CN106137989A - A kind of pharmaceutical composition based on fexofenadine hydrochloride - Google Patents
A kind of pharmaceutical composition based on fexofenadine hydrochloride Download PDFInfo
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- CN106137989A CN106137989A CN201610569182.3A CN201610569182A CN106137989A CN 106137989 A CN106137989 A CN 106137989A CN 201610569182 A CN201610569182 A CN 201610569182A CN 106137989 A CN106137989 A CN 106137989A
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- parts
- pharmaceutical composition
- fexofenadine hydrochloride
- disintegrant
- sol
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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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth 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
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
Abstract
The present invention relates to a kind of pharmaceutical composition based on fexofenadine hydrochloride, described pharmaceutical composition is made up of the raw material of following weight portion: fexofenadine hydrochloride 60 70 parts, disintegrant 8 12 parts, 5 10 parts of precipitated calcium carbonate powder, lubricant 46 parts and sweetener 24 parts；Wherein, described disintegrant is the mixture of Ac-Di-Sol and PVPP, and described lubricant is magnesium laurylsulfate and the mixture of stearic acid U.S., and described sweetener is stevioside or saccharin sodium.It is an advantage of the current invention that: the present invention, based on the pharmaceutical composition of fexofenadine hydrochloride, on the premise of ensureing medicine Fast Stripping, decreases the consumption of disintegrant；Meanwhile, pharmaceutical composition adds sweetener, and then solve the dense and bitter problem of existing medicine, improve the compliance to treatment.
Description
Technical field
The invention belongs to pharmaceutical technology field, particularly to a kind of based on fexofenadine hydrochloride
Pharmaceutical composition.
Background technology
Fexofenadine hydrochloride is a kind of second generation H1 receptor antagonist, is the carboxylated metabolite of RMI 9918, and it selects
Block to selecting property H1 acceptor, there is good antihistamine effect, but without anti-five hydroxytryptamine, cholinolytic and adrenolytic,
Therefore there is no sedation and other central nervous system effects, blood-brain barrier can not be passed through.Fexofenadine hydrochloride can also
Suppression people's nasal epithelial cells release inflammation-causing substance, also can suppress epithelial cell ICAM-1.It is applicable to treat seasonal allergic nose
The illnesss such as inflammation, chronic idiopathic urticaria, its chemical entitled a, a-dimethyl-4-[1-hydroxyl-4-[4-(hydroxy benzophenone base)-
1-piperidyl]-butyl]-phenylacetate hydrochlorate.
At present, the fexofenadine hydrochloride product of external listing is tablet and capsule, and because of it, to there is disintegration difference, onset slow
With the shortcoming such as bioavilability is low, for conventional tablet, need to add a large amount of disintegrant, ask slowly to solve medicine disintegration
Topic, is actually also similar to that the oral disnitegration tablet being prepared for as described in Publication about Document, the addition of a large amount of disintegrants, necessarily causes tablet
The surface moisture absorption is serious.Even if in addition, be prepared into tablet and capsule disintegration rapidly, but because medicine is slightly soluble in water, equally existing molten
Go out slow problem.
Patent document CN200910079332.2 discloses a kind of fexofenadine hydrochloride orally disintegrating tablet, non-containing hydrochloric acid
Fexofenadine, compound disintegrant, filler, lubricant, compound flavouring, it is characterised in that be wherein combined disintegrant for efficiently collapsing
Solve agent, addition inside and outside superdisintegrantes；Addition inside and outside compound flavouring.
Patent document US995975 discloses a kind of fexofenadine oral disnitegration tablet, and this technology gives use 3%-15%
The technology enlightenment of tablet weight disintegrant, but its evaluation index is the dissolution rate index with hydrochloric acid as medium, although can meet the requirements,
But with hydrochloric acid as dissolution medium, bigger with the error of bioavilability, therefore this technology is not also for raw material hydrochloric acid Fei Suofei
That fixed character preferably goes out the prescription of optimal Orally-disintegrating tablet.
Patent document CN201010184558.1 discloses a kind of oral disnitegration tablet containing fexofenadine or its salt, should
Oral disnitegration tablet uses the technology of inclusion to prepare, and in the presence of main ingredient and inclusion compound are with specific ratio, can efficiently solve master
The taste of medicine and the problem of disintegration, it is simple to operation, transport and storage, applied range, applicable large-scale production.
Although above fexofenadine hydrochloride preparation achieves fater disintegration, but the technological deficiency existing is dissolution difference,
Poor bioavailability.
Additionally, another problem of fexofenadine hydrochloride preparation is that it is offending, dense in combination of oral medication
And the taste of hardship and pleasant impression, it causes, to treatment poor compliance, even without compliance, and therefore producing the validity for the treatment of
Negative effect.
For above-mentioned reasons, the absorption improving oral administration medicine is the low bioavilability of the medicine solving dissolubility difference
The key point of problem.
Content of the invention
The technical problem to be solved in the present invention be to provide one can Fast Stripping, again without a large amount of
The pharmaceutical composition based on fexofenadine hydrochloride of disintegrant.
For solving above-mentioned technical problem, the technical scheme is that a kind of medicine group based on fexofenadine hydrochloride
Compound, its innovative point is: described pharmaceutical composition is made up of the raw material of following weight portion: fexofenadine hydrochloride 60-70 part,
Disintegrant 8-12 part, precipitated calcium carbonate powder 5-10 part, lubricant 4-6 part and sweetener 2-4 part；Wherein, described disintegrant is
Ac-Di-Sol and the mixture of PVPP, and the quality of Ac-Di-Sol and PVPP
Ratio is 1:1.2-1.4；Described lubricant is the beautiful mixture of magnesium laurylsulfate and stearic acid, and magnesium laurylsulfate and hard
The beautiful mass ratio of resin acid is 1:2.1-2.7；Described sweetener is stevioside or saccharin sodium.
Further, described pharmaceutical composition is made up of the raw material of following weight portion: fexofenadine hydrochloride 64-66 part,
Disintegrant 9-11 part, precipitated calcium carbonate powder 6-8 part, lubricant 4.5-5.5 part and sweetener 2.5-3.5 part；Wherein, described collapse
Solve the mixture that agent is Ac-Di-Sol and PVPP, and Ac-Di-Sol and PVPP
Mass ratio be 1:1.25-1.35；Described lubricant is magnesium laurylsulfate and the mixture of stearic acid U.S., and laruyl alcohol sulphur
The mass ratio of acid magnesium and stearic acid U.S. is 1:2.3-2.5.
Further, described pharmaceutical composition is made up of the raw material of following weight portion: fexofenadine hydrochloride 65 parts, disintegration
Agent 10 parts, 7 parts of precipitated calcium carbonate powder, lubricant 5 parts and sweetener 3 parts；Wherein, described disintegrant is cross-linked carboxymethyl fiber
Element sodium and the mixture of PVPP, and the mass ratio of Ac-Di-Sol and PVPP is 1:1.3；Described
Lubricant be the beautiful mixture of magnesium laurylsulfate and stearic acid, and magnesium laurylsulfate and the beautiful mass ratio of stearic acid are 1:
2.4。
It is an advantage of the current invention that: the present invention, based on the pharmaceutical composition of fexofenadine hydrochloride, is ensureing that medicine is quick
On the premise of dissolution, decrease the consumption of disintegrant；Meanwhile, pharmaceutical composition adds sweetener, and then solve existing
Dense and the bitter problem of medicine, improves the compliance to treatment.
Detailed description of the invention
The following examples can make professional and technical personnel that the present invention is more fully understood, but not therefore by this
It bright is limited among described scope of embodiments.
Embodiment 1
The present embodiment is based on the pharmaceutical composition of fexofenadine hydrochloride, and it is made up of the raw material of following weight portion: the non-rope of hydrochloric acid
Fei Nading 60 parts, Ac-Di-Sol 5.45 parts, PVPP 6.55 parts, 10 parts of precipitated calcium carbonate powder, laruyl alcohol
1.94 parts of magnesium sulfate, magnesium stearate 4.06 parts and stevioside 4 parts.
Embodiment 2
The present embodiment is based on the pharmaceutical composition of fexofenadine hydrochloride, and it is made up of the raw material of following weight portion: the non-rope of hydrochloric acid
Fei Nading 60 parts, Ac-Di-Sol 5 parts, PVPP 7 parts, 10 parts of precipitated calcium carbonate powder, magnesium laurylsulfate
1.62 parts, magnesium stearate 4.38 parts and stevioside 4 parts.
Embodiment 3
The present embodiment is based on the pharmaceutical composition of fexofenadine hydrochloride, and it is made up of the raw material of following weight portion: the non-rope of hydrochloric acid
Fei Nading 60 parts, Ac-Di-Sol 5.52 parts, PVPP 6.48 parts, 10 parts of precipitated calcium carbonate powder, laruyl alcohol
1.76 parts of magnesium sulfate, magnesium stearate 4.24 parts and stevioside 4 parts.
Table 1 is that embodiment 1-3 is based on each component in disintegrant in the pharmaceutical composition of fexofenadine hydrochloride and lubricant
Mass ratio contrast table.
Table 1 embodiment 1-3 is based on each component in disintegrant in the pharmaceutical composition of fexofenadine hydrochloride and lubricant
Mass ratio contrasts
Embodiment 4
The present embodiment is based on the pharmaceutical composition of fexofenadine hydrochloride, and it is made up of the raw material of following weight portion: the non-rope of hydrochloric acid
Fei Nading 70 parts, Ac-Di-Sol 3.48 parts, PVPP 4.52 parts, 5 parts of precipitated calcium carbonate powder, laruyl alcohol sulphur
Acid 1.18 parts of magnesium, magnesium stearate 2.82 parts and saccharin sodium 2 parts.
Embodiment 5
The present embodiment is based on the pharmaceutical composition of fexofenadine hydrochloride, and it is made up of the raw material of following weight portion: the non-rope of hydrochloric acid
Fei Nading 65 parts, Ac-Di-Sol 4.45 parts, PVPP 5.55 parts, 7 parts of precipitated calcium carbonate powder, laruyl alcohol sulphur
Acid 1.47 parts of magnesium, magnesium stearate 3.53 parts and stevioside 3 parts.
Table 2 contrasts table for embodiment 3-5 based on the mass ratio of component each in the pharmaceutical composition of fexofenadine hydrochloride.
Table 2 embodiment 3-5 contrasts based on the mass ratio of component each in the pharmaceutical composition of fexofenadine hydrochloride
Above-described embodiment 1-5, based on the preparation method of the pharmaceutical composition of fexofenadine hydrochloride, specifically comprises the following steps that
(1) fexofenadine hydrochloride, disintegrant, precipitated calcium carbonate powder, lubricant and sweetener are weighed by above-mentioned weight；
(2) fexofenadine hydrochloride after weighing, disintegrant and precipitated calcium carbonate powder cross 100 mesh sieves respectively, and then mixing is all
Even；
(3) in the supplementary material powder mixing, add lubricant, prepare softwood, cross 25 mesh sieve wet granulars, 60 DEG C of air blast
It is dried 50-60 minute；
(4) dry particle crosses the 18 whole grains of mesh sieve, adds sweetener always to mix 5-10 minute, mixes；
(5) compressing tablet, fills capsule or pack, to obtain final product.
Following table is the testing result based on the pharmaceutical composition of fexofenadine hydrochloride for embodiment 1-5.
As can be seen from the above table, embodiment 1-5 is based on the pharmaceutical composition of fexofenadine hydrochloride, and disintegration is rapid, in short-term
The complete dissolution of interior energy, and the present invention is in good taste based on the pharmaceutical composition of fexofenadine hydrochloride, without bitter taste.
The general principle of the present invention and principal character and advantages of the present invention have more than been shown and described.The skill of the industry
The simply explanation it should be appreciated that the present invention is not restricted to the described embodiments, described in above-described embodiment and specification for the art personnel
The 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, these
Changes and improvements both fall within scope of the claimed invention.Claimed scope by appending claims and
Its equivalent defines.
Claims (3)
1. the pharmaceutical composition based on fexofenadine hydrochloride, it is characterised in that: described pharmaceutical composition is by following weight
The raw material composition of part: fexofenadine hydrochloride 60-70 part, disintegrant 8-12 part, precipitated calcium carbonate powder 5-10 part, lubricant 4-6
Part and sweetener 2-4 part；Wherein, described disintegrant is the mixture of Ac-Di-Sol and PVPP, and
The mass ratio of Ac-Di-Sol and PVPP is 1:1.2-1.4；Described lubricant is magnesium laurylsulfate
The mixture beautiful with stearic acid, and magnesium laurylsulfate and the beautiful mass ratio of stearic acid be 1:2.1-2.7；Described sweetener is
Stevioside or saccharin sodium.
2. the pharmaceutical composition based on fexofenadine hydrochloride according to claim 1, it is characterised in that: described medicine group
Compound is made up of the raw material of following weight portion: fexofenadine hydrochloride 64-66 part, disintegrant 9-11 part, precipitated calcium carbonate powder 6-8
Part, lubricant 4.5-5.5 part and sweetener 2.5-3.5 part；Wherein, described disintegrant is Ac-Di-Sol and friendship
Join the mixture of PVP, and the mass ratio of Ac-Di-Sol and PVPP is 1:1.25-1.35；Described
Lubricant is magnesium laurylsulfate and the mixture of stearic acid U.S., and the mass ratio of magnesium laurylsulfate and stearic acid U.S. is 1:
2.3-2.5。
3. the pharmaceutical composition based on fexofenadine hydrochloride according to claim 1, it is characterised in that: described medicine group
Compound is made up of the raw material of following weight portion: fexofenadine hydrochloride 65 parts, disintegrant 10 parts, 7 parts of precipitated calcium carbonate powder, lubrication
Agent 5 parts and sweetener 3 parts；Wherein, described disintegrant is the mixture of Ac-Di-Sol and PVPP, and
The mass ratio of Ac-Di-Sol and PVPP is 1:1.3；Described lubricant is magnesium laurylsulfate and hard
The beautiful mixture of resin acid, and magnesium laurylsulfate and the beautiful mass ratio of stearic acid be 1:2.4.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610569182.3A CN106137989A (en) | 2016-07-20 | 2016-07-20 | A kind of pharmaceutical composition based on fexofenadine hydrochloride |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610569182.3A CN106137989A (en) | 2016-07-20 | 2016-07-20 | A kind of pharmaceutical composition based on fexofenadine hydrochloride |
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|---|---|
| CN106137989A true CN106137989A (en) | 2016-11-23 |
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| CN201610569182.3A Pending CN106137989A (en) | 2016-07-20 | 2016-07-20 | A kind of pharmaceutical composition based on fexofenadine hydrochloride |
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Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003041683A2 (en) * | 2001-11-16 | 2003-05-22 | Ethypharm | Orodispersible tablets containing fexofenadine |
| WO2005013987A1 (en) * | 2003-07-31 | 2005-02-17 | Sandoz Ag | Fexofenadine composition and process for preparing |
| CN101103980A (en) * | 2006-07-14 | 2008-01-16 | 海南盛科生命科学研究院 | Fexofenadine medicinal composition |
| CN101822646A (en) * | 2009-03-06 | 2010-09-08 | 北京本草天源药物研究院 | Fexofenadine hydrochloride orally disintegrating tablet and preparation method thereof |
| CN103393613B (en) * | 2013-08-14 | 2015-08-12 | 南京正宽医药科技有限公司 | A kind of fexofenadine hydrochloride tablet agent and preparation method thereof |
-
2016
- 2016-07-20 CN CN201610569182.3A patent/CN106137989A/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003041683A2 (en) * | 2001-11-16 | 2003-05-22 | Ethypharm | Orodispersible tablets containing fexofenadine |
| WO2005013987A1 (en) * | 2003-07-31 | 2005-02-17 | Sandoz Ag | Fexofenadine composition and process for preparing |
| CN101103980A (en) * | 2006-07-14 | 2008-01-16 | 海南盛科生命科学研究院 | Fexofenadine medicinal composition |
| CN101822646A (en) * | 2009-03-06 | 2010-09-08 | 北京本草天源药物研究院 | Fexofenadine hydrochloride orally disintegrating tablet and preparation method thereof |
| CN103393613B (en) * | 2013-08-14 | 2015-08-12 | 南京正宽医药科技有限公司 | A kind of fexofenadine hydrochloride tablet agent and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| 张志荣主编: "《药剂学》", 31 March 2014, 高等教育出版社 * |
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Application publication date: 20161123 |
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