CN104523683A - Clonidine hydrochloride dry suspension and preparation method thereof - Google Patents
Clonidine hydrochloride dry suspension and preparation method thereof Download PDFInfo
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- CN104523683A CN104523683A CN201410799822.0A CN201410799822A CN104523683A CN 104523683 A CN104523683 A CN 104523683A CN 201410799822 A CN201410799822 A CN 201410799822A CN 104523683 A CN104523683 A CN 104523683A
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- clonidine hydrochloride
- dry suspension
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Abstract
The invention provides a clonidine hydrochloride dry suspension and a preparation method thereof. The clonidine hydrochloride dry suspension comprises 40-90 parts of clonidine hydrochloride, 500-2000 parts of a filler, 50-180 parts of a corrigent, 40-100 parts of a suspending aid and 10-40 parts of a flocculant. The clonidine hydrochloride dry suspension provided by the invention is uniform in distribution, good in stability, large in distribution area in the stomach and intestines, fast to absorb and high in bioavailability, fast takes effect, and has medicinal effect superior to that of a clonidine hydrochloride premix.
Description
Technical field
The present invention relates to a kind of dry suspension, particularly relate to a kind of clonidine hydrochloride dry suspension and preparation method thereof.
Background technology
Dry suspension refers to that insoluble drug and proper auxiliary materials make powder or shot-like particle, faces the used time jolting that adds water and can be dispersed into suspension for oral liquid preparation.Dry suspension belongs to suspensoid, and after adding aqueous dispersion, should meet the prescription of suspensoid, the microgranule in suspension should be dispersed, should not call in the following text rapidly, should not form cake block after sedimentation, should redispersion rapidly after jolting.Desirable suspensoid except should having effectiveness and chemical stability, also should (1) sedimentation slow, jolting energy redispersion gently after sedimentation; (2) size of suspended particles should remain unchanged in long storage periods (3) easily topple over.Above-mentioned is the physical stability of suspensoid.The feature of the existing solid preparation of dry suspension (granule), as being convenient for carrying, convenient transportation, good stability etc., having again the advantage of liquid preparation, as conveniently taken, being suitable for swallowing inconvenient patient, as child, old man.
Clonidine hydrochloride slow releasing tablet is developed by Addrenex Pharmaceuticals company of the U.S., and JIUYUE in 2009 obtains U.S. FDA approval on the 29th and is used for the treatment of hypertension, specification: 0.1mg, 0.2mg.On JIUYUE 30th, 2009, Shionogi Pharma company have submitted the new drug replacement demand of additional clonidine hydrochloride slow releasing tablet indication to FDA, and within 28th, obtain in JIUYUE in 2010 ADHD that U.S. FDA ratifies to be used for the treatment of 6 ~ 17 years old Children and teenager, can be used as the adjuvant drug that single therapy also can be used as central stimulants, specification: 0.1mg, 0.2mg, becoming the first clonidine formulations being used for the treatment of ADHD got the Green Light in global range, is the α that the U.S. second of getting the Green Light after Guanfacine Hydrochloride slow releasing tablet is used for the treatment of ADHD
2-adrenoceptor agonists.Wherein the clonidine hydrochloride slow releasing tablet of 0.1mg specification in January, 2011 in U.S.'s list marketing, the sale and 0.2mg specification is not gone public so far.
China at present existing many companies produces clonidine hydrochloride raw material and is used for the treatment of the preparation of the indications such as hypertension, comprise oral tablet, dry suspension, drop pill, injection, eye drop, in addition also have clonidine transdermal patch, and the clonidine formulations being approved for treatment ADHD still belongs to internal blank.
Summary of the invention
The present invention, in order to solve existing clonidine hydrochloride poorly water-soluble, shortcoming that bioavailability is low, has invented clonidine hydrochloride dry suspension.
Composition and the mass fraction of clonidine hydrochloride dry suspension of the present invention are as follows:
Clonidine hydrochloride 40-100 part
Filler 600-2200 part
Correctives 50-200 part
Suspending agent 40-100 part
Flocculating agent 10-40 part
Preferably, the mass fraction of each composition is as follows:
Clonidine hydrochloride 50 parts
Filler 700 parts
Correctives 50 parts
Suspending agent 50 parts
Flocculating agent 10 parts
Described filler is selected from mannitol, microcrystalline Cellulose or lactose; Described correctives is selected from aspartame and stevioside; Described suspending agent be selected from methylcellulose, carboxylic propyl methocel, hydroxypropyl cellulose, sodium alginate, agar, starch slurry, polyvidone or glucosan any one or multiple; Flocculating agent is selected from disodium hydrogen phosphate,anhydrous.
Applicant is surprised to find that and selects the compositions of methylcellulose and glucosan to be suspending agent, and when the two mass ratio is 2:1, the dry suspension sedimentation volume ratio prepared is large, and redispersibility is good.
The preparation method of described clonidine hydrochloride dry suspension, is characterized in that comprising the following steps:
(1) clonidine hydrochloride taking recipe quantity crosses 80-120 mesh sieve;
(2) filler of recipe quantity, correctives, suspending agent and flocculating agent is taken respectively, after crossing 80-120 mesh sieve respectively, equal increments mix homogeneously;
(3) step (1) and (2) equal increments mix homogeneously are obtained mixed-powder, cross 30-40 mesh sieve;
(4) intermediate detect qualified after, subpackage finished product.
Compared with prior art, the present invention has following features:
(1) clonidine hydrochloride dry suspension even particle distribution of the present invention, good stability, large at the distribution area of gastrointestinal, absorb fast, bioavailability is high, drug effect is fast, drug effect is better than clonidine hydrochloride pre-mixing agent.
(2) compared with prior art, though the dry suspension that the present invention relates to is solid preparation, adds water before use and can become liquid preparation, easy mix homogeneously and time saving and energy saving, solving clonidine hydrochloride can not the use restricted problem of drinking water administration.
(3) the clonidine hydrochloride dry suspension preparation technology that the present invention relates to is simple, be easy to preserve, effect duration is long, not perishable and easily grasp dosage, the large production of applicable company.
Detailed description of the invention
Embodiment 1
Prescription 1
Clonidine hydrochloride 50g
Mannitol 700g
Aspartame 50g
Methylcellulose: glucosan (2:1) 50g
Disodium hydrogen phosphate,anhydrous 10g
Embodiment 2
Prescription 2
Clonidine hydrochloride 50g
Mannitol 700g
Aspartame 50g
Methylcellulose: glucosan (1:1) 50g
Disodium hydrogen phosphate,anhydrous 10g
Embodiment 3
Prescription 3
Clonidine hydrochloride 50g
Mannitol 700g
Aspartame 50g
Methylcellulose: glucosan (3:1) 50g
Disodium hydrogen phosphate,anhydrous 10g
Embodiment 4
Prescription 4
Clonidine hydrochloride 50g
Mannitol 700g
Aspartame 50g
Methylcellulose: glucosan (4:1) 50g
Disodium hydrogen phosphate,anhydrous 10g
Embodiment 5
Prescription 5
Clonidine hydrochloride 50g
Mannitol 700g
Aspartame 50g
Methylcellulose: glucosan (5:1) 50g
Disodium hydrogen phosphate,anhydrous 10g
Embodiment 6
Prescription 6
Clonidine hydrochloride 50g
Mannitol 700g
Aspartame 50g
Methylcellulose: glucosan (1:2) 50g
Disodium hydrogen phosphate,anhydrous 10g
Above-mentioned prescription is prepared by following production technology: the clonidine hydrochloride that (1) precision takes recipe quantity crosses 80 mesh sieves; (2) precision takes mannitol, aspartame, methylcellulose, glucosan, the disodium hydrogen phosphate,anhydrous of recipe quantity respectively, after crossing 80 mesh sieves respectively, and equal increments mix homogeneously; (3) step (1) and (2) equal increments mix homogeneously are obtained mixed-powder, cross 40 mesh sieves; (4) intermediate detection qualified after, subpackage finished product.
Test example 1 dry suspension settling property and suspendible performance test
According to " Chinese Pharmacopoeia " version in 2010 about the regulation of dry suspension sedimentation volume ratio is tested, the results are shown in following table:
From data, clonidine hydrochloride dry suspension sedimentation volume ratio of the present invention is all greater than 0.9, meets States Pharmacopoeia specifications.And select methylcellulose: the compositions of polyvidone (mass ratio is 2:1) is that the redispersibility of the prescription 1 of suspending agent is significantly better than other prescription.
Claims (4)
1. a dry suspension, comprising: clonidine hydrochloride, filler, correctives, suspending agent and flocculating agent; Wherein the mass fraction of each composition is:
Clonidine hydrochloride 50-80 part
Filler 700-1800 part
Correctives 50-160 part
Suspending agent 50-100 part
Flocculating agent 10-40 part.
2. dry suspension as claimed in claim 1, wherein the mass fraction of each composition is:
Clonidine hydrochloride 50 parts
Filler 700 parts
Correctives 50 parts
Suspending agent 50 parts
Flocculating agent 10 parts.
3. dry suspension as claimed in claim 2 or claim 3, wherein filler is selected from mannitol, microcrystalline Cellulose and lactose; Correctives is selected from aspartame and stevioside; Suspending agent be selected from methylcellulose, carboxylic propyl methocel, hydroxypropyl cellulose, sodium alginate, agar, starch slurry, polyvidone or glucosan any one or multiple; Flocculating agent is selected from disodium hydrogen phosphate,anhydrous.
4. dry suspension as claimed in claim 2 or claim 3, wherein suspending agent is the compositions of methylcellulose and glucosan, and the two mass ratio is 2:1.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410799822.0A CN104523683B (en) | 2014-12-22 | 2014-12-22 | Clonidine hydrochloride dry suspension and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410799822.0A CN104523683B (en) | 2014-12-22 | 2014-12-22 | Clonidine hydrochloride dry suspension and preparation method thereof |
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| Publication Number | Publication Date |
|---|---|
| CN104523683A true CN104523683A (en) | 2015-04-22 |
| CN104523683B CN104523683B (en) | 2017-05-17 |
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| CN201410799822.0A Active CN104523683B (en) | 2014-12-22 | 2014-12-22 | Clonidine hydrochloride dry suspension and preparation method thereof |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11357756B2 (en) | 2017-01-20 | 2022-06-14 | Warsaw Orthopedic, Inc. | Anesthetic compositions and methods comprising imidazoline compounds |
| EP4122450A1 (en) | 2021-07-20 | 2023-01-25 | Rosemont Pharmaceuticals Ltd | Liquid pharmaceutical composition of clonidine |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20140093578A1 (en) * | 2010-10-20 | 2014-04-03 | Tris Pharma, Inc. | Novel clonidine formulation |
-
2014
- 2014-12-22 CN CN201410799822.0A patent/CN104523683B/en active Active
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20140093578A1 (en) * | 2010-10-20 | 2014-04-03 | Tris Pharma, Inc. | Novel clonidine formulation |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11357756B2 (en) | 2017-01-20 | 2022-06-14 | Warsaw Orthopedic, Inc. | Anesthetic compositions and methods comprising imidazoline compounds |
| EP4122450A1 (en) | 2021-07-20 | 2023-01-25 | Rosemont Pharmaceuticals Ltd | Liquid pharmaceutical composition of clonidine |
Also Published As
| Publication number | Publication date |
|---|---|
| CN104523683B (en) | 2017-05-17 |
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Address after: 266000 3601 Tuen Jie Road, Qingdao economic and Technological Development Zone, Shandong Patentee after: Zhengda Pharmaceutical (Qingdao) Co., Ltd. Address before: 266000 3601 Tuen Jie Road, Qingdao economic and Technological Development Zone, Shandong Patentee before: Qingdao Zhengda Haier Pharmaceutical Co., Ltd. |