CN101836994A - Compound oral preparation of cefaclor and bromhexine and preparation method thereof - Google Patents
Compound oral preparation of cefaclor and bromhexine and preparation method thereof Download PDFInfo
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- CN101836994A CN101836994A CN201010191732A CN201010191732A CN101836994A CN 101836994 A CN101836994 A CN 101836994A CN 201010191732 A CN201010191732 A CN 201010191732A CN 201010191732 A CN201010191732 A CN 201010191732A CN 101836994 A CN101836994 A CN 101836994A
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- cefaclor
- bromhexine
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- oral administration
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Abstract
The invention provides a compound oral preparation of cefaclor and bromhexine and a preparation method thereof. The compound oral preparation consists of main materials and auxiliary materials, wherein the main materials comprise 250 parts of cefaclor and 8 parts of bromhexine in part by weight; and based on 250 weight parts of cefaclor, the auxiliary materials comprise 50 to 200 parts of filling agent, 50 to 200 parts of thinner, 2 to 20 parts of disintegrating agent and 2 to 10 parts of lubricant. The compound cefaclor oral preparation provided by the invention has the advantages of simple preparation method, quick disintegration in vivo, quick absorption medicament, early response and high bioavailability.
Description
Technical field
The present invention relates to a kind of cefaclor and bromhexine compound oral administration preparation and preparation method thereof.
Background technology
Cefaclor is semisynthetic second generation cephalosporin, and antimicrobial spectrum and antibacterial activity are similar to cefazolin sodium.Streptococcus pneumoniae, micrococcus scarlatinae, staphylococcus, proteus mirabilis, escherichia coli and pneumobacillus, hemophilus influenza, gonorrhea diplococcus and anaerobe etc. there is good antibacterial activity.Similar to the activity of producing enzyme gold Portugal bacterium, A type Hemolytic streptococcus, Streptococcus viridans and staphylococcus epidermidis to cefadroxil.Activity to proteus mirabilis is also stronger.Be mainly used in respiratory tract infection, as tracheitis, pneumonia, pharyngitis, tonsillitis; Urinary tract infection is as pyelonephritis, cystitis, gonococcal urethritis; Skin soft-tissue infection.
At present, domestic cefaclor capsule, cefaclor Film coated tablets, cefaclor dispersible tablet, four kinds of dosage forms of cefaclor granule of mainly existing all are to adopt the wet granulation technology preparation.
CN200410022980.1 discloses a kind of compound cefaclor dispersible tablet, it is characterized in that being prepared from by cefaclor, Bisolvon, filler, diluent, disintegrating agent, mix lubricant, by the diluent tabletting, make the first in vivo disintegrate of medicine become graininess by disintegrating agent, thereby principal agent slowly discharge onset from granule then.Though this dispersible tablet contains cefaclor and Bisolvon simultaneously, the dispose procedure of this medicine is complicated, and bioavailability is not high, and in addition, supplementary product consumption is more in its preparation process, and complicated process of preparation and production cost are higher.
Summary of the invention
Therefore, it is not high to the objective of the invention is to overcome in the prior art cefaclor and bromhexine compound oral administration preparation bioavailability, the shortcoming that complicated process of preparation and production cost are higher provides a kind of bioavailability height, preparation technology are simple and production cost is lower cefaclor and bromhexine compound oral administration preparation and preparation method thereof.
The invention provides a kind of cefaclor and bromhexine compound oral administration preparation, its composition comprises major ingredient and adjuvant, and described major ingredient is counted by weight: 8 parts of 250 parts of cefaclors and bromhexines; Cefaclor with 250 weight portions is a benchmark, and described adjuvant is counted by weight: filler 50-200 part, diluent 50-200 part, disintegrating agent 2-20 part and lubricant 2-10 part.That is, the composition of this cefaclor and bromhexine compound oral administration preparation is as follows by weight: 250 parts of cefaclors, 8 parts of bromhexines, filler 50-200 part, diluent 50-200 part, disintegrating agent 2-20 part and lubricant 2-10 part.
Wherein, described filler is preferably spray-dried lactose; Described diluent is preferably microcrystalline Cellulose, more preferably microcrystalline Cellulose 101 or 302; Described disintegrating agent can be preferably low-substituted hydroxypropyl cellulose or polyvinylpolypyrrolidone; Described lubricant is preferably micropowder silica gel and/or magnesium stearate.
Under the preferable case, in order to make cefaclor of the present invention and bromhexine compound oral administration preparation have higher bioavailability, cefaclor with 250 weight portions is a benchmark, and described adjuvant is counted by weight: filler 50-150 part, diluent 50-150 part, disintegrating agent 10-20 part and lubricant 5-10 part.
According to cefaclor provided by the invention and bromhexine compound oral administration preparation, wherein, described oral formulations can comprise the oral formulations of various routines, for example, can be capsule, tablet, dry suspension.
The present invention also further provides the preparation method of above-mentioned cefaclor and bromhexine compound oral administration preparation, and this method can comprise the steps:
(1) respectively various major ingredients and adjuvant are crossed the 50-200 mesh sieve;
(2) take by weighing various major ingredients and adjuvant, mix homogeneously respectively;
(3) tabletting or be filled in the capsule shells or direct packaging promptly gets preparation of the present invention in two aluminum bags/paper aluminum bag.
Wherein, described major ingredient is counted by weight: 8 parts of 250 parts of cefaclors and bromhexines; Cefaclor with 250 weight portions is a benchmark, and described adjuvant is counted by weight: filler 50-200 part, diluent 50-200 part, disintegrating agent 2-20 part and lubricant 2-10 part.
Under the preferable case, simplify preparation process simultaneously, can in step (1), respectively raw material and adjuvant be crossed the 80-150 mesh sieve for the bioavailability that further improves cefaclor of the present invention and bromhexine compound oral administration preparation.
In preparation method provided by the invention, describedly sieve, the operational approach and the equipment of mixing, tabletting, filling and packing is conventionally known to one of skill in the art, repeat no more herein.
The invention has the advantages that:
1. the present invention adopts directly filling of powder, packing or tabletting, need not to granulate, and compared with prior art preparation technology is simple;
2. used adjuvant is few than prior art, has saved production cost;
3. medicine of the present invention enters the interior directly disintegrate of body becomes drug powder and onset, and stripping is very fast, has improved bioavailability.
The specific embodiment
Below in conjunction with the specific embodiment the present invention is further described in detail, the embodiment that provides is only in order to illustrate the present invention, rather than in order to limit the scope of the invention.
Embodiment 1
Present embodiment is used to illustrate cefaclor provided by the invention and bromhexine compound oral administration preparation and preparation method thereof.
Respectively various major ingredients and adjuvant are crossed 100 mesh sieves, take by weighing cefaclor 250g, bromhexine 8g after sieving respectively, spraying vertical compression lactose 100g, low substituted cellulose 2g and micropowder silica gel 2g, mix homogeneously, specification with cefaclor 250mg, bromhexine 8mg/ grain is filled in the Capsules, promptly obtain cefaclor provided by the invention and bromhexine compound oral administration preparation, note is made A1.
Embodiment 2
Present embodiment is used to illustrate cefaclor provided by the invention and bromhexine compound oral administration preparation and preparation method thereof.
Respectively various major ingredients and adjuvant are crossed 120 mesh sieves, take by weighing cefaclor 250g, bromhexine 8g after sieving respectively, spraying vertical compression lactose 150g, low substituted cellulose 10g and micropowder silica gel 10g, mix homogeneously, specification tabletting with cefaclor 250mg, bromhexine 8mg/ grain, promptly obtain cefaclor provided by the invention and bromhexine compound oral administration preparation, note is made A2.
Embodiment 3
Present embodiment is used to illustrate cefaclor provided by the invention and bromhexine compound oral administration preparation and preparation method thereof.
Respectively various major ingredients and adjuvant are crossed 90 mesh sieves, take by weighing cefaclor 250g, bromhexine 8g after sieving respectively, spraying vertical compression lactose 200g, polyvinylpolypyrrolidone 2g and magnesium stearate 2g, mix homogeneously, specification direct packaging with cefaclor 250mg, bromhexine 8mg/ grain is made dry suspension in two aluminum or paper aluminum bag, promptly obtain cefaclor provided by the invention and bromhexine compound oral administration preparation, note is made A3.
Embodiment 4
Present embodiment is used to illustrate cefaclor provided by the invention and bromhexine compound oral administration preparation and preparation method thereof.
Respectively various major ingredients and adjuvant are crossed 100 mesh sieves, take by weighing cefaclor 250g, bromhexine 8g after sieving respectively, spraying vertical compression lactose 100g, polyvinylpolypyrrolidone 20g and magnesium stearate 10g, mix homogeneously, specification with cefaclor 250mg, bromhexine 8mg/ grain is filled in the Capsules, promptly obtain cefaclor provided by the invention and bromhexine compound oral administration preparation, note is made A4.
The dissolution contrast test:The dissolution of the cefaclor of comparison the present invention preparation and bromhexine compound oral administration preparation and commercially available sample cefaclor capsule (Lukang Medical Co., Ltd., Shandong), cefaclor sheet (Baiyunshan Pharmaceutical General Factory), cefaclor dispersible tablet (Shijiazhuang City Hua Xin pharmaceutical factory), cefaclor granule (Beijing Double-Crane Pharmaceutical Co., Ltd), the result is as shown in table 1.
Table 1
| Test specimen | Dissolution (%) (15min) | Dissolution (%) (30min) |
| ??A1 | ??100.35 | ??100.31 |
| ??A2 | ??99.46 | ??99.51 |
| ??A3 | ??100.02 | ??99.95 |
| ??A4 | ??101.34 | ??100.96 |
| The cefaclor capsule | ??86.47 | ??98.93 |
| The cefaclor sheet | ??88.38 | ??99.75 |
| The cefaclor dispersible tablet | ??92.63 | ??100.24 |
| The cefaclor granule | ??89.56 | ??100.08 |
The result indicates: cefaclor provided by the invention and bromhexine compound oral administration preparation have reached the stripping platform in the time of 15 minutes, other commercially available samples did not reach the stripping platform and just reach the stripping platform during at 30 minutes in the time of 15 minutes, therefore the more commercially available sample stripping of the present invention is fast, and bioavailability of the present invention is higher than commercially available sample.
Pharmacokinetics and relative bioavailability test
Method: 45 routine experimenters are divided into 5 groups at random, every group 9 people.Wherein four groups with 500mg/ people's the dosage cefaclor and the bromhexine compound oral administration preparation A1-A4 that make of oral embodiment of the invention 1-4 on an empty stomach.The 5th group is matched group, with 500mg/ people's the on an empty stomach oral cefaclor capsule of dosage (producer: Lukang Medical Co., Ltd., Shandong).Adopt microbial process to measure the concentration of different time (0.5h, 1h, 2h, 3h, 4h, 5h) cefaclor in the serum, calculate pharmacokinetic parameter and relative bioavailability.
The result: physiological disposition meets the outer two-compartment model of blood vessel, the C of A1-A4
MaxBe (8.89 ± 3.75) mg/L, T
MaxBe (0.82 ± 0.34) h, t1/2 is (0.30 ± 0.27) h, and AUC is (10.97 ± 4.31) mgh/L.The C of matched group
MaxBe (7.52 ± 3.86) mg/L, T
MaxBe (0.99 ± 0.38) h, t1/2 is (0.43 ± 0.30) h, and AUC is (8.97 ± 3.51) mgh/L.
Conclusion: cefaclor provided by the invention and bromhexine compound oral administration preparation bioavailability are higher than matched group.
Claims (6)
1. cefaclor and bromhexine compound oral administration preparation, its composition comprises major ingredient and adjuvant, described major ingredient is counted by weight: 8 parts of 250 parts of cefaclors and bromhexines; Cefaclor with 250 weight portions is a benchmark, and described adjuvant is counted by weight: filler 50-200 part, diluent 50-200 part, disintegrating agent 2-20 part and lubricant 2-10 part.
2. cefaclor according to claim 1 and bromhexine compound oral administration preparation, wherein, described filler is a spray-dried lactose, described diluent is microcrystalline Cellulose 101 or 302, described disintegrating agent is low-substituted hydroxypropyl cellulose or polyvinylpolypyrrolidone, and described lubricant is micropowder silica gel and/or magnesium stearate.
3. cefaclor according to claim 1 and 2 and bromhexine compound oral administration preparation, wherein, described adjuvant is counted by weight: filler 50-150 part, diluent 50-150 part, disintegrating agent 10-20 part and lubricant 5-10 part.
4. according to each described cefaclor and bromhexine compound oral administration preparation in the claim 1 to 3, described oral formulations comprises capsule, tablet, dry suspension.
5. according to the preparation method of each described cefaclor and bromhexine compound oral administration preparation in the claim 1 to 4, this method comprises the steps:
(1) respectively raw material and adjuvant are crossed the 50-200 mesh sieve;
(2) take by weighing raw material and adjuvant, mix homogeneously respectively;
(3) tabletting or be filled in the capsule shells or direct packaging promptly gets cefaclor of the present invention and bromhexine compound oral administration preparation in two aluminum bags/paper aluminum bag.
Wherein, described major ingredient is counted by weight: 8 parts of 250 parts of cefaclors and bromhexines; Cefaclor with 250 weight portions is a benchmark, and described adjuvant is counted by weight: filler 50-200 part, diluent 50-200 part, disintegrating agent 2-20 part and lubricant 2-10 part.
6. method according to claim 5 wherein, is crossed the 80-150 mesh sieve with raw material and adjuvant respectively in step (1).
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN201010191732A CN101836994A (en) | 2010-06-01 | 2010-06-01 | Compound oral preparation of cefaclor and bromhexine and preparation method thereof |
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| CN201010191732A CN101836994A (en) | 2010-06-01 | 2010-06-01 | Compound oral preparation of cefaclor and bromhexine and preparation method thereof |
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Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101912368A (en) * | 2010-09-26 | 2010-12-15 | 上海理工大学 | Compound cefaclor suspension and preparation method thereof |
| CN102327269A (en) * | 2011-07-14 | 2012-01-25 | 海南美大制药有限公司 | Solid lipidosome preparation of compound cefaclor medicinal composition |
| CN102525949A (en) * | 2012-01-17 | 2012-07-04 | 山东罗欣药业股份有限公司 | Cefaclor composition particles and preparation method thereof |
| CN103463093A (en) * | 2013-09-17 | 2013-12-25 | 江苏正大清江制药有限公司 | Cefaclor dry suspension composition and preparation method thereof |
| CN104147056A (en) * | 2014-08-14 | 2014-11-19 | 广州一品红制药有限公司 | Composition containing bromhexine hydrochloride |
| CN105902490A (en) * | 2016-05-20 | 2016-08-31 | 江苏正大清江制药有限公司 | Cefaclor compound solid preparation and preparation method thereof |
| CN115721687A (en) * | 2022-11-23 | 2023-03-03 | 哈尔滨誉衡制药有限公司 | Compound cefaclor capsule and preparation method thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1666743A (en) * | 2004-03-12 | 2005-09-14 | 黄本东 | Compound cefaclor dispersible tablet |
-
2010
- 2010-06-01 CN CN201010191732A patent/CN101836994A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1666743A (en) * | 2004-03-12 | 2005-09-14 | 黄本东 | Compound cefaclor dispersible tablet |
Non-Patent Citations (1)
| Title |
|---|
| 《药剂学》 20070331 周建平 《片剂的制备》 东南大学出版社 第229－230页及第237－238页 权利要求2－6 , 1 * |
Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101912368A (en) * | 2010-09-26 | 2010-12-15 | 上海理工大学 | Compound cefaclor suspension and preparation method thereof |
| CN102327269A (en) * | 2011-07-14 | 2012-01-25 | 海南美大制药有限公司 | Solid lipidosome preparation of compound cefaclor medicinal composition |
| CN102525949A (en) * | 2012-01-17 | 2012-07-04 | 山东罗欣药业股份有限公司 | Cefaclor composition particles and preparation method thereof |
| CN102525949B (en) * | 2012-01-17 | 2013-06-05 | 山东罗欣药业股份有限公司 | Cefaclor composition particles and preparation method thereof |
| CN103463093A (en) * | 2013-09-17 | 2013-12-25 | 江苏正大清江制药有限公司 | Cefaclor dry suspension composition and preparation method thereof |
| CN104147056A (en) * | 2014-08-14 | 2014-11-19 | 广州一品红制药有限公司 | Composition containing bromhexine hydrochloride |
| CN104147056B (en) * | 2014-08-14 | 2015-07-08 | 广州一品红制药有限公司 | Composition containing bromhexine hydrochloride |
| CN105902490A (en) * | 2016-05-20 | 2016-08-31 | 江苏正大清江制药有限公司 | Cefaclor compound solid preparation and preparation method thereof |
| CN115721687A (en) * | 2022-11-23 | 2023-03-03 | 哈尔滨誉衡制药有限公司 | Compound cefaclor capsule and preparation method thereof |
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Application publication date: 20100922 |