CN102727463A - Formula and preparation method for ursodeoxycholic acid soft capsules - Google Patents
Formula and preparation method for ursodeoxycholic acid soft capsules Download PDFInfo
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- CN102727463A CN102727463A CN2012102175571A CN201210217557A CN102727463A CN 102727463 A CN102727463 A CN 102727463A CN 2012102175571 A CN2012102175571 A CN 2012102175571A CN 201210217557 A CN201210217557 A CN 201210217557A CN 102727463 A CN102727463 A CN 102727463A
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- ursodesoxycholic acid
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Abstract
The present invention relates to a formula and a preparation method for ursodeoxycholic acid soft capsules. The formula comprises ursodeoxycholic acid, a vegetable oil, paraffin wax and lecithin. The present invention further discloses the preparation method for the ursodeoxycholic acid soft capsules, wherein the method has characteristics of simple operation and low cost. With the ursodeoxycholic acid soft capsules prepared by the method of the present invention, effects on liver protection and bile flow prompting by the ursodeoxycholic acid can be significantly improved. The product of the present invention can be applicable for treatments of fatty liver, cirrhosis, gallstones, and other liver and gallbladder diseases.
Description
Technical field
The present invention relates to soft capsule prescription and new preparation process thereof, this soft capsule dosage form is included in the ursodesoxycholic acid that is fit in the mounting medium as active component.
Background technology
Ursodesoxycholic acid is at present unique choice drug that is used for various cholestasis hepatopathies such as constitutional cholestasis property liver cirrhosis, primary sclerosing cholangitis by the FDA approval.Domestic production producer is numerous, and the State Bureau website shows that it is tablet that the producer of domestic production has 41 families complete, is insoluble drug through inquiry related data ursodesoxycholic acid; Make the tablet dissolution and be restricted, curative effect can be influenced, and liquid preparation helps the stripping of medicine; In order to comply with patient's adaptability; We select to process soft capsule, and specification is: 0.1g, can effectively break through the bottleneck of homemade tablet stripping problem.
Summary of the invention
One, summary of the invention
The objective of the invention is to overcome the deficiency of prior art, a kind of easy and simple to handle, with low cost, ursodesoxycholic acid soft capsule of facilitating patients is provided.Its technical scheme comprises the following steps:
1. soybean oil and Ovum Gallus domesticus Flavus lecithin are heated to 50～70 ℃, stir 15～25 minutes, melt.
2. the ursodesoxycholic acid that takes by weighing recipe quantity adds in soybean oil and the Ovum Gallus domesticus Flavus lecithin mixture, and 70～90 ℃ of insulated and stirred are even.
3. the paraffin that takes by weighing recipe quantity joins in the medicinal liquid, 70～90 ℃ of insulated and stirred 20～40 minutes.
4. cross colloid mill 2 times, insert in the material-compound tank 20～50 commentaries on classics/min and stirred 30～50 minutes, be pressed into soft capsule.
Two, creation point of the present invention, novelty and compare the advantage that has with traditional handicraft:
1, processes soft capsule, improve the stability of ursodesoxycholic acid.
Have the good isolation function, can keep apart, avoid the oxidation of effective ingredient, make product keep stable content before the deadline, guarantee the performance of effect light, responsive medicine and air, the light of oxygen.
2, with Ovum Gallus domesticus Flavus lecithin as wetting agent, improve the stripping of ursodesoxycholic acid.
Because ursodesoxycholic acid is water-soluble hardly, absorb relatively poor during oral administration.Phospholipid has the amphiphile, amphiphilic molecule structure; Two fatty acid chains are hydrophobic group, and groups such as phosphoric acid and choline are hydrophilic group, are the constituent of biological cell membrane; Phospholipid all has significant effect aspect hepatic cholagogic simultaneously; Both binding energy improve the bioavailability of ursodesoxycholic acid, so we select the wetting agent of Ovum Gallus domesticus Flavus lecithin as these article for use, are used to improve the dissolution of these article.
3, quantitatively accurately, absorb fast.
By the soft capsule of mechanical quantitative filling, dose error is little, and the each amount of eating of consumer is stablized.After the disintegrate, content can be absorbed by health with the form of liquid state soft capsule very soon in vivo.
The specific embodiment
1, principal agent character
Ursodesoxycholic acid is a white powder; Odorless, bitter in the mouth.These article are prone to dissolve in ethanol, and are insoluble in chloroform; In glacial acetic acid, be prone to dissolve, in sodium hydroxide test solution, dissolve.Water-soluble hardly, absorb relatively poor during oral administration.Therefore processing tablet, hard capsule to it all can not its absorption in vivo transhipment of fine solution.
2, method for preparing
For improving the stability of ursodesoxycholic acid, increase dissolution, accelerate to absorb, add lecithin, process soft capsule with the vegetable oil suspendible.
Concrete method for preparing is following:
1. soybean oil and Ovum Gallus domesticus Flavus lecithin are heated to 50～70 ℃, stir 15～25 minutes, melt.
2. the ursodesoxycholic acid that takes by weighing recipe quantity adds in soybean oil and the Ovum Gallus domesticus Flavus lecithin mixture, and 70～90 ℃ of insulated and stirred are even.
3. the paraffin that takes by weighing recipe quantity joins in the medicinal liquid, 70～90 ℃ of insulated and stirred 20～40 minutes.
4. cross colloid mill 2 times, insert in the material-compound tank 20～50 commentaries on classics/min and stirred 30～50 minutes, be pressed into soft capsule.
Embodiment one ursodesoxycholic acid preparation of soft capsule
Take by weighing ursodesoxycholic acid in proportion: soybean oil: paraffin: lecithin (100: 270: 27: 3), earlier soybean oil and Ovum Gallus domesticus Flavus lecithin are heated to 50～70 ℃, stirred 15～25 minutes, melt; Ursodesoxycholic acid is added in soybean oil and the Ovum Gallus domesticus Flavus lecithin mixture, 70～90 ℃ of insulated and stirred are even again; Added 70～90 ℃ of insulated and stirred of paraffin 20～40 minutes; Cross colloid mill at last 2 times, insert in the material-compound tank 20～50 commentaries on classics/min and stirred 30～50 minutes, be pressed into soft capsule and promptly get.
The stripping contrast of embodiment two ursodesoxycholic acid soft capsules and tablet
Select the prescription of six kinds of different outfit ratios to prepare the ursodesoxycholic acid soft capsule according to above-mentioned method for preparing and carry out the dissolution contrast in the ursodesoxycholic acid sheet of market circulation.The result is shown in table 1.
Table 1
Claims (5)
1. a ursodesoxycholic acid soft capsule is filled a prescription and preparation method thereof, it is characterized in that its content is the preparation of being processed by the following weight proportion raw material:
Ursodesoxycholic acid 10～40%, soybean oil 50～85%, paraffin 5.0～8.5%, lecithin 0.5～1.0%.
2. a kind of ursodesoxycholic acid soft capsule prescription according to claim 1 and preparation method thereof is characterized in that the weight proportion of each raw material in every capsules is preferred:
Ursodesoxycholic acid 100mg, soybean oil 270mg, paraffin 27mg, lecithin 3mg.
3. a kind of ursodesoxycholic acid soft capsule prescription according to claim 1 and 2 and preparation method thereof is characterized in that soybean oil and Ovum Gallus domesticus Flavus lecithin are heated to 50～70 ℃, stirs 15～25 minutes; Melt; The ursodesoxycholic acid that takes by weighing recipe quantity adds in soybean oil and the Ovum Gallus domesticus Flavus lecithin mixture, and 70～90 ℃ of insulated and stirred are even, and the paraffin that takes by weighing recipe quantity joins in the medicinal liquid; 70～90 ℃ of insulated and stirred 20～40 minutes; Cross colloid mill 2 times, insert in the material-compound tank 20～50 commentaries on classics/min and stirred 30～50 minutes, be pressed into soft capsule and promptly get.
4. a kind of ursodesoxycholic acid soft capsule prescription according to claim 1 and preparation method thereof is characterized in that the solvent that uses includes but not limited to soybean oil, Semen Maydis oil, Oleum Ricini, Semen Lini oil, Oleum Arachidis hypogaeae semen, Oleum Brassicae campestris, Oleum Sesami, olive oil, Oleum Gossypii semen, sunflower oil, cupu oil, Petiolus Trachycarpi wet goods.
5. a kind of ursodesoxycholic acid soft capsule prescription according to claim 1 and preparation method thereof is characterized in that the lecithin that uses includes but not limited to soybean oil lecithin, Ovum Gallus domesticus Flavus lecithin etc.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012102175571A CN102727463A (en) | 2012-06-28 | 2012-06-28 | Formula and preparation method for ursodeoxycholic acid soft capsules |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012102175571A CN102727463A (en) | 2012-06-28 | 2012-06-28 | Formula and preparation method for ursodeoxycholic acid soft capsules |
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| CN102727463A true CN102727463A (en) | 2012-10-17 |
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| CN2012102175571A Pending CN102727463A (en) | 2012-06-28 | 2012-06-28 | Formula and preparation method for ursodeoxycholic acid soft capsules |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104971058A (en) * | 2015-07-31 | 2015-10-14 | 北京康立生医药技术开发有限公司 | Deoxysodium cholate transdermal drug delivery system |
| CN108853051A (en) * | 2018-09-04 | 2018-11-23 | 安士制药（中山）有限公司 | A kind of ursodesoxycholic acid soft capsule and preparation method thereof |
| CN109248152A (en) * | 2018-11-02 | 2019-01-22 | 河北医科大学第二医院 | A kind of pharmaceutical preparation and preparation method thereof for treating disease in the liver and gallbladder |
| CN116120388A (en) * | 2023-02-09 | 2023-05-16 | 新沂大江化工有限公司 | Ursodeoxycholic acid production process |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101897712A (en) * | 2009-05-26 | 2010-12-01 | 北京星昊医药股份有限公司 | Ursodeoxycholic acid phospholipid composition and preparation method thereof |
-
2012
- 2012-06-28 CN CN2012102175571A patent/CN102727463A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101897712A (en) * | 2009-05-26 | 2010-12-01 | 北京星昊医药股份有限公司 | Ursodeoxycholic acid phospholipid composition and preparation method thereof |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104971058A (en) * | 2015-07-31 | 2015-10-14 | 北京康立生医药技术开发有限公司 | Deoxysodium cholate transdermal drug delivery system |
| CN108853051A (en) * | 2018-09-04 | 2018-11-23 | 安士制药（中山）有限公司 | A kind of ursodesoxycholic acid soft capsule and preparation method thereof |
| CN108853051B (en) * | 2018-09-04 | 2020-12-18 | 安士制药（中山）有限公司 | Ursodeoxycholic acid soft capsule and preparation method thereof |
| CN109248152A (en) * | 2018-11-02 | 2019-01-22 | 河北医科大学第二医院 | A kind of pharmaceutical preparation and preparation method thereof for treating disease in the liver and gallbladder |
| CN109248152B (en) * | 2018-11-02 | 2021-01-12 | 河北医科大学第二医院 | A pharmaceutical preparation for treating liver and gallbladder diseases, and its preparation method |
| CN116120388A (en) * | 2023-02-09 | 2023-05-16 | 新沂大江化工有限公司 | Ursodeoxycholic acid production process |
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Application publication date: 20121017 |