CN108619105A - A kind of Azithromycin dispersible tablet - Google Patents

A kind of Azithromycin dispersible tablet Download PDF

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Publication number
CN108619105A
CN108619105A CN201810830128.9A CN201810830128A CN108619105A CN 108619105 A CN108619105 A CN 108619105A CN 201810830128 A CN201810830128 A CN 201810830128A CN 108619105 A CN108619105 A CN 108619105A
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CN
China
Prior art keywords
azithromycin
weight
parts
disintegrant
adhesive
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.)
Pending
Application number
CN201810830128.9A
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Chinese (zh)
Inventor
朱正标
张汉华
裴雪梅
范小雪
刘耀文
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
HUANGHE PHARMACEUTICAL INDUSTRY Co Ltd JIANGSU
Original Assignee
HUANGHE PHARMACEUTICAL INDUSTRY Co Ltd JIANGSU
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by HUANGHE PHARMACEUTICAL INDUSTRY Co Ltd JIANGSU filed Critical HUANGHE PHARMACEUTICAL INDUSTRY Co Ltd JIANGSU
Priority to CN201810830128.9A priority Critical patent/CN108619105A/en
Publication of CN108619105A publication Critical patent/CN108619105A/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
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056Mouth 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
    • 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
    • A61K9/2027Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Zoology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

The present invention relates to azithromycin formulations technical fields, and in particular to a kind of Azithromycin dispersible tablet is prepared by azithromycin, disintegrant, adhesive and lubricant.The present invention organically combines azithromycin, disintegrant, adhesive and lubricant, so that tablet is steadily disintegrated rapidly using disintegrant, active material quick release, improves bioavilability, alleviates the slight illness of patient.

Description

A kind of Azithromycin dispersible tablet
Technical field
The present invention relates to azithromycin formulations technical fields, and in particular to a kind of Azithromycin dispersible tablet.
Background technology
Respiratory tract, skin, soft tissue infection and transmissible disease have caused by the common pathogen of azithromycin treatment Fine curative effect.Compared with other antibiotic, a much progress of the azithromycin in terms for the treatment of respiratory tract and soft tissue infection is Short treating period(3-5 days), dosage is 10-15 times low, daily to be only administered once.It is to clothing in a quantum jump of sexual transmitted diseases Pathogen infection need to only be administered once.Body is to the drug resistance of azithromycin better than common antibiotic or at least identical [1].Archie Mycin is a kind of macrolide antibiotics, is developed earliest by Piliva companies of Yugoslavia and transfers Pfizer companies of the U.S. Production, in 1988 list, hereafter respectively the states such as Britain, Italy, Sweden and Norway list, preparation have tablet, capsule, Granule, injection etc..China ratified azithromycin capsule import in 1992, and many producers domestic thereafter and research institution are successive Develop a variety of doses of Azithromycin Raw Material and ordinary tablet, capsule, granule, dispersible tablet, chewable tablets, freeze-dried and injection etc. Type.
But single product content of azithromycin is high, dissolubility is poor, and bioavilability is low, and patient's blood concentration is made to be unable to reach Most preferably.The present invention develops a kind of can improve releasing for azithromycin active principle with the Azithromycin dispersible tablet of quick release Speed is put, drug bioavailability is increased.
Invention content
(One)The technical issues of solution
In view of the deficiencies of the prior art, the present invention provides it is a kind of can, azithromycin point that drug effect more longlasting simpler with technique Discrete piece so that said preparation has more preferable curative effect.
(Two)Technical solution
In order to achieve the above object, the present invention is achieved by the following technical programs:
A kind of Azithromycin dispersible tablet, which is characterized in that be prepared by azithromycin, adhesive, lubricant, disintegrant.
Preferably, the azithromycin 5-15 parts by weight, adhesive 2-8 parts by weight, disintegrant 2-8 parts by weight, lubricant 0.1-2 parts by weight.
It is furthermore preferred that 10 parts by weight of the azithromycin, 4 parts by weight of adhesive, 4 parts by weight of disintegrant, 1 weight of lubricant Part.
It is furthermore preferred that the disintegrant is crospovidone, croscarmellose sodium, sodium carboxymethyl starch or corn Starch;The lubricant is talcum powder or magnesium stearate or sodium stearyl fumarate;Described adhesive is sodium carboxymethylcellulose, Povidone, copolyvidone, starch, pregelatinized starch, carragheen or high substituted carboxymethyl cellulose.
Present invention also improves a kind of preparation methods of Azithromycin dispersible tablet, include the following steps:
1)Azithromycin, some adhesive, disintegrant is taken to be placed in wet mixing pelletizer in proportion;
2)By step 1)Described in mixture mix 5-10min at 100-200r/min;
3)Remainder adhesive is added in appropriate purified water, repeating stirring makes into uniform supernatant liquid.;
4)By step 3)Described in liquid be added wet mixing pelletizer in, mix 1-2min under 100-200r/min;
5)By step 4)Described in azithromycin mixture wet granular, 50-60 °C of drying are made by oscillating granulator 40min;
6)By step 5)Described in particle be added mixing machine in, be added lubricant, 10r/min mixing 3-5min;
7)By 6)Described in granulation, packaging.
(Three)Advantageous effect
The present invention provides a kind of Azithromycin dispersible tablet, reasonable recipe, added auxiliary material without physiological activity, takes safety; Preparation method is simple, is suitble to promote production.
The present invention organically combines azithromycin, disintegrant, adhesive and lubricant, makes piece using disintegrant Steadily disintegration is rapid for agent, and active material quick release improves bioavilability, alleviates the slight illness of patient.
Present invention uses novel disintegrants, are not suitable for filler, reduce the supplementary product kind used, greatly reduce life Produce cost and quality of material management cost;Preparation release is more steady, and drug effect is more longlasting, is conducive to Rehabilitation.
Specific implementation mode
In order to make the object, technical scheme and advantages of the embodiment of the invention clearer, below in conjunction with the embodiment of the present invention, Technical scheme in the embodiment of the invention is clearly and completely described, it is clear that described embodiment is the present invention one Divide embodiment, instead of all the embodiments.Based on the embodiments of the present invention, those of ordinary skill in the art are not making The every other embodiment obtained under the premise of creative work, shall fall within the protection scope of the present invention.
Embodiment 1
A kind of Azithromycin dispersible tablet, wherein 10 parts by weight of azithromycin, 4 parts by weight of adhesive, 4 parts by weight of disintegrant, lubrication 1 parts by weight of agent;
The preparation method of Azithromycin dispersible tablet, includes the following steps:
1)10 parts by weight of azithromycin, 2 parts by weight of sodium carboxymethylcellulose are weighed, it is mixed to be placed in wet method for 4 parts by weight of crospovidone It closes in granulator;
2)By step 1)Described in mixture mix 5-10min at 100-200r/min;
3)2 parts by weight of sodium carboxymethylcellulose are added in appropriate purified water, stirring repeatedly makes into uniform supernatant liquid.;
4)By step 3)Described in liquid be added wet mixing pelletizer in, mix 1-2min under 100-200r/min;
5)By step 4)Described in azithromycin mixture wet granular, 50-60 °C of drying are made by oscillating granulator 40min;
6)By step 5)Described in particle be added mixing machine in, be added 1 parts by weight of magnesium stearate, 10r/min mixing 3-5min;
7)By 6)Described in granulation, packaging.
Embodiment 2
A kind of Azithromycin dispersible tablet, wherein 10 parts by weight of azithromycin, 4 parts by weight of adhesive, 4 parts by weight of disintegrant, lubrication 1 parts by weight of agent;
The preparation method of Azithromycin dispersible tablet, includes the following steps:
1)10 parts by weight of azithromycin, 2 parts by weight of sodium carboxymethylcellulose are weighed, 4 parts by weight of croscarmellose sodium are set In wet mixing pelletizer;
2)By step 1)Described in mixture mix 5-10min at 100-200r/min;
3)2 parts by weight of sodium carboxymethylcellulose are added in appropriate purified water, stirring repeatedly makes into uniform supernatant liquid.;
4)By step 3)Described in liquid be added wet mixing pelletizer in, mix 1-2min under 100-200r/min;
5)By step 4)Described in azithromycin mixture wet granular, 50-60 °C of drying are made by oscillating granulator 40min;
6)By step 5)Described in particle be added mixing machine in, be added 1 parts by weight of magnesium stearate, 10r/min mixing 3-5min;
7)By 6)Described in granulation, packaging.
Embodiment 3
A kind of Azithromycin dispersible tablet, wherein 10 parts by weight of azithromycin, 4 parts by weight of adhesive, 4 parts by weight of disintegrant, lubrication 1 parts by weight of agent;
The preparation method of Azithromycin dispersible tablet, includes the following steps:
1)10 parts by weight of azithromycin are weighed, 4 parts by weight of crospovidone are placed in wet mixing pelletizer;
2)By step 1)Described in mixture mix 5-10min at 100-200r/min;
3)4 parts by weight of sodium carboxymethylcellulose are added in appropriate purified water, stirring repeatedly makes into uniform supernatant liquid.;
4)By step 3)Described in liquid be added wet mixing pelletizer in, mix 1-2min under 100-200r/min;
5)By step 4)Described in azithromycin mixture wet granular, 50-60 °C of drying are made by oscillating granulator 40min;
6)By step 5)Described in particle be added mixing machine in, be added 1 parts by weight of magnesium stearate, 10r/min mixing 3-5min;
7)By 6)Described in granulation, packaging.
The above embodiments are merely illustrative of the technical solutions of the present invention, rather than its limitations;Although with reference to the foregoing embodiments Invention is explained in detail, it will be understood by those of ordinary skill in the art that:It still can be to aforementioned each implementation Technical solution recorded in example is modified or equivalent replacement of some of the technical features;And these modification or It replaces, the spirit and scope for various embodiments of the present invention technical solution that it does not separate the essence of the corresponding technical solution.

Claims (5)

1. a kind of Azithromycin dispersible tablet, which is characterized in that be prepared by azithromycin, adhesive, lubricant, disintegrant.
2. Azithromycin dispersible tablet as described in claim 1, which is characterized in that the azithromycin 5-15 parts by weight, bonding Agent 2-8 parts by weight, disintegrant 2-8 parts by weight, lubricant 0.1-2 parts by weight.
3. Azithromycin dispersible tablet as claimed in claim 2, which is characterized in that 10 parts by weight of the azithromycin, adhesive 4 Parts by weight, 4 parts by weight of disintegrant, 1 parts by weight of lubricant.
4. Azithromycin dispersible tablet as claimed in claim 3, which is characterized in that the disintegrant is crospovidone, crosslinking Sodium carboxymethylcellulose, sodium carboxymethyl starch or cornstarch;The lubricant is that talcum powder or magnesium stearate or stearic acid are rich Horse acid sodium;Described adhesive is sodium carboxymethylcellulose, povidone, copolyvidone, starch, pregelatinized starch, carragheen or height Substituted carboxymethyl cellulose.
5. the preparation method of Azithromycin dispersible tablet according to any one of claims 1 to 4, which is characterized in that including following Step:
1)Azithromycin, some adhesive, disintegrant is taken to be placed in wet mixing pelletizer in proportion;
2)By step 1)Described in mixture mix 5-10min at 100-200r/min;
3)Remainder adhesive is added in appropriate purified water, repeating stirring makes into uniform supernatant liquid;
4)By step 3)Described in liquid be added wet mixing pelletizer in, mix 1-2min under 100-200r/min;
5)By step 4)Described in azithromycin mixture wet granular, 50-60 °C of drying are made by oscillating granulator 40min;
6)By step 5)Described in particle be added mixing machine in, be added lubricant, 10r/min mixing 3-5min;
7)By 6)Described in granulation, packaging.
CN201810830128.9A 2018-07-26 2018-07-26 A kind of Azithromycin dispersible tablet Pending CN108619105A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201810830128.9A CN108619105A (en) 2018-07-26 2018-07-26 A kind of Azithromycin dispersible tablet

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN201810830128.9A CN108619105A (en) 2018-07-26 2018-07-26 A kind of Azithromycin dispersible tablet

Publications (1)

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CN108619105A true CN108619105A (en) 2018-10-09

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Application Number Title Priority Date Filing Date
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Country Status (1)

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Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020061333A1 (en) * 1999-03-30 2002-05-23 Noel Zakarian Dispersible macrolide compounds and method for production thereof
CN103550181A (en) * 2013-11-04 2014-02-05 深圳致君制药有限公司 Azithromycin dispersible tablet and preparation method thereof
CN106137990A (en) * 2016-07-29 2016-11-23 花园药业股份有限公司 Azithromycin dispersible tablet and preparation technology thereof

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020061333A1 (en) * 1999-03-30 2002-05-23 Noel Zakarian Dispersible macrolide compounds and method for production thereof
CN103550181A (en) * 2013-11-04 2014-02-05 深圳致君制药有限公司 Azithromycin dispersible tablet and preparation method thereof
CN106137990A (en) * 2016-07-29 2016-11-23 花园药业股份有限公司 Azithromycin dispersible tablet and preparation technology thereof

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
张丽娥 等: "阿奇霉素分散片的制备与溶出度测定", 《医药导报》 *

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Application publication date: 20181009