CN107823173A - A kind of acetylkitasamycin capsule and preparation method thereof - Google Patents
A kind of acetylkitasamycin capsule and preparation method thereof Download PDFInfo
- Publication number
- CN107823173A CN107823173A CN201711195211.5A CN201711195211A CN107823173A CN 107823173 A CN107823173 A CN 107823173A CN 201711195211 A CN201711195211 A CN 201711195211A CN 107823173 A CN107823173 A CN 107823173A
- Authority
- CN
- China
- Prior art keywords
- acetylkitasamycin
- capsule
- parts
- disintegrant
- lubricant
- 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.)
- Pending
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses a kind of acetylkitasamycin capsule and preparation method thereof, belong to technical field of medicine.Its content of the acetylkitasamycin capsule of the present invention is made up of acetylkitasamycin and pharmaceutic adjuvant, and the pharmaceutic adjuvant includes diluent, disintegrant, wetting agent, adhesive and lubricant.Acetylkitasamycin main ingredient mix sieving with auxiliary material by the present invention, through wet granulation, drying, whole grain and fills capsule after always mixing.Yield, mobility and the dissolution rate of dry particl can be greatly improved in acetylkitasamycin capsule prepared by the present invention, ensure the quality of product, so as to more effectively play therapeutic action.
Description
Technical field：
The present invention relates to technical field of medicine, and in particular to a kind of acetylkitasamycin capsule and preparation method thereof.
Background technology：
Acetylkitasamycin is macrolide antibiotics compounds, can be by acting on bacterial cell ribosome
5os subunits, hinder albumen synthesis and play antibacterial action.It is to gram-positive bacteria and some Gram-negative bacterias, Zhi Yuan
Body, Rickettsial, conveyor screw etc. have good therapeutic effect.The medicine is to treat light, moderate respiratory infection, urogenital system
Infection, skin soft-tissue infection's safely and effectively oral antibiotic, it is mainly used in the staphylococcus, streptococcus, lung of resistance to penicillin
Scorching streptococcal infection.Acetylkitasamycin is different from the characteristics of other macrolide bitters, is easy to oral.But acetyl
Kitasamycin is insoluble drug, and its powder, in floating shape, is unfavorable for infiltrating with dissolution medium in water, so in the formulation not
Easy disintegrating dissolution, so as to cause the degree of absorbing of human body low.
Patent CN 101209244A disclose a kind of production method of acetylkitasamycin microcapsule type powder, to improve
The bioavilability and stability of acetylkitasamycin.From chloroform, dichloromethane or acetone as organic solvent, category in technique
In the second class or the 3rd class residual solvent, general such solvent can use in Material synthesis, in medicine preparation production process
Hardly use, do not meet GMP workshop management requirements, therefore the technique of the patent is not suitable for the life of traditional oral solid pharmaceutical preparation
Production；And the technique limits the use of raw material to a certain extent, the dosage form selection of medicine is limited, although original can be improved
The dissolution rate of material, but the formula and technique can only produce the powder of microcapsule-type, and be unfavorable for producing other oral administration solid systems
Agent.
Patent CN101249080 discloses a kind of preparation method of Acetylkitasamycin dispersible tablet, using wet granulation pressure
The method of piece, it is made with the acetylkitasamycin and pharmaceutic adjuvant of percentage by weight 20~60%.But dispersible tablet prepares cost
It is higher, larger financial burden can be brought to patient.
Patent CN102429889 discloses a kind of Macrocyclolactone lactone kind medicine capsule and preparation method thereof, by from non-bright
Glue capsule shells improve the bioavilability of Macrocyclolactone lactone kind medicine.But non-gelatin class capsule shells limited source, cost is higher, and
Non- gelatin class capsule shells quality heterogeneity on domestic market, capsule shells not readily dissolve, and are unfavorable for medicine enterprise's large-scale production and pin
Sell.
The content of the invention：
The defects of based on above-mentioned prior art, the present invention explore different auxiliary material and its prescription to acetylkitasamycin particle
The influence of yield, mobility and capsule dissolubility.By selecting the stronger auxiliary material of hydrophily, as tween-80 and hydroxypropyl first are fine
Dimension element, the decentralization of solids, increase dissolution interface can be improved, and then effectively improve the dissolution of acetylkitasamycin capsule
Speed.The present invention passes through auxiliary material and prescription screening, there is provided a kind of simple production process, production cost are relatively low, are adapted to pharmaceutical industries
Metaplasia is produced, and improves the acetylkitasamycin capsule of its dissolution rate to greatest extent.
The present invention provides a kind of acetylkitasamycin capsule, and its content is made up of acetylkitasamycin and pharmaceutic adjuvant.
The pharmaceutic adjuvant includes diluent, disintegrant, wetting agent, adhesive and lubricant.Count in parts by weight, each component dosage
For：Acetylkitasamycin 250-270 parts, diluent 50.0-70.0 parts, disintegrant 10.0-20.0 parts, wetting agent 4.0-8.0 parts,
Adhesive 2.0-4.0 parts, lubricant 1.0-5.0 parts.
Preferably, the acetylkitasamycin capsule is counted in parts by weight, and each component dosage is：Acetylkitasamycin 255-
260 parts, diluent 60.0-65.0 parts, disintegrant 15.0-18.0 parts, wetting agent 5.0-6.0 parts, adhesive 2.5-3.0 parts, profit
Lubrication prescription 3.0-4.0 parts.
One kind in lactose, starch, mannitol, sucrose, sorbierite, microcrystalline cellulose, dextrin of the diluent or
It is a variety of, preferably lactose.
Described disintegrant is selected from carboxyrnethyl starch sodium, Ac-Di-Sol, PVPP, dried starch, pre- glue
Change starch starch1500, glycyl sodium starch, alginic acid, low-substituted hydroxypropyl cellulose, PVPP
In one or more, preferably carboxyrnethyl starch sodium.
Described wetting agent is in Tween-80, ethanol, lauryl sodium sulfate, Hexadecvlthio sodium succinate
One or more, preferably Tween-80.
Described adhesive is selected from hydroxypropyl methylcellulose, sodium carboxymethylcellulose, syrup, Icing Sugar, starch slurry, dextrin, sugar
One or more in slurry, mucialga of arabic gummy, gelatine size, PVP, preferably HPMC.
Described lubricant is one in magnesium stearate, talcum powder, calcium stearate, stearic acid, silica, superfine silica gel powder
Kind is a variety of, preferably talcum powder.
The present invention also provides a kind of preparation method of acetylkitasamycin capsule, by acetylkitasamycin main ingredient and disintegrant
80 mesh sieves are crossed respectively with diluent, it is standby after fully mixing；Wetting agent is measured by recipe quantity, is added into binder solution,
Mix standby；The mixed solution of the wetting agent of above-mentioned preparation and adhesive is added to mix in drug mass softwood is made, cross 40
Mesh sieve is pelletized；With 24 mesh sieve whole grains after wet granular is dried at 60 DEG C；The lubricant for weighing recipe quantity crosses 100 mesh sieves, with dry
Grain is fully mixed, and packaging in capsule is fitted into after censorship is qualified and is got product.
Beneficial effects of the present invention are：
(1) present invention passes through suitable wetting agent, adhesive and its ratio, solution by different auxiliary material and its prescription screening
The defects of acetylkitasamycin of having determined is not readily dissolved in water, its dissolution rate is significantly improved, be advantageous to improve oral acetylkitasamycin
Bioavilability.So as to avoid the medicine for increasing acetylkitasamycin bioavilability by using organic solvent and bringing
Safety risks and pharmaceutical production problem.
(2) acetylkitasamycin capsule provided by the invention, the formulations such as tablet, particle are overcome to stomach and gastral
Stimulate, and the stability of acetylkitasamycin capsule formulation is realized by the screening of auxiliary material prescription.
(3) acetylkitasamycin capsule provided by the present invention, high income, good fluidity, be advantageous to improve acetyl guitar
The uniformity of mycin capsule 's content, it is easy to capsule filling, and then ensures drug quality.
(4) acetylkitasamycin capsule preparation method thereof provided by the present invention approaches with conventional capsule preparation method, used
Supplementary material is easy to get inexpensive, and production cost is low, is advantageous to pharmaceutical industriesization production and selling.
Specific embodiment
With reference to specific embodiment, the invention will be further described, so that those skilled in the art can more preferably manage
The solution present invention can be simultaneously practiced, and illustrated embodiment is not as a limitation of the invention.
Embodiment 1：
The acetylkitasamycin capsule 's content prescription of table 1
Preparation method：
(1) by the recipe quantity of table 1 weigh acetylkitasamycin main ingredient and carboxyrnethyl starch sodium PVPP (disintegrant) and
Lactose starch microcrystalline cellulose sodium (diluent), respectively cross 80 mesh sieves, three is fully mixed, it is standby；
(2) by recipe quantity measure Tween-80 ethanol lauryl sodium sulfate (wetting agent), be added into hydroxypropyl fibre
Tie up in plain solution or carboxymethylcellulose sodium solution (binder), stir evenly standby；
(3) solution prepared by above-mentioned steps (2) is added in the material of step (1), mixed, softwood is made, cross 40 mesh
Sieve series grain, by wet granular in 60 DEG C of dryings, with 24 mesh sieve whole grains.
(4) weigh recipe quantity talcum powder magnesium stearate superfine silica gel powder (lubricant), cross 100 mesh sieves, with step (3) make
The dry particl obtained fully mixes, and after sampling censorship is qualified, is fitted into capsulae vacuus, packaging is got product.
Embodiment 2：Yield, dissolution rate and the Study of Liquidity of acetylkitasamycin capsule
The acetylkitasamycin capsule 's content prescription of table 2
(model is not protected with the 4 kinds of acetylkitasamycin capsules prepared in embodiment 1 and according to the prescription of table 2 in the present invention
In enclosing) the acetylkitasamycin capsule for preparing carries out the comparative study of yield, dissolution rate and mobility.Experimental result referring to table 3,
As a result show, the yield and dissolution rate of acetylkitasamycin capsule prepared by the inventive method are substantially better than prepared by other prescriptions
Acetylkitasamycin capsule, there is significant difference；Angle of repose refers to the free inclined-plane of powder accumulation horizon and horizontal plane formed
Maximum angular.Angle of repose is smaller, and frictional force is smaller, and the mobility of powder is better, it is considered that good fluidity during θ≤30 °, θ≤40 °
When can meet need for liquidity in production process.Test result indicates that acetylkitasamycin glue prepared in accordance with the present invention
The content mobility of capsule is substantially better than the content of other prescriptions preparation.Illustrate that the present invention advantageously reduces acetylkitasamycin
The production cost of capsule, and the uniformity of acetylkitasamycin capsule 's content is improved, it is easy to capsule filling, and then ensure medicine
Quality.
Yield, dissolution rate and the mobility result of acetylkitasamycin capsule prepared by 3 different prescriptions of table
Embodiment 3：Acetylkitasamycin capsule stability is investigated
Acetylkitasamycin capsule 's content is prepared in the method for the prescription 3 and 4 in embodiment 1, two kinds of core materials are used respectively
Gelatine capsule shell and HPMC capsule shells are filling, carry out 6 months accelerated tests.
The stability experiment result of acetylkitasamycin capsule is referring to table 4, the results showed that acetyl prepared by the inventive method
Kitasamycin capsule 's content was filling using gelatine capsule shell and HPMC capsule shells, by 6 months accelerated tests
Afterwards, dissolution rate is good, and there was no significant difference.Illustrate that acetylkitasamycin capsule prepared by the present invention can be avoided effectively and gelatin glue
Capsule crosslinks reaction, ensures stability of drug products.
The acetylkitasamycin capsule of table 4 uses the dissolution results after the accelerated experiment of different capsule shells
Embodiment described above is only to absolutely prove preferred embodiment that is of the invention and being lifted, protection model of the invention
Enclose not limited to this.The equivalent substitute or conversion that those skilled in the art are made on the basis of the present invention, in the present invention
Protection domain within.Protection scope of the present invention is defined by claims.
Claims (9)
1. a kind of acetylkitasamycin capsule, it is characterised in that the content of the acetylkitasamycin capsule is mould by acetyl guitar
Element and pharmaceutic adjuvant composition, the pharmaceutic adjuvant include diluent, disintegrant, wetting agent, adhesive and lubricant.
2. acetylkitasamycin capsule according to claim 1, it is characterised in that the acetylkitasamycin capsule is by weight
Number meter is measured, each component dosage is：Acetylkitasamycin 250-270 parts, diluent 50.0-70.0 parts, disintegrant 10.0-20.0
Part, wetting agent 4.0-8.0 parts, adhesive 2.0-4.0 parts, lubricant 1.0-5.0 parts.
3. acetylkitasamycin capsule according to claim 2, it is characterised in that the acetylkitasamycin capsule is by weight
Number meter is measured, each component dosage is：Acetylkitasamycin 255-260 parts, diluent 60.0-65.0 parts, disintegrant 15.0-18.0
Part, wetting agent 5.0-6.0 parts, adhesive 2.5-3.0 parts, lubricant 3.0-4.0 parts.
4. acetylkitasamycin capsule according to claim 1, it is characterised in that the diluent be selected from lactose, starch,
One or more in mannitol, sucrose, sorbierite, microcrystalline cellulose, dextrin, preferably lactose.
5. acetylkitasamycin capsule according to claim 1, it is characterised in that described disintegrant is selected from carboxymethylstarch
Sodium, Ac-Di-Sol, PVPP, dried starch, pregelatinized starch Starch1500, glycyl sodium starch,
One or more in alginic acid, low-substituted hydroxypropyl cellulose, PVPP, preferably carboxyrnethyl starch sodium.
6. acetylkitasamycin capsule according to claim 1, it is characterised in that described wetting agent be selected from Tween-80,
One or more in ethanol, lauryl sodium sulfate, Hexadecvlthio sodium succinate, preferably Tween-80.
7. acetylkitasamycin capsule according to claim 1, it is characterised in that described adhesive is selected from hydroxypropyl
In cellulose, sodium carboxymethylcellulose, syrup, Icing Sugar, starch slurry, dextrin, syrup, mucialga of arabic gummy, gelatine size, PVP
One or more, preferably HPMC.
8. acetylkitasamycin capsule according to claim 1, it is characterised in that described lubricant be magnesium stearate,
One or more in talcum powder, calcium stearate, stearic acid, silica, superfine silica gel powder, preferably talcum powder.
9. the preparation method of the acetylkitasamycin capsule described in claim any one of 1-8, it is characterised in that the acetyl is lucky
He is made mycin capsule by following steps：Acetylkitasamycin main ingredient crosses 80 mesh sieves respectively with disintegrant and diluent, fully
It is standby after mixing；Wetting agent is measured by recipe quantity, is added into binder solution, is mixed standby；By the wetting of above-mentioned preparation
The mixed solution of agent and adhesive, which adds to mix in drug mass, is made softwood, crosses the granulation of 40 mesh sieves；Wet granular is dry at 60 DEG C
With 24 mesh sieve whole grains after dry；The lubricant for weighing recipe quantity crosses 100 mesh sieves, is fully mixed with dry particl, loads after censorship is qualified
Packaging is got product in capsule.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711195211.5A CN107823173A (en) | 2017-11-24 | 2017-11-24 | A kind of acetylkitasamycin capsule and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711195211.5A CN107823173A (en) | 2017-11-24 | 2017-11-24 | A kind of acetylkitasamycin capsule and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107823173A true CN107823173A (en) | 2018-03-23 |
Family
ID=61645545
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201711195211.5A Pending CN107823173A (en) | 2017-11-24 | 2017-11-24 | A kind of acetylkitasamycin capsule and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN107823173A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| CN112057522A (en) * | 2020-09-18 | 2020-12-11 | 江苏康缘药业股份有限公司 | Composition and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101209244A (en) * | 2006-12-26 | 2008-07-02 | 重庆大新药业股份有限公司 | Method for producing acetylkitasamycin microcapsule type powder |
| CN101249080A (en) * | 2008-02-21 | 2008-08-27 | 徐建平 | Acetylkitasamycin dispersible tablet and method of preparing the same |
| CN102429889A (en) * | 2011-11-30 | 2012-05-02 | 无锡福祈制药有限公司 | Large ring lactone type medicament capsule and preparation method thereof |
-
2017
- 2017-11-24 CN CN201711195211.5A patent/CN107823173A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101209244A (en) * | 2006-12-26 | 2008-07-02 | 重庆大新药业股份有限公司 | Method for producing acetylkitasamycin microcapsule type powder |
| CN101249080A (en) * | 2008-02-21 | 2008-08-27 | 徐建平 | Acetylkitasamycin dispersible tablet and method of preparing the same |
| CN102429889A (en) * | 2011-11-30 | 2012-05-02 | 无锡福祈制药有限公司 | Large ring lactone type medicament capsule and preparation method thereof |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| CN112057522A (en) * | 2020-09-18 | 2020-12-11 | 江苏康缘药业股份有限公司 | Composition and preparation method thereof |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN103083278B (en) | Roxithromycin capsule and preparation method thereof | |
| CN107823173A (en) | A kind of acetylkitasamycin capsule and preparation method thereof | |
| CN101612171B (en) | Ginkgo biloba extract sustained-release pellet and preparation method thereof | |
| CN107095857A (en) | The production technology of Biomox | |
| CN109248155A (en) | A kind of roxithromycin capsules and its preparation process | |
| CN107320456A (en) | 2-acetylamino-2-deoxy-D-glucose capsule preparations and preparation method thereof | |
| CN105343028A (en) | Medicine composition with norfloxacin and method for preparing medicine composition | |
| CN102973529A (en) | Azithromycin dispersible tablet and preparation method thereof | |
| CN101125131A (en) | Method for preparing flupentixol and melitracen capsule | |
| CN113679685B (en) | Preparation method of erythromycin cydocarbonate tablet | |
| CN105919960B (en) | A kind of roxithromycin dispersing tablet and preparation method thereof | |
| CN108836973A (en) | Metformin-glibenclamide capsule and preparation method thereof | |
| CN108785256A (en) | A kind of solid dispersions and preparation method thereof | |
| CN106902097B (en) | A pharmaceutical composition for improving bioavailability of medicine | |
| CN104224725A (en) | Tebipenem pivoxil granule and preparation method thereof | |
| CN103142533B (en) | Enteric coated tablet of etoposide | |
| CN102311452A (en) | Cefixime crystal, preparation method thereof and tablet composition containing same | |
| CN108853039B (en) | Clarithromycin dispersible tablet and production process thereof | |
| CN104721146A (en) | Celecoxib solvent dispersoid, pellet capsule and preparation methods of celecoxib solvent dispersoid and pellet capsule | |
| CN113332259B (en) | Azithromycin dry suspension | |
| CN111358795A (en) | Tofacitinib citrate preparation and preparation method thereof | |
| CN114306254B (en) | Monnpiravir oral solid preparation and preparation method thereof | |
| CN102846579B (en) | Valsartan medicinal capsule and preparation method thereof | |
| CN115531350B (en) | Azilsartan capsule and preparation method thereof | |
| CN115569124B (en) | Selpatinib capsule composition and preparation method thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20180323 |
|
| RJ01 | Rejection of invention patent application after publication |