CN103040787A - Azithromycin capsule and preparation method thereof - Google Patents
Azithromycin capsule and preparation method thereof Download PDFInfo
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- CN103040787A CN103040787A CN2012105676952A CN201210567695A CN103040787A CN 103040787 A CN103040787 A CN 103040787A CN 2012105676952 A CN2012105676952 A CN 2012105676952A CN 201210567695 A CN201210567695 A CN 201210567695A CN 103040787 A CN103040787 A CN 103040787A
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- azithromycin
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Abstract
The invention relates to an azithromycin capsule which comprises azithromycin capsule comprises azithromycin, a filling agent, an adhesive and a glidant, and further relates to a preparation method of the azithromycin capsule. In the technical scheme, raw materials are made into a micropill capsule, and medicines are uniformly dispersed, so that the problem that the main medicine has low probability of absorbing water is solved, the product quality is improved, and the medicine stability is guaranteed. The capsule has the advantages of high dissolution speed and high bioavailability, and the preparation method provided by the invention is simple to operate, is under mild conditions and is suitable for large-scale industrial production.
Description
Technical field
The present invention relates to field of pharmaceutical preparations, be specifically related to a kind of azithromycin capsule agent and preparation method thereof.
Background technology
Azithromycin is the azalides antibiotic, and its mechanism of action is by being combined with the ribosomal subunit of the 50s of sensitive microbial, thereby disturbs synthetic (not the affecting the synthetic of nucleic acid) of its albumen.Be used for the treatment of clinically: 1, the acute pharyngitis, the acute tonsillitis that cause of micrococcus scarlatinae.2, the sinusitis, acute otitis media, acute bronchitis, the acute episode of chronic bronchitis that cause of sensitive bacterial.3, the pneumonia due to streptococcus pneumoniae, hemophilus influenza and the mycoplasma pneumoniae.4, urethritis and the cervicitis due to chlamydia trachomatis and the non-several drug resistance Diplococcus gonorrhoeae.5, the skin soft-tissue infection that causes of sensitive bacterial.
Absorb rapidly behind the azithromycin oral, bioavailability is 37%.Behind the oral 0.5g of single dose, peak time is 2.5～2.6 hours, and blood peak concentration of drug (Cmax) is 0.4～0.45mg/L.Azithromycin is widely distributed in vivo, and concentration can reach 10～100 times of the blood concentration same period in each tissue, concentration height in macrophage and fibroblast, and the former can be transported to inflammation part with azithromycin.It is 35～48 hours that blood after the administration of azithromycin single dose is eliminated the half-life (t1/2 β), the discharging through biliary tract with original shape 50% or more of dosage, after the administration in 72 hours about 4.5% with original shape through the urine discharge.The Binding rate of serum protein of azithromycin lowers with the increase of blood drug level, and when blood drug level was 0.02 μ g/ml, Binding rate of serum protein was 15%; When blood drug level was 2 μ g/ml, Binding rate of serum protein was 7%.Foreign data shows, light moderate renal insufficiency patient (glomerular filtration rate be 10～80ml/min) medicines for parameter without significant change, severe renal functional defect person (glomerular filtration rate is less than 10ml/min) has significant difference with normal person, and systemic exposure increases by 33%.
Azithromycin often uses the dosage form of the oral administration administrations such as capsule, tablet, granule clinically.Although the dosage forms such as bulk capacity injection are also arranged, Azithromycin injection self is easily degraded through sterilization treatment, produces impurity, uses to clinical safety and brings hidden danger.The peroral dosage form of azithromycin and granule since the azithromycin bitterness be difficult to cover with correctives etc., bring impact for the compliance of clinical use, so peroral dosage form is take capsule as main clinically, the azithromycin capsule of producing at present is the uppity problem of ubiquity moisture content index all, all can cause very large impact to product quality and stability.
Summary of the invention
The purpose of this invention is to provide a kind of azithromycin capsule agent.
Another object of the present invention provides the preparation method of described azithromycin capsule agent.
Azithromycin capsule agent provided by the invention comprises following composition by weight:
Azithromycin: 1 part;
Filler: 0.1～1.0 part;
Binding agent: 0.010.1 part;
Fluidizer: 0.1～1.0 part.
Preferably, described azithromycin capsule agent comprises following composition by weight:
Azithromycin: 1 part;
Filler: 0.2～0.5 part;
Binding agent: 0.01～0.05 part;
Fluidizer: 0.2～0.6 part.
Wherein, described filler is one or more in medical starch, pregelatinized Starch, the dextrin; Preferred pregelatinized Starch.
Wherein, described binding agent is water or the alcoholic solution of polyvinylpyrrolidone.
Wherein, the mass percent concentration of the water of described polyvinylpyrrolidone or alcoholic solution is 3～10%.
Wherein, described fluidizer is Pulvis Talci and/or magnesium stearate.The mixture that described fluidizer preferably talc powder and magnesium stearate form with arbitrary proportion.Described fluidizer most preferably Pulvis Talci and magnesium stearate by weight 5～65: 5～15 mixture that form.Pulvis Talci and magnesium stearate are hydrophobic auxiliary, when the preparation micropill, add Pulvis Talci and magnesium stearate, can bring into play the effect of lubricated, fluidizer, obstruct moisture, can avoid the adhesion between the micropill, can effectively intercept again the capsule shells water translocation in micropill, the moisture that guarantees azithromycin capsule not exceeded standard play vital effect.
Azithromycin capsule agent preparation method provided by the invention may further comprise the steps:
(1) described each composition is crossed 80～100 mesh sieves;
(2) with azithromycin and filler mixing, add binding agent soft material processed;
(3) add fluidizer to step (2) gained soft material and make micropill, be filled at last capsule shells and get final product.
In the step (3), employing is extruded the throwing circule method and is made micropill.
In the step (3), the moisture Control of described micropill is below the 4wt%.
Technical solution of the present invention has following advantage:
1, technical solution of the present invention has been made pellet capsule with raw materials such as principal agent, adjuvants, and the capsule 's content particle size distribution is even, the profile rounding, without adhesion, raw material is not suffered a loss, dispersion of medicine, overcome the easily problem of suction of principal agent, improved product quality, guaranteed the stability of medicine.
2, compare with other dosage forms, capsule dissolution rate provided by the invention is fast, bioavailability is high.
3, compare with commercially available capsule of the same type, good stability of the present invention easily stores.
4, preparation method provided by the invention is simple to operate, mild condition, suitability for mass industrialized production.
The specific embodiment
Following examples are used for explanation the present invention, but are not used for limiting the scope of the invention.
Embodiment 1
Prescription forms (weight portion):
Azithromycin: 1 part;
Pregelatinized Starch: 0.5 part;
The aqueous solution of polyvinylpyrrolidone (5wt%): 0.02 part;
Pulvis Talci: 0.05 part;
Magnesium stearate: 0.08 part.
Preparation method is as follows:
(1) each raw material is pulverized respectively, crossed 100 mesh sieves, weighing is for subsequent use.
(2) with azithromycin and pregelatinized Starch mix homogeneously, the aqueous solution that then adds polyvinylpyrrolidone is made binding agent, soft material processed.
(3) add Pulvis Talci and magnesium stearate, use to extrude and throw circule method and prepare micropill, control micropill moisture is below 4.0%, is filled into the gained micropill in the capsule shells and get final product.
Embodiment 2
Prescription forms (weight portion):
Azithromycin: 1 part;
Pregelatinized Starch: 0.4 part;
The alcoholic solution of polyvinylpyrrolidone (5wt%): 0.04 part;
Pulvis Talci: 0.4 part;
Magnesium stearate: 0.08 part.
Preparation method is as follows:
(1) each raw material is pulverized respectively, crossed 100 mesh sieves, weighing is for subsequent use.
(2) with azithromycin and pregelatinized Starch mix homogeneously, the alcoholic solution that then adds polyvinylpyrrolidone is made binding agent, soft material processed.
(3) add Pulvis Talci and magnesium stearate, use to extrude and throw circule method and prepare micropill, control micropill moisture is below 4.0%, is filled into the gained micropill in the capsule shells and get final product.
Embodiment 3
Prescription forms (weight portion):
Azithromycin: 1 part;
Pregelatinized Starch: 0.8 part;
The aqueous solution of polyvinylpyrrolidone (8wt%): 0.06 part;
Pulvis Talci: 0.3 part;
Magnesium stearate: 0.15 part.
Preparation method is as follows:
(1) each raw material is pulverized respectively, crossed 100 mesh sieves, weighing is for subsequent use.
(2) with azithromycin and pregelatinized Starch mix homogeneously, the aqueous solution that then adds polyvinylpyrrolidone is made binding agent, soft material processed.
(3) add Pulvis Talci and magnesium stearate, use to extrude and throw circule method and prepare micropill, control micropill moisture is below 4.0%, is filled into the gained micropill in the capsule shells and get final product.
Embodiment 4
Prescription forms (weight portion):
Azithromycin: 1 part;
Pregelatinized Starch: 0.25 part;
The alcoholic solution of polyvinylpyrrolidone (4wt%): 0.08 part;
Pulvis Talci: 0.15 part;
Magnesium stearate: 0.05 part.
Preparation method is as follows:
(1) each raw material is pulverized respectively, crossed 90 mesh sieves, weighing is for subsequent use.
(2) with azithromycin and pregelatinized Starch mix homogeneously, the alcoholic solution that then adds polyvinylpyrrolidone is made binding agent, soft material processed.
(3) add Pulvis Talci and magnesium stearate, use to extrude and throw circule method and prepare micropill, control micropill moisture is below 4.0%, is filled into the gained micropill in the capsule shells and get final product.
Embodiment 5
Prescription forms (weight portion):
Azithromycin: 1 part;
Pregelatinized Starch: 0.25 part;
The alcoholic solution of polyvinylpyrrolidone (9wt%): 0.015 part;
Pulvis Talci: 0.62 part;
Magnesium stearate: 0.09 part.
Preparation method is as follows:
(1) each raw material is pulverized respectively, crossed 80 mesh sieves, weighing is for subsequent use.
(2) with azithromycin and pregelatinized Starch mix homogeneously, the alcoholic solution that then adds polyvinylpyrrolidone is made binding agent, soft material processed.
(3) add Pulvis Talci and magnesium stearate, use to extrude and throw circule method and prepare micropill, control micropill moisture is below 4.0%, is filled into the gained micropill in the capsule shells and get final product.
Experimental example
Embodiment 1-5 gained capsule is carried out quality inspection by two appendix of Chinese Pharmacopoeia version in 2010, the results are shown in Table 1.
Table 1
By table 1 result as can be known, in the capsule of the present invention, stability is significantly improved, and moisture has obtained preferably control.
Although above the present invention is described in detail with a general description of the specific embodiments, on basis of the present invention, can make some modifications or improvements it, this will be apparent to those skilled in the art.Therefore, these modifications or improvements all belong to the scope of protection of present invention without departing from theon the basis of the spirit of the present invention.
Claims (10)
1. an azithromycin capsule agent is characterized in that, comprises by weight following composition:
Azithromycin: 1 part;
Filler: 0.1～1.0 part;
Binding agent: 0.01～0.1 part;
Fluidizer: 0.1～1.0 part.
2. capsule according to claim 1 is characterized in that, comprises by weight following composition:
Azithromycin: 1 part;
Filler: 0.2～0.5 part;
Binding agent: 0.01～0.05 part;
Fluidizer: 0.2～0.6 part.
3. capsule according to claim 1 and 2 is characterized in that, described filler is one or more in medical starch, pregelatinized Starch, the dextrin.
4. capsule according to claim 1 and 2 is characterized in that, described binding agent is water or the alcoholic solution of polyvinylpyrrolidone.
5. capsule according to claim 4 is characterized in that, the water of described polyvinylpyrrolidone or the mass percent concentration of alcoholic solution are 3～10%.
6. capsule according to claim 1 and 2 is characterized in that, described fluidizer is Pulvis Talci and/or magnesium stearate.
7. capsule according to claim 6 is characterized in that, described fluidizer is that Pulvis Talci and magnesium stearate are by weight 5～65: 5～15 mixture that form.
8. the preparation method of each described capsule of claim 1-7 is characterized in that, may further comprise the steps:
(1) described each composition is crossed 80～100 sieves;
(2) with azithromycin and filler mixing, add binding agent soft material processed;
(3) add fluidizer to step (2) gained soft material and make micropill, be filled at last capsule shells and get final product.
9. preparation method according to claim 8 is characterized in that, in the step (3), employing is extruded the throwing circule method and made micropill.
10. according to claim 8 or 9 described preparation methoies, it is characterized in that in the step (3), the moisture Control of described micropill is below the 4.0wt%.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012105676952A CN103040787A (en) | 2012-12-24 | 2012-12-24 | Azithromycin capsule and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
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| CN2012105676952A CN103040787A (en) | 2012-12-24 | 2012-12-24 | Azithromycin capsule and preparation method thereof |
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| CN103040787A true CN103040787A (en) | 2013-04-17 |
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| CN2012105676952A Pending CN103040787A (en) | 2012-12-24 | 2012-12-24 | Azithromycin capsule and preparation method thereof |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105078920A (en) * | 2014-05-16 | 2015-11-25 | 山东司邦得制药有限公司 | Azithromycin capsule and preparation method thereof |
| CN107582538A (en) * | 2017-06-01 | 2018-01-16 | 合肥远志医药科技开发有限公司 | Azithromycin capsule and preparation method thereof |
| CN111467362A (en) * | 2020-05-09 | 2020-07-31 | 北京四环制药有限公司 | Azithromycin medicinal composition, preparation method and application thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1662223A (en) * | 2002-06-27 | 2005-08-31 | 西拉格股份公司 | Spherical pellet containing a water-soluble active ingredient |
| EP1719503A1 (en) * | 2005-05-02 | 2006-11-08 | National Starch and Chemical Investment Holding Corporation | Use of debranched starch in extrusion-spheronization pharmaceutical pellets |
| CN102423306A (en) * | 2011-12-12 | 2012-04-25 | 珠海润都制药股份有限公司 | Azithromycin enteric capsules |
-
2012
- 2012-12-24 CN CN2012105676952A patent/CN103040787A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1662223A (en) * | 2002-06-27 | 2005-08-31 | 西拉格股份公司 | Spherical pellet containing a water-soluble active ingredient |
| EP1719503A1 (en) * | 2005-05-02 | 2006-11-08 | National Starch and Chemical Investment Holding Corporation | Use of debranched starch in extrusion-spheronization pharmaceutical pellets |
| CN102423306A (en) * | 2011-12-12 | 2012-04-25 | 珠海润都制药股份有限公司 | Azithromycin enteric capsules |
Non-Patent Citations (3)
| Title |
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| 《Pharmaceutical Technology》 20050228 Rajesh Gandhi等 Using Extrusion-Spheronization to Develop Controlled-Release Formulations of Azithromycin , * |
| F.J. OTERO-ESPINAR等: "Non-MCC materials as extrusion-spheronization aids in pellets production", 《J. DRUG DEL. SCI. TECH》 * |
| RAJESH GANDHI等: "Using Extrusion–Spheronization to Develop Controlled-Release Formulations of Azithromycin", 《PHARMACEUTICAL TECHNOLOGY》 * |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105078920A (en) * | 2014-05-16 | 2015-11-25 | 山东司邦得制药有限公司 | Azithromycin capsule and preparation method thereof |
| CN105078920B (en) * | 2014-05-16 | 2017-12-08 | 山东司邦得制药有限公司 | A kind of azithromycin capsule and preparation method thereof |
| CN107582538A (en) * | 2017-06-01 | 2018-01-16 | 合肥远志医药科技开发有限公司 | Azithromycin capsule and preparation method thereof |
| CN111467362A (en) * | 2020-05-09 | 2020-07-31 | 北京四环制药有限公司 | Azithromycin medicinal composition, preparation method and application thereof |
| CN111467362B (en) * | 2020-05-09 | 2021-07-06 | 北京四环制药有限公司 | Azithromycin medicinal composition, preparation method and application thereof |
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Application publication date: 20130417 |