CN106963739A - Prednisolone oral disnitegration tablet and preparation method thereof - Google Patents
Prednisolone oral disnitegration tablet and preparation method thereof Download PDFInfo
- Publication number
- CN106963739A CN106963739A CN201710188992.9A CN201710188992A CN106963739A CN 106963739 A CN106963739 A CN 106963739A CN 201710188992 A CN201710188992 A CN 201710188992A CN 106963739 A CN106963739 A CN 106963739A
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- CN
- China
- Prior art keywords
- prednisolone
- oral disnitegration
- disnitegration tablet
- disintegrant
- filler
- 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
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
- A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
-
- 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
- A61K9/2009—Inorganic compounds
-
- 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
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- 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
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2068—Compounds of unknown constitution, e.g. material from plants or animals
Abstract
The present invention proposes a kind of prednisolone oral disnitegration tablet and preparation method thereof, and comprising prednisolone, disintegrant, filler and stabilizer, each component percetage by weight is as follows：Prednisolone 1~5%, filler 60~85%, disintegrant 6~10% and stabilizer 5~15%, the disintegrant are the mixture of sodium carboxymethyl starch, konjaku powder and sodium bentonite.Preparation method, including by after supplementary material wet granulation the step of tabletting.The prednisolone oral disnitegration tablet dissolution rate is fast, and 3min just can dissolution completely.
Description
Technical field
The invention belongs to oral disnitegration tablet technical field, and in particular to a kind of prednisolone oral disnitegration tablet and its preparation side
Method.
Background technology
The English of prednisolone：Prednisolone；B. chemical name：11 β, 17 α, the pregnant steroid-Isosorbide-5-Nitrae-two of 21- trihydroxies
Alkene -3,20- diketone.Prednisolone has anti-inflammatory and anti-allergic effects, can suppress the hyperplasia of connective tissue, reduces capillary
Wall and membrane passage, reduce inflammatory and ooze out, and can suppress the formation and release of histamine and other toxicants.When serious
When Poisoning infects, used cooperatively with a large amount of antibacterials, can have and good cool, antitoxin, anti-inflammatory, Hemorrhagic shock and promote symptom
Mitigation.Its water-sodium retention and row's potassium effect are smaller than cortisone, and anti-inflammatory and anti-allergic effects are stronger, and side effect is less, therefore ratio
It is more common.11- ketone groups are reduced to 11- hydroxyls and aobvious pharmacological action by prednisone acetate in liver, its biological t1/2For 60 points
Clock.It can be clinically used for various acute severe bacterial infections, serious anaphylactia, collagenosis (lupus erythematosus, tubercle
Property peripheral arteritis etc.), rheumatism, nephrotic syndrome, serious bronchial astehma, thrombocytopenic purpura, granulocyte subtract
Few disease, acute lymphatic leukemia, various adrenal cortex functions are not enough disease, exfoliative dermatitis, pemphigus, neurodermatitis,
Eczema etc..
Prednisolone is the active component of medicine, when it is prepared into oral formulations, and only metacortandracin can be quick and efficient
Ground is soluble in water could to obtain good absorption in stomach and intestine, and otherwise its absorption and biological utilisation have very big obstacle.By
It is smaller in the specification of prednisolone piece, it is common for 1mg/ pieces, 2mg/ pieces and 5mg/ pieces, in preparation technology, if metacortandracin
Imperial poor dispersion, easily causes the product content uniformity, dissolution rate against regulation.People suffer from the medications such as acute cell infection disease
When, it is necessary to use taken with boiled water medicine.On the one hand when patient is taken medicine with water, old and women and children patient is particularly, usually very not
Just；Another aspect medicine is disintegrated rapidly in oral cavity, can greatly improve drug effect and play a role rapidly.Therefore, medicine oral cavity collapses
Solve preparation technique turns into one of contemporary high-tech in medicine, and very easily administering mode will be provided for all kinds of patients.At present, city
Rarely has the oral disnitegration tablet of prednisolone on field.
The content of the invention
The present invention proposes a kind of prednisolone oral disnitegration tablet, and cost height, the dissolution for solving above-mentioned prior art presence are slow
The problems such as.
The technical proposal of the invention is realized in this way：
A kind of prednisolone oral disnitegration tablet, includes prednisolone, disintegrant, filler and stabilizer, each component weight
Percentage is as follows：
Prednisolone 1~5%, filler 60~85%, disintegrant 6~10% and stabilizer 5~15%, the disintegration
Agent is the mixture of sodium carboxymethyl starch, konjaku powder and sodium bentonite.
Preferably, in some implementations of the present invention, the mass ratio of sodium carboxymethyl starch, konjaku powder and sodium bentonite
For 4~6:2~3:1~2.
Preferably, the present invention some implementation in, filler be selected from mannitol, lactose, sorbierite, pregelatinized starch with
One kind or its mixture in cornstarch.
Preferably, in some implementations of the present invention, filler is the mixture of lactose and sorbierite.
Preferably, in some implementations of the present invention, when being placed in aqueous medium, composition dissolved within 3 minutes.
Preferably, in some implementations of the present invention, when being placed in aqueous medium, composition dissolved within 2.5 minutes.
It is a further object to provide a kind of preparation method of prednisolone oral disnitegration tablet, including by supplementary material
After wet granulation the step of tabletting.
The prednisolone oral disnitegration tablet of the present invention can also contain adhesive, and adhesive can any can pharmaceutically be connect
The adhesive received.Adhesive is preferably a kind of to be selected from following water-soluble polymers：Polyvinyl alcohol, polyvinylpyrrolidone,
Methylcellulose, hydroxy propyl cellulose, any combination of hydroxymethyl cellulose or aforementioned substances.Polyvinylpyrrolidone is most
It is preferred that adhesive.
The prednisolone oral disnitegration tablet of the present invention can also contain taste enhancer, including artificial sweetener, for example
Abbas's sugar, saccharin, two dipotassium glycyrrhizinates, stevia rebaudianum, super sweet tea fixed (thaumatin) or flavoring agent are as twisted lemon acid, peppermint oil, Bai Zhu
Set oil, menthol, twist lemon, lime tree fruit, orange, grape, cherry or vanilla extract.
The present invention can also include conventional processing aid such as tablet lubricants (magnesium stearate, Sodium stearate), lubrication
Thing (silicon dioxide colloid) and wetting agent or solvation (Sodium Laurylsulfate, polysorbate).
Stabilizer used in the present invention can be industrially conventional stabilizer, and its selection is depended in medicine system
The characteristic of medicine employed in agent.Glyceryl behenate and stearoylketene fumaric acid sodium both can as a kind of lubricant or
A kind of stabilizer can be used as.
By substantial amounts of experiment screening, inventor is had found using sodium carboxymethyl starch, konjaku powder and sodium bentonite
Mixture is as disintegrant, and common disintegrants can be overcome completely, and (such as single use low-substituted hydroxypropyl cellulose, crosslinking are poly-
Vinylpyrrolidone, sodium carboxymethyl starch, microcrystalline cellulose, Ac-Di-Sol) disintegrating property that exists is poor, commonly
The fast disintegration property that disintegrant can reach is only 5min, afterwards due to raw material itself chemical characteristic and other auxiliary materials
Influence, it is difficult to increase again.
In some embodiments of the present invention, filler is the mixture of lactose and sorbierite, may be contained due to the filler
There is abundant hydrophilic radical, disintegrant of the invention is under this filler, and its disintegrating property is further enhanced.
Embodiment
Embodiment 1
A kind of prednisolone oral disnitegration tablet, includes prednisolone, disintegrant, filler and stabilizer, each component weight
Percentage is as follows：
Prednisolone 4%, lactose 58%, sorbierite 20%, disintegrant 8% and glyceryl behenate 10%.Disintegrant
For the mixture of sodium carboxymethyl starch, konjaku powder and sodium bentonite, mass ratio is 5:3:2.
Preparation method：
1) raw material prednisolone is ground to form into fine powder, crosses 80 mesh sieves；
2) by auxiliary material lactose, sorbierite, sodium carboxymethyl starch, konjaku powder, sodium bentonite and glyceryl behenic acid
Salt grinds to form fine powder respectively, crosses 80 mesh sieves；
3) lactose, sorbierite, sodium carboxymethyl starch, konjaku powder and sodium bentonite are fully mixed according to equal increments method
Close uniform, cross 60 mesh sieves, softwood is made in the ethanol solution for adding 30% in right amount, cross the granulation of 20 mesh sieves, 50 DEG C of drying；
4) by dry particle, after whole grain, then glycerol adding base behenate is mixed, and is pressed with 12mm circular dies
Piece.
Embodiment 2
A kind of prednisolone oral disnitegration tablet, includes prednisolone, disintegrant, filler and stabilizer, each component weight
Percentage is as follows：
Prednisolone 1%, lactose 50%, sorbierite 28%, disintegrant 6% and glyceryl behenate 15%.Disintegration
Agent is the mixture of sodium carboxymethyl starch, konjaku powder and sodium bentonite, and its mass ratio is 6:3:1.
Preparation method：
1) raw material prednisolone is ground to form into fine powder, crosses 80 mesh sieves；
2) by auxiliary material lactose, sorbierite, sodium carboxymethyl starch, konjaku powder, sodium bentonite and glyceryl behenic acid
Salt grinds to form fine powder respectively, crosses 80 mesh sieves；
3) lactose, sorbierite, sodium carboxymethyl starch, konjaku powder and sodium bentonite are fully mixed according to equal increments method
Close uniform, cross 60 mesh sieves, softwood is made in the ethanol solution for adding 30% in right amount, cross the granulation of 20 mesh sieves, 50 DEG C of drying；
4) by dry particle, after whole grain, then glycerol adding base behenate is mixed, and is pressed with 12mm circular dies
Piece.
Embodiment 3
A kind of prednisolone oral disnitegration tablet, includes prednisolone, disintegrant, filler and stabilizer, each component weight
Percentage is as follows：
Prednisolone 5%, cornstarch 65%, mannitol 15%, disintegrant 10% and stearoylketene fumaric acid's sodium
5%, disintegrant is the mixture of sodium carboxymethyl starch, konjaku powder and sodium bentonite, and its mass ratio is 6:3:1.
Preparation method：
1) raw material prednisolone is ground to form into fine powder, crosses 80 mesh sieves；
2) by auxiliary material cornstarch, mannitol, sodium carboxymethyl starch, konjaku powder, sodium bentonite and glyceryl mountain
Yu hydrochlorates grind to form fine powder respectively, cross 80 mesh sieves；
3) cornstarch, mannitol, sodium carboxymethyl starch, konjaku powder and sodium bentonite are filled according to equal increments method
Divide well mixed, cross 60 mesh sieves, softwood is made in the ethanol solution for adding 30% in right amount, cross 20 mesh sieves and pelletize, 50 DEG C of drying；
4) by dry particle, after whole grain, then add stearoylketene fumaric acid sodium to mix, pressed with 12mm circular dies
Piece.
Test example 1
Example 1,2 and 3 gained prednisolone oral disnitegration tablets are a piece of respectively, attached according to China's coastal port two
Record XC, the method for dissolution method first, using 0.01mol/L hydrochloric acid solutions 900ml as solvent, rotating speed is 50 turns per minute, in accordance with the law
Operation, through certain time, takes solution 10ml, filters, and takes subsequent filtrate appropriate, according to two annex IVA of China's coastal port, point
Light photometry, determines trap at 315nm wavelength, and another precision weighs prednisolone reference substance in right amount, with method operation, calculates
Every stripping quantity.Measurement result is shown in Table 1：
The embodiment 1-3 prednisolone oral disnitegration tablet dissolution results of table 1
| Dissolution time (divides) | The gained sample of embodiment 1 | The gained sample of embodiment 2 | The gained sample of embodiment 3 |
| 0.5 | 28.87 | 27.46 | 25.45 |
| 1 | 43.43 | 42.32 | 39.55 |
| 2 | 91.25 | 90.17 | 73.34 |
| 2.5 | 100.01 | 100.11 | 92.82 |
| 3 | 100.24 | 100.37 | 100.22 |
| 5 | 101.15 | 101.38 | 101.31 |
As a result show, this product is in 3 clock, and three batches of sample stripping quantities are up to 100% or so.Filler is lactose and sorb
The embodiment 1-2 of the mixture of alcohol sample was at 2.5 minutes, and its stripping quantity is up to 100%.
The foregoing is merely illustrative of the preferred embodiments of the present invention, is not intended to limit the invention, all essences in the present invention
God is with principle, and any modification, equivalent substitution and improvements made etc. should be included in the scope of the protection.
Claims (7)
1. a kind of prednisolone oral disnitegration tablet, it is characterised in that comprising prednisolone, disintegrant, filler and stabilizer, respectively
Component weight percentage is as follows：
Prednisolone 1~5%, filler 60~85%, disintegrant 6~10% and stabilizer 5~15%, the disintegrant is
The mixture of sodium carboxymethyl starch, konjaku powder and sodium bentonite.
2. prednisolone oral disnitegration tablet according to claim 1, it is characterised in that sodium carboxymethyl starch, konjaku powder
Mass ratio with sodium bentonite is 4~6:2~3:1~2.
3. prednisolone oral disnitegration tablet according to claim 1, it is characterised in that filler be selected from mannitol, lactose,
One kind or its mixture in sorbierite, pregelatinized starch and cornstarch.
4. prednisolone oral disnitegration tablet according to claim 3, it is characterised in that filler is lactose and sorbierite
Mixture.
5. prednisolone oral disnitegration tablet according to claim 1, it is characterised in that when being placed in aqueous medium, combination
Thing dissolved within 3 minutes.
6. prednisolone oral disnitegration tablet according to claim 4, it is characterised in that when being placed in aqueous medium, combination
Thing dissolved within 2.5 minutes.
7. the preparation method of prednisolone oral disnitegration tablet as claimed in claim 1 or 2, it is characterised in that including original is auxiliary
The step of expecting tabletting after wet granulation.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710188992.9A CN106963739A (en) | 2017-03-27 | 2017-03-27 | Prednisolone oral disnitegration tablet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710188992.9A CN106963739A (en) | 2017-03-27 | 2017-03-27 | Prednisolone oral disnitegration tablet and preparation method thereof |
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| Publication Number | Publication Date |
|---|---|
| CN106963739A true CN106963739A (en) | 2017-07-21 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710188992.9A Pending CN106963739A (en) | 2017-03-27 | 2017-03-27 | Prednisolone oral disnitegration tablet and preparation method thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109925288A (en) * | 2017-12-18 | 2019-06-25 | 江苏开元药业有限公司 | A kind of glucocorticoid medicine tablet and preparation method thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1418634A (en) * | 2002-12-19 | 2003-05-21 | 王登之 | Prednisolone oral disintegrant for treating acute bacterial infection, and its prepn. method |
| CN1863517A (en) * | 2003-10-07 | 2006-11-15 | 安壮奇制药公司 | Rapidly disintegrating formulation |
-
2017
- 2017-03-27 CN CN201710188992.9A patent/CN106963739A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1418634A (en) * | 2002-12-19 | 2003-05-21 | 王登之 | Prednisolone oral disintegrant for treating acute bacterial infection, and its prepn. method |
| CN1863517A (en) * | 2003-10-07 | 2006-11-15 | 安壮奇制药公司 | Rapidly disintegrating formulation |
Non-Patent Citations (2)
| Title |
|---|
| 李令媛等: "魔芋精粉作崩解剂在中药丸、片剂中的应用", 《中成药》 * |
| 马雪等: "钠基膨润土与一些常用崩解剂性能的比较", 《新疆中医药》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109925288A (en) * | 2017-12-18 | 2019-06-25 | 江苏开元药业有限公司 | A kind of glucocorticoid medicine tablet and preparation method thereof |
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| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20170721 |
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| RJ01 | Rejection of invention patent application after publication |