CN103142480A - Febuxostat nanoliposome and purpose - Google Patents
Febuxostat nanoliposome and purpose Download PDFInfo
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- CN103142480A CN103142480A CN 201110402036 CN201110402036A CN103142480A CN 103142480 A CN103142480 A CN 103142480A CN 201110402036 CN201110402036 CN 201110402036 CN 201110402036 A CN201110402036 A CN 201110402036A CN 103142480 A CN103142480 A CN 103142480A
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- febuxostat
- liposome
- nanoliposome
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- medicine
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Abstract
The invention relates to a field of medicinal preparation, especially to a preparation method and a purpose of febuxostat nanoliposome. The preparation technology comprises steps of preparation of blank liposome and the febuxostat nanoliposome, technology optimization, etc. The febuxostat nanoliposome provided by the invention is high in entrapment rate, (e.g., the febuxostat nanoliposome can wrap more than 10 times of drugs than single-chamber liposomes do), good in stability, and simple in preparation technology, and can be used to treat chronic hyperuricemia (gout).
Description
Technical field
The present invention relates to field of pharmaceutical preparations, be specifically related to the nanometer liposome preparation method and application of Febuxostat.
Background technology
Liposome technology be called " biological missile " the 4th generation the target administration technology, liposome belongs to nanoscopic drug carriers.Liposome has the following advantages as the carrier of medicine: 1. liposome vectors can be protected enveloped; 2. can effectively control drug release; 3. can by changing liposome size and electric charge, can control medicine in in-house distribution and the clearance rate in blood; 4. can change certain physical factor, such as the pH that changes the medication part, diseased region temperature etc. can obviously change the permeability of liposome membrane, makes liposome optionally discharge medicine; 5. the ligand modified liposome such as available monoclonal antibody, make the drug targeting diseased region; 6. mainly by reticuloendothelial system phagocytic, can activate the autoimmune function of body after liposome advances in human body, thereby improve the therapeutic index of medicine, reduce the therapeutic dose of medicine and reduce drug toxicity; 7. liposome itself is to human body avirulence and immunosuppressive action.Utilize this technology large quantities of known high toxicity active medicines can be applied to clinical treatment safely and effectively, anticarcinogen, Tri-Biocin, antimycotic medicine, parasiticide class medicine, protein or polypeptide drug are wherein arranged, greatly improve the clinical treatment level, alleviated patient's slight illness.
Gout be too much to reach kidney removing ability and descend owing to producing uric acid in body, the uric acid body accumulation causes urate crystal in the joint and each internal organs deposition.Therefore, the means that the treatment of gout is taked usually are: promote urate excretion and suppress uricopoiesis, and adopt adequate measure to improve related symptoms.In body, the generation of uric acid is relevant with purine metabolism, in the final step of purine metabolism, hypoxanthine generates xanthine under the effect of xanthine oxidoreductase enzyme (XOR), more further generates uric acid, and the activity that suppresses this enzyme can effectively reduce the generation of uric acid.Febuxostat is the present XOR inhibitor of up-to-date development in the world, and it acts on this oxidase by high selectivity ground, reduces in body uric acid synthetic, the reduction uric acid concentration, thus effectively treat the ventilation disease.Yet the life-time service Febuxostat has very large toxic and side effects, and its main toxicity target organs is kidney, bladder, thyroid, liver and hemopoietic system.The present invention utilizes the monopolizing characteristic of liposome, toxic and side effects is large, poor stability, the fast Febuxostat of degraded are wrapped in the microgranule that diameter is nanoscale (70-190nm) in blood, this microgranule has the class cellularity, larger according to vascular endothelial cell gap, body foci position, liposome medicament can see through this gap and arrive lesions position, release is piled up by section in focus, thereby reaches targeted delivery of drugs.The liposome major auxiliary burden is phospholipid, and that phospholipid is eliminated in blood is very slow, so liposome medicament is long in blood circulation system retention time, makes lesions position obtain the fully effect for the treatment of, improve the therapeutic index of medicine, effectively reduced the toxic and side effects of Febuxostat to the ventilation patient.
Summary of the invention
The present invention utilizes the monopolizing characteristic of liposome, toxic and side effects is large, poor stability, the fast Febuxostat of degraded are wrapped in the microgranule that diameter is nanoscale (70-190nm) in blood, microgranule mainly is comprised of Febuxostat, Ovum Gallus domesticus Flavus lecithin, cholesterol, antioxidant, buffer agent etc.This preparation technology comprises: 1. the blank liposome for preparing ideal dimensions (70-190 nm); 2. load Febuxostat to nanometer liposome by the pH gradient; 3. separate by ultrafilter membrane and buffer being free in the outer Febuxostat of liposome; 4. successively pass through the filter sterilised of 0.6 μ m and 0.22 μ m.The Febuxostat nanometer liposome envelop rate high (for example can wrap up the medicine of 10 times than unilamelar liposome) of the present invention's preparation, and good stability, preparation is simple more.Be used for the treatment of the too high disease of chronic uric acid (gout).
Claims (2)
1. the nano-lipid preparation of Febuxostat.
2. the nanometer liposome of Febuxostat is used for the treatment of the too high disease of chronic uric acid (gout).
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201110402036 CN103142480A (en) | 2011-12-07 | 2011-12-07 | Febuxostat nanoliposome and purpose |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201110402036 CN103142480A (en) | 2011-12-07 | 2011-12-07 | Febuxostat nanoliposome and purpose |
Publications (1)
| Publication Number | Publication Date |
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| CN103142480A true CN103142480A (en) | 2013-06-12 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 201110402036 Pending CN103142480A (en) | 2011-12-07 | 2011-12-07 | Febuxostat nanoliposome and purpose |
Country Status (1)
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| CN (1) | CN103142480A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105748410A (en) * | 2014-12-15 | 2016-07-13 | 北京阜康仁生物制药科技有限公司 | Preparation technique for improving dissolution rate and stability of insoluble drug |
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2011
- 2011-12-07 CN CN 201110402036 patent/CN103142480A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105748410A (en) * | 2014-12-15 | 2016-07-13 | 北京阜康仁生物制药科技有限公司 | Preparation technique for improving dissolution rate and stability of insoluble drug |
| CN105748410B (en) * | 2014-12-15 | 2020-06-05 | 北京阜康仁生物制药科技有限公司 | Preparation technology for improving dissolution rate and stability of insoluble drug |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| DD01 | Delivery of document by public notice |
Addressee: Wuhan forest road science and Technology Co., Ltd. Office Document name: Notification that Application Deemed not to be Proposed |
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| ASS | Succession or assignment of patent right |
Owner name: WUHAN LINLU TECHNOLOGY CO., LTD. Free format text: FORMER OWNER: ZHENGZHOU JINHONG RUIDA MEDICAL TECHNOLOGY CO., LTD. Effective date: 20150227 |
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| C41 | Transfer of patent application or patent right or utility model | ||
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Free format text: CORRECT: ADDRESS; FROM: 450000 ZHENGZHOU, HENAN PROVINCE TO: WUHAN, HUBEI PROVINCE |
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| TA01 | Transfer of patent application right |
Effective date of registration: 20150227 Address after: No. 666, hi tech Avenue, East Lake Development Zone, Hubei, Wuhan, B1, C, D, B, R & D building Applicant after: Wuhan forest road Technology Co., Ltd. Address before: High tech Zone bamboo street Zhengzhou city Henan province 450000 Zhengzhou City No. 100 Yuan Sheng and Xiangyuan No. 12 unit 5 Building No. 88 Applicant before: Zhengzhou Jinhong Ruida Medical Technology Co., Ltd. |
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| C05 | Deemed withdrawal (patent law before 1993) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20130612 |