CN108078953A - A kind of taste masking coated composition - Google Patents

A kind of taste masking coated composition Download PDF

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Publication number
CN108078953A
CN108078953A CN201611048841.5A CN201611048841A CN108078953A CN 108078953 A CN108078953 A CN 108078953A CN 201611048841 A CN201611048841 A CN 201611048841A CN 108078953 A CN108078953 A CN 108078953A
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CN
China
Prior art keywords
parts
composition
coated composition
plasticizer
wetting agent
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
CN201611048841.5A
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Chinese (zh)
Inventor
吴传斌
陈航平
刘阳
李革
潘文杰
张林杰
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.)
NEWORLD PHARMACEUTICAL Co Ltd
Guangzhou Zhongda Nansha Technology Innovation Industrial Park Co Ltd
Original Assignee
NEWORLD PHARMACEUTICAL Co Ltd
Guangzhou Zhongda Nansha Technology Innovation Industrial Park Co Ltd
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 NEWORLD PHARMACEUTICAL Co Ltd, Guangzhou Zhongda Nansha Technology Innovation Industrial Park Co Ltd filed Critical NEWORLD PHARMACEUTICAL Co Ltd
Priority to CN201611048841.5A priority Critical patent/CN108078953A/en
Publication of CN108078953A publication Critical patent/CN108078953A/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
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005Wall or coating material
    • A61K9/5021Organic macromolecular compounds
    • A61K9/5036Polysaccharides, e.g. gums, alginate; Cyclodextrin
    • A61K9/5042Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
    • A61K9/5047Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005Wall or coating material
    • A61K9/5021Organic macromolecular compounds
    • A61K9/5026Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates

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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 invention discloses the coated compositions of pellet, are prepared by the composition of following parts by weight:10 20 parts of hydroxypropyl methyl cellulose, 25 parts of polyacrylic resin IV10,5 15 parts of amino acrylic resin and plasticizer 5 10,5 15 parts of adhesive, lubricant 10 25,15 parts of wetting agent.The coated composition of the pellet can be quickly dissolved into acid gastric environment (pH1.0~3.0), while have undissolved characteristic in oral environment of the pH value more than 5.0, so as to reach good taste masking effect, and be conducive to the absorption of drug.

Description

A kind of taste masking coated composition
Technical field
The present invention relates to drug fields, are specifically related to a kind of taste masking coated composition.
Background technology
Many drugs particularly antibiotic all has undesirable taste, wherein it is in the majority with bitter taste, therefore, led in pharmaceutical technology Domain, this kind of drug are normally manufactured as the dosage forms such as tablet or capsule, in order to which patient takes.Although use directly with tablet or Capsule swallows administration, and the bitter taste of drug usually can be avoided greatly.But conventional tablet or capsule be not particularly suited for old man, Child or the patient of some dysphagias.For such crowd, chewable tablets, oral disintegrating tablet, dispersible tablet or liquid need to be made in drug Preparation just can guarantee good administering effect, and these preparations also require that cover bitter taste, could improve complying with for patient's medication Property.
With the progress of science, new equipment and new process continue to bring out, and sustained-release preparation is since the construction cycle is short, technology Content is high, and economic risk is small and is paid attention to by pharmaceuticals industry circle.Wherein, system is administered in the multiple unit type using pellet preparations as representative System, with its distinctive superiority, is increasingly becoming one of research hotspot of sustained-release preparation.Slow controlled release micro pill refers to drug and retardance The minipill for wrapping slow clothing film after common capsule core and preparing first is made in agent mixing pill.
Preparing auxiliary material used in pellet mainly has retarding agent, adhesive, thin-film material, plasticizer and pore-foaming agent Deng.Have slightly Ball uses blank capsule core, and drug is wrapped in capsule core surface, and most of pellets need to carry out film coating, by the thickness of film or The method of pellet weightening controls its dissolution rate, reaches slow controlled release purpose.
The auxiliary material of coating of pellets film has coating membrane material, plasticizer, pore-foaming agent, antiplastering aid etc..Sustained release coating materials have vinegar Acid cellulose and ethyl cellulose, polyacrylic resin, silicone elastomer, enteric material such as shellac, cellulose acetate phthalandione Fat, hypromellose phthalate.
At present, although coating of pellets Technical comparing is ripe, existing good slow release effect, and with good taste masking The coating of effect is actually rare.
The content of the invention
Based on this, the object of the present invention is to provide a kind of coated compositions of the pellet with good taste masking effect.
Realize that the technical solution of above-mentioned purpose is as follows.
A kind of coated composition of pellet, is prepared by the composition of following parts by weight:Hydroxypropyl methyl cellulose 10- 20 parts, IV10-25 parts of polyacrylic resin, 5-15 parts of amino acrylic resin and plasticizer 5-10,5-15 parts of adhesive, Lubricant 10-25,1-5 parts of wetting agent.
In one of the embodiments, it is prepared by the composition of following parts by weight:Hydroxypropyl methyl cellulose 10-20 Part, 12-20 parts of polyacrylic resin IV, 5-10 parts of amino acrylic resin and plasticizer 5-8,5-10 parts of adhesive moisten Lubrication prescription 15-20,1-5 parts of wetting agent.In one of the embodiments,
It is prepared by the composition of following parts by weight:15 parts of hydroxypropyl methyl cellulose, polyacrylic resin IV 18 Part, 5-6 parts of amino acrylic resin and plasticizer 5-8,5-8 parts of adhesive, 16-28 parts of lubricant, 1-5 parts of wetting agent.
In one of the embodiments, the plasticizer is triglycerides and/or triethyl citrate.
In one of the embodiments, lubricant is talcum powder.In one of the embodiments, wetting agent is
Concentration is the ethyl alcohol of 85-92%.The present invention provides a kind of coated composition of new pellet,
It can be quickly dissolved into acid gastric environment (pH1.0~3.0), while have not in oral environment of the pH value more than 5.0 The characteristic of dissolving so as to reach good taste masking effect, and is conducive to the absorption of drug.
Description of the drawings
Fig. 1 is the dressing microcapsule stripping curve figure that the present invention is embodiment 1.
Specific embodiment
Antimycotic Chinese medical extract and its preparation method and application of the present invention is made below in conjunction with specific embodiment into One step is described in detail.
Aloe extract, coptis root extract, Radix et Caulis Opuntiae Dillenii extract, cockscomb extraction in following embodiment can be in the market It is commercially available.
Embodiment 1
The coated composition of pellet described in the present embodiment is prepared by the composition of following parts by weight:Hydroxypropyl first 15 parts of base cellulose, 15 parts of polyacrylic resin IV, 8 parts of amino acrylic resin and plasticizer 6,10 parts of adhesive, profit Lubrication prescription 15,3 parts of wetting agent, the plasticizer of stating is triglycerides;The lubricant is talcum powder, and wetting agent is that concentration is 90% Ethyl alcohol.First, first according to a conventional method, it is recipe quantity Doxycycline Hyclate, polyvinylpyrrolidone, hydroxypropyl methyl cellulose is molten The blank capsule core that Yu Shuizhong is configured to liquid, 200um or so grain size is put into fluid bed and adds medicine to, and is made and is coated composition granule.
2nd, each substance of solid is made to be uniformly dispersed above-mentioned coated composition addition water again, is configured to coating solution.
3rd, it is coated composition granule and is put into fluid bed, coating solution, which is made, with step 2 is coated.The running parameter of fluid bed It is as follows:Intake 80m3/h, 35 DEG C of inlet air temperature, 30 DEG C of temperature of outgoing air, 25 DEG C of temperature of charge, coating solution delivery rate 3.9g/ Min, atomizing pressure 1.5bar, obtains micro-capsule, conventionally, in addition appropriate auxiliary material, be made granule to get.
As shown in Figure 1, X-axis is time/MIN, Y-axis is cumulative percentage release %.It is micro- from coating made from the present embodiment Capsule stripping curve figure can be seen that when it is 1.0 (being similar to stomach acid or alkali environment) that dressing microcapsule, which is in pH value, and dressing microcapsule is fast Instant solution, and when dressing microcapsule be in be similar to oral cavity acid or alkali environment when, i.e. pH value is 5.0 stripping curve, and dressing microcapsule is molten Solution is slow, can be maintained for a long time insoluble.
Embodiment 2
The coated composition of pellet described in the present embodiment is prepared by the composition of following parts by weight:Hydroxypropyl first 20 parts of base cellulose, 12 parts of polyacrylic resin IV, 5 parts of amino acrylic resin and plasticizer 8,10 parts of adhesive, profit Lubrication prescription 15,2 parts of wetting agent, the plasticizer of stating is triglycerides;The lubricant is talcum powder, and wetting agent is that concentration is 85% Ethyl alcohol.
For preparation method with reference to described in embodiment 1, the rate of dressing microcapsule dissolution is similar to Example 1.
Embodiment 3
The coated composition of pellet described in the present embodiment is prepared by the composition of following parts by weight:Hydroxypropyl first 20 parts of base cellulose, IV10 parts of polyacrylic resin, 15 parts of amino acrylic resin and plasticizer 5,8 parts of adhesive, lubrication Agent 25,5 parts of wetting agent, the plasticizer of stating is triglycerides;The lubricant is talcum powder, and wetting agent is that concentration is 90% Ethyl alcohol.
For preparation method with reference to described in embodiment 1, the rate of dressing microcapsule dissolution is similar to Example 1.
Embodiment 4
The coated composition of pellet described in the present embodiment is prepared by the composition of following parts by weight:Hydroxypropyl first 15 parts of base cellulose, 18 parts of polyacrylic resin IV, 6 parts of amino acrylic resin and plasticizer 6,6 parts of adhesive, lubrication Agent 20,5 parts of wetting agent, the plasticizer of stating is triglycerides;The lubricant is talcum powder, and wetting agent is that concentration is 89% Ethyl alcohol.
For preparation method with reference to described in embodiment 1, the rate of dressing microcapsule dissolution is similar to Example 1.
Each technical characteristic of embodiment described above can be combined arbitrarily, to make description succinct, not to above-mentioned reality It applies all possible combination of each technical characteristic in example to be all described, as long as however, the combination of these technical characteristics is not deposited In contradiction, the scope that this specification is recorded all is considered to be.The above is implemented
Example only expresses the several embodiments of the present invention, and description is more specific and in detail, but can not therefore manage It solves as the limitation to patent of invention scope.It should be pointed out that for those of ordinary skill in the art, this is not being departed from On the premise of inventive concept, various modifications and improvements can be made, these belong to protection scope of the present invention.Therefore, originally The protection domain of patent of invention should be determined by the appended claims.

Claims (6)

1. a kind of coated composition of pellet, it is characterized in that, it is prepared by the composition of following parts by weight:Hydroxypropyl methyl is fine Tie up 10-20 parts of element, IV10-25 parts of polyacrylic resin, 5-15 parts of amino acrylic resin and plasticizer 5-10, adhesive 5-15 parts, lubricant 10-25,1-5 parts of wetting agent.
2. the coated composition of pellet according to claim 1, it is characterized in that, by the composition preparation of following parts by weight Into:10-20 parts of hydroxypropyl methyl cellulose, 12-20 parts of polyacrylic resin IV, 5-10 parts of amino acrylic resin, Yi Jizeng Mould agent 5-8,5-10 parts, lubricant 15-20 of adhesive, 1-5 parts of wetting agent.
3. the coated composition of pellet according to claim 1, it is characterized in that, by the composition preparation of following parts by weight Into:15 parts of hydroxypropyl methyl cellulose, 18 parts of polyacrylic resin IV, 5-6 parts of amino acrylic resin and plasticizer 5- 8,5-8 parts of adhesive, 16-28 parts of lubricant, 1-5 parts of wetting agent.
4. according to the coated composition of claim 1-3 any one of them pellets, it is characterized in that, the plasticizer is glycerine three Ester and/or triethyl citrate.
5. according to the coated composition of claim 1-3 any one of them pellets, it is characterized in that, lubricant is talcum powder.
6. according to the coated composition of claim 1-3 any one of them pellets, it is characterized in that, wetting agent is that concentration is 85- 92% ethyl alcohol.
CN201611048841.5A 2016-11-21 2016-11-21 A kind of taste masking coated composition Pending CN108078953A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201611048841.5A CN108078953A (en) 2016-11-21 2016-11-21 A kind of taste masking coated composition

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN201611048841.5A CN108078953A (en) 2016-11-21 2016-11-21 A kind of taste masking coated composition

Publications (1)

Publication Number Publication Date
CN108078953A true CN108078953A (en) 2018-05-29

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CN201611048841.5A Pending CN108078953A (en) 2016-11-21 2016-11-21 A kind of taste masking coated composition

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Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1579494A (en) * 2004-01-13 2005-02-16 贵州益佰制药股份有限公司 Micropill of traditional Chinese medicine and its preparation method
CN1660104A (en) * 2005-01-13 2005-08-31 贵州圣济堂制药有限公司 Enteric coated tablet of glipizide and preparation method
CN1660248A (en) * 2004-12-20 2005-08-31 叶耀良 Dan e Fukang preparation and preparing method
CN101361703A (en) * 2008-09-24 2009-02-11 宋洪涛 Sirolimos sustained and controlled release preparation and preparation method thereof
CN101579524A (en) * 2009-03-27 2009-11-18 中山大学 Taste-masking coated composition, coated liquid and formulation
CN102614132A (en) * 2012-03-16 2012-08-01 中国医药集团总公司四川抗菌素工业研究所 Paliperidone extended-release mini pill
CN103397013A (en) * 2013-07-10 2013-11-20 浙江众益制药股份有限公司 Medicine composition pancreatin enteric capsule and preparation method thereof
CN105125524A (en) * 2015-10-20 2015-12-09 中牧南京动物药业有限公司 Tilmicosin enteric-coated pellets and preparation method thereof

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1579494A (en) * 2004-01-13 2005-02-16 贵州益佰制药股份有限公司 Micropill of traditional Chinese medicine and its preparation method
CN1660248A (en) * 2004-12-20 2005-08-31 叶耀良 Dan e Fukang preparation and preparing method
CN1660104A (en) * 2005-01-13 2005-08-31 贵州圣济堂制药有限公司 Enteric coated tablet of glipizide and preparation method
CN101361703A (en) * 2008-09-24 2009-02-11 宋洪涛 Sirolimos sustained and controlled release preparation and preparation method thereof
CN101579524A (en) * 2009-03-27 2009-11-18 中山大学 Taste-masking coated composition, coated liquid and formulation
CN102614132A (en) * 2012-03-16 2012-08-01 中国医药集团总公司四川抗菌素工业研究所 Paliperidone extended-release mini pill
CN103397013A (en) * 2013-07-10 2013-11-20 浙江众益制药股份有限公司 Medicine composition pancreatin enteric capsule and preparation method thereof
CN105125524A (en) * 2015-10-20 2015-12-09 中牧南京动物药业有限公司 Tilmicosin enteric-coated pellets and preparation method thereof

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Application publication date: 20180529