CN102525979B - Infant ibuprofen composition - Google Patents
Infant ibuprofen composition Download PDFInfo
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- CN102525979B CN102525979B CN 201210029059 CN201210029059A CN102525979B CN 102525979 B CN102525979 B CN 102525979B CN 201210029059 CN201210029059 CN 201210029059 CN 201210029059 A CN201210029059 A CN 201210029059A CN 102525979 B CN102525979 B CN 102525979B
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Abstract
The invention discloses an infant ibuprofen composition and relates to the technical field of medicinal preparations. The composition comprises the following components: 13 to 32 weight percent of ibuprofen, 32 to 40 weight percent of mannitol, 2 to 4 weight percent of gelatin, 0.2 to 1.0 weight percent of xanthan gum, 32 to 40 weight percent of hydroxypropyl-beta-cyclodextrin with medium substitution degree, and 0.1 to 0.15 weight percent of sucralose. The invention also discloses infant ibuprofen composition lyophilized orally disintegrating tablets containing the composition. The lyophilized orally disintegrating tablets have simple components, can be taken without water, are not required to be chewed, are quickly absorbed, have high bioavailability, a low side effect, a low liver first-pass effect and good mouthfeel, and can be taken by infant patients, the disintegration time in oral cavities of human bodies does not exceed 2 seconds, and the residue in intestines is low.
Description
Technical field
The present invention relates to technical field of medicine, be specifically related to a kind of infant ibuprofen composition and contain infant ibuprofen composition freeze-dry orally disintegrating tablet that above-mentioned composition makes and preparation method thereof.
Background technology
Ibuprofen is a kind of efficient non-steroidal anti-inflammatory antipyretic analgesic, has the characteristics rapid, longer duration of bringing down a fever, and is widely used in clinically children's's the treatment of bringing down a fever.Ibuprofen and acetaminophen, aspirin, diclofenac become four large pillar products on China antipyretic analgesic market together.But ibuprofen has the characteristic of oneself in clinical practice, is all safely and effectively antipyretic, and when body temperature was higher than 39.2 ℃, ibuprofen was than more effective with the acetaminophen of dosage, and fever time is longer.Pharmacodynamic study proves: the analgesia of this medicine, refrigeration function are respectively 28 times and 20 times of aspirin, and its untoward reaction is lacked than aspirin and light.
At present in the preparation take ibuprofen as major ingredient, there are 13 kinds of dosage forms to be put into China's list of OTC medicines, it is one of maximum OTC antipyretic analgesic of preparation variety, in national basic medical medicine catalogue, ibuprofen is one of three Class A products of non-steroidal anti-inflammatory analgesic.The huge market demand, potentiality are very wide.
Mainly be dispersant, sustained-release preparation to the research of ibuprofen both at home and abroad, the conventional dosage forms GI irritation is large, and bioavailability is low, and even feels sick, the side effect such as the vomiting, erythra are larger, is not suitable for especially pediatric patient and takes.And oral formulations needs with water delivery service or slice, thin piece hardness very large more, this patient for dysphagia or water intaking inconvenience takes and has certain difficulty, particularly take very inconvenient for child patient, the ibuprofen oral disintegrating tablets of selling on the market is with multiple auxiliary materials and disintegrating agent, utilizes traditional tablet machine compacting to form, 30 seconds of the minimum needs of its disintegration time in human oral cavity, and in the mouth grains of sand sense is arranged, the child also is not suitable for, Given this, proposes the present invention.Infant ibuprofen composition freeze-dry orally disintegrating tablet component of the present invention is simple, need not water when taking, need not to chew, disintegration time was no more than for 2 seconds in human oral cavity, absorbed fast, bioavailability is high, intestinal is residual few, and side effect is low, and liver first-pass effect is little, mouthfeel is good, is particularly suitable for the infant patient and takes.
Summary of the invention
Technical problem to be solved by this invention is to provide a kind of composition simple, easily manufactured, rapid-action infant ibuprofen composition and contain infant ibuprofen composition freeze-dry orally disintegrating tablet that above-mentioned composition makes and preparation method thereof.
Technical problem to be solved by this invention realizes by the following technical solutions.
A kind of infant ibuprofen composition, the prescription of said composition is made of principal agent and accessory drugs, it is characterized in that: wherein principal agent is ibuprofen, accessory drugs comprises skeleton agent, forming agent, odor mask, correctives, mannitol is selected in described skeleton agent, and described forming agent is selected gelatin and xanthan gum, and described odor mask is selected medium substitution value hydroxypropyl-beta-schardinger dextrin-, described correctives is selected sucralose, wherein principal agent and accessory drugs by weight the prescription total amount in shared ratio be:
Described compositions preferably includes following composition:
Another object of the present invention provides a kind of infant ibuprofen composition freeze-dry orally disintegrating tablet that contains above-mentioned infant ibuprofen composition, and this freeze-dry orally disintegrating tablet component is simple, need not water when taking, need not to chew, disintegration time was no more than for 2 seconds in human oral cavity, and is rapid-action, and intestinal is residual few, liver first-pass effect is little, absorb fully, side effect is low, and mouthfeel is good, be particularly suitable for the infant patient and take, its composition by following weight portion is prepared from:
Described infant ibuprofen composition freeze-dry orally disintegrating tablet, it preferably is prepared from by following composition:
Described infant ibuprofen composition freeze-dry orally disintegrating tablet specification is 50mg/ sheet or 100mg/ sheet.
For realizing a further object of the present invention, a kind of preparation method of infant ibuprofen composition freeze-dry orally disintegrating tablet adopts following technical scheme:
A) the medium substitution value hydroxypropyl-beta-schardinger dextrin-of recipe quantity is dissolved in the purified water of 70%-80% of prescription water total amount, under stirring, be heated to 65 ℃, the ibuprofen that slowly adds recipe quantity, continue to stir 14 hours, treat medium substitution value hydroxypropyl-beta-schardinger dextrin-with after the ibuprofen enclose, add mannitol, the sucralose of recipe quantity;
B) gelatin and the xanthan gum with recipe quantity is dissolved in the purified water of prescription water consumption 20%-30%, is heated to fully dissolving;
C) merge above-mentioned a, two kinds of solution of b and stir;
D) regulate pH value to 7.0-7.5 with sodium bicarbonate;
E) according to infant ibuprofen composition freeze-dry orally disintegrating tablet specification, after determining loading amount, medicinal liquid after merging is moved in the drug-containing dish by loading amount, and put into freeze drying box, medicinal liquid is carried out freezing (cryogenic temperature is-20 ℃--50 ℃), evacuation dry (baking temperature is at+5 ℃-+20 ℃, and vacuum is 0.1 handkerchief-20 handkerchief), the control moisture is no more than 1.0%;
F) after infant ibuprofen composition freeze-dry orally disintegrating tablet drying, in freeze drying box, seal;
G) will cut drug-containing dish behind the medicament taking-up freeze drying box that freeze, and carry out finished product packing.
We have formulated relevant detection method for the disintegration rate of infant ibuprofen composition freeze-dry orally disintegrating tablet:
1, disintegration
According to inspection technique disintegration (two appendix x of Chinese Pharmacopoeia version in 2010 A), the stainless steel shaft of hanging basket by the upper end hung on the metal rack, immerse in the 1000ml beaker, and when regulating the hanging basket position it being descended screen cloth apart from beaker bottom 25mm, fill temperature in the beaker and be 37 ℃ ± 1 ℃ water, screen cloth is at underwater 15mm place when regulating height of water level hanging basket being risen.
Except as otherwise herein provided, get 5 groups of test samples (every group of dosage is 200mg), be set up respectively in the glass tubing of stating hanging basket, add baffle plate, start disintegration tester and check, each sheet all should all disintegrates in 1.1 seconds.
Result such as following table:
Dosage equates, the disintegration time of different Genprils
The disintegration rate that can find out infant ibuprofen composition freeze-dry orally disintegrating tablet of the present invention from above experimental result is faster than the ibuprofen oral disintegrating tablets of ibuprofen ordinary tablet, the manufacturing of traditional pressing.
The selected adjuvant of infant ibuprofen composition freeze-dry orally disintegrating tablet all is the adjuvants that are suitable for this tablet of preparation, water-soluble hardly according to the research ibuprofen, for improving its dissolubility, so add medium substitution value hydroxypropyl-beta-schardinger dextrin-in prescription, consumption is the 100%-300% of ibuprofen quality in the prescription.Use medium substitution value hydroxypropyl-beta-schardinger dextrin-in this prescription, be that to have a haemolysis little because of it, stimulate slightly, the advantages such as metabolism occur in human body hardly, and month. be conducive to improve dissolubility, stability and the bioavailability of medicine, and can improve the quality of medicament.
Since infant ibuprofen composition freeze-dry orally disintegrating tablet of the present invention mainly in order to satisfy child's medication demand, and the ibuprofen taste is pungent, for improving the compliance of children, has added the correctives sucralose in prescription.In traditional production application, aspartame flavour mouthfeel is pretty good, but easily decomposes, and is unstable; Cyclamate, glucide safety are subjected to dispute to a certain extent, and bitterness after easily producing.And the sucralose sweet feel is very near sucrose, and is very stable, safe to heat, acid, alkali.Simultaneously, sucralose is not utilized by the dental caries pathogenic bacteria, can reduce pathogenic bacteria in the oral cavity, and the acid amount of generation and streptococcus cell effectively play the dental caries effect in the adhesion of dental surface, and useful especially teenager teeth is healthy; The sucralose good stability can long term storage, and can not be damaged in freezing dry process, is fit to industrial applications.
This dosage form has the following advantages:
The first disintegrate is rapid, and drug effect is fast.Infant ibuprofen composition freeze-dry orally disintegrating tablet of the present invention is rapidly disintegrate in 2 seconds in mouth, is beneficial to the rapid stripping of medicine, shortens dissolution time, accelerates to absorb, and liver first-pass effect is little, makes its fast performance curative effect.
The second drug absorption is abundant.Infant ibuprofen composition freeze-dry orally disintegrating tablet of the present invention is fully disintegrate in the oral cavity, makes the absorption of medicine more abundant, is conducive to like this improve the bioavailability of medicine.
The 3rd taking convenience, mouthfeel is good.Infant ibuprofen composition freeze-dry orally disintegrating tablet of the present invention needn't be used water delivery service, and saliva can make its complete disintegrate, and foreign sense in mouthful is owing to wherein adding the compliance that the sweet child of being conducive to of suitable correctives cool taste flavor takes medicine.Compare with liquid preparation and accurately advantage of dosage arranged.
The specific embodiment
For technological means, creation characteristic that the present invention is realized, reach purpose and effect is easy to understand, below in conjunction with specific embodiment, further set forth the present invention.
Embodiment 1
Preparation infant ibuprofen composition freeze-dry orally disintegrating tablet,
Prescription: 1000 amounts
Preparation technology:
Medium substitution value hydroxypropyl-the beta-schardinger dextrin-of recipe quantity is dissolved in 80% the purified water of prescription water total amount, under stirring, be heated to 65 ℃, the ibuprofen that slowly adds recipe quantity, continue to stir 14 hours, treat that medium substitution value hydroxypropyl-beta-schardinger dextrin-is with after the ibuprofen enclose, the mannitol that adds recipe quantity, sucralose, gelatin and the xanthan gum of recipe quantity are dissolved in the purified water of prescription water consumption 20%, be heated to fully dissolving, merge above-mentioned two kinds of solution and stir, regulate pH value to 7.0-7.5 with sodium bicarbonate, according to infant ibuprofen composition freeze-dry orally disintegrating tablet specification, after determining loading amount, the medicinal liquid after merging is pressed in the loading amount packing drug-containing dish, and put into freeze drying box, carry out freezing to medicinal liquid, after infant ibuprofen composition freeze-dry orally disintegrating tablet drying, in freeze drying box, seal cutting after taking out, packing.
Embodiment 2
Preparation infant ibuprofen composition freeze-dry orally disintegrating tablet,
Prescription: 1000 amounts
Preparation technology:
Medium substitution value hydroxypropyl-the beta-schardinger dextrin-of recipe quantity is dissolved in 80% the purified water of prescription water total amount, under stirring, be heated to 65 ℃, the ibuprofen that slowly adds recipe quantity, continue to stir 14 hours, treat that medium substitution value hydroxypropyl-beta-schardinger dextrin-is with after the ibuprofen enclose, the mannitol that adds recipe quantity, sucralose, gelatin and the xanthan gum of recipe quantity are dissolved in the purified water of prescription water consumption 20%, be heated to fully dissolving, merge above-mentioned two kinds of solution and stir, regulate pH value to 7.0-7.5 with sodium bicarbonate, according to infant ibuprofen composition freeze-dry orally disintegrating tablet specification, after determining loading amount, the medicinal liquid after merging is pressed in the loading amount packing drug-containing dish, and put into freeze drying box, carry out freezing to medicinal liquid, after infant ibuprofen composition freeze-dry orally disintegrating tablet drying, in freeze drying box, seal cutting after taking out, packing.
Embodiment 3
Preparation infant ibuprofen composition freeze-dry orally disintegrating tablet,
Prescription: 1000 amounts
Preparation technology:
Medium substitution value hydroxypropyl-the beta-schardinger dextrin-of recipe quantity is dissolved in 80% the purified water of prescription water total amount, under stirring, be heated to 65 ℃, the ibuprofen that slowly adds recipe quantity, continue to stir 14 hours, treat that medium substitution value hydroxypropyl-beta-schardinger dextrin-is with after the ibuprofen enclose, the mannitol that adds recipe quantity, sucralose, gelatin and the xanthan gum of recipe quantity are dissolved in the purified water of prescription water consumption 20%, be heated to fully dissolving, merge above-mentioned two kinds of solution and stir, regulate pH value to 7.0-7.5 with sodium bicarbonate, according to infant ibuprofen composition freeze-dry orally disintegrating tablet specification, after determining loading amount, the medicinal liquid after merging is pressed in the loading amount packing drug-containing dish, and put into freeze drying box, carry out freezing to medicinal liquid, after infant ibuprofen composition freeze-dry orally disintegrating tablet drying, in freeze drying box, seal cutting after taking out, packing.
Above demonstration and described ultimate principle of the present invention and principal character and advantage of the present invention.The technical staff of the industry should understand; the present invention is not restricted to the described embodiments; that describes in above-described embodiment and the description just illustrates principle of the present invention; without departing from the spirit and scope of the present invention; the present invention also has various changes and modifications, and these changes and improvements all fall in the claimed scope of the invention.The claimed scope of the present invention is defined by appending claims and equivalent thereof.
Claims (5)
1. infant ibuprofen composition, the prescription of said composition is made of principal agent and accessory drugs, it is characterized in that: wherein principal agent is ibuprofen, accessory drugs comprises skeleton agent, forming agent, odor mask, correctives, mannitol is selected in described skeleton agent, and described forming agent is selected gelatin and xanthan gum, and described odor mask is selected medium substitution value hydroxypropyl-beta-schardinger dextrin-, described correctives is selected sucralose, wherein principal agent and accessory drugs by weight the prescription total amount in shared ratio be:
2. a kind of infant ibuprofen composition according to claim 1, it is characterized in that: described compositions preferably includes following composition:
3. infant ibuprofen composition freeze-dry orally disintegrating tablet that contains infant ibuprofen composition claimed in claim 1, it is characterized in that: described freeze-dry orally disintegrating tablet is prepared from by the composition of following weight portion:
4. infant ibuprofen composition freeze-dry orally disintegrating tablet according to claim 3, it is characterized in that: it preferably is prepared from by the composition of following weight portion:
5. the preparation method of an infant ibuprofen composition freeze-dry orally disintegrating tablet, it is characterized in that: described preparation method adopts following technical scheme:
A) the medium substitution value hydroxypropyl-beta-schardinger dextrin-of recipe quantity is dissolved in the purified water of 70%-80% of prescription water total amount, under stirring, be heated to 65 ℃, the ibuprofen that slowly adds recipe quantity, continue to stir 14 hours, treat medium substitution value hydroxypropyl-beta-schardinger dextrin-with after the ibuprofen enclose, add mannitol, the sucralose of recipe quantity;
B) gelatin and the xanthan gum with recipe quantity is dissolved in the purified water of prescription water consumption 20%-30%, is heated to fully dissolving;
C) merge above-mentioned a, two kinds of solution of b and stir;
D) regulate pH value to 7.0-7.5 with sodium bicarbonate;
E) according to infant ibuprofen composition freeze-dry orally disintegrating tablet specification, after determining loading amount, medicinal liquid after merging is moved in the drug-containing dish by loading amount, and put into freeze drying box, medicinal liquid is carried out freezing (cryogenic temperature is-20 ℃--50 ℃), evacuation dry (baking temperature is at+5 ℃-+20 ℃, and vacuum is 0.1 handkerchief-20 handkerchief), the control moisture is no more than 1.0%;
F) after infant ibuprofen composition freeze-dry orally disintegrating tablet drying, in freeze drying box, seal;
G) will cut drug-containing dish behind the medicament taking-up freeze drying box that freeze, and carry out finished product packing.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201210029059 CN102525979B (en) | 2012-02-07 | 2012-02-07 | Infant ibuprofen composition |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201210029059 CN102525979B (en) | 2012-02-07 | 2012-02-07 | Infant ibuprofen composition |
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| CN102525979A CN102525979A (en) | 2012-07-04 |
| CN102525979B true CN102525979B (en) | 2013-03-27 |
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| CN 201210029059 Active CN102525979B (en) | 2012-02-07 | 2012-02-07 | Infant ibuprofen composition |
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Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN103432125B (en) * | 2013-09-10 | 2015-04-01 | 北京首儿药厂 | Preparation method of compound zinc gluconate and ibuprofen granules |
| CN111658622A (en) * | 2020-07-24 | 2020-09-15 | 山东新华制药股份有限公司 | Oral instant film agent containing ibuprofen inclusion compound and preparation method thereof |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1582221A1 (en) * | 2004-03-31 | 2005-10-05 | Chiesi S.A. | Pharmaceutical oral compositions with a taste masking effect |
| CN1931168A (en) * | 2005-09-12 | 2007-03-21 | 北京正光恒业控释制剂研究中心 | Oral disintegrated difenidol hydrochloride tablet and its prepn process |
| CN101134022A (en) * | 2006-08-31 | 2008-03-05 | 海南海灵制药厂有限公司 | Lyophilized orally disintegrating tablets with better mechanical property and method for preparing the same |
| WO2010144943A1 (en) * | 2009-05-20 | 2010-12-23 | Ozpharma Pty Ltd | Buccal and/or sublingual therapeutic formulation |
| WO2011110939A2 (en) * | 2010-03-11 | 2011-09-15 | Rubicon Research Private Limited | Pharmaceutical compositions of substituted benzhydrylpiperazines |
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2012
- 2012-02-07 CN CN 201210029059 patent/CN102525979B/en active Active
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1582221A1 (en) * | 2004-03-31 | 2005-10-05 | Chiesi S.A. | Pharmaceutical oral compositions with a taste masking effect |
| CN1931168A (en) * | 2005-09-12 | 2007-03-21 | 北京正光恒业控释制剂研究中心 | Oral disintegrated difenidol hydrochloride tablet and its prepn process |
| CN101134022A (en) * | 2006-08-31 | 2008-03-05 | 海南海灵制药厂有限公司 | Lyophilized orally disintegrating tablets with better mechanical property and method for preparing the same |
| WO2010144943A1 (en) * | 2009-05-20 | 2010-12-23 | Ozpharma Pty Ltd | Buccal and/or sublingual therapeutic formulation |
| WO2011110939A2 (en) * | 2010-03-11 | 2011-09-15 | Rubicon Research Private Limited | Pharmaceutical compositions of substituted benzhydrylpiperazines |
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