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CN109077999A - A kind of long-acting slow-release Tilmicosin injection and preparation method thereof - Google Patents

A kind of long-acting slow-release Tilmicosin injection and preparation method thereof Download PDF

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Publication number
CN109077999A
CN109077999A CN201811012891.7A CN201811012891A CN109077999A CN 109077999 A CN109077999 A CN 109077999A CN 201811012891 A CN201811012891 A CN 201811012891A CN 109077999 A CN109077999 A CN 109077999A
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Prior art keywords
injection
tilmicosin
oil
long
organic solvent
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Pending
Application number
CN201811012891.7A
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Chinese (zh)
Inventor
田红卫
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Individual
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Priority to CN201811012891.7A priority Critical patent/CN109077999A/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/127Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/24Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/28Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/14Drugs for genital or sexual disorders; Contraceptives for lactation disorders, e.g. galactorrhoea
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Endocrinology (AREA)
  • Dispersion Chemistry (AREA)
  • Gynecology & Obstetrics (AREA)
  • Reproductive Health (AREA)
  • Biophysics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The present invention provides a kind of long-acting slow-release Tilmicosin injection, including Tilmicosin 300g, organic solvent 100-500ml, injection oil 200-500mlg, cholesterol 0.1g, phosphatidase 0 .5g, the organic solvent includes acetone, chloroform, carbon tetrachloride, the solvent of Tilmicosin can be mixed and can dissolved with grease, and the injection oil is injection soybean oil, injection corn oil, rilanit special.The beneficial effects of the present invention are: prior art effective dose on pig uses the generation that can cause intoxicating phenomenon, the present invention uses a kind of long-acting slow-release technology, the residence time of drug in blood can be extended, extend the action time of drug, it is absorbed Tilmicosin slowly, is unlikely to so that drug is absorbed in the short time and is poisoned.

Description

A kind of long-acting slow-release Tilmicosin injection and preparation method thereof
Technical field
The present invention relates to a kind of long-acting slow-release Tilmicosin injections and preparation method thereof.
Background technique
Tilmicosin is by a kind of dedicated antibiotic of the semi-synthetic livestock and poultry of hydrolysate of tylosin, is 80 years 20th century The semi-synthetic dedicated antibiotic of macrolides livestock and poultry of generation exploitation is mainly used for preventing and treating domestic animal pneumonia (by pleuropneumonia unwrapping wire bar Bacterium, Pasteurella, mycoplasma infection cause), the mazoitis of avian mycoplasmas disease and lactating mammal.
Tilmicosin injection is larger to cardiac toxic at present, especially applies on pig, and Tilmicosin is to Pigs Hearts dysentery Property larger obtained using intramuscular injection 10mg/kg weight, that is, the poisoning such as compact breathing, vomiting occur and faint from fear using conclusion Symptom, but be unlikely to cause death, using 15mg/kg weight, critical case is dead quickly, uses 30mg/kg to general case Weight can cause death in 15 minutes, and the death rate is up to 80%.It is i.e. lethal that ox is once injected intravenously 5mg/kg.Ox subcutaneous injection 50mg/kg can cause myocardium toxicity, and 150mg/kg can be lethal, and pig, primate and horse intravenous injection also have lethal dangerous.
Summary of the invention
Effective dose is using the generation that can cause intoxicating phenomenon on pig for the prior art, and the present invention is using a kind of long-acting slow-release Technology can extend the residence time of drug in blood, extend the action time of drug, be absorbed Tilmicosin slowly, no It is poisoned as drug is absorbed in the short time.
Technical solution: a kind of long-acting slow-release Tilmicosin injection, including Tilmicosin 300g, organic solvent 100- 500ml, injection oil 200-500mlg, cholesterol 0.1g, phosphatidase 0 .5g, the organic solvent includes acetone, chloroform, four chlorinations Carbon, can mix with grease and can dissolve the solvent of Tilmicosin, the injection oil be injection soybean oil, injection corn oil, Rilanit special.
Further, the Tilmicosin 300g, organic solvent 100-500ml, injection oil 200-500mlg, cholesterol 0.1g, phosphatidase 0 .5g, dissolved total amount are 1000ml.
It further, further include glycerol formal.
The invention further relates to a kind of preparation method of long-acting slow-release Tilmicosin injection, liposome technology is applied to this hair In bright, carrier is done with oil-based solvent, takes organic solvent, Tilmicosin, phosphatide, cholesterol is added and is allowed to dissolve, injection is added Oily constant volume.Filtering encapsulating after detection is qualified, 100 degrees Celsius of sterilizing 30 minutes.
Compared with the prior art, the present invention has the following advantages:
The scope of application and dosage of the Tilmicosin injection of the prior art and adverse reaction are as follows:
[usage and dosage] subcutaneous injection: ox, every 1kg weight 0.033ml.Only inject 1 time.
[adverse reaction] this product is mainly cardiovascular system to the toxic effect of animal, can cause tachycardia and convergent force Weaken.It is i.e. lethal that ox is once injected intravenously 5mg/kg.Pig, primate and horse intravenous injection also have lethal dangerous.Ox-hide Lower injection 50mg/kg can cause myocardium toxicity, and 150mg/kg can be lethal.
The scope of application, usage and dosage and adverse reaction (through using result to obtain) of the invention:
[usage and dosage] subcutaneous injection: ox, every 1kg weight 0.05ml.Pig per kilogram of body weight 0.06ml is only injected 1 time.
[adverse reaction] this product is mainly cardiovascular system to the toxic effect of animal, can cause tachycardia and convergent force Weaken.It is i.e. lethal that ox is once injected intravenously 5mg/kg.Pig, primate and horse intravenous injection also have lethal dangerous.Ox-hide Lower injection 100mg/kg can cause myocardium toxicity, and 200mg/kg can be lethal.Pig subcutaneous injection 100mg/kg can cause myocardium toxicity, 200mg/kg can be lethal.
The two compares, and the principle of slow-absorbing of the present invention emerges from out, dosage can increase on the basis of original and The risk of medication poisoning is not increased, and the present invention applies on pig and also solves the problems, such as easily to be poisoned, and can be widely applied.
Specific embodiment
Tilmicosin injection of the present invention, it includes the following component of 1000ml, Tilmicosin 300g, organic solvent 100- 500ml, injection oil 200-500mlg, cholesterol 0.1g, phosphatidase 0 .5g.
Heretofore described organic solvent includes that acetone, chloroform, carbon tetrachloride etc. can mix with grease and can dissolve and replace The solvent of meter Kao Xing.Qs glycerin formal can also be added and improve dissolution rate.The injection oil is injection soybean oil, injection Corn oil, rilanit special etc..
The preparation method of Tilmicosin injection of the invention, liposome technology are applied in the present invention, use oil-based solvent Carrier is done, takes organic solvent appropriate, Tilmicosin, phosphatide, cholesterol is added and is allowed to dissolve, oil for injection constant volume is added.Detection Filtering encapsulating after qualified, 100 degrees Celsius of sterilizing 30 minutes to get.
Embodiment 1:
Chloroform 500ml is taken, Tilmicosin 300g, phosphatidase 0 .5g, cholesterol 0.1g is added and is allowed to be completely dissolved, injection oil is added extremely 1000ml filters encapsulating after the assay was approved, and 100 degrees Celsius sterilize for 30 minutes to obtain the final product.
Embodiment 2:
It takes acetone 400ml, glycerol formal 100ml after mixing, Tilmicosin 300g, phosphatidase 0 .5g, cholesterol is added 0.1g heating is allowed to dissolve, and soybean oil is added to 1000ml, filters encapsulating after the assay was approved, 100 degrees Celsius of sterilizings in 30 minutes are ?.
Basic principles and main features and advantages of the present invention of the invention have been shown and described above.The skill of the industry Art personnel should be recognized that.The present invention is not limited by examples detailed above, and original of the invention is only illustrated in examples detailed above and specification Reason, various changes and improvements may be made to the invention under the premise without departing from the spirit and scope of the present invention, these change and change Into all fall within the protetion scope of the claimed invention, the claimed scope of the invention is by appended claims and its equivalent Object defines.

Claims (6)

1. a kind of long-acting slow-release Tilmicosin injection, it is characterised in that: including Tilmicosin 300g, organic solvent 100- 500ml, injection oil 200-500mlg, cholesterol 0.1g, phosphatidase 0 .5g, the organic solvent includes acetone, chloroform, four chlorinations Carbon, can mix with grease and can dissolve the solvent of Tilmicosin, the injection oil be injection soybean oil, injection corn oil, Rilanit special.
2. a kind of long-acting slow-release Tilmicosin injection according to claim 1, it is characterised in that: the Tilmicosin 300g, organic solvent 100-500ml, injection oil 200-500mlg, cholesterol 0.1g, phosphatidase 0 .5g, dissolved total amount are 1000ml。
3. a kind of long-acting slow-release Tilmicosin injection according to claim 1 or 2, which is characterized in that further include glycerol Formal.
4. a kind of preparation method of long-acting slow-release Tilmicosin injection, it is characterised in that: liposome technology is applied to the present invention In, carrier is done with oil-based solvent, takes organic solvent, Tilmicosin 300g, phosphatidase 0 .5g, cholesterol 0.1g is added and is allowed to dissolve, Be added and inject oily constant volume, detect it is qualified after filtering encapsulating, 100 degrees Celsius of sterilizing 30 minutes.
5. a kind of preparation method of long-acting slow-release Tilmicosin injection according to claim 4, it is characterised in that: described Organic solvent be chloroform 500ml, Tilmicosin 300g is added, phosphatidase 0 .5g, cholesterol 0.1g are allowed to be completely dissolved, note is added It penetrates after oil dissolution to 1000ml, filters encapsulating after the assay was approved, 100 degrees Celsius sterilize for 30 minutes to obtain the final product.
6. a kind of preparation method of long-acting slow-release Tilmicosin injection according to claim 4, it is characterised in that: described Organic solvent be acetone 400ml, glycerol formal 100ml mixture, it is solid that Tilmicosin 300g, phosphatidase 0 .5g, gallbladder is added Alcohol 0.1g heating is allowed to dissolve, and injection oil 1000ml is added, and the injection oil is soybean oil, filters encapsulating after the assay was approved, 100 degrees Celsius sterilize for 30 minutes to obtain the final product.
CN201811012891.7A 2018-08-31 2018-08-31 A kind of long-acting slow-release Tilmicosin injection and preparation method thereof Pending CN109077999A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201811012891.7A CN109077999A (en) 2018-08-31 2018-08-31 A kind of long-acting slow-release Tilmicosin injection and preparation method thereof

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108392467A (en) * 2018-05-30 2018-08-14 山东德信生物科技有限公司 A kind of Tilmicosin injection and preparation method thereof

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108392467A (en) * 2018-05-30 2018-08-14 山东德信生物科技有限公司 A kind of Tilmicosin injection and preparation method thereof

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Application publication date: 20181225