CN107157947A - A kind of 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate piece and preparation method thereof - Google Patents

A kind of 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate piece and preparation method thereof Download PDF

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Publication number
CN107157947A
CN107157947A CN201710309015.XA CN201710309015A CN107157947A CN 107157947 A CN107157947 A CN 107157947A CN 201710309015 A CN201710309015 A CN 201710309015A CN 107157947 A CN107157947 A CN 107157947A
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CN
China
Prior art keywords
propen
chloromethyl
amine polymer
carbonate
oxirane
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CN201710309015.XA
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Chinese (zh)
Inventor
刘敏
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Fonda Medical Technology (suzhou) Co Ltd
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Fonda Medical Technology (suzhou) Co Ltd
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Priority to CN201710309015.XA priority Critical patent/CN107157947A/en
Publication of CN107157947A publication Critical patent/CN107157947A/en
Pending legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/74Synthetic polymeric materials
    • A61K31/785Polymers containing nitrogen
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2009Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The invention discloses a kind of 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate piece and preparation method thereof, the component that the 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate piece includes by mass percentage has:2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate 78.79%;Microcrystalline cellulose 102 13.92%;Sodium carbonate 0.10%;Zinc stearate 0.19%;Water 7.00%.The step of preparation method, includes:2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate and microcrystalline cellulose 102 are mixed;Sodium carbonate liquor is added in mixture;Granulation;Sieving;Zinc stearate is added, and is mixed;Tabletting;It is coated.The present invention is used for the high phosphorus disease for treating end-stage renal disease Syndrome patients.The preparation method of the present invention employs sodium carbonate as stabilizer, therefore the 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate tablet of the present invention has more stable disintegration time, and its active constituents of medicine has more preferable validity to patient.

Description

A kind of 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate piece and preparation method thereof
Technical field
The invention belongs to medical research and development technology field, in particular to a kind of 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate piece and its preparation side Method.
Background technology
2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate is a kind of cross-linked polymer that will not be absorbed by the body, be 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate piece activity into Point.It carries multiple amidos, is connected by a carbon atom with polymer backbone, chemical structural formula is as follows:
Wherein, a and b represent primary amine group number, and a+b=9;
C represents crosslinked group number, and c=1;
M represents to extend the quantity of 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate in polymer network.
2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate is water insoluble, the similar sevelamer hydrochloride of the mechanism of action, by oral, in the effect of stomach hydrochloric acid in gastric juice Under, change into sevelamer hydrochloride.These amidos can in enteron aisle Partial protons, and with ion exchange and hydrogen bond and phosphoric acid point Son combine, formed it is insoluble, not by absorption phosphoric acid sevelamer compound, eventually through swill, excrement is excreted.Carbonic acid Sevelamer reduces its absorption, the effect of reduction serium inorganic phosphorus concentration is reached, for treating late period kidney by combining the phosphorus in intestines and stomach Sick Syndrome patients' high phosphorus disease.
The content of the invention
It is comprehensive for treating end-stage renal disease it is an object of the invention to provide a kind of 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate piece and preparation method thereof The high phosphorus disease of combination of syndromes patient.
To realize above-mentioned technical purpose and the technique effect, the present invention is achieved through the following technical solutions:
A kind of 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate piece, by mass percentage(%w/w), including following components:
Active component:2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate 78.79%;
Diluent:Microcrystalline cellulose -102 13.92%;
Stabilizer:Sodium carbonate 0.10%;
Lubricant:Zinc stearate 0.19%;
Adhesive:Water 7.00%.
A kind of preparation method of 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate piece, comprises the following steps:
Step 1)2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate and microcrystalline cellulose -102 are well mixed;
Step 2)Sodium carbonate liquor is added in the mixture of 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate and microcrystalline cellulose -102;
Step 3)By the granulating mixture of 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate, microcrystalline cellulose -102 and sodium carbonate liquor;
Step 4)Powder is sieved;
Step 5)Zinc stearate is added in powder after sizing, and is well mixed;
Step 6)Tabletting;
Step 7)It is coated.
Further, step 4)In, the size of powder sieving is 24 mesh.
The beneficial effects of the invention are as follows:
The invention provides a kind of 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate piece and preparation method thereof, the height for treating end-stage renal disease Syndrome patients Phosphorus disease.The preparation method of the present invention employs sodium carbonate to be had as stabilizer, therefore the 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate tablet of the present invention More stable disintegration time, its active constituents of medicine has more preferable validity to patient.
Described above is only the general introduction of technical solution of the present invention, in order to better understand the technological means of the present invention, And can be practiced according to the content of specification, below with presently preferred embodiments of the present invention and coordinate accompanying drawing describe in detail as after. The embodiment of the present invention is shown in detail by following examples and its accompanying drawing.
Brief description of the drawings
Accompanying drawing described herein is used for providing a further understanding of the present invention, constitutes the part of the application, this hair Bright schematic description and description is used to explain the present invention, does not constitute inappropriate limitation of the present invention.In the accompanying drawings:
Fig. 1 is the process chart of preparation method of the present invention.
Embodiment
Below with reference to the accompanying drawings and in conjunction with the embodiments, the present invention is described in detail.
A kind of 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate piece, by taking every sheet weight 1050mg as an example, the weight of its concrete component is as follows:
Active component:2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate 827.3g;
Diluent:The 146.2g of microcrystalline cellulose -102;
Stabilizer:Sodium carbonate 1g;
Lubricant:Zinc stearate 2g;
Adhesive:Water 73.5g.
Shown in reference picture 1, the preparation method of the 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate piece comprises the following steps:
Step 1)2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate and microcrystalline cellulose -102 are well mixed;
Step 2)Sodium carbonate liquor is added in the mixture of 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate and microcrystalline cellulose -102;
Step 3)By the granulating mixture of 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate, microcrystalline cellulose -102 and sodium carbonate liquor;
Step 4)Powder is sieved, 24 mesh;
Step 5)Zinc stearate is added in powder after sizing, and is well mixed;
Step 6)Tabletting;
Step 7)It is coated.
The preferred embodiments of the present invention are the foregoing is only, are not intended to limit the invention, for the skill of this area For art personnel, the present invention can have various modifications and variations.Within the spirit and principles of the invention, that is made any repaiies Change, equivalent substitution, improvement etc., should be included in the scope of the protection.

Claims (3)

1. a kind of 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate piece, it is characterised in that by mass percentage(%w/w), including following components:
Active component:2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate 78.79%;
Diluent:Microcrystalline cellulose -102 13.92%;
Stabilizer:Sodium carbonate 0.10%;
Lubricant:Zinc stearate 0.19%;
Adhesive:Water 7.00%.
2. a kind of method of the 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate piece prepared described in claim 1, it is characterised in that comprise the following steps:
Step 1)2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate and microcrystalline cellulose -102 are well mixed;
Step 2)Sodium carbonate liquor is added in the mixture of 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate and microcrystalline cellulose -102;
Step 3)By the granulating mixture of 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate, microcrystalline cellulose -102 and sodium carbonate liquor;
Step 4)Powder is sieved;
Step 5)Zinc stearate is added in powder after sizing, and is well mixed;
Step 6)Tabletting;
Step 7)It is coated.
3. the method according to claim 2 for preparing 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate piece, it is characterised in that:Step 4)In, powder mistake The size of sieve is 24 mesh.
CN201710309015.XA 2017-05-04 2017-05-04 A kind of 2-Propen-1-amine polymer with(chloromethyl)oxirane carbonate piece and preparation method thereof Pending CN107157947A (en)

Priority Applications (1)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111450068A (en) * 2019-01-21 2020-07-28 江苏先声药业有限公司 Sevelamer carbonate pharmaceutical composition and preparation method thereof

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006050315A2 (en) * 2004-11-01 2006-05-11 Genzyme Corporation Aliphatic amine polymer salts for tableting
CN102908325A (en) * 2012-11-12 2013-02-06 南京生命能科技开发有限公司 Sevelamer carbonate medical tablet composition and preparation method thereof
CN104434866A (en) * 2014-12-30 2015-03-25 济南康和医药科技有限公司 Sevelamer carbonate effervescent tablets and preparation method thereof
CN104546781A (en) * 2014-12-22 2015-04-29 青岛正大海尔制药有限公司 Sevelamer carbonate tablet and preparation method thereof
CN104739786A (en) * 2013-12-25 2015-07-01 杭州民生滨江制药有限公司 Sevelamer carbonate tablet and preparation method thereof

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006050315A2 (en) * 2004-11-01 2006-05-11 Genzyme Corporation Aliphatic amine polymer salts for tableting
CN102908325A (en) * 2012-11-12 2013-02-06 南京生命能科技开发有限公司 Sevelamer carbonate medical tablet composition and preparation method thereof
CN104739786A (en) * 2013-12-25 2015-07-01 杭州民生滨江制药有限公司 Sevelamer carbonate tablet and preparation method thereof
CN104546781A (en) * 2014-12-22 2015-04-29 青岛正大海尔制药有限公司 Sevelamer carbonate tablet and preparation method thereof
CN104434866A (en) * 2014-12-30 2015-03-25 济南康和医药科技有限公司 Sevelamer carbonate effervescent tablets and preparation method thereof

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111450068A (en) * 2019-01-21 2020-07-28 江苏先声药业有限公司 Sevelamer carbonate pharmaceutical composition and preparation method thereof

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Application publication date: 20170915