CN107536804A - Fexofenadine hydrochloride dry suspensoid agent and preparation method thereof - Google Patents

Abstract

The present invention relates to fexofenadine hydrochloride dry suspensoid agent and preparation method thereof, active constituents of medicine is fexofenadine hydrochloride, it is characterised in that the component including following percentage by weight is prepared：Fexofenadine hydrochloride 1% ~ 3%, filler 20% ~ 70%, flavouring 20% ~ 70%, glidant 0.1% ~ 0.5%, suspending agent 0.3% ~ 0.8%, adhesive 3% ~ 9%, cosolvent 0.5% ~ 2%.A kind of fexofenadine hydrochloride dry suspensoid agent of the present invention solves the patient compliance sex chromosome mosaicism in use of Fexofenadine customization agent in background technology, the fexofenadine hydrochloride preparation that suitable old man children and dysphagia patients use in providing, and solid dispersions solution is employed in preparation and is pelletized, both it is small to have solved this product content, caused content problem of non-uniform, it is poor also to solve this product dissolubility simultaneously, the problem of caused dissolution is slow.

Description

Fexofenadine hydrochloride dry suspensoid agent and preparation method thereof

Technical field

The present invention relates to field of medicine preparations, more particularly to a kind of antihistamine, more particularly to fexofenadine hydrochloride is done Supensoid agent and preparation method thereof.

Background technology

Fexofenadine hydrochloride is a kind of second generation H1 receptor antagonists, be mainly used in treat seasonal allergic rhinitis and Chronic idiopathic urticaria.The people that the whole world has 40% or so at present suffers from anaphylactia, and wherein children's quantity is most.Hydrochloric acid is non- Fexofenadine is treatment allergic rhinitis, the new drug of chronic idiopathic urticaria.It is the active generation of resistance amine medicine RMI 9918 Thank to product, eliminate parent Fei Nading cardiac toxic, it is impossible to which through blood-brain barrier, body absorption is fast, and oral rear 1-1.5 is small When reach Cmax, half-life period is 11-14 hours.Fexofenadine hydrochloride, which removes, possesses the excellent of second generation histamine H 1 receptor antagonist Outside point, following advantage is also equipped with：1）Mechanism of action is clear and definite；2）Long half time, long action time；3）Not by liver metabolism, energy It is used safely in the patient of hepatic disorder, to liver not damaged；4）Action character is obvious：Fexofenadine hydrochloride is to allergia nose Scorching and better tolerance effective with Chronic Spontaneous nettle rash, has certain suppression to make to skin rash block and flush caused by histamine With；5）Adverse reaction is light less, there are no cardiac toxic.

Have fexofenadine hydrochloride preparation both at home and abroad at present to be approved to list, the formulation that foreign countries ratify listing is tablet, glue Capsule, suspension and the compound preparation with pseudoephedrine, the formulation of country's approval listing is tablet and capsule, but is not had both at home and abroad The dry suspensoid agent for having fexofenadine hydrochloride reports.

As the extension of average human life and age increase the decline of swallow, oral tablet administration mode turns into A problem of concern.According to statistics, there is 50% patient not feel well for preparation prescription to answer；The patient for having 35% feels Tablet and capsule are difficult to swallow or have dysphagia, particularly the elderly and children this wide range of crowd, have impact on medicine The compliance for the treatment of.In paediatrics, gerontal patient crowd, population proportion increasingly increases, so the field is to Oral Dry Suspensions type There is widespread demand.The incidence of disease of current global anaphylactia increasingly raises, wherein most with children's quantity.Fexofenadine hydrochloride Being scheduled on the formulation of domestic approval listing includes tablet and capsule, there is no a kind of suitable child patient, gerontal patient, aphetite disorder to suffer from The new oral formulation that the special populations such as person use.Moreover, the dosage very little of fexofenadine hydrochloride preparation, the uniformity of preparation It is poor, while the dissolubility of this product is poor, dissolution is slow.

The content of the invention

It is an object of the invention to provide it is a kind of it is easy to use, dissolubility is good, the fexofenadine hydrochloride of preparation good evenness Determine dry suspensoid agent.

Another object of the present invention is to provide a kind of preparation method of fexofenadine hydrochloride dry suspensoid agent.

In order to solve problem present in background technology, foregoing invention purpose is realized, the present invention adopts the following technical scheme that：

Fexofenadine hydrochloride dry suspensoid agent,

Fexofenadine hydrochloride dry suspensoid agent, its active constituents of medicine are fexofenadine hydrochloride, including following percentage by weight Component be prepared：Fexofenadine hydrochloride 1% ~ 3%, filler 20% ~ 70%, flavouring 20% ~ 70%, glidant 0.1% ~ 0.5%th, suspending agent 0.3% ~ 0.8%, adhesive 3% ~ 9%, cosolvent 0.5% ~ 2%.

Described filler is mannitol.

Described adhesive is sodium carboxymethylcellulose or PVP K30 or its mixing.

Described suspending agent is xanthans, carragheen, Arabic gum, gelatin, sodium carboxymethylcellulose, cross-linked carboxymethyl fibre Tie up one or more mixing in plain sodium, PVP, pectin, guar gum, sodium alginate.

Described flavouring is that the one or more in sucrose, lactose, starch, mannitol, saleratus, cellulose family are mixed Close.

The invention also discloses a kind of preparation method of fexofenadine hydrochloride dry suspensoid agent, the fexofenadine hydrochloride The preparation method of dry suspensoid agent comprises the following steps to be prepared：

（1）, weigh fexofenadine hydrochloride and adhesive by recipe quantity, add the ethanol of recipe quantity 95%, stirring and dissolving, contained Drug solns are standby；

（2）, filler, cosolvent are weighed by recipe quantity, be placed in multi-functional granulator coater top spray device, open equipment, add Enter the above-mentioned drug solns that contain and carry out top spray granulation, pellet through sieves whole grain is made, then mix with additional suspending agent, glidant, flavouring Close uniformly, subpackage dress, produce.

A kind of fexofenadine hydrochloride dry suspensoid agent of the present invention solves Fexofenadine customization agent in background technology and used In patient compliance sex chromosome mosaicism, there is provided the fexofenadine hydrochloride preparation for being adapted to old man children and dysphagia patients to use, And solid dispersions solution is employed in preparation and is pelletized, both solve that this product content is small, and caused content is uneven asks The problem of topic, while it is poor also to solve this product dissolubility, caused dissolution are slow.

Embodiment

Below by embodiment, the present invention is described further.

Embodiment 1：

Fexofenadine hydrochloride dry suspensoid agent is prepared, using following prescription：（Unit：g）

And it is prepared using following preparation method：

1st, fexofenadine hydrochloride, polyoxyethylene sorbitan monoleate and PVP K30 are weighed by recipe quantity, adds recipe quantity 95% Ethanol, stirring and dissolving obtain drug containing solution for standby；

2nd, mannitol, sucrose, microcrystalline cellulose and sodium carboxymethylcellulose are weighed by recipe quantity, is placed in multi-functional granulator coater In top spray device, equipment is opened, the drug solns that contain that step 1 obtains is added and carries out top spray granulation, it is whole that obtained particle crosses 24 mesh sieves Grain, then be well mixed with additional xanthans, Abbas's sweet tea, essence and silica, subpackage, which fills, to be produced.

2nd, mannitol, sucrose, microcrystalline cellulose and sodium carboxymethylcellulose are weighed by recipe quantity, is wrapped as multi-functional granulation In clothing machine top spray device, equipment to be opened, the above-mentioned drug solns that contain is added and carries out top spray granulation, obtained particle crosses 24 mesh sieve whole grains, then It is well mixed, subpackage dress, produces with additional xanthans, Aspartame, essence and silica.

Fexofenadine hydrochloride dry suspensoid agent made from the present embodiment, solid dispersions solution is employed in preparation process Pelletized, solve the problems, such as that the small caused content of active constituents of medicine content is uneven, while also solve this product dissolving The problem of property is poor, and bioavilability is not high.

Embodiment 2：

Fexofenadine hydrochloride dry suspensoid agent is prepared, using following prescription：

Name of material	Dosage	Ratio	Purposes
				Fexofenadine hydrochloride	10.0	1%	Active component
Mannitol	598	59.8%	Filler
				Lactose	200.0	20%	Flavouring
Microcrystalline cellulose	100.0	10%	Filler
				Sodium carboxymethylcellulose	50.0	3%	Adhesive
PVP K30	10.0	3%	Adhesive
				Polyoxyethylene sorbitan monoleate	12.0	1.2%	Cosolvent
Sodium alginate	5.0	0.5%	Suspending agent
				Aspartame	5.0	0.5%	Flavouring
Essence	8.0	0.8%	Essence
				Silica	2.0	0.2%	Glidant

Preparation method and embodiment 1 are identical.

Claims (6)

1. fexofenadine hydrochloride dry suspensoid agent, its active constituents of medicine is fexofenadine hydrochloride, it is characterised in that including such as The component of lower percentage by weight is prepared：Fexofenadine hydrochloride 1% ~ 3%, filler 20% ~ 70%, flavouring 20% ~ 70% , glidant 0.1% ~ 0.5%, suspending agent 0.3% ~ 0.8%, adhesive 3% ~ 9%, cosolvent 0.5% ~ 2%.

2. fexofenadine hydrochloride dry suspensoid agent according to claim 1, it is characterised in that described filler is sweet dew Alcohol, microcrystalline cellulose or its combination.

3. fexofenadine hydrochloride dry suspensoid agent according to claim 1, it is characterised in that described adhesive is carboxylic first Base sodium cellulosate or PVP K30 or its mixing.

4. fexofenadine hydrochloride dry suspensoid agent according to claim 1, it is characterised in that described suspending agent is xanthan Glue, carragheen, Arabic gum, gelatin, sodium carboxymethylcellulose, Ac-Di-Sol, PVP, pectin, Gua Ershu One or more mixing in glue, sodium alginate.

5. fexofenadine hydrochloride dry suspensoid agent according to claim 1, it is characterised in that described flavouring be sucrose, One or more mixing in lactose, starch, mannitol, saleratus, cellulose family.

6. according to the preparation method of fexofenadine hydrochloride dry suspensoid agent described in claim 1 ~ 5 any one, it is characterised in that Comprise the following steps to be prepared：

（1）, weigh fexofenadine hydrochloride and adhesive by recipe quantity, add the ethanol of recipe quantity 95%, stirring and dissolving, contained Drug solns are standby；

（2）, filler, cosolvent are weighed by recipe quantity, be placed in multi-functional granulator coater top spray device, open equipment, add Enter the above-mentioned drug solns that contain and carry out top spray granulation, pellet through sieves whole grain is made, then mix with additional suspending agent, glidant, flavouring Close uniformly, subpackage dress, produce.