CN108938588A - A kind of Ezetimibe piece - Google Patents
A kind of Ezetimibe piece Download PDFInfo
- Publication number
- CN108938588A CN108938588A CN201810936735.3A CN201810936735A CN108938588A CN 108938588 A CN108938588 A CN 108938588A CN 201810936735 A CN201810936735 A CN 201810936735A CN 108938588 A CN108938588 A CN 108938588A
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- CN
- China
- Prior art keywords
- ezetimibe
- pectin
- ezetimibe piece
- piece
- piece according
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
Abstract
The present invention relates to pharmaceutical technology fields, more specifically, it is related to a kind of Ezetimibe piece, it is made of the raw material of following weight percents: Ezetimibe: 12%, lactose: 40%, polyethylene glycol: 11%, filler: 13%, lubricant: 8%, pectin: 5%, carrotene: 1%, violaxanthin: 2%, cauline leaf is containing calcium oxalate: 5%, disintegrating agent: 3%, Ezetimibe piece disclosed by the invention can be segmented to be dissolved in human body, improves safety of Ezetimibe piece during medication, and improves Ezetimibe piece absorbed absorptivity in human body.
Description
Technical field
The present invention relates to pharmaceutical technology fields, more particularly, to a kind of Ezetimibe piece.
Background technique
Ezetimibe is white crystalline powder, readily soluble in ethyl alcohol, methanol and acetone, almost insoluble in water, and fusing point is about
It is 160 DEG C, stable at room temperature, Ezetimibe piece clinic main ingredient is used for primary hypercholesterolemia, and Ezetimibe mainly leads to
It crosses and acts on small intestine realization to the inhibiting effect of cholesterol absorption, the absorption of other nutriments will not be impacted, patient
Other lipid-lowering medicines are better than to its tolerance, adverse reaction is less.
Wherein, Ezetimibe belongs to II class medicine in BCS categorizing system, has the characteristics that dissolubility is low, permeability is high,
Currently, tablet usually is made in Ezetimibe, for Ezetimibe tablet during taking, drug will be dissolved in gastric juice just can be by
Absorb and then play curative effect, currently, the otherness that commercially available tablet discharges in gastric juice is larger, the fluctuation of body absorption situation compared with
Greatly, the availability of the medicine is adversely affected, therefore, it is necessary to be improved in terms of auxiliary material, to reduce preparation release
Otherness improves the stability of bioavilability, has great importance in the research of Ezetimibe.
However, release difference of the Ezetimibe piece in the prior art in gastric juice is larger, body absorption fluctuation is larger,
The RSD of the dissolution rate of Ezetimibe piece in the prior art is bigger simultaneously, so as to cause Ezetimibe piece in human body
The drug effect in portion can not the release of continued smooth will lead to if the dissolution rate of Ezetimibe piece is too fast to human organ and group
The injury knitted pharmacologically has certain side effect.
It is therefore proposed that a kind of Ezetimibe piece to solve the above problems is actually necessary.
Summary of the invention
The present invention in order to overcome at least one of the drawbacks of the prior art described above (deficiency), provides a kind of Ezetimibe piece.
In order to solve the above technical problems, technical scheme is as follows: a kind of Ezetimibe piece, by following weight percent
The raw material of ratio is made:
12% lactose 40% of Ezetimibe
11% filler 13% of polyethylene glycol
8% pectin 5% of lubricant
1% violaxanthin 2% of carrotene
Cauline leaf 5% disintegrating agent 3% containing calcium oxalate.
Further, the pectin is jelly powder.
Further, the cauline leaf is dried by the cauline leaf of polygonaceae plant garden sorrel containing calcium oxalate and is milled.
Further, the filler is mannitol or starch.
Further, the lubricant is made of acetone, sodium stearyl fumarate and glycerol, weight percent 6:
1:3。
Further, the disintegrating agent is made of crospovidone, low-substituted hydroxypropyl cellulose, weight percent
For 7:3.
Further, the carrotene is beta carotene.
Compared with prior art, the beneficial effect of technical solution of the present invention is: Ezetimibe piece can be segmented in human body into
Row dissolution, improves safety of Ezetimibe piece during medication, and improve Ezetimibe piece and be absorbed in human body
Absorptivity.
Detailed description of the invention
Fig. 1 is the dissolution curve of Ezetimibe piece when not having to add pectin in the present invention.
Fig. 2 is addition concentration of pectin in the present invention when being 2%, the dissolution curve of Ezetimibe piece.
When Fig. 3 is that addition concentration of pectin is 5% in the present invention, the dissolution curve of Ezetimibe piece.
When Fig. 4 is that addition concentration of pectin is 8% in the present invention, the dissolution curve of Ezetimibe piece.
Specific embodiment
The attached figures are only used for illustrative purposes and cannot be understood as limitating the patent；In order to better illustrate this embodiment, attached
Scheme certain components to have omission, zoom in or out, does not represent the size of actual product；To those skilled in the art,
The omitting of some known structures and their instructions in the attached drawings are understandable.
In the description of the present invention, it should be noted that unless otherwise clearly defined and limited, term " installation " " connects
Connect " it shall be understood in a broad sense, for example, it may be being fixedly connected, it may be a detachable connection, or be integrally connected；It can be machine
Tool connection, is also possible to be electrically connected；It can be directly connected, be also possible to be indirectly connected with by intermediary, it may be said that two
Connection inside element.For the ordinary skill in the art, above-mentioned term can be understood in the present invention with concrete condition
Concrete meaning.The following further describes the technical solution of the present invention with reference to the accompanying drawings and examples.
Embodiment one
A kind of Ezetimibe piece, is made of the raw material of following weight percents:
12% lactose 40% of Ezetimibe
11% filler 18% of polyethylene glycol
Lubricant 8%
1% violaxanthin 2% of carrotene
Cauline leaf 5% disintegrating agent 3% containing calcium oxalate
According to the method measurement under Chinese Pharmacopoeia annex item, paddle method, temperature is 37 DEG C, and revolving speed is 50 revs/min, dissolution
Medium is that 500ml contains in the 0.1M hydrochloric acid solution of 0.45% lauryl sodium sulfate, with UV detector in wavelength
It is detected under 233nm, obtains the dissolution determination in embodiment one as a result, and forming dissolution curve as shown in Figure 1.
In the present embodiment, due to there is no addition pectin, and the dosage of filler is increased, still, since filler is
Made of mannitol or starch, therefore, when Ezetimibe piece under clothes for patients, gastric acid and Ezetimibe piece interact, filling
Agent is easy to decompose so that Ezetimibe largely discharges within the short time after taking, and largely discharged in the short time according to folding wheat
Cloth is easy to form damage to the gastric mucosa and enteron aisle of human body, and since pectin substance is one of plant cell wall component, it is present in
In intercellular layer between flanking cell wall, play the coherent effect of cell, therefore, pectin can play protection Ezetimibe
Effect so that Ezetimibe slow release under the action of gastric acid, to protect the health of human body viscera, further, since
Pectin has certain nourishing the stomach effect, can mitigate and eat used time side effects of pharmaceutical drugs.
Embodiment two
A kind of Ezetimibe piece, is made of the raw material of following weight percents:
12% lactose 40% of Ezetimibe
11% filler 16% of polyethylene glycol
8% pectin 2% of lubricant
1% violaxanthin 2% of carrotene
Cauline leaf 5% disintegrating agent 3% containing calcium oxalate
According to the method measurement under Chinese Pharmacopoeia annex item, paddle method, temperature is 37 DEG C, and revolving speed is 50 revs/min, dissolution
Medium is that 500ml contains in the 0.1M hydrochloric acid solution of 0.45% lauryl sodium sulfate, with UV detector in wavelength
It is detected under 233nm, obtains the dissolution determination in embodiment one as a result, and forming the dissolution curve as shown in Fig. 2
Figure.
In the present embodiment, 2% pectin is added in Ezetimibe piece, and increases by 3% filler, due to the use of pectin
Measure smaller, therefore, Ezetimibe is cracking under the action of gastric acid just to react with pectin, but relative to embodiment one,
Also play the effect of slow release.
Embodiment three
A kind of Ezetimibe piece, is made of the raw material of following weight percents:
12% lactose 40% of Ezetimibe
11% filler 13% of polyethylene glycol
8% pectin 5% of lubricant
1% violaxanthin 2% of carrotene
Cauline leaf 5% disintegrating agent 3% containing calcium oxalate
According to the method measurement under Chinese Pharmacopoeia annex item, paddle method, temperature is 37 DEG C, and revolving speed is 50 revs/min, dissolution
Medium is that 500ml contains in the 0.1M hydrochloric acid solution of 0.45% lauryl sodium sulfate, with UV detector in wavelength
It is detected under 233nm, obtains the dissolution determination in embodiment one as a result, shown in specific ginseng table 1, and form such as Fig. 3
Shown in dissolution curve.
In the present embodiment, 5% pectin is added in Ezetimibe piece, Ezetimibe can be wrapped in piece by 5% tartaric acid
In agent, by with just gradually discharged after the reacting of gastric acid, therefore, the Ezetimibe being dissolved in filler can be made to release one step ahead
It puts after acting on human body, then slowly discharges the Ezetimibe wrapped up by tartaric acid, release time is long, the suction convenient for human body to drug
It receives, convenient for protecting the enteron aisle of human body.
Example IV
A kind of Ezetimibe piece, is made of the raw material of following weight percents:
12% lactose 40% of Ezetimibe
11% filler 10% of polyethylene glycol
8% pectin 8% of lubricant
1% violaxanthin 2% of carrotene
Cauline leaf 5% disintegrating agent 3% containing calcium oxalate
According to the method measurement under Chinese Pharmacopoeia annex item, paddle method, temperature is 37 DEG C, and revolving speed is 50 revs/min, dissolution
Medium is that 500ml contains in the 0.1M hydrochloric acid solution of 0.45% lauryl sodium sulfate, with UV detector in wavelength
It is detected under 233nm, obtains the dissolution determination in embodiment one as a result, shown in specific ginseng table 1, and form such as Fig. 1
Shown in dissolution curve.
In the present embodiment, the pectin that 8% is added in Ezetimibe piece, causes to fill due to increasing for tartaric acid content
The reduction of object, therefore, at the beginning when Ezetimibe release slowly, be unfavorable for quickly treating human body, in addition, excessive fruit
Acid leads to a large amount of releases of Ezetimibe after medication a period of time, is unfavorable for the intestinal health of human body.
Each embodiment dissolution determination result
| Embodiment | Embodiment one | Embodiment two | Embodiment three | Example IV |
| Time 5 minutes | 5% | 8 | 8 | 8 |
| Time 10 minutes | 38 | 29 | 16 | 16 |
| Time 15 minutes | 78 | 51 | 51 | 36 |
| Time 20 minutes | 95 | 70 | 58 | 58 |
| Time 25 minutes | 100 | 88 | 88 | 72 |
| Time 30 minutes | -------- | 100 | 93 | 92 |
| Time 35 minutes | -------- | -------- | 100 | 100 |
It to sum up tests, can be clear that, one Ezetimibe solution rate of embodiment is too fast, it is easy to damage the stomach of human body,
Embodiment two extends 5 minutes release time after being added to 2% pectin, and in the third embodiment, pass through addition 5%
After pectin, releasing by parts can be played the role of, and in example IV, after 8% pectin is added, segmentation dissolution is not occurred
The phenomenon that, it dissolves out slower.
In figure, description positional relationship only for illustration, should not be understood as the limitation to this patent；Obviously, this hair
Bright the above embodiment is merely an example for clearly illustrating the present invention, and is not to embodiments of the present invention
It limits.For those of ordinary skill in the art, other different forms can also be made on the basis of the above description
Variation or variation.There is no necessity and possibility to exhaust all the enbodiments.It is all the spirit and principles in the present invention it
Any modifications, equivalent replacements, and improvements made by interior etc., should all be included in the scope of protection of the claims of the present invention.
Claims (7)
1. a kind of Ezetimibe piece, which is characterized in that be made of the raw material of following weight percents:
12% lactose 40% of Ezetimibe
11% filler 13% of polyethylene glycol
8% pectin 5% of lubricant
1% violaxanthin 2% of carrotene
Cauline leaf 5% disintegrating agent 3% containing calcium oxalate.
2. Ezetimibe piece according to claim 1, which is characterized in that the pectin is jelly powder.
3. Ezetimibe piece according to claim 1, which is characterized in that the cauline leaf is containing calcium oxalate by polygonaceae plant garden sorrel
Cauline leaf dry and be milled.
4. Ezetimibe piece according to claim 1, which is characterized in that the filler is mannitol or starch.
5. Ezetimibe piece according to claim 1, which is characterized in that the lubricant is by acetone, stearic furmaric acid
Sodium and glycerol composition, weight percent 6:1:3.
6. Ezetimibe piece according to claim 1, which is characterized in that the disintegrating agent is by crospovidone, low substitution
Hydroxypropyl cellulose composition, weight percent 7:3.
7. Ezetimibe piece according to claim 1, which is characterized in that the carrotene is beta carotene.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810936735.3A CN108938588B (en) | 2018-08-16 | 2018-08-16 | Ezetimibe tablet |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810936735.3A CN108938588B (en) | 2018-08-16 | 2018-08-16 | Ezetimibe tablet |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN108938588A true CN108938588A (en) | 2018-12-07 |
| CN108938588B CN108938588B (en) | 2021-06-22 |
Family
ID=64469529
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201810936735.3A Active CN108938588B (en) | 2018-08-16 | 2018-08-16 | Ezetimibe tablet |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN108938588B (en) |
Citations (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1744827A (en) * | 2003-01-31 | 2006-03-08 | 帝斯曼知识产权资产管理有限公司 | The composition that comprises the novelty of carotenoid |
| CN102227212A (en) * | 2008-09-30 | 2011-10-26 | 力奇制药公司 | Novel ezetimibe formulations |
| WO2013066279A1 (en) * | 2011-10-13 | 2013-05-10 | Mahmut Bilgic | Solid dosage forms comprising ezetimibe |
| CN103655481A (en) * | 2012-09-18 | 2014-03-26 | 江苏柯菲平医药有限公司 | Preparation method of ezetimibe orally-taken preparation |
| WO2015082562A1 (en) * | 2013-12-05 | 2015-06-11 | Alrise Biosystems Gmbh | Process for the production of drug formulations for oral administration |
| CN105106157A (en) * | 2015-09-25 | 2015-12-02 | 青岛华之草医药科技有限公司 | Ezetimibe composition tablets for treating hyperlipidemia |
| CN105106135A (en) * | 2015-09-28 | 2015-12-02 | 青岛华之草医药科技有限公司 | Ezetimibe pharmaceutical composition dry suspension for treatment of cardio-cerebral vascular system diseases |
| CN105213340A (en) * | 2015-10-29 | 2016-01-06 | 无锡福祈制药有限公司 | A kind of Ezetimibe sheet and preparation method thereof |
| CN108366971A (en) * | 2015-12-09 | 2018-08-03 | 阿尔特刚股份有限公司 | With the soft capsule discharged independent of pH |
-
2018
- 2018-08-16 CN CN201810936735.3A patent/CN108938588B/en active Active
Patent Citations (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1744827A (en) * | 2003-01-31 | 2006-03-08 | 帝斯曼知识产权资产管理有限公司 | The composition that comprises the novelty of carotenoid |
| CN102227212A (en) * | 2008-09-30 | 2011-10-26 | 力奇制药公司 | Novel ezetimibe formulations |
| WO2013066279A1 (en) * | 2011-10-13 | 2013-05-10 | Mahmut Bilgic | Solid dosage forms comprising ezetimibe |
| CN103655481A (en) * | 2012-09-18 | 2014-03-26 | 江苏柯菲平医药有限公司 | Preparation method of ezetimibe orally-taken preparation |
| WO2015082562A1 (en) * | 2013-12-05 | 2015-06-11 | Alrise Biosystems Gmbh | Process for the production of drug formulations for oral administration |
| CN105106157A (en) * | 2015-09-25 | 2015-12-02 | 青岛华之草医药科技有限公司 | Ezetimibe composition tablets for treating hyperlipidemia |
| CN105106135A (en) * | 2015-09-28 | 2015-12-02 | 青岛华之草医药科技有限公司 | Ezetimibe pharmaceutical composition dry suspension for treatment of cardio-cerebral vascular system diseases |
| CN105213340A (en) * | 2015-10-29 | 2016-01-06 | 无锡福祈制药有限公司 | A kind of Ezetimibe sheet and preparation method thereof |
| CN108366971A (en) * | 2015-12-09 | 2018-08-03 | 阿尔特刚股份有限公司 | With the soft capsule discharged independent of pH |
Non-Patent Citations (2)
| Title |
|---|
| PORNSAK SRIAMORNSAK等: ""Swelling and erosion of pectin matrix tablets and their impact on drug release behavior"", 《EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS》 * |
| 冷柏榕、严相平: "影响依折麦布片溶出度的关键工艺参数研究", 《中国药业》 * |
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| CN108938588B (en) | 2021-06-22 |
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