CN105797166A - Method for preparing liquid preparation through inclusion of acetaminophen by hydroxypropyl cyclodextrin - Google Patents
Method for preparing liquid preparation through inclusion of acetaminophen by hydroxypropyl cyclodextrin Download PDFInfo
- Publication number
- CN105797166A CN105797166A CN201610191048.4A CN201610191048A CN105797166A CN 105797166 A CN105797166 A CN 105797166A CN 201610191048 A CN201610191048 A CN 201610191048A CN 105797166 A CN105797166 A CN 105797166A
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- CN
- China
- Prior art keywords
- acetaminophen
- hydroxypropyl cyclodextrin
- inclusion
- liquid preparation
- heating
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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
- A61K9/0087—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
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- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
-
- 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
- A61K9/10—Dispersions; Emulsions
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Dispersion Chemistry (AREA)
- Pain & Pain Management (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses a method for preparing a liquid preparation through inclusion of acetaminophen by hydroxypropyl cyclodextrin.The method comprises the steps of weighing acetaminophen, adding purified water, and conducting heating dissolving and stirring to obtain acetaminophen dissolving solution; adding hydroxypropyl cyclodextrin to the acetaminophen dissolving solution to obtain hydroxypropyl cyclodextrin and acetaminophen saturated solution; heating the hydroxypropyl cyclodextrin and acetaminophen saturated solution, and conducting uniform stirring to achieve sufficient inclusion, so that the liquid preparation is obtained.In this way, the preparation has the advantages that taste is good, and operation is easy and convenient.
Description
Technical field
The present invention relates to medicine syrup field, the method particularly relating to make liquid preparation with hydroxypropyl cyclodextrin inclusion acetaminophen.
Background technology
Acetaminophen, molecular formula C8H9NO2, it is generally white crystalline powder, has antipyretic effect, for cat fever, arthralgia, neuralgia, migraine, cancer pain and postoperative analgesia etc..But owing to its mouthfeel is not good enough, common people are difficult to swallow, it is administered orally so often to coordinate paramedicines to be processed into syrup etc.；
Further, since acetaminophen dissolubility in water is low, need to adding the adjuvants such as propylene glycol to increase its dissolubility, make the acetaminophen of dissolving have one kerosene taste, mouthfeel is also bad, and adult fortunately takes, but is detrimental to drinking of children.
Summary of the invention
The technical problem that present invention mainly solves is to provide the method making liquid preparation with hydroxypropyl cyclodextrin inclusion acetaminophen, it is thus achieved that make liquid preparation with hydroxypropyl cyclodextrin inclusion acetaminophen.
For solving above-mentioned technical problem, the technical scheme that the present invention adopts is: the method that offer hydroxypropyl cyclodextrin inclusion acetaminophen makes liquid preparation, comprises the following steps:
(1) weigh acetaminophen, add purified water, heating for dissolving, stirring, it is thus achieved that acetaminophen lysate；
(2) in acetaminophen lysate, hydroxypropyl cyclodextrin is added, it is thus achieved that the saturated solution of hydroxypropyl cyclodextrin and acetaminophen；
(3) saturated solution of hydroxypropyl cyclodextrin with acetaminophen is heated, stir, so as to abundant inclusion, namely make product.
Preferably, the acetaminophen in described step (1) and described purified water ratio in mass ratio are 1:10-1:30.
Preferably, in described step (1), described heating for dissolving temperature is 40-80 DEG C, and described mixing time is 0.5-2 hour.
Preferably, in described step (2), the hydroxypropyl cyclodextrin of addition and acetaminophen ratio in mass ratio are 3:1-10:1.
Preferably, in described step (3), heating-up temperature is 40-80 DEG C, and mixing time is 1-4 hour.
The invention has the beneficial effects as follows: present invention hydroxypropyl cyclodextrin inclusion acetaminophen makes the method for liquid preparation by hydroxypropyl cyclodextrin inclusion acetaminophen, no longer will dissolve acetaminophen with propylene glycol and glycerol, in order to strengthen mouthfeel while raising dissolubility.
Detailed description of the invention
Technical scheme in the embodiment of the present invention will be clearly and completely described below, it is clear that described embodiment is only a part of embodiment of the present invention, rather than whole embodiments.Based on the embodiment in the present invention, all other embodiments that those of ordinary skill in the art obtain under not making creative work premise, broadly fall into the scope of protection of the invention.
The embodiment of the present invention includes:
The method making liquid preparation with hydroxypropyl cyclodextrin inclusion acetaminophen, comprises the following steps:
(1) weigh acetaminophen, add purified water, heating for dissolving, stirring, it is thus achieved that acetaminophen lysate；
(2) in acetaminophen lysate, hydroxypropyl cyclodextrin is added, it is thus achieved that the saturated solution of hydroxypropyl cyclodextrin and acetaminophen；
(3) saturated solution of hydroxypropyl cyclodextrin with acetaminophen is heated, stir, so as to abundant inclusion, namely make product.
Preferably, the acetaminophen in described step (1) and described purified water ratio in mass ratio are 1:10-1:30.
Preferably, in described step (1), described heating for dissolving temperature is 40-80 DEG C, and described mixing time is 0.5-2 hour.
Preferably, in described step (2), the hydroxypropyl cyclodextrin of addition and acetaminophen ratio in mass ratio are 3:1-10:1.
Preferably, in described step (3), heating-up temperature is 40-80 DEG C, and mixing time is 1-4 hour.
Specific embodiment 1:
Take acetaminophen 1 part, add purified water 10 parts～30 parts, heat 40～80 DEG C of dissolvings, stir 0.5～2 hour, make dissolving；
Take the acetaminophen solution after dissolving, add hydroxypropyl cyclodextrin 3 parts～10 parts, stir 1～4 hour at 40～80 DEG C so that it is fully inclusion.
Present invention hydroxypropyl cyclodextrin inclusion acetaminophen is made the method for liquid preparation and is provided the benefit that:
(1) no longer dissolve acetaminophen with propylene glycol and glycerol, be prevented effectively from kerosene taste when drinking medicine, increase acetaminophen dissolubility in liquid preparation (syrup, oral administration mixed suspension etc.), to strengthen mouthfeel and absorption simultaneously.
(2) obtain Ridenol by the method for the saturated acetaminophen of hydroxypropyl cyclodextrin, it is adaptable to adult and child, expand the scope of application.
The foregoing is only embodiments of the invention; not thereby the scope of the claims of the present invention is limited; every equivalent structure utilizing description of the present invention to make or equivalence flow process conversion; or directly or indirectly it is used in other relevant technical field, all in like manner include in the scope of patent protection of the present invention.
Claims (5)
1. the method making liquid preparation with hydroxypropyl cyclodextrin inclusion acetaminophen, it is characterised in that comprise the following steps:
(1) weigh acetaminophen, add purified water, heating for dissolving, stirring, it is thus achieved that acetaminophen lysate；
(2) in acetaminophen lysate, hydroxypropyl cyclodextrin is added, it is thus achieved that the saturated solution of hydroxypropyl cyclodextrin and acetaminophen；
(3) saturated solution of hydroxypropyl cyclodextrin with acetaminophen is heated, stir, so as to abundant inclusion, namely make product.
2. method according to claim 1, it is characterised in that the acetaminophen in described step (1) and described purified water ratio in mass ratio are 1:10-1:30.
3. method according to claim 1, it is characterised in that in described step (1), described heating for dissolving temperature is 40-80 DEG C, and described mixing time is 0.5-2 hour.
4. method according to claim 1, it is characterised in that in described step (2), the hydroxypropyl cyclodextrin of addition and acetaminophen ratio in mass ratio are 3:1-10:1.
5. method according to claim 1, it is characterised in that in described step (3), heating-up temperature is 40-80 DEG C, mixing time is 1-4 hour.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610191048.4A CN105797166A (en) | 2016-03-30 | 2016-03-30 | Method for preparing liquid preparation through inclusion of acetaminophen by hydroxypropyl cyclodextrin |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610191048.4A CN105797166A (en) | 2016-03-30 | 2016-03-30 | Method for preparing liquid preparation through inclusion of acetaminophen by hydroxypropyl cyclodextrin |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105797166A true CN105797166A (en) | 2016-07-27 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610191048.4A Pending CN105797166A (en) | 2016-03-30 | 2016-03-30 | Method for preparing liquid preparation through inclusion of acetaminophen by hydroxypropyl cyclodextrin |
Country Status (1)
| Country | Link |
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| CN (1) | CN105797166A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105944112A (en) * | 2016-06-20 | 2016-09-21 | 颜秋羊 | Preparing method for including acetaminophen with hydroxypropyl cyclodextrin |
Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4727064A (en) * | 1984-04-25 | 1988-02-23 | The United States Of America As Represented By The Department Of Health And Human Services | Pharmaceutical preparations containing cyclodextrin derivatives |
| CN102415994A (en) * | 2011-12-06 | 2012-04-18 | 张恒建 | Preparation formula of paracetamol oral solution capable of being prepared into frozen state for patient to take |
| CN102600119A (en) * | 2012-02-07 | 2012-07-25 | 海南卫康制药(潜山)有限公司 | Pediatric acetaminophen composition |
| CN102985069A (en) * | 2010-05-19 | 2013-03-20 | 联康药业克雷恩特塞提斯制药实验室有限责任公司 | Stable ready to use injectable paracetamol formulation |
| KR20140131205A (en) * | 2013-05-03 | 2014-11-12 | 주식회사 한독 | Pharmaceutical composition containing highly water-soluble drug for sustained release |
| CN105343893A (en) * | 2015-12-11 | 2016-02-24 | 中国药科大学 | Preparation method of acetaminophen-2-hydroxypropyl-beta-cyclodextrin inclusion compound |
-
2016
- 2016-03-30 CN CN201610191048.4A patent/CN105797166A/en active Pending
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4727064A (en) * | 1984-04-25 | 1988-02-23 | The United States Of America As Represented By The Department Of Health And Human Services | Pharmaceutical preparations containing cyclodextrin derivatives |
| CN102985069A (en) * | 2010-05-19 | 2013-03-20 | 联康药业克雷恩特塞提斯制药实验室有限责任公司 | Stable ready to use injectable paracetamol formulation |
| CN102415994A (en) * | 2011-12-06 | 2012-04-18 | 张恒建 | Preparation formula of paracetamol oral solution capable of being prepared into frozen state for patient to take |
| CN102600119A (en) * | 2012-02-07 | 2012-07-25 | 海南卫康制药(潜山)有限公司 | Pediatric acetaminophen composition |
| KR20140131205A (en) * | 2013-05-03 | 2014-11-12 | 주식회사 한독 | Pharmaceutical composition containing highly water-soluble drug for sustained release |
| CN105343893A (en) * | 2015-12-11 | 2016-02-24 | 中国药科大学 | Preparation method of acetaminophen-2-hydroxypropyl-beta-cyclodextrin inclusion compound |
Non-Patent Citations (1)
| Title |
|---|
| 王晓辉等: ""对乙酰氨基酚制剂研究进展"", 《武警后勤学院学报（医学版）》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105944112A (en) * | 2016-06-20 | 2016-09-21 | 颜秋羊 | Preparing method for including acetaminophen with hydroxypropyl cyclodextrin |
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| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20160727 |
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| RJ01 | Rejection of invention patent application after publication |