CN103284958B - A kind of Cefdinir composition granule and preparation method thereof - Google Patents

A kind of Cefdinir composition granule and preparation method thereof Download PDF

Info

Publication number
CN103284958B
CN103284958B CN201310248312.XA CN201310248312A CN103284958B CN 103284958 B CN103284958 B CN 103284958B CN 201310248312 A CN201310248312 A CN 201310248312A CN 103284958 B CN103284958 B CN 103284958B
Authority
CN
China
Prior art keywords
cefdinir
sucrose
hpmc
ethanol
present
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.)
Active
Application number
CN201310248312.XA
Other languages
Chinese (zh)
Other versions
CN103284958A (en
Inventor
韩后良
张宗林
李明杰
王金星
刘延珍
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Shandong Luoxin Pharmaceutical Group Hengxin Pharmacy Co., Ltd.
Shandong Yu Xin pharmaceutcal corporation, Ltd
Shandong Luoxin Pharmaceutical Group Co Ltd
Original Assignee
SHANDONG HENGXIN PHARMACEUTICAL Co Ltd
Shandong Yu Xin Pharmaceutcal Corp Ltd
Shandong Luoxin Pharmaceutical Group Co Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by SHANDONG HENGXIN PHARMACEUTICAL Co Ltd, Shandong Yu Xin Pharmaceutcal Corp Ltd, Shandong Luoxin Pharmaceutical Group Co Ltd filed Critical SHANDONG HENGXIN PHARMACEUTICAL Co Ltd
Priority to CN201310248312.XA priority Critical patent/CN103284958B/en
Publication of CN103284958A publication Critical patent/CN103284958A/en
Application granted granted Critical
Publication of CN103284958B publication Critical patent/CN103284958B/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Abstract

The present invention relates to field of medicine preparations, specifically disclose a kind of Cefdinir composition granule and preparation method thereof.Cefdinir composition granule effective ingredient of the present invention comprises cefdinir, pregelatinized starch, 50% ethanol, HPMC, sucrose.The preferred cefdinir of the present invention, pregelatinized starch, 50% ethanol, HPMC, sucrose are as the effective ingredient of cefdinir granules, mutual synergism improves stability and the dissolution of cefdinir, and mouthfeel is better than existing product, improve the compliance of patient medication, be conducive to safe handling and the long term storage of clinical medicine.

Description

A kind of Cefdinir composition granule and preparation method thereof
Technical field
The present invention relates to field of medicine preparations, be specifically related to a kind of Cefdinir composition granule and preparation method thereof.
Background technology
Cefdinir; English Cefdinir Capsules by name; chemistry (6R by name; 7R)-7-[[(2-amino-4-thiazolyl)-(oximido) acetyl group] is amino]-3-vinyl-8-oxo-5-thia-1-azabicyclo [4.2.0] oct-2-ene-2-carboxylic acid, chemical constitution is as follows:
Cefdinir belongs to semisynthetic, the oral third generation cephalosporin of wide spectrum, and its synthesis by anti-bacteria cell wall produces antibacterial action.This product all has antibacterial activity to gram positive bacteria and negative bacterium, and stablizes most of beta-lactamase, so the microorganism of many penicillin resistants and cephalosporin is responsive to this product.Clinically be used for the treatment of tonsillitis, sinusitis, otitis media, acute bronchitis, pneumonia, abdominal cavity, urogenital infections etc.
Cefdinir raw material is micro-yellow powder shape, and poorly water-soluble, easily produces electrostatic, poor fluidity, and unstable under hot and humid condition, and related substance raises, and affects its safety and effectiveness.Therefore, suitable appropriate drug component just becomes the key factor affecting cefdinir preparation quality, develops a kind of cefdinir granule be made up of phase suitable drugs component and can bring positive effect for the safe and effective application of cefdinir undoubtedly.As patent CN201010176154.8 discloses a kind of cephalosporin suspension granule and preparation method thereof, which employs active component, stabilizing agent, excipient, suspending agent, disintegrating agent, correctives coloring agent binding agent, spice various ingredients, wherein embodiment 4 specifically discloses a kind of technical scheme of cefdinir mix suspension grain, although can bring certain improvement for cefdinir preparation quality, too much compositional selecting also becomes the not high influence factor of cefdinir stability, dissolution.
Summary of the invention
In view of this, the object of the present invention is to provide a kind of Cefdinir composition granule and preparation method thereof, make described cefdinir granules can improve stability (as the aspect such as labelled amount, related substance) and the dissolution of cefdinir.
For achieving the above object, the invention provides following technical scheme:
A kind of Cefdinir composition granule, effective ingredient comprises cefdinir, pregelatinized starch, 50% ethanol, HPMC, sucrose.
As preferably, with parts by weight, described effective ingredient comprises 40-100 part cefdinir, 5-20 part pregelatinized starch, 50-70 part 50% ethanol, 15-20 part HPMC, 400-450 part sucrose.
More preferably, described effective ingredient comprises 50 parts of cefdinirs, 5 parts of pregelatinized starchs, 60 part of 50% ethanol, 20 portions of HPMC, 430 portions of sucrose.
For existing cefdinir granules stability and the not high defect of dissolution, particularly in the labelled amount, related substance equistability of long term storage and extreme environment, the present invention is through long-term further investigation, consider the impact between various effective ingredient, optimize the compositing formula of cefdinir granules, select cefdinir, pregelatinized starch, 50% ethanol, HPMC, sucrose as effective ingredient, improve its stability under hot and humid environment and dissolution.
The various components that the present invention adopts, not only synergism adds the stability of cefdinir granules, and it also has some advantages separately, if starch is the nutrient substance of needed by human.Under the effect of the digestive enzyme in human body, starch can become glucose molecule gradually.Glucose has critical role in field of biology, energy source and the metabolism intermediate product of living cells, it is that one can directly absorb, supplement the carbohydrate of heat energy, it is the main source of needed by human body energy, be oxidized to carbon dioxide and water in vivo, and supply heat simultaneously, or store with glycogen form.The function of detoxification of liver can be promoted, have protective effect to liver.Energy goods and materials the most common in organism.Pregelatinized starch is compared with native starch, and it has many advantages: 1. good fluidity, and no matter be dry or wet, mobility is all fine, and has bonding and disintegrating property concurrently.2. compressibility is good, is applicable to direct compression of full-powder.3. there is self-lubrication, reduce the strength that tablet ejects from mould circle.4. good disintegrative.5. to the solubility of portion of cold water.6. inoperative with principal agent, and have the function of stable medicine, easily cause variable color to wet, heat sensitive medicine such as the wet granulation such as vitamin C, aspirin, content and drug effect decline, and after using this product instead, facilitate the stability of principal agent, extend useful life.
Sucrose is a kind of natural organic matter, and sucrose extracts from sugar crop Radix Betae or Caulis Sacchari sinensis, and the end product that people eats rear decomposition is carbon dioxide and water.Sucrose has unique function, and the sweet taste as sucrose is pure stable, is easy to dissolve and toning, can also crystallizes out rapidly from saturated solution; Sucrose has osmosis, and harmful microbe can be suppressed to grow; Sucrose has water absorption and water-retaining property.Sucrose in Cefdinir composition granule of the present invention is with low cost, but also granule can be made to have good water absorption and water-retaining property.
In addition, the present invention also provides a kind of preparation method of Cefdinir composition granule, with cefdinir, pregelatinized starch, 50% ethanol, HPMC, sucrose for effective ingredient, cefdinir is crossed 120 mesh sieves for subsequent use, it is for subsequent use that 80 orders pulverized by sucrose; Take cefdinir, pregelatinized starch, HPMC, sucrose fully mixes, with 50% ethanol soft material, 20 order wet granulations, by granule about 65 DEG C forced air dryings, dry granule 16 order granulate, sieve 80 orders and get final product.
As preferably, with parts by weight, each effective ingredient content is:
40-100 part cefdinir, 5-20 part pregelatinized starch, 50-70 part 50% ethanol, 15-20 part HPMC, 400-450 part sucrose.
More preferably, with parts by weight, each effective ingredient content is:
50 parts of cefdinirs, 5 parts of pregelatinized starchs, 60 part of 50% ethanol, 20 portions of HPMC, 430 portions of sucrose.
Product disclosed in prepared Cefdinir composition granule and CN201010176154.8 patent is carried out high humidity high temperature exposure experiments to light, accelerated test and long term test by the present invention, result shows, when accelerated test and long term test, the indexs such as principal agent labelled amount and related substance are more stable, compared with the control sample prepared with prior art, the present invention's amplitude of variation in every respect is all less than the amplitude of variation of control sample, and stability is stronger.Meanwhile, result also shows product dissolution of the present invention higher than control sample.Thus, the present invention also provides a kind of Cefdinir composition granule prepared by preparation method of the present invention.
From above technical scheme, the preferred cefdinir of the present invention, pregelatinized starch, 50% ethanol, HPMC, sucrose are as the effective ingredient of cefdinir granules, mutual synergism improves stability and the dissolution of cefdinir, and mouthfeel is better than existing product, improve the compliance of patient medication, be conducive to safe handling and the long term storage of clinical medicine.
Detailed description of the invention
The invention discloses a kind of Cefdinir composition granule and preparation method thereof, those skilled in the art can use for reference present disclosure, and suitable improving technique parameter realizes.Special needs to be pointed out is, all similar replacements and change apparent to those skilled in the art, they are all deemed to be included in the present invention.The method of the invention is described by preferred embodiment, related personnel obviously can not depart from content of the present invention, spirit and scope compound as herein described and preparation method are changed or suitably change with combination, realize and apply the technology of the present invention.
In the present invention, the amount of all cefdinirs is all with C 14h 13n 5o 5s 2meter.Below in conjunction with embodiment, set forth the present invention further.
Embodiment 1: prepare Cefdinir composition granule of the present invention
Cefdinir is crossed 120 mesh sieves for subsequent use, it is for subsequent use that 80 orders pulverized by sucrose; Take cefdinir, pregelatinized starch, HPMC, sucrose fully mixes, with 50% ethanol soft material, 20 order wet granulations, by granule about 65 DEG C forced air dryings, dry granule 16 order granulate, sieve 80 orders, and middle product detect, subpackage and get final product.
Embodiment 2: prepare Cefdinir composition granule of the present invention
Cefdinir is crossed 120 mesh sieves for subsequent use, it is for subsequent use that 80 orders pulverized by sucrose; Take cefdinir, pregelatinized starch, HPMC, sucrose fully mixes, with 50% ethanol soft material, 20 order wet granulations, by granule about 65 DEG C forced air dryings, dry granule 16 order granulate, sieve 80 orders, and middle product detect, subpackage and get final product.
Embodiment 3: prepare Cefdinir composition granule of the present invention
Cefdinir is crossed 120 mesh sieves for subsequent use, it is for subsequent use that 80 orders pulverized by sucrose; Take cefdinir, pregelatinized starch, HPMC, sucrose fully mixes, with 50% ethanol soft material, 20 order wet granulations, by granule about 65 DEG C forced air dryings, dry granule 16 order granulate, sieve 80 orders, and middle product detect, subpackage and get final product.
Embodiment 4: prepare Cefdinir composition granule of the present invention
Cefdinir is crossed 120 mesh sieves for subsequent use, it is for subsequent use that 80 orders pulverized by sucrose; Take cefdinir, pregelatinized starch, HPMC, sucrose fully mixes, with 50% ethanol soft material, 20 order wet granulations, by granule about 65 DEG C forced air dryings, dry granule 16 order granulate, sieve 80 orders, and middle product detect, subpackage and get final product.
Embodiment 5: preparation contrast Cefdinir composition granule
Cefdinir is crossed 120 mesh sieves for subsequent use, it is for subsequent use that 80 orders pulverized by sucrose; Take cefdinir, HPMC, sucrose fully mixes, with 50% ethanol soft material, 20 order wet granulations, by granule about 65 DEG C forced air dryings, dry granule 16 order granulate, sieve 80 orders, and middle product detect, subpackage and get final product.
Embodiment 6: Product checking result
Get embodiment of the present invention 1-4 sample and embodiment 5 sample (reference substance 1), CN201010176154.8 patent Example 4 product (reference substance 2), carry out Product checking, the results are shown in Table 1.
Table 1 Product checking result
As seen from the above table, product prepared by the present invention is before the test not carrying out various extreme environment, its testing result such as stability and dissolution and existing reference substance no significant difference, and mouthfeel is better than reference substance, add the compliance that patient takes, show that cefdinir granules quality prepared by the present invention meets existing standard.
Embodiment 7: high temperature, high humidity, exposure experiments to light
Get the embodiment of the present invention 4 sample and embodiment 5 sample (control sample 1), CN201010176154.8 patent Example 4 product (control sample 2), put respectively in the container of sealing clean, carry out high temperature, high humidity, exposure experiments to light, experimental condition is as follows:
High temperature: place 10 days at 60 DEG C of temperature, in the 5th day and sampling in the 10th day, detect by stability high spot reviews project, result of the test compared with 0 day.
High humidity: place 10 days under 25 DEG C of conditions respectively at relative humidity 90% ± 5%, in the 5th day and sampling in the 10th day, detect by stability high spot reviews project, result of the test compared with 0 day.
Illumination: being placed in illumination is place 10 days under the condition of 4500Lx, and in the 5th day and sampling in the 10th day, detect by stability high spot reviews project, result of the test compared with 0 day.
Testing result is in table 2
The hot and humid exposure experiments to light testing result of table 2
As can be seen from table 2 data, the embodiment of the present invention 4 product, under high temperature, high humidity, illumination condition, all will be stablized than control sample in moisture, dissolution, related substance and labelled amount etc.
Embodiment 8: accelerated test
Get the embodiment of the present invention 4 sample and embodiment 5 sample (control sample 1), CN201010176154.8 patent Example 4 product (control sample 2), place 6 months under temperature 40 DEG C ± 2 DEG C, relative humidity are the condition of 75% ± 5% respectively, respectively at the 1st, 2,3,6 sampling at the end of month once, measure by stability high spot reviews project.Result of the test is in table 3.
Table 3 accelerated test result
As can be seen from table 3 data, the embodiment of the present invention 3 product, under temperature 40 DEG C ± 2 DEG C, relative humidity are the condition of 75% ± 5%, all will be stablized than control sample in moisture, dissolution, related substance and labelled amount etc.
Embodiment 9: long term test
Get the embodiment of the present invention 4 sample and embodiment 5 sample (control sample 1), CN201010176154.8 patent Example 4 product (control sample 2), it is 20 DEG C in temperature respectively, relative humidity is place 12 months under the condition of 60% ± 10%, respectively at the 3rd, 6,9,12 sampling at the end of month once, measure by stability high spot reviews project.Result of the test is in table 4.
Table 4 long-term test results
As can be seen from table 4 data, the embodiment of the present invention 4 product is 20 DEG C in temperature, and relative humidity is under the condition of 60% ± 10%, all will stablize than control sample in moisture, dissolution, related substance and labelled amount etc.
The above is only the preferred embodiment of the present invention; it should be pointed out that for those skilled in the art, under the premise without departing from the principles of the invention; can also make some improvements and modifications, these improvements and modifications also should be considered as protection scope of the present invention.

Claims (5)

1. a Cefdinir composition granule, it is characterized in that, with parts by weight, described effective ingredient is made up of 40-100 part cefdinir, 5-20 part pregelatinized starch, 50-70 part 50% ethanol, 15-20 part HPMC, 400-450 part sucrose.
2. Cefdinir composition granule according to claim 1, it is characterized in that, with parts by weight, described effective ingredient is made up of 50 parts of cefdinirs, 5 portions of pregelatinized starchs, 60 part of 50% ethanol, 20 portions of HPMC, 430 portions of sucrose.
3. the preparation method of a Cefdinir composition granule, it is characterized in that, with cefdinir, pregelatinized starch, 50% ethanol, HPMC, sucrose for effective ingredient, cefdinir is crossed 120 mesh sieves for subsequent use, it is for subsequent use that 80 orders pulverized by sucrose; Take cefdinir, pregelatinized starch, HPMC, sucrose fully mixes, with 50% ethanol soft material, 20 order wet granulations, by granule about 65 DEG C forced air dryings, dry granule 16 order granulate, sieve 80 orders and get final product;
Each effective ingredient content is:
40-100 part cefdinir, 5-20 part pregelatinized starch, 50-70 part 50% ethanol, 15-20 part HPMC, 400-450 part sucrose.
4. preparation method according to claim 3, it is characterized in that, with parts by weight, each effective ingredient content is:
50 parts of cefdinirs, 5 parts of pregelatinized starchs, 60 part of 50% ethanol, 20 portions of HPMC, 430 portions of sucrose.
5. the Cefdinir composition granule that described in claim 3-4 any one prepared by preparation method.
CN201310248312.XA 2013-06-21 2013-06-21 A kind of Cefdinir composition granule and preparation method thereof Active CN103284958B (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201310248312.XA CN103284958B (en) 2013-06-21 2013-06-21 A kind of Cefdinir composition granule and preparation method thereof

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN201310248312.XA CN103284958B (en) 2013-06-21 2013-06-21 A kind of Cefdinir composition granule and preparation method thereof

Publications (2)

Publication Number Publication Date
CN103284958A CN103284958A (en) 2013-09-11
CN103284958B true CN103284958B (en) 2015-07-29

Family

ID=49086856

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201310248312.XA Active CN103284958B (en) 2013-06-21 2013-06-21 A kind of Cefdinir composition granule and preparation method thereof

Country Status (1)

Country Link
CN (1) CN103284958B (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103637992B (en) * 2013-12-19 2015-04-08 石家庄市华新药业有限责任公司 Cefdinir granular preparation and preparation method thereof
CN115607553B (en) * 2021-07-16 2024-02-23 广州白云山天心制药股份有限公司 Medicine containing cefdinir
CN114983964A (en) * 2022-06-24 2022-09-02 广东恒健制药有限公司 Cefdinir granules and preparation method thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101816635A (en) * 2010-05-17 2010-09-01 广东恒健制药有限公司 Cephalosporin suspension granule and preparation method thereof
CN102058561A (en) * 2010-12-30 2011-05-18 江苏亚邦强生药业有限公司 Cefdinir capsule and preparation method thereof
CN102266306A (en) * 2011-07-13 2011-12-07 石家庄四药有限公司 Cefdinir capsules and preparation method thereof

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101816635A (en) * 2010-05-17 2010-09-01 广东恒健制药有限公司 Cephalosporin suspension granule and preparation method thereof
CN102058561A (en) * 2010-12-30 2011-05-18 江苏亚邦强生药业有限公司 Cefdinir capsule and preparation method thereof
CN102266306A (en) * 2011-07-13 2011-12-07 石家庄四药有限公司 Cefdinir capsules and preparation method thereof

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
周永健等.第三代口服头孢菌素-头孢地尼.《天津药学》.2003,第15卷(第2期),第66-68页. *

Also Published As

Publication number Publication date
CN103284958A (en) 2013-09-11

Similar Documents

Publication Publication Date Title
CN101816635B (en) Cephalosporin suspension granule and preparation method thereof
CN103349646B (en) A kind of pharmaceutical composition of cefaclor granule, its preparation method and application
CN103284958B (en) A kind of Cefdinir composition granule and preparation method thereof
CN102525963B (en) Netilmicin sulfate lyophiled powder injection and preparation method thereof
CN101912368A (en) Compound cefaclor suspension and preparation method thereof
CN102286045B (en) Roxithromycin monohydrate crystal, preparation method thereof and compound dry suspension containing roxithromycin monohydrate crystal and ambroxol hydrochloride composition
CN103446075B (en) A kind of Cefaclor Capsules and preparation method thereof
CN103330685A (en) Cefaclor granule and preparation method thereof
CN103893132B (en) A kind of cefdinir granules and preparation technology thereof
CN103301075B (en) A kind of cefixime composition mix suspension grain agent and preparation method thereof
CN104688713A (en) Cefradine capsule and preparation method thereof
CN105534937A (en) Cefadroxil tablet and preparation method thereof
CN103622916B (en) Cefixime dry suspension and preparation method thereof
CN103919744B (en) A kind of Cefteram Pivoxil Tablets and preparation technology thereof
CN103520120B (en) A kind of L-084 composition granule
CN104546735A (en) Pediatric tosufloxacin tosilate granule and preparation method thereof
CN102342949B (en) Application of phlorhizin in preparation of drug for treating hyperuricemia
CN102311452A (en) Cefixime crystal, preparation method thereof and tablet composition containing same
CN103263398B (en) Cefdinir composition capsule and preparation method thereof
CN104382849B (en) A kind of cefaclor dry suspension and preparation method thereof
CN105496984A (en) Cefixime capsule stable in quality and preparation method thereof
CN106588954B (en) A kind of anti-infectives amoxycillin crystalline compounds and combinations thereof
CN109846827A (en) A kind of Cefixime mix suspension grain agent and preparation method thereof
CN104130303A (en) Cobamamide compound and medicinal composition thereof
CN104523688B (en) Ampicillin and probenecid capsules and preparation method 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
ASS Succession or assignment of patent right

Owner name: SHANDONG LUOXIN PHARMACY GROUP CO., LTD.

Free format text: FORMER OWNER: SHANDONG LUOXIN PHARMACY STOCK CO., LTD.

Effective date: 20150630

Owner name: SHANDONG YUXIN PHARMACEUTICAL CO., LTD. SHANDONG H

Effective date: 20150630

C41 Transfer of patent application or patent right or utility model
C53 Correction of patent for invention or patent application
CB03 Change of inventor or designer information

Inventor after: Han Houliang

Inventor after: Zhang Zonglin

Inventor after: Li Mingjie

Inventor after: Wang Jinxing

Inventor after: Liu Yanzhen

Inventor before: Zhang Zonglin

Inventor before: Li Mingjie

Inventor before: Wang Jinxing

Inventor before: Liu Yanzhen

COR Change of bibliographic data

Free format text: CORRECT: INVENTOR; FROM: ZHANG ZONGLIN LI MINGJIE WANG JINXING LIU YANZHEN TO: HAN HOULIANG ZHANG ZONGLIN LI MINGJIE WANG JINXING LIU YANZHEN

TA01 Transfer of patent application right

Effective date of registration: 20150630

Address after: Seven of 276017 Shandong province Linyi city Luozhuang District No. 18

Applicant after: Shandong Luo Xin Pharmaceutical Group Plc

Applicant after: Shandong Yu Xin pharmaceutcal corporation, Ltd

Applicant after: SHANDONG HENGXIN PHARMACEUTICAL CO., LTD.

Address before: Seven of 276017 Shandong province Linyi city Luozhuang District No. 18

Applicant before: SHANDONG LUOXIN PHARMACY STOCK Co., LTD.

C14 Grant of patent or utility model
GR01 Patent grant
CP01 Change in the name or title of a patent holder
CP01 Change in the name or title of a patent holder

Address after: 276017 18 Luo Qi Road, Luozhuang District, Linyi, Shandong

Co-patentee after: Shandong Yu Xin pharmaceutcal corporation, Ltd

Patentee after: Shandong Luo Xin Pharmaceutical Group Plc

Co-patentee after: Shandong Luoxin Pharmaceutical Group Hengxin Pharmacy Co., Ltd.

Address before: 276017 18 Luo Qi Road, Luozhuang District, Linyi, Shandong

Co-patentee before: Shandong Yu Xin pharmaceutcal corporation, Ltd

Patentee before: Shandong Luo Xin Pharmaceutical Group Plc

Co-patentee before: SHANDONG HENGXIN PHARMACEUTICAL CO., LTD.