CN105395499B - A kind of stable glyceride tablet and preparation method thereof - Google Patents
A kind of stable glyceride tablet and preparation method thereof Download PDFInfo
- Publication number
- CN105395499B CN105395499B CN201510886866.1A CN201510886866A CN105395499B CN 105395499 B CN105395499 B CN 105395499B CN 201510886866 A CN201510886866 A CN 201510886866A CN 105395499 B CN105395499 B CN 105395499B
- Authority
- CN
- China
- Prior art keywords
- preparation
- mannose ester
- glyceride
- tablet
- stable
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
Classifications
-
- 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
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Molecular Biology (AREA)
- Medicinal Preparation (AREA)
Abstract
本发明涉及一种稳定的甘糖酯片及其制备方法，属于医药制剂技术领域。所述甘糖酯片包括：甘糖酯和制剂辅料，所述的制剂辅料是填充剂、崩解剂、粘合剂和润滑剂。本发明甘糖酯片具有质量稳定、崩解和溶出迅速、吸收快、生物利用度高、硬度适中、稳定性好、服用方便、制备工艺简单等优点。The invention relates to a stable glyceride tablet and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Said glyceride tablet comprises: glyceride and preparation auxiliary materials, said preparation auxiliary materials are filler, disintegrant, binder and lubricant. The glyceride tablet of the invention has the advantages of stable quality, rapid disintegration and dissolution, rapid absorption, high bioavailability, moderate hardness, good stability, convenient taking, simple preparation process and the like.
Description
Technical field
The present invention relates to tablets more particularly to mannose ester piece and preparation method thereof.
Background technique
Mannose ester be sodium alginate hydrolysis, esterification made of polymannuronate propyl ester sodium sulfate salt, belong to reducing blood lipid,
The marine drug of antithrombotic, for treating hyperlipidemia.Tablet can cover the bad smell of drug, be easy to swallow；Medicine can be improved
The stability and bioavilability of object, can overcome the disadvantages that the deficiency of other solid dosage forms, are widely used.Existing mannose ester piece, which exists, to be collapsed
The solution defect that result of extraction is poor, bioavilability is low, influences its therapeutic effect clinically, collapses therefore, it is necessary to develop
Solve that the time is short, the rapid mannose ester piece of drug-eluting.
Summary of the invention
A kind of the object of the present invention is to provide disintegration times short, rapid mannose ester piece of drug-eluting and preparation method thereof.
1. a kind of stable mannose ester piece, which is characterized in that include mannose ester, filler, disintegrating agent, adhesive and profit
Lubrication prescription.Wherein, the filler is selected from the mixture of sucrose and pregelatinized starch, and the disintegrating agent is selected from cross-linked carboxymethyl
Cellulose, the adhesive are selected from 70% syrup；The lubricant is selected from magnesium stearate.
2. a kind of stable mannose ester piece according to claim 1, it is characterised in that: the mannose ester raw material
Medicine at least contains 90% or more particle of the partial size less than 10 μm.
3. a kind of stable mannose ester piece according to claim 1, it is characterised in that: the pre- glue of the filler
The weight ratio for changing starch and disintegrating agent cross-linked carboxymethyl cellulose is 1:1.
4. a kind of stable mannose ester piece according to claim 1, it is characterised in that: specification is the every of 50mg/ piece
In 1000, by mannose ester 50g, sucrose 36g, pregelatinized starch 4.5g, cross-linked carboxymethyl cellulose 4.5g, 70% syrup, 30 g
And magnesium stearate 0.6g, ethyl alcohol 3.33ml composition.
5. a kind of preparation method of stable mannose ester piece according to claim 4, it is characterised in that: including with
Lower step:
(1) it pre-processes: mannose ester raw material being pulverized using airslide disintegrating mill, raw material particle size D50 after micronization
It is 1~10 μm, sucrose, cross-linked carboxymethyl cellulose reach the requirement of 40 mesh；Starch, pregelatinized starch, magnesium stearate cross 80 mesh
The requirement of sieve；
(2) total mix: magnesium stearate is added to increase mobility after mannose ester and sucrose mixing, mixes, it is auxiliary to add other
Material mixes；
(3) tabletting: 18~26 DEG C of temperature between tabletting, relative humidity are controlled 45~65%.
The present invention can be prepared as follows:
(1) mannose ester raw material is pulverized using airslide disintegrating mill, raw material particle size D50 is 1~10 μ after micronization
M, sucrose, cross-linked carboxymethyl cellulose smash it through 40 meshes, and starch, pregelatinized starch, magnesium stearate cross 80 meshes after crushing,
It is spare；
(2) mixing granulation: weighed mannose ester raw material, cane sugar powder, starch and 1/2 pregelatinized starch are put into wet process and mixed
It closes in granulator, dry-mixed about 5 minutes, the wet mixing of recipe quantity syrup is added, discharging is shut down when material is slightly blocking, with 16 mesh nylon screens
Granulation；
(3) it dries: wet granular is placed in drying tray, thickness generally in 2.5cm, is sent into baking oven, 60~75 DEG C of temperature bakings
It is dry, control loss on drying≤9.0%.Particle dries in the air to room temperature, discharging after drying；
(4) whole grain: 14 mesh nylon screen whole grains of dried particle；
(5) total mix: granule materials are put into three-dimensional motion mixer, and remaining 1/2 pregelatinized starch and stearic acid is added
Magnesium, total mix 10 minutes, discharging；
(6) tabletting, coating, aluminum-plastic packaged.
Specific embodiment
The invention will now be further described with reference to specific embodiments, the advantages and features of the present invention will be with description and
It is apparent.But examples are merely exemplary for these, and it is not intended to limit the scope of the present invention in any way.Those skilled in the art
Member it should be understood that without departing from the spirit and scope of the invention can details to technical solution of the present invention and form into
Row modifications or substitutions, but these modifications and replacement are fallen within the protection scope of the present invention.
Form is described in further detail above content of the invention again by the following examples, but should not manage this
Solution is only limitted to example below for the range of the above-mentioned theme of the present invention, and all technologies realized based on above content of the present invention are belonged to
In the scope of the present invention.
Embodiment 1
Prescription 1(is based on 1000)
Mannose ester (is given money as a gift pure) 50g
Sucrose 36g
Pregelatinized starch 4.5g
Cross-linked carboxymethyl cellulose 4.5g
Magnesium stearate 0.6g
70% syrup about 30g
Ethyl alcohol 3.33ml
Preparation method:
(1) mannose ester raw material is pulverized using airslide disintegrating mill, raw material particle size D50 is 1~10 μ after micronization
M, sucrose, cross-linked carboxymethyl cellulose smash it through 40 meshes, and starch, pregelatinized starch, magnesium stearate cross 80 meshes after crushing,
It is spare；
(2) mixing granulation: weighed mannose ester raw material, cane sugar powder, starch and 1/2 pregelatinized starch are put into wet process and mixed
It closes in granulator, dry-mixed about 5 minutes, the wet mixing of recipe quantity syrup is added, discharging is shut down when material is slightly blocking, with 16 mesh nylon screens
Granulation；
(3) it dries: wet granular is placed in drying tray, thickness generally in 2.5cm, is sent into baking oven, 60~75 DEG C of temperature bakings
It is dry, control loss on drying≤9.0%.Particle dries in the air to room temperature, discharging after drying；
(4) whole grain: 14 mesh nylon screen whole grains of dried particle；
(5) total mix: granule materials are put into three-dimensional motion mixer, and remaining 1/2 pregelatinized starch and stearic acid is added
Magnesium, total mix 10 minutes, discharging；
(6) tabletting, coating, aluminum-plastic packaged.
Embodiment 2
Prescription 2(is based on 1000)
Mannose ester (is given money as a gift pure) 50g
Sucrose 32g
Pregelatinized starch 4.0g
Cross-linked carboxymethyl cellulose 4.0g
Magnesium stearate 0.6g
70% syrup about 30g
Ethyl alcohol 3.33ml
The preparation method is the same as that of Example 1.
Embodiment 3
Prescription 3(is based on 1000)
Mannose ester (is given money as a gift pure) 50g
Sucrose 30g
Pregelatinized starch 5.0g
Cross-linked carboxymethyl cellulose 5.0g
Magnesium stearate 0.6g
70% syrup about 30g
Ethyl alcohol 3.33ml
The preparation method is the same as that of Example 1.
Comparing embodiment 1
Prescription 4(is based on 1000)
Mannose ester (is given money as a gift pure) 50g
Sucrose 36g
Cross-linked carboxymethyl cellulose 4.5g
Magnesium stearate 0.6g
70% syrup about 30g
Ethyl alcohol 3.33ml
The preparation method is the same as that of Example 1.
Comparing embodiment 2
Prescription 5(is based on 1000)
Mannose ester (is given money as a gift pure) 50g
Pregelatinized starch 4.5g
Cross-linked carboxymethyl cellulose 4.5g
Magnesium stearate 0.6g
70% syrup about 30g
Ethyl alcohol 3.33ml
The preparation method is the same as that of Example 1.
1 long-term stable experiment assay of test example
Quasi- listing sample is placed on 25 DEG C of temperature, relative humidity 60% lower 36 months, respectively at 0,3,6,12,24 and 36
It samples, is measured using high performance liquid chromatography (" Chinese Pharmacopoeia " 2015 editions four general rules 0512), using external standard method when the moon
Content is calculated, assay the results are shown in Table 1.The result shows that the stability of active constituent mannose ester is bright in mannose ester piece of the invention
It is aobvious to be better than comparing embodiment.
2 bioavailability study of test example
4 beasle dogs (being male) are administered orally, they are fed respectively with the embodiment of the present invention 1, relatively in fact
The mannose ester piece (25 DEG C of temperature, relative humidity 60% are lower to place 12 months) of example 1, comparing embodiment 2 is applied, dosage is 10.0 μ g/
Only (in terms of mannose ester), the interval time being administered every time is 7 days.After giving drug, blood sample is acquired under different time, and carry out
Mannose ester maximum haemoconcentration (Cmax) and bioavilability (AUC0→48) calculating.Acquisition time be 0h, 0.25h, 0.5h,
1h、2h、4h、6h、8h、12h、24h、32h、48h。
Table 2 provides the mannose ester that 4 beasle dogs are given with the embodiment of the present invention 1, comparing embodiment 1, comparing embodiment 2
The resulting average result of piece.As seen from table, mannose ester maximum haemoconcentration and the biology benefit of mannose ester piece (embodiment 1) of the present invention
Expenditure is apparently higher than comparing embodiment.
It should be noted that the foregoing is merely illustrative of the preferred embodiments of the present invention, it is not intended to restrict the invention
Range, all made any modification, equivalent replacement and improvement etc. within the spirit and principles in the present invention should all include
Within protection scope of the present invention.
The measurement of 3 dissolution rate of test example
It is measured according to dissolution rate and drug release determination method (" Chinese Pharmacopoeia " 2015 editions four general rules, 0,931 second methods).Take this
Invention mannose ester piece each 6, respectively using pH1.2 hydrochloric acid, water as solvent, revolving speed is 75 revs/min, is operated according to methods, respectively at 5,
10, solution is taken to filter in right amount within 15,30,45 minutes, as test solution；Another precision weighs mannose ester reference substance about 25mg, sets
In 25ml measuring bottle, adds the appropriate ultrasound of acetonitrile to make to dissolve, and be diluted to scale, shake up.Precision measures 1ml and sets in 100ml measuring bottle, adds
Dissolution medium is diluted to scale, shakes up, as reference substance solution.Take test solution and control solution respectively, according to it is ultraviolet-can
See spectrophotometry (" Chinese Pharmacopoeia " 2015 editions four general rules 0401), calculate dissolution rate, the results are shown in Table 3, table 4:
As can be seen that dissolution of the mannose ester piece in pH1.2 hydrochloric acid, water obtained by the method for the present invention is uniform, the 45th
Minute can reach higher dissolution rate, hence it is evident that be better than comparing embodiment.Illustrate that mannose ester piece of the invention has quality stabilization, collapses
Solution and dissolution are rapidly, to absorb that fast, bioavilability is high, hardness is moderate, stability is good, convenient to take, preparation process is simple etc. excellent
Point.Meanwhile the preparation method in the method for the present invention is suitable for expanded production.
Claims (1)
1. a kind of mannose ester piece, which is characterized in that specification is every 1000 tablet recipe of 50mg/ piece are as follows:
Mannose ester (is given money as a gift pure) 50g
Sucrose 36g
Pregelatinized starch 4.5g
Cross-linked carboxymethyl cellulose 4.5g
Magnesium stearate 0.6g
70% syrup 30g
Ethyl alcohol 3.33ml
Wherein, the weight ratio of pregelatinized starch and cross-linked carboxymethyl cellulose is 1:1.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510886866.1A CN105395499B (en) | 2015-12-07 | 2015-12-07 | A kind of stable glyceride tablet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510886866.1A CN105395499B (en) | 2015-12-07 | 2015-12-07 | A kind of stable glyceride tablet and preparation method thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN105395499A CN105395499A (en) | 2016-03-16 |
| CN105395499B true CN105395499B (en) | 2019-02-15 |
Family
ID=55461499
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510886866.1A Active CN105395499B (en) | 2015-12-07 | 2015-12-07 | A kind of stable glyceride tablet and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105395499B (en) |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103070841A (en) * | 2013-01-16 | 2013-05-01 | 青岛正大海尔制药有限公司 | Mannose ester sustained release tablets and preparation method thereof |
| CN103099796A (en) * | 2013-02-19 | 2013-05-15 | 青岛正大海尔制药有限公司 | Propylene glycol marinate sulfate-containing sustained-release preparation and preparation method thereof |
| CN103127014A (en) * | 2013-02-19 | 2013-06-05 | 青岛正大海尔制药有限公司 | Propylene glycol mannurate sulfate dispersible tablet and preparation method thereof |
-
2015
- 2015-12-07 CN CN201510886866.1A patent/CN105395499B/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103070841A (en) * | 2013-01-16 | 2013-05-01 | 青岛正大海尔制药有限公司 | Mannose ester sustained release tablets and preparation method thereof |
| CN103099796A (en) * | 2013-02-19 | 2013-05-15 | 青岛正大海尔制药有限公司 | Propylene glycol marinate sulfate-containing sustained-release preparation and preparation method thereof |
| CN103127014A (en) * | 2013-02-19 | 2013-06-05 | 青岛正大海尔制药有限公司 | Propylene glycol mannurate sulfate dispersible tablet and preparation method thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| CN105395499A (en) | 2016-03-16 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN104887641B (en) | Pabuk former times profit cloth gastric floating tablet and preparation method thereof | |
| ES2659716T3 (en) | Process for the manufacture of a pharmaceutical product comprising citric acid, magnesium oxide, potassium bicarbonate and sodium picosulfate, pharmaceutical composition comprising granules obtained by such process and intermediate products thereof | |
| RS59576B1 (en) | Apixaban formulations | |
| Okunlola et al. | Microsphere formulations of ambroxol hydrochloride: influence of Okra (Abelmoschus esculentus) mucilage as a sustained release polymer | |
| CN105412026B (en) | Acotiamide hydrochloride hydrate piece and preparation method thereof | |
| Riley et al. | Surface properties of yam (Dioscorea sp.) starch powders and potential for use as binders and disintegrants in drug formulations | |
| CN104523686B (en) | Acotiamide hydrochloride medicinal preparation and preparation method thereof | |
| CN110420192A (en) | A kind of isosorbide mononitrate sustained release tablets and preparation method | |
| CN103816134B (en) | A kind of valsatan medicinal composition and preparation method thereof | |
| CN102805740A (en) | Rivastigmine capsules and preparation method thereof | |
| CN105395499B (en) | A kind of stable glyceride tablet and preparation method thereof | |
| CN106074423A (en) | Diabecron sustained-release tablet agent and preparation method thereof | |
| JP2576927B2 (en) | Fine grain nucleus | |
| CN104473901B (en) | Cefdinir capsule and preparation method thereof | |
| CN103690508A (en) | Tablet composition containing pitavastatin calcium and preparation method of tablet | |
| CN104069078B (en) | Atorvastatin calcium pharmaceutical composition and preparation method thereof | |
| CN106265557A (en) | Pharmaceutical composition containing ticagrelor | |
| Singh et al. | Pharmaceutical characterization of amoxicillin trihydrate as mucoadhesive microspheres in management of H. pylori | |
| CN105434375A (en) | Levetiracetam tablet and preparation method thereof | |
| CN119074676A (en) | A composition containing acotiamide hydrochloride and preparation method thereof | |
| Kumar et al. | Formulation and evaluation of antidiabetic tablets: Effect of absorption enhancser | |
| Jain et al. | Formulation and evaluation of colon specific tablet containing microsponges of metoprolol succinate. | |
| Noor et al. | Formulation development and in vitro evaluation of immediate release fenofibrate pellets | |
| CN106619646A (en) | Preparation method of tegafur, gimeracil and oteracil potassium composition | |
| CN117338743B (en) | Preparation method of Fudosteine tablet |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| CB02 | Change of applicant information | ||
| CB02 | Change of applicant information |
Address after: 266000 3601 Tuen Jie Road, Qingdao economic and Technological Development Zone, Shandong Applicant after: CP PHARMACEUTICAL (QINGDAO) Co.,Ltd. Address before: 266000 3601 Tuen Jie Road, Qingdao economic and Technological Development Zone, Shandong Applicant before: Qingdao Zhengda Haier Pharmaceutical Co.,Ltd. |
|
| GR01 | Patent grant | ||
| GR01 | Patent grant | ||
| CP03 | Change of name, title or address | ||
| CP03 | Change of name, title or address |
Address after: No.3601 Tuanjie Road, Qingdao Economic and Technological Development Zone, Shandong Province 266426 Patentee after: Qingdao Guoxin Pharmaceutical Co.,Ltd. Country or region after: China Address before: 266000 3601 Tuen Jie Road, Qingdao economic and Technological Development Zone, Shandong Patentee before: CP PHARMACEUTICAL (QINGDAO) Co.,Ltd. Country or region before: China |