CN106890146A - A kind of Oseltamivir phosphate dispersible tablet and preparation method thereof - Google Patents
A kind of Oseltamivir phosphate dispersible tablet and preparation method thereof Download PDFInfo
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- CN106890146A CN106890146A CN201510957809.8A CN201510957809A CN106890146A CN 106890146 A CN106890146 A CN 106890146A CN 201510957809 A CN201510957809 A CN 201510957809A CN 106890146 A CN106890146 A CN 106890146A
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- Prior art keywords
- oseltamivir phosphate
- dispersible tablet
- content
- tablet according
- lubricant
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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
- A61K9/2004—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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
-
- 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
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- 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
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
Abstract
The present invention provides a kind of Oseltamivir phosphate dispersible tablet and preparation method thereof.The dispersible tablet is that the Oseltamivir phosphate of 30%-50% and the pharmaceutical excipient of 50%-70% are constituted by percentage by weight.The preparation method that the present invention is provided is that Oseltamivir phosphate is stirred into mixing granulation by wet method with suitable auxiliary material, and whole grain, compressing tablet obtains Oseltamivir phosphate dispersible tablet.Dispersible tablet of the invention can rapidly be disintegrated dispersed in water, suitable children, the elderly, it is unable to leave the bed and severely-disabled patient, and uniform dispersion can be configured to, can meet different weight children demand with suitable measuring device, the inventive method is easy to get, prepare simply, be suitable to industrialized production, there is larger application value.
Description
Technical field
The present invention relates to pharmaceutical preparation, and in particular to a kind of preparation of pharmaceutical preparation, more particularly to a kind of phosphoric acid Ao Sita
Wei dispersible tablet and preparation method thereof.
Background technology
Oseltamivir is a class neuraminic acid enzyme inhibitor, entitled (3R, 4R, the 5S) 4- acetamide -5- amino -3- of chemistry
(2-ethoxyethyl acetates of 1- third) carboxylic acid, ethyl ester phosphate of -1- hexamethylenes -1, trade name；Molecular formula C16H28N2O4H3PO4；Average molecular
Amount 410.4.Trade name Tamiflu (tamiflu) is Oseltamivir phosphate (oseltamivir, OS) capsule preparations, by Switzerland's Roche
Company's development and production, FDA (Food and Drug Adminstration) (FDA) is approved as the first-selection of anti-avian influenza in approval listing in 1999, WHO
Medicine.For be grown up and more than 1 years old children the treatment of A type and influenza B, also can be used for adult and 13 years old and more than 13 years old be blue or green
The prevention of juvenile A type and influenza B.Oseltamivir phosphate is recommended according to body weight to difference the children of more than 1 years old
Dosage (≤15kg 30mg, 2 times a day；＞ 15-23kg 45mg, 2 times a day；＞ 23-40kg 60mg, daily 2；＞ 40kg
75mg, 2 times a day), presently commercially available Oseltamivir phosphate preparation in addition to capsule, also granule, dry suspensoid agent.But granule
High cost, easy deliquescence, palatability are slightly worse；Multiple dose dry suspensoid agent has higher requirements to condition of storage and packaging material；Capsule agent dose
Too big, for child patient, especially underage child patient is difficult accurate administration, it is impossible to ensure the security of administration, and uncomfortable
Children and the elderly these people for swallowing inconvenience are closed to take.Accordingly, it would be desirable to further improve formulation.
The content of the invention
The technical problems to be solved by the invention are to overcome above-mentioned weak point, the new Oseltamivir phosphate of research and design
Pharmaceutical dosage form, can meet the demand of different weight children's personalized medicine, and preparation process is simple, finished product hardness are higher, and
It reaches the requirement for being easy to pack, store and transport.
The present invention provides a kind of Oseltamivir phosphate dispersible tablet, is the phosphoric acid Ao Sita of 30%-50% by percentage by weight
Wei and 50%-70% are constituted with pharmaceutical excipient.
Described pharmaceutical excipient includes filler, disintegrant, adhesive, sweetener, aromatic and lubricant.
In Oseltamivir phosphate dispersible tablet：
The content of the filler is 20%-50%, selected from microcrystalline cellulose, amylum pregelatinisatum, sorbierite or mannitol
In one or more, preferably sorbierite or mannitol.
The content of the disintegrant is 5%-25%, is formed sediment selected from PVPP, Ac-Di-Sol, carboxymethyl
Powder sodium or low-substituted hydroxypropyl cellulose, preferably sodium carboxymethyl starch or PVPP.
The content of described adhesive is 0.5%-3%, selected from PVP (polyvinylpyrrolidone) or starch.
The content of the sweetener is 0.5%-2%, selected from Aspartame or saccharin sodium, preferably saccharin sodium.
The content of the aromatic is 0-5%, selected from orange essence, flavoring banana essence or mixing water fruity flavor.
The content of the lubricant is 0.5%-3%, selected from superfine silica gel powder or magnesium stearate.
It is a further object of the present invention to provide a kind of preparation method of Oseltamivir phosphate dispersible tablet, the method bag
Include following steps：
A) Oseltamivir phosphate and disintegrant, filler, sweetener were crushed into 80 mesh sieves；
B) each raw material in addition to adhesive, lubricant, aromatic is well mixed, be subsequently adding adhesive be made it is soft
Material, and then it is crushed to wet granular by 20 mesh sieves；
C) after wet granular fluidized bed drying (60 DEG C) 2h, whole grain is mixed with 24 mesh sieves with lubricant and aromatic；Mixing is equal
It is even rear tabletted, obtain final product Oseltamivir phosphate dispersible tablet.
Beneficial effects of the present invention：
1) preferably, taste good improves the compliance of children to Oseltamivir phosphate dispersible tablet dispersion effect.
2) Oseltamivir phosphate dispersible tablet prepared by the present invention, is uniformly dispersed, for needing 30-60mg for 2 minutes in water
The patient of dosage, it is easy to be configured to the administration of dispersion liquid divided dose.
3) the Oseltamivir phosphate dispersible tablet that the present invention is prepared using wet granulation compressing dry granulation, to process conditions and equipment
It is required that simple, production cost is relatively low.
Oseltamivir phosphate dispersible tablet of the invention can be rapidly disintegrated in water it is dispersed, suitable children, the elderly,
It is unable to leave the bed and severely-disabled patient, and uniform dispersion can be configured to, different weight children can be met with suitable measuring device
Medication demand, raw material of the present invention is easy to get, and prepares simply, is suitable to industrialized production, there is larger application value.
Specific embodiment
Embodiment 1
1) Oseltamivir phosphate was crushed into 80 mesh, recipe quantity PVP K30 was dissolved in 50% ethanol water,
5% softwood is formulated as, it is standby；
2) according to the form below formula ratio weighs raw material, filler, disintegrant and sweetener respectively, is well mixed in pot of pelletizing,
Granulator mixing speed 200rpm, shear knife rotating speed 1800rpm, recipe quantity adhesive is poured into granulator, liquid feeding and granulation
During granulator mixing speed 200rpm, shear knife rotating speed 1800rpm, the wet mixing time controls at 10 minutes altogether；
3) softwood is crossed into 20 eye mesh screens, (60 DEG C of EAT, dry 2h) is dried in fluid bed (Glatt, GPCG2), 24
Mesh whole grain, adds lubricant and lemon extract during whole grain, mixed in V-Mixer (Yali Machinery, DGN-II)
Even rear compressing tablet, obtains final product 1000 Oseltamivir phosphate dispersible tablets.
The hardness of slice, thin piece is measured with hardness tester (Shanghai Huanghai Sea medicine inspection instrument company, YPD-200C).
Obtained Oseltamivir phosphate dispersible tablet is according to following method detection dispersing uniformity, dissolution rate.
Dispersing uniformity：Test sample 2 is taken, is put in 20 DEG C ± 1 DEG C of 100ml water, shaken 2 minutes, should be all disintegrated simultaneously
By No. two sieves.
Dissolution test：Using paddle method, medium is 900ml 0.1M HCl solutions, and rotating speed is 50rpm, the detection of HPLC methods
15min dissolution rates.
Formula and testing result：
It is dispersed that the above results show that dispersible tablet of the invention can rapidly be disintegrated in water.
According to state food and drug administration " normal oral solid pharmaceutical preparation dissolution rate technological guidance principle "
(2015), quick releasing formulation dissolution carries out terminal point control, and general 30min-60min dissolution rates are more than 85%, dispersion of the invention
Piece reaches 91%.
Embodiment 2
Preparation method is with embodiment 1, and the component and testing result of Oseltamivir phosphate dispersible tablet are as follows：
Formula and testing result：
Embodiment 3
Preparation method is with embodiment 1, and the component and testing result of Oseltamivir phosphate dispersible tablet are as follows：
Formula and testing result：
Embodiment 4
Preparation method is with embodiment 1, and the component and testing result of Oseltamivir phosphate dispersible tablet are as follows:
Formula and testing result：
Embodiment 6
Preparation method is with embodiment 1, and the component of Oseltamivir phosphate dispersible tablet and detection are as follows：
Prescription and testing result：
。
Claims (10)
1. a kind of Oseltamivir phosphate dispersible tablet, it is characterised in that the Oseltamivir phosphate dispersible tablet is by percentage by weight
The Oseltamivir phosphate of 30%-50% and the pharmaceutical excipient composition of 50%-70%.
2. Oseltamivir phosphate dispersible tablet according to claim 1, it is characterised in that the pharmaceutical excipient includes filling
Agent, disintegrant, adhesive, sweetener, aromatic and lubricant.
3. Oseltamivir phosphate dispersible tablet according to claim 2, it is characterised in that the Oseltamivir phosphate dispersible tablet
In, the content of filler is 20%-50%；The content of disintegrant is 5%-25%；The content of adhesive is 0.5%-3%；It is sweet
The content of taste agent is 0.5%-2%；The content of aromatic is 0-5%；The content of lubricant is 0.5%-3%.
4. the Oseltamivir phosphate dispersible tablet according to Claims 2 or 3, it is characterised in that the filler is selected from crystallite
One or more in cellulose, amylum pregelatinisatum, sorbierite or mannitol, preferably sorbierite or mannitol.
5. the Oseltamivir phosphate dispersible tablet according to Claims 2 or 3, it is characterised in that the disintegrant is selected from crosslinking
PVP, Ac-Di-Sol, sodium carboxymethyl starch or low-substituted hydroxypropyl cellulose, preferably sodium carboxymethyl starch or
PVPP.
6. the Oseltamivir phosphate dispersible tablet according to Claims 2 or 3, it is characterised in that described adhesive is selected from poly- second
Alkene pyrrolidone or starch.
7. the Oseltamivir phosphate dispersible tablet according to Claims 2 or 3, it is characterised in that the sweetener is selected from A Si
Ba Tian or saccharin sodium, preferably saccharin sodium.
8. the Oseltamivir phosphate dispersible tablet according to Claims 2 or 3, it is characterised in that the aromatic is selected from orange
Essence, flavoring banana essence or mixing water fruity flavor.
9. the Oseltamivir phosphate dispersible tablet according to Claims 2 or 3, it is characterised in that the lubricant is selected from micro mist
Silica gel or magnesium stearate.
10. as claimed in claim 1 a kind of preparation method of Oseltamivir phosphate dispersible tablet, it is characterised in that the method includes
Following steps：
A) Oseltamivir phosphate and disintegrant, filler, sweetener were crushed into 80 mesh sieves；
B) each raw material in addition to adhesive, lubricant, aromatic is well mixed, is subsequently adding adhesive and is made softwood, entered
And pass through 20 mesh sieves and be crushed to wet granular；
C) after 60 DEG C of wet granular fluid bed dries 2h, whole grain is mixed with 24 mesh sieves with lubricant and aromatic；Pressed after well mixed
Piece is made, Oseltamivir phosphate dispersible tablet is obtained final product.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510957809.8A CN106890146A (en) | 2015-12-18 | 2015-12-18 | A kind of Oseltamivir phosphate dispersible tablet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510957809.8A CN106890146A (en) | 2015-12-18 | 2015-12-18 | A kind of Oseltamivir phosphate dispersible tablet and preparation method thereof |
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| Publication Number | Publication Date |
|---|---|
| CN106890146A true CN106890146A (en) | 2017-06-27 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201510957809.8A Pending CN106890146A (en) | 2015-12-18 | 2015-12-18 | A kind of Oseltamivir phosphate dispersible tablet and preparation method thereof |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111544413A (en) * | 2020-04-21 | 2020-08-18 | 遂成药业股份有限公司 | Oseltamivir phosphate capsule and preparation process thereof |
| CN114159397A (en) * | 2021-11-02 | 2022-03-11 | 北京微智瑞医药科技有限公司 | Oseltamivir phosphate micro-tablet and preparation method and preparation thereof |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1706383A (en) * | 2004-06-04 | 2005-12-14 | 杭州民生药业集团有限公司 | Dispersant rotundine tablet and its prepn process |
| WO2010143207A1 (en) * | 2009-06-11 | 2010-12-16 | Rubicon Research Private Limited | Taste-masked oral formulations of influenza antivirals |
| CN103340835A (en) * | 2013-07-11 | 2013-10-09 | 孙卫东 | Orally disintegrating tablet suitable for infants and children and preparation method thereof |
| CN104000789A (en) * | 2014-04-15 | 2014-08-27 | 孙文娟 | Adefovir dipivoxil dispersible tablet and preparation method thereof |
-
2015
- 2015-12-18 CN CN201510957809.8A patent/CN106890146A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1706383A (en) * | 2004-06-04 | 2005-12-14 | 杭州民生药业集团有限公司 | Dispersant rotundine tablet and its prepn process |
| WO2010143207A1 (en) * | 2009-06-11 | 2010-12-16 | Rubicon Research Private Limited | Taste-masked oral formulations of influenza antivirals |
| CN103340835A (en) * | 2013-07-11 | 2013-10-09 | 孙卫东 | Orally disintegrating tablet suitable for infants and children and preparation method thereof |
| CN104000789A (en) * | 2014-04-15 | 2014-08-27 | 孙文娟 | Adefovir dipivoxil dispersible tablet and preparation method thereof |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111544413A (en) * | 2020-04-21 | 2020-08-18 | 遂成药业股份有限公司 | Oseltamivir phosphate capsule and preparation process thereof |
| CN114159397A (en) * | 2021-11-02 | 2022-03-11 | 北京微智瑞医药科技有限公司 | Oseltamivir phosphate micro-tablet and preparation method and preparation thereof |
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| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| CB02 | Change of applicant information | ||
| CB02 | Change of applicant information |
Address after: 201210 Shanghai Pudong New Area China (Shanghai) free trade test area No. 1999 Zhang Heng Road No. 7 Applicant after: Shanghai Double Star Thai Pharmaceutical Technology Co., Ltd. Address before: 201203 Shanghai city Pudong New Area Bing Road No. 306 building 3 floor No. 1 Applicant before: SHANGHAI SUNTECH PHARMACEUTICAL CO., LTD. |
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| WD01 | Invention patent application deemed withdrawn after publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20170627 |