CN103446075B - A kind of Cefaclor Capsules and preparation method thereof - Google Patents
A kind of Cefaclor Capsules and preparation method thereof Download PDFInfo
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- CN103446075B CN103446075B CN201310398644.6A CN201310398644A CN103446075B CN 103446075 B CN103446075 B CN 103446075B CN 201310398644 A CN201310398644 A CN 201310398644A CN 103446075 B CN103446075 B CN 103446075B
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- cefaclor
- polyvinyl alcohol
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Abstract
The invention discloses a kind of Cefaclor Capsules and preparation method thereof, said preparation is mixed by Cefaclor inclusion compound and pharmaceutically acceptable auxiliary material, does is described Cefaclor inclusion compound prepared from as follows: by polyvinyl alcohol-polyethyleneglycol-graft copolymer (Kollicoat? IR) be dissolved in ethanol, add Cefaclor, in stirring, drying under reduced pressure is except ethanol, encapsulating capsule and get final product. Good stability, the stripping of preparation of the present invention are rapid, and its production technology is simple, are applicable to suitability for industrialized production.
Description
Technical field
The invention belongs to medical technical field, in particular to a kind of Cefaclor Capsules and preparation method thereof.
Background technology
Cephalosporins is to play bactericidal action by anti-bacteria Cell wall synthesis, stable to most beta lactamases, is permittedFecund penicillase and cephalosporinase bacterial strain are still to cephalosporins medicaments insensitive. Cephalosporins in vitro and in vivoTo gram-positive cocci as pneumococcus, micrococcus scarlatinae, gram-Negative bacillus as Bacillus influenzae (comprise produce enzyme strain),Moraxelle catarrhalis (comprise and produce enzyme strain), Escherichia coli, proteus mirabilis, all good antibacterial works of tool of gonococcus (comprise and produce enzyme strain)With. Cephalosporins in vitro to streptococcus pneumonia, para-influenza Bacillus, proteus vulgaris, Klebsiella Pneumoniae, kill morePasteurella, Providian bacterium, Salmonella, Shigella, serratia marcesens, special-shaped citric acid bacteria, malonate citric acidBacterium is also had an antibacterial activity.
Cephalosporins is the semisynthetic antibiotics that contains cephem in molecule, and it belongs to beta-lactam antibiosisElement is the derivative of the 7-amino-cephalosporanic acid in beta-lactam antibiotic. Cynnematin is efficient, low toxicity, clinical practice are wideGeneral, have that has a broad antifungal spectrum, antibacterial action are strong, penicillin resistant enzyme, allergic reaction be compared with advantages such as PCs are rare, it not only canDestroy the cell membrane of bacterium, can also sterilization within the breeding period of bacterium, and body is not almost had to toxicity. Cefaclor isRepresentative a kind of medicine in cephalosporins.
Cefaclor raw material quality under wet, heat condition is unstable, easily degraded, therefore Cefaclor preparation in the marketQuality stability generally poor, preparation need lucifuge, sealing preserve. In addition, because Cefaclor is slightly soluble in water, therefore its capsuleConventionally have the bad problem of suspendible effect, add after a certain amount of water-soluble solution, solution suspendible effect is poor and occur lamination,The performance that is difficult to while taking ensure dosage and affect drug effect.
Summary of the invention
For the deficiencies in the prior art, the present invention, by preparation prescription and technique are improved, provides a kind of stabilityGood, stripping is rapid, the simple Cefaclor Capsules of technique and preparation method thereof.
The inventor studies by lot of experiments, has finally obtained the technical scheme that realizes as follows goal of the invention:
A kind of Cefaclor Capsules, is mixed by Cefaclor inclusion compound and pharmaceutically acceptable auxiliary material, describedCefaclor inclusion compound is prepared from as follows: by polyvinyl alcohol-polyethyleneglycol-graft copolymer (KollicoatIR)Be dissolved in ethanol, add Cefaclor, in stirring drying under reduced pressure except ethanol, encapsulating capsule and get final product.
Preferably, above-mentioned Cefaclor Capsules, wherein Cefaclor and polyvinyl alcohol-polyethyleneglycol-graft copolymer weightAmount is than being 1:1-6.
Further preferably, above-mentioned Cefaclor Capsules, wherein Cefaclor and polyvinyl alcohol-polyethylene glycol grafting are altogetherPolymers weight ratio is 1:2-4.
Again further preferably, above-mentioned Cefaclor Capsules, wherein said polyvinyl alcohol-polyethylene glycol graft copolymerizationThing is the graft copolymer that polyvinyl alcohol and polyethylene glycol are prepared by the weight ratio of 3:1.
The pharmaceutically acceptable auxiliary material adopting in Cefaclor Capsules of the present invention comprises filler; Described fillingAgent is selected from one or more in sucrose, lactose, sweet mellow wine, pregelatinized starch, starch, maltose, dextrin and xylitol.
Second object of the present invention is to provide a kind of preparation method of above-mentioned Cefaclor Capsules, comprise the steps: byPolyvinyl alcohol-polyethyleneglycol-graft copolymer is dissolved in ethanol, adds Cefaclor, and in stirring, drying under reduced pressure, except ethanol, obtains headSpore clo inclusion compound; By described Cefaclor inclusion compound and pharmaceutically acceptable auxiliary materials and mixing, obtain Cefaclor Capsules.
The preparation method of above-mentioned Cefaclor Capsules, wherein said polyvinyl alcohol-polyethyleneglycol-graft copolymer be byThe graft copolymer that polyvinyl alcohol and polyethylene glycol are prepared by the weight ratio of 3:1.
The preparation method of above-mentioned Cefaclor Capsules, wherein said pharmaceutically acceptable auxiliary material comprises filler; DescribedFiller be selected from a kind of or many in sucrose, lactose, sweet mellow wine, pregelatinized starch, starch, maltose, dextrin and xylitolKind.
The inventor is creatively dissolved in KollicoatIR in ethanolic solution, adds Cefaclor, stirs, and subtractsPress dry the dry ethanol that removes, because Cefaclor is almost insoluble in ethanol, thus be suspended in ethanolic solution, along with falling of concentration of alcoholLow, KollicoatIR slowly separates out, and medicine is wrapped up, and has avoided the impact of moisture, and therefore the stability of preparation obtainsSignificantly improve. Because KollicoatIR is water-soluble good, thus can promote the stripping of the medicine of Cefaclor Capsules, simultaneously thisBright preparation process thereof is simple, is applicable to suitability for industrialized production.
Specific embodiment
Following examples further describe preparation process of the present invention and beneficial effect, and embodiment is only for the order of illustration, do not limit the scope of the invention, the apparent change that simultaneously those of ordinary skill in the art make according to the present invention andWithin modification is also contained in the scope of the invention.
Embodiment 1
Preparation technology:
Cefaclor is crossed 100 mesh sieves, KollicoatIR(3:1) be dissolved in absolute ethyl alcohol, add Cefaclor, stirEvenly also drying under reduced pressure, except ethanol, mixes dried particle with the sucrose of crossing 100 mesh sieves, encapsulating capsule packaging.
Embodiment 2
Preparation technology:
Cefaclor is crossed 100 mesh sieves, KollicoatIR(3:1) be dissolved in absolute ethyl alcohol, add Cefaclor, stirEvenly also drying under reduced pressure, except ethanol, mixes dried particle encapsulating Nang Bao with sweet mellow wine, the lactose of crossing 100 mesh sievesDress.
Embodiment 3
Preparation technology:
Cefaclor is crossed 100 mesh sieves, KollicoatIR(3:1) be dissolved in absolute ethyl alcohol, add Cefaclor, stirEvenly also drying under reduced pressure, except ethanol, mixes dried particle with sweet mellow wine, sucrose, encapsulating capsule packaging. Contrast is implementedExample 1
Preparation technology:
Cefaclor, KollicoatIR(3:1), sweet mellow wine, sucrose all crosses 100 mesh sieves, recipe quantity takes, and mixes allEven, encapsulating capsule packaging.
Comparative example 2
Preparation technology:
Cefaclor is crossed 100 mesh sieves, and polyvinyl alcohol, polyethylene glycol are dissolved in ethanol, adds Cefaclor to stirAnd drying under reduced pressure is except ethanol, and dried particle is mixed with sweet mellow wine, sucrose, encapsulating capsule packaging.
Comparative example 3
Preparation technology:
Cefaclor, KollicoatIR(3:1) cross 100 mesh sieves, mix, add absolute ethyl alcohol appropriate, granulate, dryDry, dried particle is mixed to encapsulating capsule packaging with sweet mellow wine, sucrose.
Comparative example 4
Preparation technology:
Cefaclor is crossed 100 mesh sieves, and Eudragit E is dissolved in absolute ethyl alcohol, adds Cefaclor, stirs alsoDrying under reduced pressure, except ethanol, mixes dried particle with sweet mellow wine, sucrose, encapsulating capsule packaging.
Dissolution rate and the determination of related substances of embodiment 4 Cefaclor Capsules
1, dissolution determination. According to Chinese pharmacopoeia annex XC the second method square law device, taking water 900mL as dissolution medium, rotating speedFor 50rmin, respectively at 5,30min spot sampling 10mL, filter, supplement synthermal dissolution medium 10mL, accurate amount simultaneouslyGet subsequent filtrate 5mL and put in 25mL measuring bottle, then be diluted with water to scale, measure absorbance at 264nm wavelength place. The results are shown in Table 1.
2, determination of related substances. Take respectively Cefaclor Capsules prepared by embodiment 1-3 and comparative example 1-4 suitableAmount, adds 0.27% sodium dihydrogen phosphate (pH2.5) and dissolves and dilute, and gets subsequent filtrate as need testing solution, according to Chinese pharmacopoeiaUnder 2010 editions Cefaclor raw material items, measure, single impurity must not cross 0.5%. The results are shown in Table 2.
Table 1 dissolution determination result
| Sample source | 5min dissolution rate (%) | 30min dissolution rate (%) |
| Embodiment 1 | 95.8 | 99.6 |
| Embodiment 2 | 94.3 | 99.1 |
| Embodiment 3 | 93.5 | 100.6 |
| Comparative example 1 | 92.3 | 98.2 |
| Comparative example 2 | 54.6 | 94.1 |
| Comparative example 3 | 93.2 | 95.5 |
| Comparative example 4 | 28.4 | 85.1 |
Can find out from the result of the test of table 1: embodiment 1-3 and comparative example's 1,3 sample stripping is rapid, 5min baseThis stripping completely; Comparative example 2 is because polyvinyl alcohol, polyethylene glycol are only physical mixture, and polyvinyl alcohol has necessarilySlow release effect, therefore stripping is slow; Comparative example 4 causes drug-eluting after adopting acrylic resin to replace KollicoatIRSlowly.
Table 2 determination of related substances result
| Sample source | 0 day (%) | 40 DEG C, 75%RH accelerates 6 months (%) |
| Embodiment 1 | 0.24 | 0.35 |
| Embodiment 2 | 0.16 | 0.31 |
| Embodiment 3 | 0.15 | 0.37 |
| Comparative example 1 | 0.17 | 1.21 |
| Comparative example 2 | 0.28 | 1.54 |
| Comparative example 3 | 0.26 | 1.26 |
| Comparative example 4 | 0.27 | 0.55 |
Can find out from the result of the test of table 2: adopt the embodiment 1-3 sample stability of the technology of the present invention good, accelerate 6Month, related substance changes little; Comparative example 1,3 is only Cefaclor and KollicoatIR(3:1) physical mixture,Not by raw material parcel, therefore related substance increases obviously; In comparative example 2, polyvinyl alcohol, polyethylene glycol do not form graft copolymerizationThing, does not have the effect of parcel main ingredient of the present invention; Comparative example's 4 use acrylic resins replace KollicoatIR, relevantMaterial increases to obviously compared with the technology of the present invention in accelerating to investigate, may be relevant with acrylic resin character.
Claims (5)
1. a Cefaclor Capsules, is characterized in that: mixed with pharmaceutically acceptable auxiliary material by Cefaclor inclusion compound andBecome, described Cefaclor inclusion compound is prepared from as follows: polyvinyl alcohol-polyethyleneglycol-graft copolymer is dissolved in to secondIn alcohol, add Cefaclor, in stirring, drying under reduced pressure, except ethanol, to obtain final product, and wherein Cefaclor and polyvinyl alcohol-polyethylene glycol connectGraft copolymer weight ratio is 1:1-6, and described polyvinyl alcohol-polyethyleneglycol-graft copolymer is by polyvinyl alcohol and polyethylene glycolThe graft copolymer of preparing by the weight ratio of 3:1.
2. Cefaclor Capsules according to claim 1, is characterized in that: Cefaclor and polyvinyl alcohol-polyethylene glycolGraft copolymer weight ratio is 1:2-4.
3. Cefaclor Capsules according to claim 1, is characterized in that: described pharmaceutically acceptable auxiliary material comprises to be filled outFill agent.
4. Cefaclor Capsules according to claim 3, is characterized in that: described filler is selected from sucrose, lactose, sweetOne or more in dew alcohol, pregelatinized starch, starch, maltose, dextrin and xylitol.
5. a preparation method for Cefaclor Capsules according to claim 1, it is characterized in that comprising the steps: byPolyvinyl alcohol-polyethyleneglycol-graft copolymer is dissolved in ethanol, adds Cefaclor, and in stirring, drying under reduced pressure, except ethanol, obtains headSpore clo inclusion compound; By described Cefaclor inclusion compound and pharmaceutically acceptable auxiliary materials and mixing, obtain Cefaclor Capsules, described inPolyvinyl alcohol-polyethyleneglycol-graft copolymer be grafting that polyvinyl alcohol and polyethylene glycol are prepared by the weight ratio of 3:1 altogetherPolymers, described pharmaceutically acceptable auxiliary material comprises filler; Described filler is selected from sucrose, lactose, sweet mellow wine, pregelatinatedOne or more in starch, starch, maltose, dextrin and xylitol.
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN104173318A (en) * | 2014-08-29 | 2014-12-03 | 四川制药制剂有限公司 | Preparation method of cefaclor capsule |
| CN104161740A (en) * | 2014-08-29 | 2014-11-26 | 四川制药制剂有限公司 | Cefaclor capsule composition |
| CN107095856A (en) * | 2017-04-26 | 2017-08-29 | 四川制药制剂有限公司 | Cefaclor Capsules production technology |
| CN108743547B (en) * | 2018-06-28 | 2021-04-13 | 苏州盛达药业有限公司 | Cefaclor granules and preparation method thereof |
| CN112137984B (en) * | 2020-10-30 | 2023-02-03 | 四川制药制剂有限公司 | Cefaclor capsule and preparation process thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101460148A (en) * | 2006-04-10 | 2009-06-17 | 鲁汶天主教大学研究开发部 | Solid dispersion of poorly soluble drugs in graft copolymers |
| CN102793687A (en) * | 2012-08-24 | 2012-11-28 | 哈药集团制药总厂 | Cefaclor capsule and preparation method thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101460148A (en) * | 2006-04-10 | 2009-06-17 | 鲁汶天主教大学研究开发部 | Solid dispersion of poorly soluble drugs in graft copolymers |
| CN102793687A (en) * | 2012-08-24 | 2012-11-28 | 哈药集团制药总厂 | Cefaclor capsule and preparation method thereof |
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Effective date of registration: 20160427 Address after: Friendship road 311800 Zhejiang city of Zhuji province Tao Street No. 31 Applicant after: Zhejiang Yadong Pharmaceutical Co., Ltd., Huiyingbi Group Address before: Lishui Economic Development Zone, Nanjing City, Jiangsu province 211200 zhe Ning Road No. 369 Applicant before: Nanjing Zhengliang Medical Technology Co.,Ltd. |
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Effective date of registration: 20170527 Address after: Friendship road 311800 Zhejiang city of Zhuji province Tao Street No. 33 Patentee after: Echo Qi group Zhejiang Qi Qi Pharmaceutical Co., Ltd. Address before: Friendship road 311800 Zhejiang city of Zhuji province Tao Street No. 31 Patentee before: Zhejiang Yadong Pharmaceutical Co., Ltd., Huiyingbi Group |