silymarin 5%-20%, soybean lecithin 5%-25%, described other substrate is: PEG400: 50%-80%, polyethylene glycol 6000: 0%-3%, glycerol 10%-20%, or vegetable oil 50%-80%, Cera Flava 2%-5%, more than each composition weight satisfy 100%.
3, silymarin soft capsule according to claim 1 is characterized in that, described vegetable oil is one or several of soybean oil, Oleum Cocois, Oleum Camelliae, vegetable oil, Oleum Ricini.
4, a kind of silymarin soft capsule preparation method, it is characterized in that, water intaking flies silibin and soybean phospholipid mixes with substrate, the shared percentage by weight of silymarin is 4%-40%, soybean lecithin 4%-50%, the percentage by weight of each component of substrate is: PEG400 is: 30%-95%, polyethylene glycol 6000 is: 0%-5%, glycerol 5%-40%, or vegetable oil 30%-95%, Cera Flava 1%-10%, heat 50-100 ℃ of dissolving or elder generation silymarin and soybean phospholipid are heated in ethanol, after the phospholipidization, add above-mentioned substrate mix homogeneously again, with the gelatin is the capsule skin, be pressed into soft capsule, packing obtains finished product.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410052608 CN1233318C (en) | 2004-07-08 | 2004-07-08 | Hepadestal soft capsule and its preparing method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410052608 CN1233318C (en) | 2004-07-08 | 2004-07-08 | Hepadestal soft capsule and its preparing method |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1586468A CN1586468A (en) | 2005-03-02 |
| CN1233318C true CN1233318C (en) | 2005-12-28 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN 200410052608 Expired - Fee Related CN1233318C (en) | 2004-07-08 | 2004-07-08 | Hepadestal soft capsule and its preparing method |
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Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102772308B (en) * | 2012-08-14 | 2013-09-18 | 惠州市九惠制药股份有限公司 | Silymarin phospholipid compound, mask containing same and preparation method of same |
| KR102394648B1 (en) * | 2019-03-25 | 2022-05-09 | (주)아모레퍼시픽 | Composition for enhancing bioavailability of silymarin |
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- 2004-07-08 CN CN 200410052608 patent/CN1233318C/en not_active Expired - Fee Related
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| Publication number | Publication date |
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| CN1586468A (en) | 2005-03-02 |
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