CN107773561A - A kind of methanesulfonic acid Lome Tapai capsule and preparation method thereof - Google Patents
A kind of methanesulfonic acid Lome Tapai capsule and preparation method thereof Download PDFInfo
- Publication number
- CN107773561A CN107773561A CN201610708603.6A CN201610708603A CN107773561A CN 107773561 A CN107773561 A CN 107773561A CN 201610708603 A CN201610708603 A CN 201610708603A CN 107773561 A CN107773561 A CN 107773561A
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- CN
- China
- Prior art keywords
- methanesulfonic acid
- acid lome
- lome tapai
- tapai
- capsule
- 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.)
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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
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4468—Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
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- Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Preparation (AREA)
Abstract
The present invention relates to a kind of methanesulfonic acid Lome Tapai capsule and preparation method thereof.The methanesulfonic acid Lome Tapai capsule of the present invention, comprising active component methanesulfonic acid Lome Tapai and as disintegrant and the hydroxypropylcellulose of adhesive.The present invention can not only be disintegrated rapidly and Fast Stripping, and technique is simple, steady quality.
Description
Technical field
The invention belongs to pharmaceutical technology field, is related to a kind of pharmaceutical formulation and preparation method thereof, is specifically related to one
Kind methanesulfonic acid Lome Tapai capsule and preparation method thereof.
Background technology
Methanesulfonic acid Lome Tapai (Lomitapidemesylate) is that the oral small molecule developed by Aegerion companies is micro-
Plastochondria triglycerides transport protein (MTP) inhibitor, in December, 2012 are ratified to list by U.S. FDA, trade name Lojuxda,
It is used to treat hypercholesterolia, including primary hypercholesterolemia and familial form hypercholesterolemia for treating.Its chemistry
Entitled N- (2,2,2- trifluoroethyl) -9- [4- [4- [4,-(trifluoromethyl) [1,1,-biphenyl -2- base] formamido] piperidines -
1- yls] butyl] -9-H- fluorenyl -9- carboxamide mesylate salts.
Methanesulfonic acid Lome Tapai is a kind of medicine of the indissoluble in water and acid, using the preparation method result of extraction of routine
Difference, quality stability are bad.Pharmaceutically, in order to accelerate dissolution, generally use reduces raw material particle size and adds suitable disintegrant,
To obtain the effect of rapid disintegration and Fast Stripping.
It is easily tacky after methanesulfonic acid Lome Tapai raw material moisture absorption, cause hardness to become big, cause disintegration difficult, dissolution rate becomes
Slowly.So if auxiliary material selects bad, easy moisture absorption, quality is unstable during causing finished product storage.
The content of the invention
In view of the deficiencies of the prior art, the present invention provides a kind of methanesulfonic acid Lome Tapai capsule and preparation method thereof, the first
Sulfonic acid Lome Tapai capsule can not only be disintegrated rapidly and Fast Stripping, and technique is simple, steady quality.
The present invention is achieved by the following technical solutions：
A kind of methanesulfonic acid Lome Tapai capsule, includes active component methanesulfonic acid Lome Tapai and pharmaceutic adjuvant, it is characterised in that medicine
By the use of accessory package containing the hydroxypropylcellulose as disintegrant and adhesive.
Further, described methanesulfonic acid Lome Tapai capsule, it is characterised in that include the group of following weight percentage
Point：20% methanesulfonic acid Lome Tapai, 30% hydroxypropylcellulose, 40% filler, 5% cosolvent, 5% lubricant.
Further, described methanesulfonic acid Lome Tapai passes through 200 mesh sieves.
Further, hydroxypropylcellulose, filler and lubricant pass through 80 mesh sieves.
Preferably, the filler is from the one or more in microcrystalline cellulose, pregelatinized starch, lactose.
Preferably, the cosolvent selects lauryl sodium sulfate.
Preferably, the lubricant is from the one or more in magnesium stearate, talcum powder, silica.
The preparation method of described methanesulfonic acid Lome Tapai capsule, is operated as follows：
1）Methanesulfonic acid Lome Tapai is crossed into 200 mesh sieves, filler, hydroxypropylcellulose cross 80 mesh sieves, are well mixed, obtain methanesulfonic acid
Lome Tapai premixing flour；
2）Compound concentration is 5%~60% ethanol solution, and its dosage is methanesulfonic acid Lome Tapai, hydroxypropylcellulose, filler, helped
The 45%~55% of solvent and lubricant gross weight；The cosolvent ethanol solution of half weight is dissolved, obtains the ethanol of cosolvent
Solution；
3）Methanesulfonic acid Lome Tapai premixing flour is placed in wet granulator, the ethanol solution of cosolvent is added, according to material
Granulating situation adds remaining ethanol solution and purified water, and the wet granular of 14 mesh sieves was made in stirring；
4）Wet granular is dried；Whole grain；
5）Particle is mixed with crossing together with 80 mesh sieve lubricants, fills, produces methanesulfonic acid Lome Tapai capsule.
Further, the filler is microcrystalline cellulose, and the cosolvent is lauryl sodium sulfate, the lubricant
It is magnesium stearate.
Further, described（4）Step, it is dried using 50 DEG C~60 DEG C of temperature, the moisture of particle after drying
Control is below 1.0%.
The beneficial effect that the present invention reaches is：
（1）The present invention is from hydroxypropylcellulose as disintegrant, and under conditions of same humidity, the equilibrium water of hydroxypropylcellulose contains
Amount only has the half of PVP class material, it is moist to reduce drawing for product so that product quality in prolonged storage is more steady
It is fixed；
（2）The particle diameter of bulk drug has a great impact to the dissolution rate of product, by being carried out to the particle diameter of methanesulfonic acid Lome Tapai
Control, using the methanesulfonic acid Lome Tapai less than 200 mesh particle diameters, can make product in the case of without using super-disintegrant
With good dissolution rate.
（3）The production process of the methanesulfonic acid Lome Tapai capsule of the present invention is simple, and product quality is homogeneous, good in economic efficiency,
The steady quality in prolonged storage, the requirement of Clinical practice can be met.
Embodiment
The preferred embodiments of the present invention are illustrated below, it will be appreciated that preferred embodiment described herein is only used
In the description and interpretation present invention, it is not intended to limit the present invention.
In following examples, adhesive and disintegrant of the hydroxypropylcellulose as the present invention, microcrystalline cellulose, pregelatinated form sediment
Powder, lactose are as filler, and lauryl sodium sulfate is as cosolvent, and magnesium stearate, talcum powder, silica are as lubrication
Agent.
Embodiment 1
Methanesulfonic acid Lome Tapai 20g
Hydroxypropylcellulose 30g
Microcrystalline cellulose 40g
Lauryl sodium sulfate 5g
Magnesium stearate 5g
It is made 1000
Preparation method：
1）Methanesulfonic acid Lome Tapai is crossed into 200 mesh sieves, filler, hydroxypropylcellulose cross 80 mesh sieves, are well mixed, obtain methanesulfonic acid
Lome Tapai premixing flour；
2）Compound concentration is 60% ethanol solution, and its dosage is methanesulfonic acid Lome Tapai, hydroxypropylcellulose, filler, cosolvent
With the 55% of lubricant gross weight；The cosolvent ethanol solution of half weight is dissolved, obtains the ethanol solution of cosolvent；
3）Methanesulfonic acid Lome Tapai premixing flour is placed in wet granulator, the ethanol solution of cosolvent is added, according to material
Granulating situation adds remaining ethanol solution and purified water, and the wet granular of 14 mesh sieves was made in stirring；
4）Wet granular is dried；Whole grain；
5）Particle is mixed together with the lubricant for crossing 80 mesh sieves, fills, produces methanesulfonic acid Lome Tapai capsule.
Embodiment 2
Methanesulfonic acid Lome Tapai 20g
Hydroxypropylcellulose 30g
Pregelatinized starch 40g
Lauryl sodium sulfate 5g
Magnesium stearate 5g
It is made 1000
Preparation method is the same as embodiment 1.
Embodiment 3
In order to investigate the product of embodiment 1-2 preparations, respectively in high temperature（60℃±2℃）, high humidity (92.5% ± 5%), illumination
（4500LX±500LX）Under conditions of place 10 days, carry out factors influencing.
In terms of above result of the test, the product that is produced under the process conditions is influenceed small, quality by temperature, humidity, illumination
Stability is good.
Finally it should be noted that：The preferred embodiments of the present invention are these are only, are not intended to limit the invention, although
The present invention is described in detail with reference to embodiment, for those skilled in the art, it still can be to foregoing
Technical scheme described in embodiment is modified, or equivalent substitution is carried out to which part technical characteristic, but all at this
Within the spirit and principle of invention, any modification, equivalent substitution and improvements made etc., the protection model of the present invention should be included in
Within enclosing.
Claims (10)
1. a kind of methanesulfonic acid Lome Tapai capsule, includes active component methanesulfonic acid Lome Tapai and pharmaceutic adjuvant, it is characterised in that
Pharmaceutic adjuvant includes the hydroxypropylcellulose as disintegrant and adhesive.
2. methanesulfonic acid Lome Tapai capsule according to claim 1, it is characterised in that including following weight percentage
Component：
20% methanesulfonic acid Lome Tapai, 30% hydroxypropylcellulose, 40% filler, 5% cosolvent, 5% lubricant.
3. methanesulfonic acid Lome Tapai capsule according to claim 2, it is characterised in that described methanesulfonic acid Lome Tapai warp
Cross 200 mesh sieves.
4. methanesulfonic acid Lome Tapai capsule according to claim 2, it is characterised in that hydroxypropylcellulose, filler and profit
Lubrication prescription passes through 80 mesh sieves.
5. methanesulfonic acid Lome Tapai capsule according to claim 2, it is characterised in that the filler selects microcrystalline cellulose
One or more in element, pregelatinized starch, lactose.
6. methanesulfonic acid Lome Tapai capsule according to claim 2, it is characterised in that the cosolvent selects dodecyl
Sodium sulphate.
7. methanesulfonic acid Lome Tapai capsule according to claim 2, it is characterised in that the lubricant selects stearic acid
One or more in magnesium, talcum powder, silica.
8. according to the preparation method of any described methanesulfonic acid Lome Tapai capsule of claim 2~7, grasped as follows
Make： 1）Methanesulfonic acid Lome Tapai is crossed into 200 mesh sieves, filler, hydroxypropylcellulose cross 80 mesh sieves, are well mixed, obtain methanesulfonic acid
Lome Tapai premixing flour； 2）Compound concentration is 5%~60% ethanol solution, and its dosage is methanesulfonic acid Lome Tapai, hydroxypropyl fiber
Element, filler, the 45%~55% of cosolvent and lubricant gross weight；The cosolvent ethanol solution of half weight is dissolved, obtained
The ethanol solution of cosolvent； 3）Methanesulfonic acid Lome Tapai premixing flour is placed in wet granulator, the ethanol for adding cosolvent is molten
Liquid, remaining ethanol solution and purified water are added according to the granulating situation of material, the wet granular of 14 mesh sieves was made in stirring； 4）
Wet granular is dried, whole grain； 5）By particle with cross 80 mesh sieve lubricants together with mix, fill, produce methanesulfonic acid Lome he
Send capsule.
9. the preparation method of methanesulfonic acid Lome Tapai capsule according to claim 8, it is characterised in that the filler is
Microcrystalline cellulose, the cosolvent are lauryl sodium sulfate, and the lubricant is magnesium stearate.
10. the preparation method of methanesulfonic acid Lome Tapai capsule according to claim 8, it is characterised in that described（4）Step
Suddenly, it is dried using 50 DEG C~60 DEG C of temperature, the moisture of particle is controlled below 1.0% after drying.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610708603.6A CN107773561A (en) | 2016-08-24 | 2016-08-24 | A kind of methanesulfonic acid Lome Tapai capsule and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610708603.6A CN107773561A (en) | 2016-08-24 | 2016-08-24 | A kind of methanesulfonic acid Lome Tapai capsule and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107773561A true CN107773561A (en) | 2018-03-09 |
Family
ID=61387864
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610708603.6A Pending CN107773561A (en) | 2016-08-24 | 2016-08-24 | A kind of methanesulfonic acid Lome Tapai capsule and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN107773561A (en) |
-
2016
- 2016-08-24 CN CN201610708603.6A patent/CN107773561A/en active Pending
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| PB01 | Publication | ||
| PB01 | Publication | ||
| WD01 | Invention patent application deemed withdrawn after publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20180309 |