CN101869548A - Oral sustained-release dry suspension taking azithromycin as main ingredient - Google Patents
Oral sustained-release dry suspension taking azithromycin as main ingredient Download PDFInfo
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- CN101869548A CN101869548A CN200910082232A CN200910082232A CN101869548A CN 101869548 A CN101869548 A CN 101869548A CN 200910082232 A CN200910082232 A CN 200910082232A CN 200910082232 A CN200910082232 A CN 200910082232A CN 101869548 A CN101869548 A CN 101869548A
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- azithromycin
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Abstract
The invention relates to oral sustained-release dry suspension taking azithromycin as a main ingredient. The oral sustained-release dry suspension is prepared from the azithromycin serving as the main active ingredient and pharmaceutically acceptable supplementary materials by pharmaceutical technology. The oral sustained-release dry suspension of the invention has the advantages of greatly increasing the patient compliance, reducing the number of missing taking medicine, along with stable and controllable quality, safety and effectiveness.
Description
Technical field
The present invention is the oral sustained-release dry suspension of main component for a kind of azithromycin, belongs to medical technical field.
Background technology
Azithromycin chemical name 9a-azepine-9a-methyl-9-deoxidation-9a-a-homoerythromycin A is the most frequently used clinically anti-infective, and to the infection that multiple sensitive strain causes, the treatment works well.(azithromycin Azi) has, long half time stable to acid to azithromycin, and drug level height, evident in efficacy in infection site tissue and the cell, advantages such as safety and better tolerance.
Azithromycin reaches antibacterial action by suppressing ribosome 50s protein subunit matter surface.It has antibacterial activity to multiple aerobic and anaerobism gram positive bacteria, can suppress many important aerobic and anaerobic gram negative bacterias.To the isolating common pathogen of genitourinary system, as the urea bacteria of the carbamide of chlamydia trachomatis and dissolved urea, azithromycin all has activity, and atypia respiratory tract pathogenic bacterium, Chlamydia pneumoniae, mycoplasma pneumoniae are also had bacteriostatic activity.Clinical isolating campylobacter jejuni is higher than erythromycin, Clarithromycin to the sensitivity of azithromycin.Clinical isolating helicobacter pylori is very responsive to azithromycin.For some bacterial strains that produce beta lactamase, as producing enzyme Staphylococcus aureus, hemophilus influenza, haemophilus parainfluenzae, morazella catarrhalis etc., azithromycin all can be suppressed effectively.
Because the azithromycin interior concentration of histiocyte in vivo can reach more than the 3mg/kg, considerably beyond many former minimum inhibitory concentrations that cause a disease, thereby has bactericidal action.Azithromycin is bactericidal action to hemophilus influenza, legionella pneumophilia, Chlamydia pneumoniae, streptococcus pneumoniae and chlamydia trachomatis etc.
The bioavailability of oral azithromycin 500mg is 37% on an empty stomach.It is 0.4～0.45mg/L that the 500mg single oral dose reached the peak blood concentration in 2.5 hours, and peak blood drug level slightly rises behind the multiple dosing.Area under curve in 0～72 hour (AUC) is 3.39mg/ (L.h).The plasma protein binding rate of azithromycin is low, is 50% during blood drug level 0.2mg/L, is 12% during 0.5mg/L.
The azithromycin tissue permeability is good, and tissue concentration is the same period 10～100 times of blood drug level.Oral back 12 hours to 3 days of single dose 500mg, the concentration in tonsil, lung, prostate, the female reproductive system reaches 1～9mg/L, surpasses the minimum inhibitory concentration of respiratory tract, urogenital tract encountered pathogenic bacteria.Medicine is held time in tissue for a long time, at prostate, tonsil Chinese medicine t
1/2Reach 2.3 days to 3.2 days.
Oral Azithromycin dosage forms commonly used at present has tablet, capsule, granule etc.The patient that tablet and capsule are not suitable for child, old people and dysphagia takes, and to the child, divided dose is not accurate enough when taking; Though being fit to the patient of child, old people and dysphagia, granule and dry suspension take, but because macrolide antibiotics multi-flavor road is extremely bitter, though flavoring in addition when preparation, but still can not cover the bitterness of medicine effectively, thereby patient's medication compliance extreme difference.Thereby how can overcome effectively and cover bitterness and improve the dissolution of medicine, be the key issue of the oral Azithromycin for Suspension of preparation.
Summary of the invention
A kind of is the oral sustained-release dry suspension of main component with the azithromycin, it is characterized in that, the excipient substance that contains active component azithromycin and pharmaceutically acceptable salt thereof or hydrate and be fit to.
Azithromycin as claimed in claim 1 is the oral sustained-release dry suspension of main component, it is characterized in that, wherein main active is azithromycin and pharmaceutically acceptable salt and its hydrate, is preferably azithromycin dihydrate.Potency of azithromycin is 250mg～2000mg in the per unit dosage.
Described excipient substance comprises microsphere excipient, correctives, thickening agent, fluidizer, coloring agent.Wherein main component azithromycin and microsphere excipient form sustained-release micro-spheres, as the main constituent of said preparation.
Medicine carrying microballoons is by fusion-condensation process preparation, and detailed process is as follows:
A. medicine and microsphere excipient add the molten mixture that forms pastille;
B. the molten mixture that obtains among the step a is joined in the nebulizer, atomizing forms the droplet of medicine carrying;
C. the medicine carrying droplet among the step b, cooling curing forms medicine carrying microballoons.
Described microsphere excipient is poloxamer and higher fatty acids glyceride, and preferred poloxamer 407 and mountain need acid glyceride.
Described lubricant includes but not limited to magnesium stearate, calcium stearate, zinc stearate, colloidal silica, hard acyl fumaric acid sodium, Pulvis Talci, glyceryl monostearate, Macrogol 4000, polyethylene glycol 6000, Polyethylene Glycol 8000, sodium benzoate, adipic acid, fumaric acid, boric acid, sodium chloride, sodium laurylsulfate or magnesium laurylsulfate.
Described correctives comprises conventional correctives such as cherry essence, flavoring banana essence and pH buffering correctives, promptly reaches the purpose of covering bitterness by regulating environment PH, and this type of material includes but not limited to, alkaline matters such as magnesium hydroxide, anhydrous sodium phosphate.
Described thickening agent includes but not limited to xanthan gum, guar gum, locust bean gum, tragacanth gum, sodium carboxymethyl cellulose, polyvinylpyrrolidone, hydroxypropyl cellulose.
Also contain filler such as sucrose in the said preparation; Coloring agent is as FD﹠amp; C aluminum color lake, titanium dioxide;
Described azithromycin is the oral sustained-release dry suspension preparation technology of main component roughly following (describing in detail in an embodiment):
A. prepare medicine carrying microballoons by as above method;
B. with medicine carrying microballoons and correctives mix homogeneously;
C. in said mixture, add filler, coloring agent, thickening agent, mix homogeneously;
D. in said mixture, add fluidizer, mix homogeneously, packing is promptly.
Described azithromycin is the oral sustained-release dry suspension of main component, can be used for the patient's of oral drugs difficulties such as old age, child various bacterial infections.
The specific embodiment
Embodiment 1 azithromycin oral slow-release dry suspension
Prescription:
Preparation method:
A. get recipe quantity azithromycin dihydrate, behenic acid glyceride, poloxamer 407, preliminary mixture is pulverized, and crosses 40 mesh sieves, is heated to 90 ℃, and fusion keeps at least 80%, and best 90% medicine is a crystalline state.
B. with above-mentioned gained medicine carrying melt liquid, under the condition that keeps temperature, join in the rotary atomizer, atomizing, cooling obtains medicine carrying microballoons.Used nebulizer such as Niro A/S, the FX1 100mm rotary atomizer of production.
C. with step b gained medicine carrying microballoons and the magnesium hydroxide of crossing 40 mesh sieves, anhydrous sodium phosphate, fully mix homogeneously.
D. powder and the hyprolose of crossing 40 mesh sieves, xanthan gum, titanium dioxide, artificial cherry essence, artificial flavoring banana essence, fully mix homogeneously will be obtained among the step c.
E. silicon dioxide is crossed 40 mesh sieves, joins in the steps d gained medicated powder, abundant mix homogeneously, packing, every bag of about 24.45g.
Embodiment 2 azithromycin oral slow-release dry suspensions
Prescription:
Preparation method:
A. get recipe quantity azithromycin dihydrate, behenic acid glyceride, poloxamer 407, preliminary mixture is pulverized, and crosses 40 mesh sieves, is heated to 90 ℃, and fusion keeps at least 80%, and best 90% medicine is a crystalline state.
B. with above-mentioned gained medicine carrying melt liquid, under the condition that keeps temperature, join in the rotary atomizer, atomizing, cooling obtains medicine carrying microballoons.Used nebulizer such as Niro A/S, the FX1100mm rotary atomizer of production.
C. with step b gained medicine carrying microballoons and the magnesium hydroxide of crossing 40 mesh sieves, anhydrous sodium phosphate, fully mix homogeneously.
D. powder and the hyprolose of crossing 40 mesh sieves, xanthan gum, titanium dioxide, artificial cherry essence, artificial flavoring banana essence, fully mix homogeneously will be obtained among the step c.
E. silicon dioxide is crossed 40 mesh sieves, joins in the steps d gained medicated powder, abundant mix homogeneously, packing, every bag of 12.22g.
Claims (10)
1. one kind is the oral sustained-release dry suspension of main component with the azithromycin, it is characterized in that, the excipient substance that contains active component azithromycin and pharmaceutically acceptable salt thereof or hydrate and be fit to.
2. azithromycin as claimed in claim 1 is the oral sustained-release dry suspension of main component, it is characterized in that, wherein main active is azithromycin and pharmaceutically acceptable salt and its hydrate, is preferably azithromycin dihydrate.Potency of azithromycin is 250mg～2000mg in the per unit dosage.
3. azithromycin as claimed in claim 2 is the oral sustained-release dry suspension of main component, it is characterized in that, described excipient substance comprises microsphere excipient, correctives, thickening agent, fluidizer, coloring agent.
4. azithromycin as claimed in claim 3 is the oral sustained-release dry suspension of main component, it is characterized in that, wherein main component azithromycin and microsphere excipient form sustained-release micro-spheres, as the main constituent of said preparation.
5. azithromycin as claimed in claim 4 is the oral sustained-release dry suspension of main component, it is characterized in that, described microsphere excipient is poloxamer and higher fatty acids glyceride, preferred poloxamer 407 He behenic acid glyceride.
6. azithromycin as claimed in claim 5 is the oral sustained-release dry suspension of main component, it is characterized in that described lubricant includes but not limited to magnesium stearate, calcium stearate, zinc stearate, colloidal silica, hard acyl fumaric acid sodium, Pulvis Talci, glyceryl monostearate, Macrogol 4000, polyethylene glycol 6000, Polyethylene Glycol 8000, sodium benzoate, adipic acid, fumaric acid, boric acid, sodium chloride, sodium laurylsulfate or magnesium laurylsulfate.
7. azithromycin as claimed in claim 6 is the oral sustained-release dry suspension of main component, it is characterized in that, described correctives comprises conventional correctives such as cherry essence, flavoring banana essence, with pH buffering correctives, promptly reach the purpose of covering bitterness by regulating environment PH, this type of material includes but not limited to, alkaline matters such as magnesium hydroxide, anhydrous sodium phosphate.
8. azithromycin as claimed in claim 7 is the oral sustained-release dry suspension of main component, it is characterized in that described thickening agent includes but not limited to xanthan gum, guar gum, locust bean gum, tragacanth gum, sodium carboxymethyl cellulose, polyvinylpyrrolidone, hydroxypropyl cellulose.
9. azithromycin as claimed in claim 8 is the oral sustained-release dry suspension of main component, it is characterized in that, also contains filler such as sucrose in the said preparation; Coloring agent is as FD﹠amp; C aluminum color lake, titanium dioxide.
10. azithromycin as claimed in claim 9 is the oral sustained-release dry suspension of main component, can be used for the patient's of oral drugs difficulties such as old age, child various bacterial infections.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200910082232A CN101869548A (en) | 2009-04-21 | 2009-04-21 | Oral sustained-release dry suspension taking azithromycin as main ingredient |
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| Application Number | Priority Date | Filing Date | Title |
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| CN200910082232A CN101869548A (en) | 2009-04-21 | 2009-04-21 | Oral sustained-release dry suspension taking azithromycin as main ingredient |
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| CN101869548A true CN101869548A (en) | 2010-10-27 |
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| CN200910082232A Pending CN101869548A (en) | 2009-04-21 | 2009-04-21 | Oral sustained-release dry suspension taking azithromycin as main ingredient |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102028660A (en) * | 2010-12-29 | 2011-04-27 | 江苏黄河药业股份有限公司 | Gliclazide oral sustained-release dry-mixed suspension and preparation method thereof |
| CN103054813A (en) * | 2012-12-31 | 2013-04-24 | 广东先强药业有限公司 | Azithromycin oral sustained-release dry suspension and preparation method thereof |
| CN106692060A (en) * | 2017-01-17 | 2017-05-24 | 景德镇牧堂陶瓷科技有限公司 | Azithromycin dry suspension with good stability and preparation technology thereof |
| CN111643455A (en) * | 2020-06-22 | 2020-09-11 | 健民药业集团股份有限公司 | Azithromycin sustained-release dry suspension and preparation method thereof |
-
2009
- 2009-04-21 CN CN200910082232A patent/CN101869548A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102028660A (en) * | 2010-12-29 | 2011-04-27 | 江苏黄河药业股份有限公司 | Gliclazide oral sustained-release dry-mixed suspension and preparation method thereof |
| CN102028660B (en) * | 2010-12-29 | 2011-12-07 | 江苏黄河药业股份有限公司 | Gliclazide oral sustained-release dry-mixed suspension and preparation method thereof |
| CN103054813A (en) * | 2012-12-31 | 2013-04-24 | 广东先强药业有限公司 | Azithromycin oral sustained-release dry suspension and preparation method thereof |
| CN106692060A (en) * | 2017-01-17 | 2017-05-24 | 景德镇牧堂陶瓷科技有限公司 | Azithromycin dry suspension with good stability and preparation technology thereof |
| CN111643455A (en) * | 2020-06-22 | 2020-09-11 | 健民药业集团股份有限公司 | Azithromycin sustained-release dry suspension and preparation method thereof |
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Application publication date: 20101027 |