CN101209244A - Method for producing acetylkitasamycin microcapsule type powder - Google Patents
Method for producing acetylkitasamycin microcapsule type powder Download PDFInfo
- Publication number
- CN101209244A CN101209244A CNA2006101707212A CN200610170721A CN101209244A CN 101209244 A CN101209244 A CN 101209244A CN A2006101707212 A CNA2006101707212 A CN A2006101707212A CN 200610170721 A CN200610170721 A CN 200610170721A CN 101209244 A CN101209244 A CN 101209244A
- Authority
- CN
- China
- Prior art keywords
- acetylkitasamycin
- production method
- type powder
- powder
- microcapsule type
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Images
Landscapes
- Medicinal Preparation (AREA)
Abstract
The invention provides a production method of acetylkitasamycin microcapsuled powder, and the microcapsuled acetylkitasamycin powder is obtained by spray drying after mixing 1 part by weight of acetylkitasamycin power and 0.01 to 1 part by weight of cellulose in 10 to 300 parts by weight of organic solvent. The selected cellulose can be ethyl cellulose and methyl cellulose, and the organic solvent can select chloroform, dichloromethane or acetone. The method of the invention can further add non-ionic surfactant in the organic solvent so as to increase the solubility of the drug. In addition, anti-adhesion agent can also be added in the organic solvent, or anti-adhesion powder is added in the microcapsuled finished product, so as to reduce the self-adhesion of the drug and increase the hydrophilic property and solubility of the drug. The production method of acetylkitasamycin microcapsuled powder of the invention has the advantages of improving the dissolution rate of the raw materials and improving the oral bioavailability of the preparation, furthermore, the produced acetylkitasamycin microcapsuled powder is also the powder with the thermodynamic stability.
Description
Technical field
The present invention relates to medical manufacture field, particularly the production method of acetylkitasamycin microcapsule type powder.
Background technology
Acetylkitasamycin (Acetylkitasamycin, Acetylleucomycin) is the macrolide antibiotics chemical compound, effective to gram positive bacteria and some negative bacterium, mycoplasma, Li Keshi body, spirillum etc., this medicine is light, the medium-sized respiratory tract infection of treatment, urogenital infections. the oral antibiotic that skin soft-tissue infection is effective and safe is mainly used in penicillin-fast staphylococcus, streptococcus, streptococcus pneumoniae infection.Acetylkitasamycin has overcome the bitterness of other macrolide antibiotics, is convenient to orally, is particularly suited for children.But existing Acetylkitasamycin is by the crystalline powder that dropping forms in water after the kitasamycin acidylate, is insoluble drug, and its powder is floating shape in water, and unfavorable oral, bioavailability is low.
Summary of the invention
The Acetylkitasamycin that the present invention is devoted to solve crystal formation is insoluble in the problem of water, provides a kind of production method of acetylkitasamycin microcapsule type powder, with bioavailability and the stability of improving Acetylkitasamycin.
The production method of acetylkitasamycin microcapsule type powder of the present invention comprises the following steps:
1,1 weight portion crystal formation Acetylkitasamycin and 0.01-1 weight portion cellulose are mixed in 10-300 weight portion organic solvent;
2, spray drying obtains the microcapsule-type Acetylkitasamycin.
The non-ionic surface active agent that can also add the 0.01-0.2 weight portion in the above-mentioned steps 1, it can increase the dissolubility of medicine, the preferred poloxamer of used non-ionic surface active agent (Poloxamer), system is by polyoxyethylene and polyoxypropylene copolymerization and a kind of non-ionic surface active agent that obtains, have another name called pool Luo Nike (Pluronic), as poloxamer F68.
The antitackiness agent that can also add the 0.001-0.02 weight portion in the above-mentioned steps 1 or 2, it can join in the organic solvent in step 1, also can be added in the acetylkitasamycin microcapsule type powder that step 2 spray drying obtains with Powdered.The preferred differential silica gel of used antitackiness agent, it can reduce the adhesive of medicine itself, increases the hydrophilic and the dissolubility of medicine.
The cellulosic preferable amount of stabilizing agent is the 0.01-0.1 weight portion.Used cellulose comprises ethyl cellulose, methylcellulose, ethyl cellulose viscosity as 4,7,10,20,45,100cps; Methylcellulose viscosity as 17～23,350～550,2200～2800,4000～5000mpa.s.
Be applicable to that organic solvent of the present invention has chloroform, dichloromethane, acetone etc.
When step 1 is mixed various material, add cellulose, non-ionic surface active agent, antitackiness agent mix homogeneously again after can earlier Acetylkitasamycin being dissolved in organic solvent, add the Acetylkitasamycin mix homogeneously again after also can be earlier cellulose and non-ionic surface active agent being dissolved in organic solvent.
The control inlet temperature was 100～130 ℃ when above-mentioned steps 2 was carried out spray drying; 60～100 ℃ of outlet temperatures; The compressed-air actuated pressure 245～441Kpa in porch; Charging rate 0.5～1L/h, in cyclone separator, separate microcapsule type powder.
The production technology of acetylkitasamycin microcapsule type powder of the present invention has improved the dissolution of its raw material and the oral administration biaavailability of preparation, can be applicable to the industrialized great production of Acetylkitasamycin.Resulting microcapsule-type Acetylkitasamycin is thermodynamically stable powder, is stored in 50 ℃ of investigations that experimentize and finds after one month that it still is the microcapsule-type solid.
The microcapsule-type Acetylkitasamycin helps the extensive distribution of this medicine in internal organs, improve its blood drug level in tissues such as liver and bile, lung, kidney muscle, be of value to the various infection due to the treatment G+ bacterium more, be specially adapted to last lower respiratory infection and epidermis soft tissue infection that staphylococcus aureus, streptococcus pneumoniae and staphylococcus epidermidis cause.The acetylkitasamycin microcapsule type powder that the inventive method is produced is rapid-action, is particularly useful for the infection due to treatment children's's the G+ bacterium.
Description of drawings
Fig. 1 is the microphotograph of Acetylkitasamycin raw material powder;
Fig. 2 is the microphotograph of the acetylkitasamycin microcapsule type pressed powder of the inventive method preparation.
The specific embodiment
Below by embodiment, and specify the present invention in conjunction with the accompanying drawings, but the scope that does not limit the present invention in any way.
Example 1.
Getting 10 gram Acetylkitasamycins is dissolved in the 250ml chloroform, add 1 gram ethyl cellulose (viscosity 10cps) dissolving again, mix homogeneously, outlet temperature is carried out spray drying in about 8～12 minutes under 100 ℃, promptly get stable microcapsule-type pressed powder, add 0.12 gram again and go into differential silica gel mix homogeneously.When being stored under 50 ℃, still the microcapsule-type solid after one month.
As shown in Figure 1, by microscopic examination, the Acetylkitasamycin raw material powder is big or small irregular flakelike powder, and the Acetylkitasamycin after the inventive method preparation is the spherical shape microcapsule type powder (see figure 2) of rule, this acetylkitasamycin microcapsule type pressed powder was stored one month under 50 ℃ of environmental conditions, still was the microcapsule-type pressed powder through the microscopic proof.
Example 2.
Getting 5 gram Acetylkitasamycins is dissolved in the 150ml acetone, add 0.05 gram and go into differential silica gel, add 5 gram ethyl cellulose (viscosity 20cps) dissolvings again, mix homogeneously, outlet temperature is carried out spray drying in about 10 minutes under 90 ℃, promptly get stable microcapsule-type pressed powder.When being stored under 50 ℃, still the microcapsule-type solid after one month.
Example 3.
Getting 6 gram Acetylkitasamycins is dissolved in the 200ml dichloromethane, add 0.32 gram ethyl cellulose (viscosity 45cps) dissolving again, mix homogeneously, outlet temperature is carried out spray drying in about 12 minutes under 80 ℃, promptly get stable microcapsule-type pressed powder, add 0.04 gram again and go into differential silica gel mix homogeneously.When being stored under 50 ℃, still the microcapsule-type solid after one month.
Example 4.
Getting 10 gram Acetylkitasamycins is dissolved in the 250ml dichloromethane, add 0.5 gram ethyl cellulose (viscosity 45cps) and 2 gram F68 dissolvings again, mix homogeneously, outlet temperature is down carried out spray drying in about 12 minutes at 70 ℃, promptly gets stable microcapsule-type pressed powder and adds 0.03 gram again and go into differential silica gel mix homogeneously.When being stored under 50 ℃, still the microcapsule-type solid after one month.
Example 5.
Getting 5 gram Acetylkitasamycins is dissolved in the 150ml dichloromethane, add 0.1 gram and go into differential silica gel, add 5 gram methylcellulose (viscosity 20mpa.s) dissolvings again, mix homogeneously, outlet temperature is carried out spray drying in about 10 minutes under 100 ℃, promptly get stable microcapsule-type pressed powder.When being stored under 50 ℃, still the microcapsule-type solid after one month.
Claims (10)
1. the production method of an acetylkitasamycin microcapsule type powder comprises the following steps:
(1) 1 weight portion Acetylkitasamycin and 0.01-1 weight portion cellulose are mixed in 10-300 weight portion organic solvent;
(2) spray drying obtains the microcapsule-type Acetylkitasamycin.
2. the production method of acetylkitasamycin microcapsule type powder as claimed in claim 1 is characterized in that: the non-ionic surface active agent that adds the 0.01-0.2 weight portion in step (1).
3. the production method of acetylkitasamycin microcapsule type powder as claimed in claim 2, it is characterized in that: described non-ionic surface active agent is a poloxamer.
4. the production method of acetylkitasamycin microcapsule type powder as claimed in claim 1, it is characterized in that: cellulosic consumption is the 0.01-0.1 weight portion.
5. the production method of acetylkitasamycin microcapsule type powder as claimed in claim 1, it is characterized in that: described cellulose is ethyl cellulose and/or methylcellulose.
6. the production method of acetylkitasamycin microcapsule type powder as claimed in claim 5 is characterized in that: described ethyl cellulose viscosity is selected from 4,7,10,20,45,100cps; Methylcellulose viscosity is selected from 17～23,350～550,2200～2800,4000～5000mpa.s.
7. the production method of acetylkitasamycin microcapsule type powder as claimed in claim 1, it is characterized in that: described organic solvent is selected from: chloroform, dichloromethane, acetone.
8. the production method of acetylkitasamycin microcapsule type powder as claimed in claim 1, it is characterized in that: the control inlet temperature was 100～130 ℃ when described step (2) was carried out spray drying, 60～100 ℃ of outlet temperatures, the compressed-air actuated pressure 245～441Kpa in porch, charging rate 0.5～1L/h, in cyclone separator, separate microcapsule type powder.
9. the production method of acetylkitasamycin microcapsule type powder as claimed in claim 1, it is characterized in that: the antitackiness agent that adds the 0.001-0.02 weight portion in step (1) is in organic solvent, and perhaps the antitackiness agent powder with the 0.001-0.02 weight portion mixes with the acetylkitasamycin microcapsule type powder that obtains through step (2) spray drying.
10. the production method of acetylkitasamycin microcapsule type powder as claimed in claim 9, it is characterized in that: described antitackiness agent is a differential silica gel.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200610170721A CN101209244B (en) | 2006-12-26 | 2006-12-26 | Method for producing acetylkitasamycin microcapsule type powder |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200610170721A CN101209244B (en) | 2006-12-26 | 2006-12-26 | Method for producing acetylkitasamycin microcapsule type powder |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101209244A true CN101209244A (en) | 2008-07-02 |
| CN101209244B CN101209244B (en) | 2010-05-19 |
Family
ID=39609608
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200610170721A Expired - Fee Related CN101209244B (en) | 2006-12-26 | 2006-12-26 | Method for producing acetylkitasamycin microcapsule type powder |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101209244B (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102526168A (en) * | 2012-02-21 | 2012-07-04 | 华南理工大学 | Micro-capsules of anti-influenza-virus effective part of phyllanthus urinaria, and preparation method and application thereof |
| CN107823173A (en) * | 2017-11-24 | 2018-03-23 | 武汉人福药业有限责任公司 | A kind of acetylkitasamycin capsule and preparation method thereof |
| CN111700875A (en) * | 2020-06-24 | 2020-09-25 | 广州一品红制药有限公司 | Method for improving bioavailability of acetylkitasamycin and pharmaceutical composition containing acetylkitasamycin |
-
2006
- 2006-12-26 CN CN200610170721A patent/CN101209244B/en not_active Expired - Fee Related
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102526168A (en) * | 2012-02-21 | 2012-07-04 | 华南理工大学 | Micro-capsules of anti-influenza-virus effective part of phyllanthus urinaria, and preparation method and application thereof |
| CN107823173A (en) * | 2017-11-24 | 2018-03-23 | 武汉人福药业有限责任公司 | A kind of acetylkitasamycin capsule and preparation method thereof |
| CN111700875A (en) * | 2020-06-24 | 2020-09-25 | 广州一品红制药有限公司 | Method for improving bioavailability of acetylkitasamycin and pharmaceutical composition containing acetylkitasamycin |
| CN111700875B (en) * | 2020-06-24 | 2022-06-14 | 广州一品红制药有限公司 | Method for improving bioavailability of acetylkitasamycin and pharmaceutical composition containing acetylkitasamycin |
Also Published As
| Publication number | Publication date |
|---|---|
| CN101209244B (en) | 2010-05-19 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN103610649B (en) | Medicament microsphere and preparation method thereof | |
| CN105012303A (en) | Fumarate salt of (alpha S, beta R)-6-bromo-alpha-[2-(dimethylamino)ethyl]-2-methoxy-alpha-1-naphthalenyl-beta-phenyl-3-quinolineethanol | |
| WO2010075664A1 (en) | A highly efficient and long-acting slow-release formulation of poorly soluble drugs and preparation method thereof | |
| CN103087042B (en) | Salts of sitafloxacin and pharmaceutical purposes thereof | |
| CN104644547B (en) | A kind of long-acting cefotaxime sodium injection and preparation method thereof | |
| US8962017B2 (en) | Formulation of silymarin with high efficacy and prolonged action and the preparation method thereof | |
| CN101209244B (en) | Method for producing acetylkitasamycin microcapsule type powder | |
| CN101756910B (en) | Lung targeting ceftiofur microsphere and preparation method | |
| US20120029064A1 (en) | formulation of silibinin with high efficacy and prolonged action and the preparation method thereof | |
| CN101658677A (en) | Lovastatin-sulfobutyl ether-beta-cyclodextrin inclusion compound, preparation and preparation method thereof | |
| CN103156814B (en) | A kind of Azithromycin enteric composition and preparation method | |
| CN102481287B (en) | Pharmaceutical composition of temozolomide comprising vitamin c or vitamin c derivative and preparation method thereof | |
| CN110464846A (en) | A kind of Meloxicam composition, preparation and the preparation method and application thereof | |
| CN101792149A (en) | Spherical silicon dioxide hollow material and preparation method thereof | |
| CN104490762A (en) | Tranexamic acid external semisolid preparation and preparation method thereof | |
| CN105919978A (en) | Preparation method of amoxicillin microsphere slow-release capsule | |
| CN102210655B (en) | Cefpiramide sodium micro-spheres and preparing method thereof | |
| JPWO2007102447A1 (en) | Adhesive microcapsules | |
| CN104739806A (en) | Oral insulin complex micro-capsules and preparation method | |
| CN101773478A (en) | Pulmonary targeting microsphere of veterinary ceftiofur hydrochloride and preparation method thereof | |
| JP2001503734A (en) | Potassium, sodium and trisoxaprozin salt pharmaceutical compositions | |
| CN114681406B (en) | Carilazine long-acting slow-release microsphere and preparation method thereof | |
| CN102304259A (en) | Preparation method of fibroin blending material with gradually degrading performance | |
| CN104784205A (en) | Nano calcium carbonate for intestinal lead removal | |
| CN101259115A (en) | Orally-administered insulin soft capsule for treating diabetes and preparation thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C41 | Transfer of patent application or patent right or utility model | ||
| TA01 | Transfer of patent application right |
Effective date of registration: 20090918 Address after: No. 22, creative road, Beibei District, Chongqing, China: 400700 Applicant after: CHONGQING DAXIN PHARMACEUTICAL Co.,Ltd. Address before: No. 22, creative road, Beibei District, Chongqing, China: 400700 Applicant before: CHONGQING DAXIN PHARMACEUTICAL Co.,Ltd. Co-applicant before: PEKING UNIVERSITY FOUNDER GROUP Co.,Ltd. |
|
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| C56 | Change in the name or address of the patentee |
Owner name: PKU INTERNATIONAL HEALTHCARE GROUP CHONGQING DAXIN Free format text: FORMER NAME: CHONGQING DAXIN PHARMACEUTICAL CO., LTD. Owner name: PKU HEAL THCARE CHONGQING DAXIN PHARMACEUTICAL CO. Free format text: FORMER NAME: PKU INTERNATIONAL HEALTHCARE GROUP CHONGQING DAXIN PHARMACEUTICAL CO., LTD. |
|
| CP01 | Change in the name or title of a patent holder |
Address after: 400700 No. 22, creative road, Beibei District, Chongqing Patentee after: CHONGQING DAXIN PHARMACEUTICAL Co.,Ltd. Address before: 400700 No. 22, creative road, Beibei District, Chongqing Patentee before: Peking University International Hospital Group Chongqing Daxin Pharmaceutical Co.,Ltd. Address after: 400700 No. 22, creative road, Beibei District, Chongqing Patentee after: Peking University International Hospital Group Chongqing Daxin Pharmaceutical Co.,Ltd. Address before: 400700 No. 22, creative road, Beibei District, Chongqing Patentee before: CHONGQING DAXIN PHARMACEUTICAL Co.,Ltd. |
|
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20100519 Termination date: 20171226 |
|
| CF01 | Termination of patent right due to non-payment of annual fee |