CN103908440A - Polyene phosphatidylcholine capsule and preparation method thereof - Google Patents
Polyene phosphatidylcholine capsule and preparation method thereof Download PDFInfo
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- CN103908440A CN103908440A CN201310019561.1A CN201310019561A CN103908440A CN 103908440 A CN103908440 A CN 103908440A CN 201310019561 A CN201310019561 A CN 201310019561A CN 103908440 A CN103908440 A CN 103908440A
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- polyene phosphatidylcholine
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Abstract
The invention relates to a polyene phosphatidylcholine capsule and a preparation method thereof, and belongs to the field of medicine preparations. Polyene phosphatidylcholine has unstable characteristic, different-degree phosphatide hydrolysis is generated during long-term storage of polyene phosphatidylcholine, and leads to content reduction of polyene phosphatidylcholine and generation increase of a toxic substance lysophosphatidylcholine. The invention provides the polyene phosphatidylcholine capsule which comprises polyene phosphatidylcholine and medium-chain triglyceride, and is substantially improved in stability compared with a current marked product Essentiale N. The polyene phosphatidylcholine capsule also comprises one or more pharmaceutically accepted excipient. Additionally, the invention also aims at providing a method for preparing the polyene phosphatidylcholine capsule, and the method is simple in preparation technology and is convenient for industrialized production.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, in particular to a kind of polyene phosphatidylcholine capsule and preparation method thereof.
Background technology
Polyene phosphatidylcholine is a kind of lecithin in high purity extracting from soybean phospholipid, contains a large amount of unsaturated fatty acids, is mainly linoleic acid (accounting for 70%), linolenic acid and oleic acid.Polyene phosphatidylcholine is consistent with important endogenous phospholipid in chemical constitution, and has following physiological function: the form and the stable bile that make the energy balance that impaired liver function and enzyme activity recover normal, regulate liver, promote hepatic tissue regeneration, neutral fat and cholesterol are changed into easy metabolism.At present the listing dosage form of polyene phosphatidylcholine comprises two kinds of injection and capsules, and wherein capsule is the polyene phosphatidylcholine capsule of commodity Essentiale N/Essentiale Forte N (Sanofi-Aventis (Beijing) drugmaker) by name.
Polyene phosphatidylcholine has unsettled feature, in long term storage process, can there is phospholipid hydrolysis in various degree, cause the generation of the decline of polyene phosphatidylcholine content and toxicant LYSO-PHOSPHATIDYLCHOLINE LYSOPC to increase, this is unfavorable for keeping effect of polyene phosphatidylcholine capsule.Therefore, need the polyene phosphatidylcholine capsule of exploitation good stability badly.
Summary of the invention
The object of the present invention is to provide a kind of polyene phosphatidylcholine capsule, it comprises polyene phosphatidylcholine and median chain triglyceride oil, wherein the weight ratio of polyene phosphatidylcholine and median chain triglyceride oil is 228: 22.8～456, preferably, the weight ratio of polyene phosphatidylcholine and median chain triglyceride oil is 228: 45.6～228, preferred, the weight ratio of polyene phosphatidylcholine and median chain triglyceride oil is 228: 912～1368.
Optionally, polyene phosphatidylcholine capsule of the present invention also can comprise one or more pharmaceutically acceptable excipient, such as thickening agent, diluent, antioxidant etc.Thickening agent is selected from one or more in glyceryl monostearate, PEG6000, tween 80, wherein the weight ratio of polyene phosphatidylcholine and thickening agent is 228: 1～200, preferably, the weight ratio of polyene phosphatidylcholine and thickening agent is 228: 10～100, preferred, the weight ratio of polyene phosphatidylcholine and thickening agent is 228: 30～70.Diluent is selected from ethanol, is preferably dehydrated alcohol, and its consumption is restriction especially not, can eligibly select as the case may be.Antioxidant is selected from one or more in alpha-tocopherol, Vitamin E acetate, VC cetylate, BHA, wherein the weight ratio of polyene phosphatidylcholine and antioxidant is 228: 0.01～10, preferably, the weight ratio of polyene phosphatidylcholine and antioxidant is 228: 0.05～1, preferred, the weight ratio of polyene phosphatidylcholine and antioxidant is 228: 0.1～0.5.
In a specific embodiments, polyene phosphatidylcholine capsule of the present invention comprises following components by weight percent:
In another embodiment, polyene phosphatidylcholine capsule of the present invention comprises following components by weight percent:
In another specific embodiments, polyene phosphatidylcholine capsule of the present invention comprises following components by weight percent:
Another object of the present invention is to provide a kind of method of preparing polyene phosphatidylcholine capsule of the present invention, it comprises the following steps:
(1) in dispersion machine, add recipe quantity median chain triglyceride oil;
(2) when stirring, gradation slowly adds the polyene phosphatidylcholine of having pulverized of recipe quantity, and stirs;
(3) when stirring, optionally add one or more pharmaceutically acceptable excipient of recipe quantity, and stir;
(4) carry out capsule charge.
The dispersing speed of wherein controlling step (2) or (3) is 3000-10000rpm, and preferred, rotating speed is 5000-8000rpm.
The temperature of wherein controlling step (2) or (3) is 55-85 DEG C, and preferred, temperature is 55-65 DEG C.
Wherein the indegree that adds of the polyene phosphatidylcholine of step (2) does not limit especially, for example, can be 2-10 time.
Wherein the pharmaceutically acceptable excipient of step (3) is selected from thickening agent, diluent or antioxidant.Thickening agent is selected from one or more in glyceryl monostearate, PEG6000, tween 80; Diluent is selected from ethanol (for example dehydrated alcohol); Antioxidant is selected from one or more in alpha-tocopherol, Vitamin E acetate, VC cetylate, BHA.
Polyene phosphatidylcholine capsule of the present invention is at 40 ± 2 DEG C, RH75% ± 5% is placed 3 months, compared with the Essentiale N/Essentiale Forte N of placing under the same terms, the rate of change of the content of polyene phosphatidylcholine and related substance (LYSO-PHOSPHATIDYLCHOLINE LYSOPC) is all little than Essentiale N/Essentiale Forte N capsule, shows that polyene phosphatidylcholine of the present invention is more stable.In addition, the preparation method technique of polyene phosphatidylcholine capsule of the present invention is simple, is convenient to suitability for industrialized production.
Term " median chain triglyceride oil (MCT) ", claims again midchain oil, pungent certain herbaceous plants with big flowers acid glyceride, is the mixture of the triglyceride of satisfied fatty acid (being mainly sad and certain herbaceous plants with big flowers acid).Median chain triglyceride oil is available from extracting from the hard drying nest of endosperm of Cocoa Cortex cocois radicis (Cocos nucifera L.) or the oil of the dry endosperm of African Elaeis guineensis Jacq. (Elaeis guineensis Jacq.).In the time preparing median chain triglyceride oil from the endosperm of Cocoa Cortex cocois radicis, can use fractionated coconut oil.The satisfied fatty acid of minimum 8-10 the carbon atom with 95% of median chain triglyceride oil.
The content of polyene phosphatidylcholine capsule of the present invention and the assay method of related substance are well known in the art, for example, referring to the high performance liquid chromatography of 2010 editions two annex VD of Pharmacopoeia of People's Republic of China, and combination by reference herein.
Detailed description of the invention
Below in conjunction with specific embodiment, the present invention is conducted further description, but in the present invention, these and other embodiment only do not limit the scope of the invention for illustrating.Equally, the invention is not restricted to any concrete preferred embodiment described herein.It should be appreciated by those skilled in the art that the replacement that is equal to that the technology of the present invention feature is done, or improve accordingly, within still belonging to protection scope of the present invention.
Embodiment 1
To prepare 1000 polyene phosphatidylcholine capsules as example, to dispersion machine (IKA T65, Guangzhou Yi Ke laboratory technique company limited) in add 22.8g median chain triglyceride oil, the cutter head of dispersion machine is immersed in below liquid level, open and stir, rotating speed is 7500rpm, the polyene phosphatidylcholine that 228g has been pulverized divides 5 times and slowly adds and stir, control temperature at 55-65 DEG C, then add 1g glyceryl monostearate and 0.01g alpha-tocopherol and stir, control temperature at 55-65 DEG C, then sampling detects intermediate, finally according to carrying out capsule charge after intermediate cubage loading amount.
Embodiment 2
To prepare 1000 polyene phosphatidylcholine capsules as example, to dispersion machine (IKA T65, Guangzhou Yi Ke laboratory technique company limited) in add 456g median chain triglyceride oil, the cutter head of dispersion machine is immersed in below liquid level, open and stir, rotating speed is 7500rpm, the polyene phosphatidylcholine that 228g has been pulverized divides 5 times and slowly adds and stir, control temperature at 55-65 DEG C, then add 200g glyceryl monostearate and 10g alpha-tocopherol and stir, control temperature at 55-65 DEG C, then sampling detects intermediate, finally according to carrying out capsule charge after intermediate cubage loading amount.
Embodiment 3
To prepare 1000 polyene phosphatidylcholine capsules as example, (IKAT65 in dispersion machine, Guangzhou Yi Ke laboratory technique company limited) add 45.6g median chain triglyceride oil, the cutter head of dispersion machine is immersed in below liquid level, open and stir, rotating speed is 7500rpm, the polyene phosphatidylcholine that 228g has been pulverized divides 5 times and slowly adds and stir, control temperature at 55-65 DEG C, then add 10g glyceryl monostearate and 0.05g alpha-tocopherol and stir, control temperature at 55-65 DEG C, then sampling detects intermediate, finally according to carrying out capsule charge after intermediate cubage loading amount.
Embodiment 4
To prepare 1000 polyene phosphatidylcholine capsules as example, to dispersion machine (IKA T65, Guangzhou Yi Ke laboratory technique company limited) in add 228g median chain triglyceride oil, the cutter head of dispersion machine is immersed in below liquid level, open and stir, rotating speed is 7500rpm, the polyene phosphatidylcholine that 228g has been pulverized divides 5 times and slowly adds and stir, control temperature at 55-65 DEG C, then add 100g glyceryl monostearate and 1g alpha-tocopherol and stir, control temperature at 55-65 DEG C, then sampling detects intermediate, finally according to carrying out capsule charge after intermediate cubage loading amount.
Embodiment 5
To prepare 1000 polyene phosphatidylcholine capsules as example, to dispersion machine (IKA T65, Guangzhou Yi Ke laboratory technique company limited) in add 91.2g median chain triglyceride oil, the cutter head of dispersion machine is immersed in below liquid level, open and stir, rotating speed is 7500rpm, the polyene phosphatidylcholine that 228g has been pulverized divides 5 times and slowly adds and stir, control temperature at 55-65 DEG C, then add 30g glyceryl monostearate and 0.1g alpha-tocopherol and stir, control temperature at 55-65 DEG C, then sampling detects intermediate, finally according to carrying out capsule charge after intermediate cubage loading amount.
Embodiment 6
To prepare 1000 polyene phosphatidylcholine capsules as example, to dispersion machine (IKA T65, Guangzhou Yi Ke laboratory technique company limited) in add 136.8g median chain triglyceride oil, the cutter head of dispersion machine is immersed in below liquid level, open and stir, rotating speed is 7500rpm, the polyene phosphatidylcholine that 228g has been pulverized divides 5 times and slowly adds and stir, control temperature at 55-65 DEG C, then add 70g glyceryl monostearate and 0.5g alpha-tocopherol and stir, control temperature at 55-65 DEG C, then sampling detects intermediate, finally according to carrying out capsule charge after intermediate cubage loading amount.
Embodiment 7
To prepare 1000 polyene phosphatidylcholine capsules as example, to dispersion machine (IKA T65, Guangzhou Yi Ke laboratory technique company limited) in add 114g median chain triglyceride oil, the cutter head of dispersion machine is immersed in below liquid level, open and stir, rotating speed is 7500rpm, the polyene phosphatidylcholine that 228g has been pulverized divides 5 times and slowly adds and stir, control temperature at 55-65 DEG C, then add 50g glyceryl monostearate and 0.3g alpha-tocopherol and stir, control temperature at 55-65 DEG C, then sampling detects intermediate, finally according to carrying out capsule charge after intermediate cubage loading amount.
Embodiment 8
By the polyene phosphatidylcholine capsule of embodiment 1-7 and Essentiale N/Essentiale Forte N capsule, at 40 ± 2 DEG C, RH75% ± 5% is placed 3 months, and result is as follows:
Claims (10)
1. a polyene phosphatidylcholine capsule, it comprises polyene phosphatidylcholine and median chain triglyceride oil, and wherein the weight ratio of polyene phosphatidylcholine and median chain triglyceride oil is 228: 22.8～456.
2. the polyene phosphatidylcholine capsule of claim 1, wherein the weight ratio of polyene phosphatidylcholine and median chain triglyceride oil is 228: 45.6～228.
3. the polyene phosphatidylcholine capsule of claim 2, wherein the weight ratio of polyene phosphatidylcholine and median chain triglyceride oil is 228: 91.2～136.8.
4. the polyene phosphatidylcholine capsule of any one in claim 1-3, it also can comprise one or more pharmaceutically acceptable excipient.
5. the polyene phosphatidylcholine capsule of claim 4, wherein said excipient is selected from thickening agent, diluent or antioxidant.
6. the polyene phosphatidylcholine capsule of claim 5, wherein said thickening agent is selected from one or more in glyceryl monostearate, PEG6000, tween 80, and wherein the weight ratio of polyene phosphatidylcholine and thickening agent is 228: 1～200.
7. the polyene phosphatidylcholine capsule of claim 5, wherein said diluent is selected from ethanol.
8. the polyene phosphatidylcholine capsule of claim 5, wherein said antioxidant is selected from one or more in alpha-tocopherol, Vitamin E acetate, VC cetylate, BHA, and wherein the weight ratio of polyene phosphatidylcholine and antioxidant is 228: 0.01～10.
9. the polyene phosphatidylcholine capsule of any one in claim 1-8, it comprises following components by weight percent:
10. a method of preparing the polyene phosphatidylcholine capsule of any one in claim 1-9, it comprises the following steps:
(1) in dispersion machine, add recipe quantity median chain triglyceride oil;
(2) when stirring, gradation slowly adds the polyene phosphatidylcholine of having pulverized of recipe quantity, and stirs;
(3) when stirring, optionally add one or more pharmaceutically acceptable excipient of recipe quantity, and stir;
(4) carry out capsule charge,
The dispersing speed of wherein controlling step (2) or (3) is 3000-10000rpm, and the temperature of controlling step (2) or (3) is 55-85 DEG C.
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106606780A (en) * | 2015-10-26 | 2017-05-03 | 深圳澳美制药技术开发有限公司 | Polyene phosphatidyl choline composition, polyene phosphatidyl choline soft capsule and preparation methods |
| CN106619560A (en) * | 2015-10-27 | 2017-05-10 | 四川海思科制药有限公司 | Polyene phosphatidyl choline capsule and preparation process thereof |
| CN108778263A (en) * | 2016-03-28 | 2018-11-09 | 维达克制药有限公司 | Stabilizing pharmaceutical composition and application thereof for local application |
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| CN1887279A (en) * | 2006-08-10 | 2007-01-03 | 北京国仁堂医药科技发展有限公司 | Soft polyene phosphatidylcholinecapsule and its prepn process |
| CN101045062A (en) * | 2007-02-04 | 2007-10-03 | 杨喜鸿 | Polyenephophatidylcholine enteric coated preparation, its preparing method and application |
| CN101579310A (en) * | 2009-05-27 | 2009-11-18 | 沈阳药科大学 | Decataxel self-microemulsifying composition and preparation method thereof |
| CN101756907A (en) * | 2009-03-13 | 2010-06-30 | 北京瑞伊人科技发展有限公司 | Oral solid preparation containing polyene phosphatidyl choline and preparation method thereof |
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Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN1887279A (en) * | 2006-08-10 | 2007-01-03 | 北京国仁堂医药科技发展有限公司 | Soft polyene phosphatidylcholinecapsule and its prepn process |
| CN101045062A (en) * | 2007-02-04 | 2007-10-03 | 杨喜鸿 | Polyenephophatidylcholine enteric coated preparation, its preparing method and application |
| CN101756907A (en) * | 2009-03-13 | 2010-06-30 | 北京瑞伊人科技发展有限公司 | Oral solid preparation containing polyene phosphatidyl choline and preparation method thereof |
| CN101579310A (en) * | 2009-05-27 | 2009-11-18 | 沈阳药科大学 | Decataxel self-microemulsifying composition and preparation method thereof |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106606780A (en) * | 2015-10-26 | 2017-05-03 | 深圳澳美制药技术开发有限公司 | Polyene phosphatidyl choline composition, polyene phosphatidyl choline soft capsule and preparation methods |
| CN106606780B (en) * | 2015-10-26 | 2020-05-19 | 深圳澳美制药技术开发有限公司 | Polyene phosphatidyl choline composition, soft capsule and preparation method thereof |
| CN106619560A (en) * | 2015-10-27 | 2017-05-10 | 四川海思科制药有限公司 | Polyene phosphatidyl choline capsule and preparation process thereof |
| CN108778263A (en) * | 2016-03-28 | 2018-11-09 | 维达克制药有限公司 | Stabilizing pharmaceutical composition and application thereof for local application |
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