CN1236814C - Faropenem pharmaceutical composition containing glutathione - Google Patents
Faropenem pharmaceutical composition containing glutathione Download PDFInfo
- Publication number
- CN1236814C CN1236814C CN 200410077880 CN200410077880A CN1236814C CN 1236814 C CN1236814 C CN 1236814C CN 200410077880 CN200410077880 CN 200410077880 CN 200410077880 A CN200410077880 A CN 200410077880A CN 1236814 C CN1236814 C CN 1236814C
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- Prior art keywords
- faropenem
- glutathion
- sodium
- hydrate
- compositions
- 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.)
- Expired - Lifetime
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- 229960000379 faropenem Drugs 0.000 title claims abstract description 61
- RWSXRVCMGQZWBV-WDSKDSINSA-N glutathione Chemical compound OC(=O)[C@@H](N)CCC(=O)N[C@@H](CS)C(=O)NCC(O)=O RWSXRVCMGQZWBV-WDSKDSINSA-N 0.000 title claims abstract description 47
- 229960003180 glutathione Drugs 0.000 title claims abstract description 44
- HGGAKXAHAYOLDJ-FHZUQPTBSA-N 6alpha-[(R)-1-hydroxyethyl]-2-[(R)-tetrahydrofuran-2-yl]pen-2-em-3-carboxylic acid Chemical compound S([C@@H]1[C@H](C(N1C=1C(O)=O)=O)[C@H](O)C)C=1[C@H]1CCCO1 HGGAKXAHAYOLDJ-FHZUQPTBSA-N 0.000 title claims abstract description 27
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 9
- 108010024636 Glutathione Proteins 0.000 title abstract 3
- 239000000203 mixture Substances 0.000 claims abstract description 29
- 150000003839 salts Chemical class 0.000 claims abstract description 16
- 235000003969 glutathione Nutrition 0.000 claims description 41
- MOGICMVNWAUWMK-HIXRZVNASA-L disodium;(5r,6s)-6-[(1r)-1-hydroxyethyl]-7-oxo-3-[(2r)-oxolan-2-yl]-4-thia-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate;pentahydrate Chemical compound O.O.O.O.O.[Na+].[Na+].S([C@@H]1[C@H](C(N1C=1C([O-])=O)=O)[C@H](O)C)C=1[C@H]1CCCO1.S([C@@H]1[C@H](C(N1C=1C([O-])=O)=O)[C@H](O)C)C=1[C@H]1CCCO1 MOGICMVNWAUWMK-HIXRZVNASA-L 0.000 claims description 34
- 239000008187 granular material Substances 0.000 claims description 27
- 238000002360 preparation method Methods 0.000 claims description 18
- 239000003814 drug Substances 0.000 claims description 17
- 239000000843 powder Substances 0.000 claims description 14
- 239000003826 tablet Substances 0.000 claims description 13
- 239000002775 capsule Substances 0.000 claims description 12
- 239000003795 chemical substances by application Substances 0.000 claims description 11
- 238000002347 injection Methods 0.000 claims description 9
- 239000007924 injection Substances 0.000 claims description 9
- 239000003708 ampul Substances 0.000 claims description 4
- 150000004677 hydrates Chemical class 0.000 claims description 3
- 238000000034 method Methods 0.000 claims description 3
- 230000035479 physiological effects, processes and functions Effects 0.000 claims description 2
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 14
- 239000011734 sodium Substances 0.000 description 14
- 229910052708 sodium Inorganic materials 0.000 description 14
- 229920002472 Starch Polymers 0.000 description 13
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 description 13
- 229940079593 drug Drugs 0.000 description 13
- 239000008107 starch Substances 0.000 description 13
- 235000019698 starch Nutrition 0.000 description 13
- 239000000243 solution Substances 0.000 description 9
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 8
- 230000001476 alcoholic effect Effects 0.000 description 6
- 238000001035 drying Methods 0.000 description 6
- 238000005516 engineering process Methods 0.000 description 6
- 238000012856 packing Methods 0.000 description 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 5
- 239000000126 substance Substances 0.000 description 5
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 4
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 4
- 229920001353 Dextrin Polymers 0.000 description 4
- 239000004375 Dextrin Substances 0.000 description 4
- 229920000881 Modified starch Polymers 0.000 description 4
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 4
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 4
- 229930006000 Sucrose Natural products 0.000 description 4
- 239000003963 antioxidant agent Substances 0.000 description 4
- 230000003078 antioxidant effect Effects 0.000 description 4
- 235000006708 antioxidants Nutrition 0.000 description 4
- 230000003115 biocidal effect Effects 0.000 description 4
- 235000019425 dextrin Nutrition 0.000 description 4
- 239000002552 dosage form Substances 0.000 description 4
- 238000011156 evaluation Methods 0.000 description 4
- 238000007689 inspection Methods 0.000 description 4
- 235000019359 magnesium stearate Nutrition 0.000 description 4
- 239000000741 silica gel Substances 0.000 description 4
- 229910002027 silica gel Inorganic materials 0.000 description 4
- 229960002920 sorbitol Drugs 0.000 description 4
- 239000005720 sucrose Substances 0.000 description 4
- 238000005303 weighing Methods 0.000 description 4
- 241000894006 Bacteria Species 0.000 description 3
- 206010013786 Dry skin Diseases 0.000 description 3
- 239000000853 adhesive Substances 0.000 description 3
- 230000001070 adhesive effect Effects 0.000 description 3
- 239000002671 adjuvant Substances 0.000 description 3
- 238000004090 dissolution Methods 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 238000011160 research Methods 0.000 description 3
- 206010059866 Drug resistance Diseases 0.000 description 2
- 241000192125 Firmicutes Species 0.000 description 2
- 229930182555 Penicillin Natural products 0.000 description 2
- JGSARLDLIJGVTE-MBNYWOFBSA-N Penicillin G Chemical compound N([C@H]1[C@H]2SC([C@@H](N2C1=O)C(O)=O)(C)C)C(=O)CC1=CC=CC=C1 JGSARLDLIJGVTE-MBNYWOFBSA-N 0.000 description 2
- 239000003242 anti bacterial agent Substances 0.000 description 2
- 230000000844 anti-bacterial effect Effects 0.000 description 2
- 229940088710 antibiotic agent Drugs 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 208000015181 infectious disease Diseases 0.000 description 2
- HHXMXAQDOUCLDN-RXMQYKEDSA-N penem Chemical compound S1C=CN2C(=O)C[C@H]21 HHXMXAQDOUCLDN-RXMQYKEDSA-N 0.000 description 2
- 229940049954 penicillin Drugs 0.000 description 2
- 239000002994 raw material Substances 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- 239000007916 tablet composition Substances 0.000 description 2
- 206010067484 Adverse reaction Diseases 0.000 description 1
- 108020004256 Beta-lactamase Proteins 0.000 description 1
- 229930186147 Cephalosporin Natural products 0.000 description 1
- 241000194033 Enterococcus Species 0.000 description 1
- 241000194032 Enterococcus faecalis Species 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 241000588724 Escherichia coli Species 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- 241000589517 Pseudomonas aeruginosa Species 0.000 description 1
- 206010057190 Respiratory tract infections Diseases 0.000 description 1
- 241000191940 Staphylococcus Species 0.000 description 1
- 241000193998 Streptococcus pneumoniae Species 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 230000006838 adverse reaction Effects 0.000 description 1
- 150000001336 alkenes Chemical class 0.000 description 1
- 208000026935 allergic disease Diseases 0.000 description 1
- 230000007815 allergy Effects 0.000 description 1
- 150000008064 anhydrides Chemical class 0.000 description 1
- 239000004599 antimicrobial Substances 0.000 description 1
- 230000001580 bacterial effect Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 239000003781 beta lactamase inhibitor Substances 0.000 description 1
- -1 beta-lactam compound Chemical class 0.000 description 1
- 102000006635 beta-lactamase Human genes 0.000 description 1
- 229940126813 beta-lactamase inhibitor Drugs 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 229940124587 cephalosporin Drugs 0.000 description 1
- 150000001780 cephalosporins Chemical class 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 238000000354 decomposition reaction Methods 0.000 description 1
- 230000007812 deficiency Effects 0.000 description 1
- 230000007850 degeneration Effects 0.000 description 1
- 239000000890 drug combination Substances 0.000 description 1
- 229940032049 enterococcus faecalis Drugs 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 210000004907 gland Anatomy 0.000 description 1
- 238000000892 gravimetry Methods 0.000 description 1
- 230000007062 hydrolysis Effects 0.000 description 1
- 238000006460 hydrolysis reaction Methods 0.000 description 1
- 239000012535 impurity Substances 0.000 description 1
- 206010022000 influenza Diseases 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 238000011068 loading method Methods 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 230000003647 oxidation Effects 0.000 description 1
- 238000007254 oxidation reaction Methods 0.000 description 1
- 150000002961 penems Chemical class 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 238000007699 photoisomerization reaction Methods 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 206010040872 skin infection Diseases 0.000 description 1
- ICSAXRANXQSPQP-VUKDEKJYSA-M sodium;(5r,6s)-6-[(1r)-1-hydroxyethyl]-7-oxo-3-[(2r)-oxolan-2-yl]-4-thia-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate Chemical compound [Na+].S([C@@H]1[C@H](C(N1C=1C([O-])=O)=O)[C@H](O)C)C=1[C@H]1CCCO1 ICSAXRANXQSPQP-VUKDEKJYSA-M 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 229940031000 streptococcus pneumoniae Drugs 0.000 description 1
- 208000019206 urinary tract infection Diseases 0.000 description 1
- 229940126085 β‑Lactamase Inhibitor Drugs 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Abstract
The invention relates to a faropenem pharmaceutical composition containing glutathione, which contains faropenem or pharmaceutically acceptable salt or hydrate thereof and glutathione or pharmaceutically acceptable salt thereof, wherein the weight ratio of the two is 25: 1-1: 1, and the composition is a stable pharmaceutical composition.
Description
Technical field
The present invention relates to a kind of stable Pharmaceutical composition, be particularly related to and contain faropenem or its pharmaceutically acceptable salt or medicinal compound of hydrate, said composition contains pharmaceutically acceptable salt of glutathion or its, and wherein both weight ratio scopes are 25: 1～1: 1.
Background technology:
Early 1940s, penicillin is applied to clinical, has drawn back antibiotic curtain.Penicillin antibiotics and cephalosporin are two maximum class antibiotic of clinical practice, but along with clinically extensive application and abuse, drug resistance constantly increases, and its range of application is restricted.Penem is the novel beta-lactam compound of a class, and is stable to dehydropeptidase of kidney, do not need and the beta-lactamase inhibitor drug combination.
Faropenem sodium is a kind of synthetic blue or green enzyme alkene class broad ectrum antibiotic, and antibacterial action is strong, but its instability is easy to hydrolysis, oxidation, photoisomerization etc.Faropenem demonstrates broad-spectrum antibacterial activity to aerobic and anaerobic gram positive bacteria, gram-negative bacteria, and particularly the activity to anaerobe such as gram positive bacterias such as drug-fast staphylococcus, enterococcus and bacteroids all is better than existing Perorally administrable antimicrobial agent; But to the activity of bacillus pyocyaneus a little less than.All very stable to various beta-lactamases, less generation drug resistance.
The faropenem oral absorption is effective, and the half-life is about 1 hour in the blood.Day dosage is 450～900mg (divides 3 times oral).General clinical research result shows that the effective percentage of treatment respiratory infections is 78.6%; The urinary tract infection effective percentage is 73.4%; The skin infection effective percentage is 88.6%; The surgical infection effective percentage is 89.0%; It is 87.5% that department of obstetrics and gynecology infect effective percentage; It is 74.1% that ear nose section infects effective percentage; It is 87.3% that ophthalmology infects effective percentage; It is 86.8% that the dentistry and the department of stomatology infect effective percentage.Clinical isolated bacterial clearance rate is respectively: golden Portugal bacterium is 79.2%; Bacterium is 92.0% in blue or green Portugal; Streptococcus pneumoniae is 78.3%; Enterococcus faecalis is 91.8%; Escherichia coli are 91.3%; Pneumobacillus is 81.5%; Hemophilus influenza is 66.7%.Adverse reaction rate is 4.9%, is slight gastrointestinal symptom and allergy symptoms.
Faropenem is the penems antibiotics of Japanese Suntory company exploitation, obtains the chemical compound patent in 1986 in Japan, and the patent No. is JP61,207387.Nineteen ninety and 1992 Japanese Yamanouchi drugmaker and U.S. Wyeth-Ayerst company obtain the clinical licence of these product respectively, carry out its clinical research jointly.And with at first got permission listing in 1997 in Japan, commodity are called Farom.
Faropenem belongs to first and is used for clinical penem antibiotic, both can be oral, again can administrated by injection, and be applicable to the patient of different gradient of infection.Its curative effect and safety have obtained fully certainly.
But the faropenem preparation causes the preparation instability owing to the reason of multiple reason, particularly chemical constitution, easy decomposition and degeneration, the content of the preparation of producing related substance (impurity) after placing 6 months is elevated to 5% at present, causes the product active constituent content to reduce, and affects the treatment.
The present invention adds glutathion through research in the preparation of faropenem, improved the stability of faropenem greatly, has prolonged effect duration.
Summary of the invention:
In order to overcome the deficiencies in the prior art part, researcher of the present invention finds that having added glutathion in the faropenem preparation of sodium increases the Faropenem sodium stability of formulation greatly.
The object of the present invention is to provide a kind of stable Pharmaceutical composition, it is characterized in that containing faropenem and glutathion.
Another object of the present invention is to provide the dosage form of the compositions that contains faropenem and glutathion, finally reach the purpose of stable pharmaceutical composition of the present invention.
The invention provides a kind of faropenem of physiology effective dose or Pharmaceutical composition of its pharmaceutically acceptable salt or its hydrate of containing, contain pharmaceutically acceptable salt of glutathion or its in the said composition.
Compositions of the present invention, wherein faropenem or its pharmaceutically acceptable salt or hydrate and glutathion weight ratio scope are 25: 1～1: 1.Preferably 25: 1～6: 1.
Compositions of the present invention, wherein said faropenem or its pharmaceutically acceptable salt or hydrate are Faropenem sodium 2.5 hydrates, and glutathion is a reduced glutathion.
Compositions of the present invention, be unit dosage form, these unit dosage forms can be pharmaceutical preparation unit dosage forms commonly used, as: the tablet of unit dose, capsule, granule or injection powder pin, for tablet, capsule or injection powder pin, unit dose refers to every, every capsules, every injection, for granule, unit dose is meant every bag granule, every bottle of granule, or every gram granule.
Compositions of the present invention, if tablet or capsule wherein in each tablet or the capsule, contain Faropenem sodium 2.5 hydrate 123.5mg, reduced glutathion 20mg, other are the medicine acceptable carrier.If granule contains Faropenem sodium 2.5 hydrate 123.5mg in every gram granule, reduced glutathion 10mg, other are the medicine acceptable carrier.If powder ampoule agent for injection in every powder ampoule agent for injection, contains Faropenem sodium 2.5 hydrate 125mg, reduced glutathion 5mg.
The present invention also provides the preparation method of the present composition, and this method comprises faropenem or its pharmaceutically acceptable salt or its hydrate and glutathion or its blended step of acceptable salt pharmaceutically.
Preparation of the present invention according to the needs of preparation, can add galenic pharmacy medicine acceptable carrier commonly used.Can be prepared into finished product preparation according to the conventional method of galenic pharmacy, and be applied to suitability for industrialized production.
Following data declaration beneficial effect of the present invention by experiment:
Evaluation contains the stability of the tablet of Faropenem sodium and glutathion
The study on the stability of faropenem sodium tablet
| Tablet formulation (mg) | Time | Appearance character | Content % | Related substance % | Dissolution % |
| Faropenem sodium 123.5, glutathion 20, pregelatinized Starch 40, carboxymethyl starch sodium 30, magnesium stearate 6, the 5%PVP95% alcoholic solution | 0 day | Faint yellow | 101.33 | 0.31 | 92.1 |
| March | Faint yellow | 98.47 | 1.62 | 91.5 | |
| June | Faint yellow | 98.44 | 2.02 | 91.2 |
Evaluation contains the capsular stability of Faropenem sodium and glutathion
The capsular study on the stability of Faropenem sodium
| Capsule prescription (mg) | Time | Appearance character | Content % | Related substance % | Dissolution % |
| Faropenem sodium 123.5, glutathion 20, carboxymethyl starch sodium 60, micropowder silica gel 6, the 5%PVP95% alcoholic solution | 0 day | Faint yellow granule | 102.50 | 0.50 | 92.4 |
| March | Faint yellow granule | 100.32 | 1.51 | 93.9 | |
| June | Faint yellow granule | 99.54 | 2.11 | 94.3 |
Evaluation contains the stability of the granule of Faropenem sodium and glutathion
The study on the stability of faropenem sodium granules
| Granule prescription (mg) | The time | Appearance character | The dry mistake | Content | Relevant thing | Dissolve |
| Between | Heavy % | ％ | Matter % | Property % | ||
| Faropenem sodium 247, glutathion 20, D-sorbitol 270, sucrose 290, carboxymethyl starch sodium 150, dextrin 20, Herba Menthae essence, 5%PVP95% alcoholic solution | 0 day | Faint yellow granule | 5.38 | 101.83 | 0.31 | 92.1 |
| March | Faint yellow granule | 5.66 | 100.28 | 1.36 | 91.4 | |
| June | Faint yellow granule | 5.44 | 99.23 | 2.27 | 91.2 |
Evaluation contains the stability of the injectable powder of Faropenem sodium and glutathion.
The study on the stability of Faropenem sodium powder pin
| Prescription (mg) | Appearance character | Content % (calculating) with anhydride | Related substance % |
| Faropenem sodium 250, glutathion 5 | White or light yellow crystalline powder | 92.48 | 0.72 |
| Faropenem sodium 250, glutathion 10 | White or light yellow crystalline powder | 93.35 | 0.52 |
| Faropenem sodium 250, glutathion 15 | White or light yellow crystalline powder | 93.38 | 0.51 |
The specific embodiment:
Following examples only limit to the present invention is done nearly step explanation, but are not any limitation of the invention.
Embodiment 1
The prescription of faropenem sodium tablet and preparation technology
Tablet formulation
Faropenem sodium 123.5g crude drug
Pregelatinized Starch 40.0g excipient
Glutathion 20.0g antioxidant
Carboxymethyl starch sodium 30.0g disintegrating agent
Magnesium stearate 6.0g lubricant
5%PVP95% alcoholic solution suitable amount of adhesive
Make 1000 altogether, every heavy 0.22g contains principal agent and counts 0.10g with faropenem.
Preparation technology
With the crude drug drying, pulverize, cross 100 mesh sieves; Adjuvants such as pregelatinized Starch, carboxymethyl starch sodium, magnesium stearate are dry respectively, pulverize, and it is standby to cross 80 mesh sieves; Accurately take by weighing crude drug, the pregelatinized Starch of recipe quantity, glutathion, the half carboxymethyl starch sodium mix homogeneously of measuring of recipe quantity, 5%PVP alcohol (95%) solution 18 mesh sieves are granulated, 40 ℃ of dryings.The magnesium stearate and the remaining carboxymethyl starch sodium that add recipe quantity, mix homogeneously is crossed 18 mesh sieve granulate, measures the granule drug content, determines that sheet is heavy, and tablet machine tabletting core is measured tablet weight variation, wraps white stomach dissolution type film-coat, atomizing pressure 1kg/cm
2, hydrojet speed 20g/min, 50 ℃ of hot blast temperatures, bag stops hydrojet to increasing weight 5%, transfers 60 ℃ of hot blast temperatures, and coating pan is rotated further 10min.Measure tablet weight variation, quality inspection, packing is promptly.
Embodiment 2
Capsular prescription of Faropenem sodium and preparation
The capsule prescription
Faropenem sodium 123.5g crude drug
Glutathion 20g antioxidant
Carboxymethyl starch sodium 60g disintegrating agent
Micropowder silica gel 6g fluidizer
5%PVP95% alcoholic solution suitable amount of adhesive
Make 1000 altogether, the tolerant heavy 0.21g of every intragranular contains principal agent and counts 0.10g with faropenem.
Preparation technology
With the crude drug drying, pulverize, cross 100 mesh sieves; Micropowder silica gel, carboxymethyl starch sodium, etc. adjuvant dry respectively, pulverize, it is standby to cross 80 mesh sieves; Accurately take by weighing the crude drug of recipe quantity, the glutathion of recipe quantity, carboxymethyl starch sodium mix homogeneously, 5%PVP ethanol (95%) solution 18 mesh sieves are granulated, 40 ℃ of dryings.The micropowder silica gel that adds recipe quantity, mix homogeneously is crossed 18 mesh sieve granulate, measures the granule drug content, determines that content is heavy, the capsule of packing into No. 2, it is different to measure the capsule method of double differences.Quality inspection, packing promptly.
Embodiment 3
The prescription of faropenem sodium granules and preparation
The granule prescription
Faropenem sodium 247g crude drug
D-sorbitol 270g correctives
Sucrose 290g correctives
Glutathion 20g antioxidant
Carboxymethyl starch sodium 150g disintegrating agent
Dextrin 20g binding agent
An amount of correctives of Herba Menthae essence
5%PVP95% alcoholic solution suitable amount of adhesive
Make 1000 bags altogether, every bag heavy 1.0g contains principal agent in faropenem 0.20g.
Preparation technology
With the crude drug drying, pulverize, it is standby to cross 100 mesh sieves; Adjuvants such as D-sorbitol, carboxymethyl starch sodium, sucrose, dextrin are dry respectively, pulverize, and it is standby to cross 80 mesh sieves; Accurately take by weighing the crude drug of recipe quantity, the D-sorbitol of recipe quantity, glutathion, carboxymethyl starch sodium, sucrose, dextrin mix homogeneously spray into 5%PVP ethanol (95%) solution that contains Herba Menthae essence, and 18 mesh sieves are granulated, 40 ℃ of dryings.Cross 18 order granulate, measure the granule drug content, determine loading amount, the dress sample, gravimetry difference, quality inspection, packing is promptly.
Embodiment 4
The prescription and the preparation of Faropenem sodium powder pin
Powder pin prescription
Faropenem sodium 125g crude drug
Glutathion 5g antioxidant
Make 1000 bottles altogether, every bottle contains principal agent and counts 0.10g with faropenem.
Preparation technology
Under aseptic condition, accurately take by weighing the aseptic raw material 125g of Faropenem sodium, the aseptic raw material 5g of glutathion, mix homogeneously is checked uniformity of dosage units, packing, gland, quality inspection, packing is promptly.
Claims (9)
1. one kind contains the faropenem of physiology effective dose or the Pharmaceutical composition of its pharmaceutically acceptable salt or its hydrate, it is characterized in that, contains pharmaceutically acceptable salt of glutathion or its in the said composition.
2. the compositions of claim 1 is characterized in that, faropenem or its pharmaceutically acceptable salt or hydrate and glutathion weight ratio scope are 25: 1～6: 1.
3. the compositions of claim 1 is characterized in that, described faropenem or its pharmaceutically acceptable salt or hydrate are Faropenem sodium 2.5 hydrates, and glutathion is a reduced glutathion.
4. the compositions of claim 3 is characterized in that, the weight ratio of Faropenem sodium 2.5 hydrates and reduced glutathion is 25: 1～6: 1.
5. the compositions of claim 1 is characterized in that, said composition is tablet, capsule, granule or injection powder pin.
6. the compositions of claim 5 is characterized in that, said composition is tablet or capsule, wherein in the tablet or capsule of unit dose, contains Faropenem sodium 2.5 hydrate 123.5mg, reduced glutathion 20mg, and other are the medicine acceptable carrier.
7. the compositions of claim 5 is characterized in that, said composition is a granule, wherein contains Faropenem sodium 2.5 hydrate 123.5mg in the granule of unit dose, reduced glutathion 10mg.
8. the compositions of claim 5 is characterized in that, said composition is a powder ampoule agent for injection, wherein in the unit dose powder ampoule agent for injection, contains Faropenem sodium 2.5 hydrate 125mg, reduced glutathion 5mg.
9. the preparation of compositions method of claim 1 is characterized in that, comprises faropenem or its pharmaceutically acceptable salt or its hydrate and glutathion or its blended step of acceptable salt pharmaceutically.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410077880 CN1236814C (en) | 2004-09-16 | 2004-09-16 | Faropenem pharmaceutical composition containing glutathione |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410077880 CN1236814C (en) | 2004-09-16 | 2004-09-16 | Faropenem pharmaceutical composition containing glutathione |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1616080A CN1616080A (en) | 2005-05-18 |
| CN1236814C true CN1236814C (en) | 2006-01-18 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200410077880 Expired - Lifetime CN1236814C (en) | 2004-09-16 | 2004-09-16 | Faropenem pharmaceutical composition containing glutathione |
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| Country | Link |
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| CN (1) | CN1236814C (en) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101756924B (en) * | 2008-12-24 | 2011-04-13 | 鲁南制药集团股份有限公司 | Sustained-release tablets of faropenem sodium |
| CN101904822B (en) * | 2009-06-04 | 2011-11-09 | 鲁南制药集团股份有限公司 | Faropenem sodium freeze-drying powder and preparation method thereof |
| CN101744782B (en) * | 2010-01-24 | 2012-03-21 | 鲁南贝特制药有限公司 | Tablet containing faropenem sodium |
-
2004
- 2004-09-16 CN CN 200410077880 patent/CN1236814C/en not_active Expired - Lifetime
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| Publication number | Publication date |
|---|---|
| CN1616080A (en) | 2005-05-18 |
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Owner name: SHANDONG XINSHIDAI PHARMACEUTICAL INDUSTRY CO., LT Free format text: FORMER OWNER: ZHONGHAI BIO-TECHNOLOGY DEVELOPMENT CO., LTD., SHENYANG CITY Effective date: 20131023 |
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Effective date of registration: 20131023 Address after: 273400 Shandong province Feixian County North Ring Road No. 1 Patentee after: SHANDONG NEW TIME PHARMACEUTICAL Co.,Ltd. Address before: South Street in Dongling District of Shenyang city in Liaoning province 110016 129 Lane 28 Building No. 2 Patentee before: J&HEALTH BIOTECHNOLOGY CO.,LTD. |
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