CN100522175C - Sustained release tablet of oleanolic acid and its preparation method - Google Patents
Sustained release tablet of oleanolic acid and its preparation method Download PDFInfo
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- CN100522175C CN100522175C CN 200410044333 CN200410044333A CN100522175C CN 100522175 C CN100522175 C CN 100522175C CN 200410044333 CN200410044333 CN 200410044333 CN 200410044333 A CN200410044333 A CN 200410044333A CN 100522175 C CN100522175 C CN 100522175C
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- oleanolic acid
- slow releasing
- releasing tablet
- preparation
- slow
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Abstract
The invention relates to a sustained release tablet of oleanolic acid and its preparation method, wherein the preparation comprises micronized oleanolic acid, slow release material, bulking agent, surface active agent and lubricating agent, the preparing process comprises mixing the micronized oleanolic acid, slow release material, bulking agent, surface active agent, lubricating agent according to a finite proportion, finally employing direct tabletting technique or wet process tabletting method then tabletting.
Description
Technical field
The invention belongs to pharmaceutical preparation, relate to a kind of slow release formulation that is applicable to acute, chronic hepatitis, specifically relate to slow releasing tablet of oleanolic acid and preparation method thereof.
Background technology
(Oleanolic Acid OA) is pentacyclic triterpenoid to oleanolic acid, is distributed widely in plant kingdom, is a kind of natural product chemistry composition.This product has the certain protection effect to hepatic injury, and the serum alanine aminotransferase of rising is descended, and promotes liver cell regeneration, quickens the reparation of slough.It is treatment acute icterohepatitis and the more satisfactory medicine of chronic viral hepatitis, and the low side effect of toxicity is few.
China is at present commercially available has only oleanolic acid ordinary tablet and capsule, and dosage form is single.Because oleanolic acid is fat-soluble by force, the dissolution of its preparation is low, causes the absorption by human body availability poor, and this has influenced giving full play to of its curative effect greatly.On the other hand, oleanolic acid tablet and capsule all needed take medicine in one three times, and this hepatopath to the need long-term prescription has increased a lot of troubles undoubtedly.
Summary of the invention
The objective of the invention is provides slow releasing tablet of a kind of oleanolic acid and preparation method thereof in order to overcome above-mentioned the deficiencies in the prior art.Its only needed take medicine once in one, just can continue 24 hours curative effects, can be used as the liver-protective good medicine of efficient, safety, low toxicity, long-acting, taking convenience.
Pharmaceutical formulation of the present invention is composed of the following components by weight percentage:
A, oleanolic acid 10～75%
B, slow-release material 5～50%
C, filler 15～80%
D, surfactant 0～2%
E, lubricant 0.1～5%
Preparation of the present invention uses the direct compression prepared, also can use tablet forming technique preparation behind the wet granulation.Concrete preparation method is as described below:
(1) direct compression technology:
Principal agent, slow-release material, filler, surfactant are taken by weighing respectively according to quantity.Cross 80 mesh sieve mixings, add again behind the lubricant mixing, promptly get the oleanolic acid slow releasing tablet by the standard quantity tabletting.
(2) wet granule compression tablet technology:
Principal agent, slow-release material, filler, the surfactant amount of connecing are taken by weighing respectively.Cross 80 mesh sieve mixings, with 50～70% alcohol granulations, 60 ℃ of dry back granulate are pressed the standard quantity tabletting behind the adding lubricant mixing, promptly get the oleanolic acid slow releasing tablet.
Principal agent is selected oleanolic acid for use in the slow releasing tablet of the present invention, and its particle diameter is 48～150um, preferred 70～120um.
Slow-release material can be selected one of hypromellose (HPMC), ethyl cellulose (EC), Aquacoat (Surelease), acrylic resin (Eudragit RS100, Eudragit RL100, Eudragit RS30D, Eudragit RL30D, Eudragit RS PO, Eudragit RL PO, Eudragit NE30) or their mixture in the slow releasing tablet of the present invention.
Filler can be selected microcrystalline Cellulose (MCC), lactose, starch, calcium hydrogen phosphate or their mixture in the slow releasing tablet of the present invention.
Optional polyoxyethylene sorbitan monoleate, sodium lauryl sulphate, the sucrose stearate selected of surfactant in the slow releasing tablet of the present invention.
Lubricant can be selected micropowder silica gel, Pulvis Talci, magnesium stearate, Stepanol MG, sodium stearyl fumarate, sucrose stearate etc. for use in the slow releasing tablet of the present invention.
Slow releasing tablet of the present invention only needed take medicine once in one as the ideal medicament of treatment acute, chronic hepatitis, with existing that preparation is compared, good effect, safe, toxicity is low, taking convenience.
Specific embodiment
Embodiment 1:
Pharmaceutical formulation of the present invention is made up of following component:
Oleanolic acid 60.0g
Hypromellose 40.0g
Lactose 120.0g
Sodium lauryl sulphate 1.0g
Magnesium stearate 2.0g
Make 1000 altogether
Adopt the direct compression prepared.Concrete preparation method is as described below: oleanolic acid, hypromellose, lactose, sodium lauryl sulphate take by weighing respectively according to quantity, cross 80 mesh sieve mix homogeneously; Mix with magnesium stearate, the mixing that sieves is pressed the standard quantity tabletting, promptly gets slow releasing tablet again.
Embodiment 2:
Pharmaceutical formulation of the present invention is made up of following component:
Oleanolic acid 60.0g
Hypromellose 35.0g
Ethyl cellulose 10.0g
Lactose 80.0g
Starch 40.0g
Sucrose stearate 4.0g
Make 1000 altogether
Adopt the wet granule compression tablet prepared.Concrete preparation method is as described below: oleanolic acid, hypromellose, ethyl cellulose, lactose, starch are taken by weighing respectively according to quantity, cross 80 mesh sieve mix homogeneously; Use 50% alcohol granulation, behind 60 ℃ of dry 4h, granulate adds sucrose stearate again, presses the standard quantity direct compression behind the mixing, promptly gets the oleanolic acid slow releasing tablet.
Embodiment 3:
Pharmaceutical formulation of the present invention is made up of following component:
Oleanolic acid 180.0g
Eudragit?RS?PO 15.0g
Eudragit?RL?PO 15.0g
Microcrystalline Cellulose 50.0g
Starch 40.0g
Sodium stearyl fumarate 3.0g
Make 1000 altogether
This dosage form adopts direct compression technology, uses the preparation of conventional tablet pharmaceutical equipment.Concrete preparation method is as described below: oleanolic acid, Eudragit RS PO, Eudragit RL PO, microcrystalline Cellulose, starch are taken by weighing respectively according to quantity, cross 80 mesh sieve mix homogeneously, use 50% alcohol granulation, behind 60 ℃ of dry 4h, granulate, add sodium stearyl fumarate, press the standard quantity direct compression behind the mixing, promptly get the oleanolic acid slow releasing tablet.
Through investigating, the release in vitro degree of the oleanolic acid slow releasing tablet that the foregoing description is made is: 1h:10～30%:6h:40～70%; 12h: 〉=75%.
At this preamble, the specific embodiment of preferred embodiment has been described the present invention.Yet should be understood that those skilled in the art can not make various changes or modifications the present invention departing from spirit of the present invention, but these equivalent form of values fall within equally in the application's appended claims institute restricted portion.
Claims (6)
1, a kind of oleanolic acid slow releasing tablet is characterized in that: it is principal agent that medicament active composition adopts micronized oleanolic acid, and other composition is an adjuvant, and pharmaceutical formulation of the present invention is made up of following component by weight percentage:
A, oleanolic acid 10～75%, micronized oleanolic acid particle diameter is 48～150um;
B, slow-release material 5～50%, slow-release material are one or several the combination in hypromellose, ethyl cellulose, Aquacoat and the acrylic resin;
C, filler 15～80%;
D, surfactant 0～2%;
E, lubricant 0.1～5%.
2, oleanolic acid slow releasing tablet as claimed in claim 1 is characterized in that: described filler is one or more the combination in microcrystalline Cellulose, lactose and the starch.
3, oleanolic acid slow releasing tablet as claimed in claim 1 is characterized in that: described surfactant is sodium lauryl sulphate or sucrose stearate.
4, oleanolic acid slow releasing tablet as claimed in claim 1 is characterized in that: described lubricant is micropowder silica gel, magnesium stearate, Stepanol MG, sodium stearyl fumarate or sucrose stearate.
5, a kind of method for preparing oleanolic acid slow releasing tablet as claimed in claim 1; it is characterized in that: said preparation adopts direct compression technology; concrete preparation method is as described below: micronized oleanolic acid, slow-release material, filler, surfactant are taken by weighing according to quantity; mix homogeneously; again with mix lubricant after direct compression, promptly get the oleanolic acid slow releasing tablet.
6, a kind of method for preparing oleanolic acid slow releasing tablet as claimed in claim 1; it is characterized in that: tablet forming technique prepared after said preparation adopted wet granulation; concrete preparation method is as described below: micronized oleanolic acid, slow-release material, filler, surfactant are taken by weighing according to quantity; behind the mix homogeneously with 50～75% alcohol granulations; 60 ℃ of dry back granulate; tabletting after the adding mix lubricant promptly gets the oleanolic acid slow releasing tablet.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410044333 CN100522175C (en) | 2004-05-26 | 2004-05-26 | Sustained release tablet of oleanolic acid and its preparation method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410044333 CN100522175C (en) | 2004-05-26 | 2004-05-26 | Sustained release tablet of oleanolic acid and its preparation method |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1704062A CN1704062A (en) | 2005-12-07 |
| CN100522175C true CN100522175C (en) | 2009-08-05 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200410044333 Expired - Fee Related CN100522175C (en) | 2004-05-26 | 2004-05-26 | Sustained release tablet of oleanolic acid and its preparation method |
Country Status (1)
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| CN (1) | CN100522175C (en) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102106860A (en) * | 2010-09-27 | 2011-06-29 | 林秀坤 | Anti-liver-cancer effect of Oleanolic acid and pharmaceutic preparation |
| CN102114022A (en) * | 2010-09-27 | 2011-07-06 | 林秀坤 | Application of oleanolic acid in resisting colon cancer and pharmaceutical preparations thereof |
| CN102114023A (en) * | 2010-09-27 | 2011-07-06 | 林秀坤 | Oleanolic acid with anti-oophoroma action and pharmaceutical preparations thereof |
| CN102114021A (en) * | 2010-09-27 | 2011-07-06 | 林秀坤 | Application of oleanolic acid in resisting breast cancer and pharmaceutical preparations thereof |
| CN102133219A (en) * | 2010-09-27 | 2011-07-27 | 林秀坤 | Anti-cervical cancer effect of oleanolic acid and pharmaceutical preparation thereof |
| CN102151275A (en) * | 2010-11-07 | 2011-08-17 | 林秀坤 | Pancreatic cancer-resisting effect of oleanolic acid and pharmaceutical preparation of oleanolic acid |
-
2004
- 2004-05-26 CN CN 200410044333 patent/CN100522175C/en not_active Expired - Fee Related
Non-Patent Citations (6)
| Title |
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| 抗肝炎中药研究开发的现状与展望. 肖小河等.传染病药学，第11卷第2期. 2001 |
| 抗肝炎中药研究开发的现状与展望. 肖小河等.传染病药学，第11卷第2期. 2001 * |
| 用固体分散法提高齐墩果酸片溶出速率. 徐晓阳等.黑龙江医药，第10卷第6期. 1997 |
| 用固体分散法提高齐墩果酸片溶出速率. 徐晓阳等.黑龙江医药，第10卷第6期. 1997 * |
| 药剂学. 屠锡德，694，719，1113，1114，人民卫生出版社. 2004 |
| 药剂学. 屠锡德，694，719，1113，1114，人民卫生出版社. 2004 * |
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| Publication number | Publication date |
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| CN1704062A (en) | 2005-12-07 |
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Owner name: HANGZHOU MINSHENG MEDCINE CO., LTD. Free format text: FORMER NAME: HANGZHOU MINSHENG PHARMACEUTICAL GROUP CO. |
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Address after: No. 108 Tong Road, Hangzhou, Zhejiang, Yuhang Patentee after: Hangzhou Minsheng Pharmaceutical Co., Ltd. Address before: No. 108 Tong Road, Hangzhou, Zhejiang, Yuhang Patentee before: Hangzhou Minsheng Pharmaceutical Group Co., Ltd. |
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Owner name: GUANGZHOU RENHENG PHARMACEUTICAL TECHNOLOGY CO., L Free format text: FORMER OWNER: HANGZHOU MINSHENG PHARMACEUTICAL CO., LTD. Effective date: 20150528 |
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Effective date of registration: 20150528 Address after: 510305 west side of the third floor of A4 building, 171 Haizhuqu District Road, Guangdong, Guangzhou Patentee after: Guangzhou Ren Heng Pharmaceutical Technology Co., Ltd Address before: 310011 No. 108 Tong Road, Hangzhou, Zhejiang, Yuhang Patentee before: Hangzhou Minsheng Pharmaceutical Co., Ltd. |
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| CF01 | Termination of patent right due to non-payment of annual fee |