CN111166718A - Ornidazole injection and preparation process thereof - Google Patents
Ornidazole injection and preparation process thereof Download PDFInfo
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- CN111166718A CN111166718A CN201911161579.9A CN201911161579A CN111166718A CN 111166718 A CN111166718 A CN 111166718A CN 201911161579 A CN201911161579 A CN 201911161579A CN 111166718 A CN111166718 A CN 111166718A
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- ornidazole
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- acetic acid
- sodium acetate
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- IPWKIXLWTCNBKN-UHFFFAOYSA-N Madelen Chemical compound CC1=NC=C([N+]([O-])=O)N1CC(O)CCl IPWKIXLWTCNBKN-UHFFFAOYSA-N 0.000 title claims abstract description 58
- 229960002313 ornidazole Drugs 0.000 title claims abstract description 58
- 238000002347 injection Methods 0.000 title claims abstract description 44
- 239000007924 injection Substances 0.000 title claims abstract description 44
- 238000002360 preparation method Methods 0.000 title claims abstract description 19
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims abstract description 57
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims abstract description 27
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 23
- QIJRTFXNRTXDIP-UHFFFAOYSA-N (1-carboxy-2-sulfanylethyl)azanium;chloride;hydrate Chemical compound O.Cl.SCC(N)C(O)=O QIJRTFXNRTXDIP-UHFFFAOYSA-N 0.000 claims abstract description 19
- 229960001305 cysteine hydrochloride Drugs 0.000 claims abstract description 19
- 239000007974 sodium acetate buffer Substances 0.000 claims abstract description 18
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims abstract description 16
- 230000001954 sterilising effect Effects 0.000 claims abstract description 16
- 239000008215 water for injection Substances 0.000 claims abstract description 14
- 238000003756 stirring Methods 0.000 claims abstract description 12
- 239000003708 ampul Substances 0.000 claims abstract description 8
- 238000001914 filtration Methods 0.000 claims abstract description 8
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract description 8
- 238000007789 sealing Methods 0.000 claims abstract description 8
- VMHLLURERBWHNL-UHFFFAOYSA-M Sodium acetate Chemical compound [Na+].CC([O-])=O VMHLLURERBWHNL-UHFFFAOYSA-M 0.000 claims abstract description 6
- 239000001632 sodium acetate Substances 0.000 claims abstract description 6
- 235000017281 sodium acetate Nutrition 0.000 claims abstract description 6
- BHZOKUMUHVTPBX-UHFFFAOYSA-M sodium acetic acid acetate Chemical compound [Na+].CC(O)=O.CC([O-])=O BHZOKUMUHVTPBX-UHFFFAOYSA-M 0.000 claims description 16
- 238000004519 manufacturing process Methods 0.000 claims description 4
- 239000000243 solution Substances 0.000 abstract description 18
- 206010067484 Adverse reaction Diseases 0.000 abstract description 4
- 230000006838 adverse reaction Effects 0.000 abstract description 4
- 238000000034 method Methods 0.000 abstract description 4
- 239000000872 buffer Substances 0.000 abstract description 3
- 208000015181 infectious disease Diseases 0.000 description 8
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 7
- 239000007788 liquid Substances 0.000 description 5
- 241000606125 Bacteroides Species 0.000 description 3
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 3
- 230000000052 comparative effect Effects 0.000 description 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 241000192001 Pediococcus Species 0.000 description 2
- 230000007547 defect Effects 0.000 description 2
- 239000008103 glucose Substances 0.000 description 2
- YZEUHQHUFTYLPH-UHFFFAOYSA-N 2-nitroimidazole Chemical compound [O-][N+](=O)C1=NC=CN1 YZEUHQHUFTYLPH-UHFFFAOYSA-N 0.000 description 1
- 206010060921 Abdominal abscess Diseases 0.000 description 1
- 206010056519 Abdominal infection Diseases 0.000 description 1
- 208000004881 Amebiasis Diseases 0.000 description 1
- 208000008710 Amebic Dysentery Diseases 0.000 description 1
- 208000006503 Amebic Liver Abscess Diseases 0.000 description 1
- 206010001980 Amoebiasis Diseases 0.000 description 1
- 206010001986 Amoebic dysentery Diseases 0.000 description 1
- 208000031729 Bacteremia Diseases 0.000 description 1
- 241000606124 Bacteroides fragilis Species 0.000 description 1
- 241001135228 Bacteroides ovatus Species 0.000 description 1
- 241000606123 Bacteroides thetaiotaomicron Species 0.000 description 1
- 241000606215 Bacteroides vulgatus Species 0.000 description 1
- 208000004020 Brain Abscess Diseases 0.000 description 1
- 206010007882 Cellulitis Diseases 0.000 description 1
- 241000193403 Clostridium Species 0.000 description 1
- 208000035473 Communicable disease Diseases 0.000 description 1
- 206010011985 Decubitus ulcer Diseases 0.000 description 1
- 208000004145 Endometritis Diseases 0.000 description 1
- 241000186394 Eubacterium Species 0.000 description 1
- 241000605909 Fusobacterium Species 0.000 description 1
- 201000000628 Gas Gangrene Diseases 0.000 description 1
- 241000606790 Haemophilus Species 0.000 description 1
- 241000590002 Helicobacter pylori Species 0.000 description 1
- 206010063741 Hepatic amoebiasis Diseases 0.000 description 1
- 206010024652 Liver abscess Diseases 0.000 description 1
- 241000544912 Melanoides Species 0.000 description 1
- 201000009906 Meningitis Diseases 0.000 description 1
- 206010051458 Myometritis Diseases 0.000 description 1
- 206010048685 Oral infection Diseases 0.000 description 1
- 206010033119 Ovarian abscess Diseases 0.000 description 1
- 206010058674 Pelvic Infection Diseases 0.000 description 1
- 208000009019 Pericoronitis Diseases 0.000 description 1
- 206010057249 Phagocytosis Diseases 0.000 description 1
- 208000004210 Pressure Ulcer Diseases 0.000 description 1
- 208000010362 Protozoan Infections Diseases 0.000 description 1
- 206010040047 Sepsis Diseases 0.000 description 1
- 206010062255 Soft tissue infection Diseases 0.000 description 1
- 241001502500 Trichomonadida Species 0.000 description 1
- 208000025865 Ulcer Diseases 0.000 description 1
- 206010046914 Vaginal infection Diseases 0.000 description 1
- 201000008100 Vaginitis Diseases 0.000 description 1
- 206010048038 Wound infection Diseases 0.000 description 1
- 206010000269 abscess Diseases 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 229940024606 amino acid Drugs 0.000 description 1
- 235000001014 amino acid Nutrition 0.000 description 1
- 150000001413 amino acids Chemical group 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 229940088710 antibiotic agent Drugs 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 239000006184 cosolvent Substances 0.000 description 1
- 210000002249 digestive system Anatomy 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 235000019441 ethanol Nutrition 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 208000007565 gingivitis Diseases 0.000 description 1
- 229940037467 helicobacter pylori Drugs 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 238000010253 intravenous injection Methods 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 231100000252 nontoxic Toxicity 0.000 description 1
- 230000003000 nontoxic effect Effects 0.000 description 1
- 208000004480 periapical periodontitis Diseases 0.000 description 1
- 201000001245 periodontitis Diseases 0.000 description 1
- 206010034674 peritonitis Diseases 0.000 description 1
- 230000008782 phagocytosis Effects 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 208000001297 phlebitis Diseases 0.000 description 1
- 208000013223 septicemia Diseases 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 241001148471 unidentified anaerobic bacterium Species 0.000 description 1
- 241001515965 unidentified phage Species 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
- A61K47/183—Amino acids, e.g. glycine, EDTA or aspartame
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Dermatology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses an ornidazole injection and a preparation process thereof, wherein the ornidazole injection comprises the following components in parts by weight: 500-1000 g of ornidazole, 1-10 g of cysteine hydrochloride, 500-1000 g of propylene glycol, a proper amount of acetic acid and 3000-6000 ml of water for injection; the preparation process comprises the following steps: adding cysteine hydrochloride, propylene glycol and water for injection into a preparation tank; adding proper amount of acetic acid/sodium acetate; adding ornidazole, stirring and dissolving; sterilizing and filtering to 0.22 μm, sealing ampoule by nitrogen, and sterilizing at 121 deg.C for 15 min. The ornidazole injection adopts cysteine hydrochloride and propylene glycol, so that the solubility of ornidazole in water is improved; through the acetic acid/sodium acetate buffer pair, the adverse reaction caused by the fact that a single pH value regulator is used in the traditional method to enable the pH value of the solution to be too low is avoided, and the stability of the solution under the lower pH value through the use of the buffer pair can be guaranteed.
Description
Technical Field
The invention relates to the technical field of medicinal preparations, in particular to an ornidazole injection and a preparation process thereof.
Background
The ornidazole injection is the third generation nitroimidazole antibiotics, which are used for anaerobic bacteria infection, protozoan infection, trichomonad infection and the like. The ornidazole injection is also suitable for:
1. used for treating diseases caused by Bacteroides fragilis, Bacteroides dirichi, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus, Clostridium, Eubacterium, Pediococcus and Pediococcus, helicobacter pylori, Bacteroides melanoides, Fusobacterium, CO2The infectious diseases caused by sensitive anaerobes such as the bacteriophage phagocytosis and the gingival bacteroides comprise: (1) abdominal infection: peritonitis, intra-abdominal abscess, liver abscess, etc.; (2) pelvic infection: endometritis, myometritis, salpingo-ovarian abscess, pelvic cavity soft tissue infection, Haemophilus vaginitis, etc.; (3) oral infection: periodontitis, periapical periodontitis, pericoronitis, acute ulcerative gingivitis, and the like; (4) surgical infection: wound infection, epidermal abscess, decubitus ulcer infection, cellulitis, gas gangrene, etc.; (5) brain infection: meningitis, brain abscesses; (6) and severe anaerobic infection such as septicemia and bacteremia.
2. Can be used for preventing infection before operation and treating anaerobic infection after operation.
3. Can be used for treating severe amebiasis of digestive system, such as amebic dysentery, amebic liver abscess, etc.
The ornidazole injection is a main dosage form of ornidazole drugs, and is widely applied clinically, but the existing ornidazole injection still has the following problems:
(1) ornidazole is easy to dissolve in ethanol and slightly soluble in water; the solubility is increased under an acidic condition, the dissolution condition is greatly improved when the acidity of the solution reaches below 3.0, but the pH value of the solution prepared by clinically using the low-pH-value solution and a glucose solution is still lower, so that the adverse reaction is large when the solution is administrated by intravenous drip, and phlebitis is generated;
(2) there are also documents or patents which prepare the ornidazole injection by adding absolute ethyl alcohol in a prescription, but the absolute ethyl alcohol has great production safety problem, needs an explosion-proof workshop and has high requirement on production environment; and in the production process, the absolute ethyl alcohol is very easy to volatilize, so that the content is not uniform.
Disclosure of Invention
The invention aims to provide an ornidazole injection and a preparation process thereof aiming at the defects and the defects of the prior art, which not only avoids the adverse reaction caused by the fact that the pH value of the solution is too low by using a single pH value regulator in the traditional method, but also can ensure the stability of the solution at a lower pH value by using a buffer pair.
In order to solve the problems in the prior art, the invention adopts the following technical scheme: an ornidazole injection is prepared from the following components in parts by weight: 500-1000 g of ornidazole, 1-10 g of cysteine hydrochloride, 500-1000 g of propylene glycol, 3000-6000 ml of water for injection and acetic acid-sodium acetate buffer; wherein the dosage of the acetic acid-sodium acetate buffer pair ensures that the pH value of the ornidazole injection is 4.8-5.2.
In one embodiment, the invention provides an ornidazole injection, which is prepared from the following components in percentage by weight: 500mg of ornidazole, 1mg of cysteine hydrochloride, 500mg of propylene glycol, 3ml of acetic acid-sodium acetate buffer pair and injection water; wherein the dosage of the acetic acid-sodium acetate buffer pair ensures that the pH value of the ornidazole injection is 4.8-5.2.
In one embodiment, the invention provides an ornidazole injection, which is prepared from the following components in percentage by weight: 500mg of ornidazole, 5mg of cysteine hydrochloride, 1000mg of propylene glycol, acetic acid-sodium acetate buffer pair and 3ml of water for injection; wherein the dosage of the acetic acid-sodium acetate buffer pair ensures that the pH value of the ornidazole injection is 4.8-5.2.
In one embodiment, the invention provides an ornidazole injection, which is prepared from the following components in percentage by weight: 1000mg of ornidazole, 10mg of cysteine hydrochloride, 1000mg of propylene glycol, 6ml of acetic acid-sodium acetate buffer pair and injection water; wherein the dosage of the acetic acid-sodium acetate buffer pair ensures that the pH value of the ornidazole injection is 4.8-5.2.
The invention also provides a preparation process of the ornidazole injection, which comprises the following steps:
(1) adding cysteine hydrochloride, propylene glycol and 60-80% of water for injection in a formula amount into a preparation tank;
(2) adding proper amount of acetic acid and proper amount of sodium acetate;
(3) adding ornidazole, stirring and dissolving;
(4) sterilizing and filtering to 0.22 μm, sealing the ampoule by filling nitrogen, and sterilizing at 121 deg.C for 15 min.
After the technical scheme is adopted, the invention has the following beneficial effects:
the stabilizer cysteine hydrochloride is added in the prescription, the cysteine hydrochloride is a common auxiliary material of the injection, and the cysteine hydrochloride is amino acid normally existing in a human body and is completely nontoxic as a pharmaceutic adjuvant; in addition, the propylene glycol is used as a solubilizer and a cosolvent in the formula, so that the solubility of the ornidazole in water is further improved, and the pH value of the solution is stabilized to about 5.0 through an acetic acid/sodium acetate buffer pair, thereby not only avoiding the adverse reaction caused by the over-low pH value of the solution due to the use of a single pH value regulator in the traditional method, but also ensuring the stability of the solution at a lower pH value through the use of the buffer pair.
Detailed Description
In order to make the objects, technical solutions and advantages of the present invention more apparent, the present invention is described in further detail below with reference to specific embodiments. It should be understood that the detailed description and specific examples, while indicating the invention, are intended for purposes of illustration only and are not intended to limit the scope of the invention.
Example 1: an ornidazole injection, its prescription is
The preparation process comprises the following steps:
(1) firstly, adding 60 percent of water according to the prescription amount;
(2) sequentially adding cysteine hydrochloride, propylene glycol and acetic acid/sodium acetate according to the prescription amount, and stirring for dissolving;
(3) then adding ornidazole, stirring and dissolving to make the pH value of the solution be 4.8,
(4) and adding water for injection to the total amount.
(5) Sterilizing and filtering with 0.22 μm, sealing ampoule with nitrogen, and sterilizing at 121 deg.C for 15 min.
Example 2: an ornidazole injection, its prescription is
The preparation process comprises the following steps:
(1) firstly, adding water with the amount of 80 percent of the prescription amount,
(2) sequentially adding cysteine hydrochloride, propylene glycol and acetic acid/sodium acetate according to the prescription amount, stirring and dissolving,
(3) then adding ornidazole, stirring and dissolving to make the pH value of the solution be 5.0,
(4) and adding water for injection to the total amount.
(5) Sterilizing and filtering with 0.22 μm, sealing ampoule with nitrogen, and sterilizing at 121 deg.C for 20 min.
Example 3: an ornidazole injection, its prescription is
The preparation process comprises the following steps:
(1) firstly, adding water with the amount of 80 percent of the prescription amount,
(2) sequentially adding cysteine hydrochloride, propylene glycol and acetic acid/sodium acetate according to the prescription amount, stirring and dissolving,
(3) then adding ornidazole, stirring and dissolving to make the pH value of the solution be 5.0,
(4) and adding water for injection to the total amount.
(5) Sterilizing and filtering with 0.22 μm, sealing ampoule with nitrogen, and sterilizing at 121 deg.C for 20 min.
Comparative example 1: an ornidazole injection, its prescription is
The preparation process comprises the following steps:
(1) firstly, adding 60 percent of water according to the prescription amount,
(2) adding the propylene glycol with the prescription amount, stirring and dissolving,
(3) then hydrochloric acid is used for adjusting the pH value to 2.5, ornidazole is added, stirring and dissolving are carried out,
(4) and adding water for injection to the total amount.
(5) Sterilizing and filtering with 0.22 μm, sealing ampoule with nitrogen, and sterilizing at 121 deg.C for 20 min.
Comparative example 2: an ornidazole injection, its prescription is
The preparation process comprises the following steps:
(1) adding the prescribed amount of propylene glycol and ornidazole into a liquid preparation tank, stirring and dissolving,
(2) and then adding absolute ethyl alcohol to full dose.
(3) Sterilizing and filtering with 0.22 μm, sealing ampoule with nitrogen, and sterilizing at 121 deg.C for 20 min.
The ornidazole injection prepared by the embodiment has a pH value of about 5.0 after being matched with a 5% glucose solution, meets the requirement of an intravenous injection administration route on the pH value of the solution, and the test comparison result is shown in the following table 1; the ornidazole injection prepared by the prescription process has simple and safe preparation process and stable product content, and the test comparison results are shown in the following table 2.
Table 1 results of compatibility with 5% dextrose solution
| Traits | pH value | Comprehensive evaluation | |
| Example 1 | Pale yellow clear liquid | 5.0 | Meets the requirement of the pH value range of the injection |
| Example 2 | Pale yellow clear liquid | 5.0 | Meets the requirement of the pH value range of the injection |
| Example 3 | Pale yellow clear liquid | 4.9 | Meets the requirement of the pH value range of the injection |
| Comparative example 1 | Yellow clear liquid | 3.6 | Out of the pH range of the injection |
TABLE 2 quality comparison
Through the research of the preparation of a plurality of batches of samples, the quality condition is as follows
It will be evident to those skilled in the art that the invention is not limited to the details of the foregoing illustrative embodiments, and that the present invention may be embodied in other specific forms without departing from the spirit or essential attributes thereof. The present embodiments are therefore to be considered in all respects as illustrative and not restrictive, the scope of the invention being indicated by the appended claims rather than by the foregoing description, and all changes which come within the meaning and range of equivalency of the claims are therefore intended to be embraced therein.
Furthermore, it should be understood that although the present description refers to embodiments, not every embodiment may contain only a single embodiment, and such description is for clarity only, and those skilled in the art should integrate the description, and the embodiments may be combined as appropriate to form other embodiments understood by those skilled in the art.
Claims (5)
1. The ornidazole injection is characterized by being prepared from the following components in parts by weight: 500-1000 g of ornidazole, 1-10 g of cysteine hydrochloride, 500-1000 g of propylene glycol, 3000-6000 ml of water for injection and acetic acid-sodium acetate buffer; wherein the dosage of the acetic acid-sodium acetate buffer pair ensures that the pH value of the ornidazole injection is 4.8-5.2.
2. The ornidazole injection as claimed in claim 1, characterised in that it is made up of the following components: 500mg of ornidazole, 1mg of cysteine hydrochloride, 500mg of propylene glycol, acetic acid-sodium acetate buffer pair and 3ml of water for injection; wherein the dosage of the acetic acid-sodium acetate buffer pair ensures that the pH value of the ornidazole injection is 4.8-5.2.
3. The ornidazole injection as claimed in claim 1, characterised in that it is made up of the following components: 500mg of ornidazole, 5mg of cysteine hydrochloride, 1000mg of propylene glycol, acetic acid-sodium acetate buffer pair and 3ml of water for injection; wherein the dosage of the acetic acid-sodium acetate buffer pair ensures that the pH value of the ornidazole injection is 4.8-5.2.
4. The ornidazole injection as claimed in claim 1, characterised in that it is made up of the following components: 1000mg of ornidazole, 10mg of cysteine hydrochloride, 1000mg of propylene glycol, acetic acid-sodium acetate buffer pair and 6ml of water for injection; wherein the dosage of the acetic acid-sodium acetate buffer pair ensures that the pH value of the ornidazole injection is 4.8-5.2.
5. The process for preparing ornidazole injection as claimed in claim 1, characterised in that it comprises the following steps:
(1) adding cysteine hydrochloride, propylene glycol and 60-80% of water for injection in a formula amount into a preparation tank;
(2) adding proper amount of acetic acid and proper amount of sodium acetate;
(3) adding ornidazole, stirring and dissolving;
(4) sterilizing and filtering to 0.22 μm, sealing the ampoule by filling nitrogen, and sterilizing at 121 deg.C for 15 min.
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Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006071912A2 (en) * | 2004-12-27 | 2006-07-06 | Johnson & Johnson Consumer Companies, Inc. | A method for treating or preventing pruritic and neurogenic skin disorders by applying sertaconazole |
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| WO2006071912A2 (en) * | 2004-12-27 | 2006-07-06 | Johnson & Johnson Consumer Companies, Inc. | A method for treating or preventing pruritic and neurogenic skin disorders by applying sertaconazole |
| CN102335126A (en) * | 2010-07-22 | 2012-02-01 | 山东方明药业股份有限公司 | Ornidazole injection and its preparation method |
| CN102552127A (en) * | 2012-01-31 | 2012-07-11 | 石家庄开发区博欣医药科技开发有限公司 | Ornidazole injection |
| CN103040740A (en) * | 2013-01-25 | 2013-04-17 | 山西普德药业股份有限公司 | Ornidazole injection and preparation technology thereof |
| CN104983678A (en) * | 2015-08-04 | 2015-10-21 | 山东齐都药业有限公司 | Ornidazole infusion preparation and preparation technology thereof |
| CN107041868A (en) * | 2016-02-05 | 2017-08-15 | 南京卡文迪许生物工程技术有限公司 | A kind of stable ornidazole injection and S-ornidazole injection and preparation method thereof |
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