WO2021120268A1 - Onguent de mupirocine et procédé de préparation associé - Google Patents

Onguent de mupirocine et procédé de préparation associé Download PDF

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Publication number
WO2021120268A1
WO2021120268A1 PCT/CN2019/128624 CN2019128624W WO2021120268A1 WO 2021120268 A1 WO2021120268 A1 WO 2021120268A1 CN 2019128624 W CN2019128624 W CN 2019128624W WO 2021120268 A1 WO2021120268 A1 WO 2021120268A1
Authority
WO
WIPO (PCT)
Prior art keywords
polyethylene glycol
mupirocin
parts
ointment
suspension
Prior art date
Application number
PCT/CN2019/128624
Other languages
English (en)
Chinese (zh)
Inventor
戴小华
程璐
朱克旭
吴剑
张言君
Original Assignee
福元药业有限公司
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by 福元药业有限公司 filed Critical 福元药业有限公司
Publication of WO2021120268A1 publication Critical patent/WO2021120268A1/fr

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Classifications

    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/351—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
    • 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
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • 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
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • 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
    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • 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

Definitions

  • This application relates to the technical field of chemical medicine preparations, in particular to a mupirocin ointment and a preparation method thereof.
  • Mupirocin Ointment trade name: It is a new type of topical antibiotic, a metabolite produced in the culture of Pseudomonas fluorescens, namely Pseudomonas A. This product was approved by the FDA in 1987. Mupirocin's chemical structure and mechanism of action are different from other types of antibiotics, and it can avoid the development of drug resistance in the near future; it has high activity against common skin gram-positive bacteria, especially under acidic conditions; it has strong antibacterial effect; it does not produce contact allergies Reaction, non-irritating and toxic, safe to use.
  • mupirocin is a safe and effective new topical antibiotic for clinical use. Mupirocin is produced by the fermentation of Pseudomonas fluorescens. It has antibacterial effect and has a molecular structure with other known antibacterial agents. And metabolites with different mechanisms of action, which are mainly pseudomonas acid A, with a structure similar to isoleucine.
  • Mupirocin has strong antibacterial activity against various gram-positive cocci related to skin infections, and is also effective against drug-resistant Staphylococcus aureus; it has a certain antibacterial effect against certain gram-negative bacteria, and it is compatible with other antibiotics. No cross-resistance.
  • the ointment base is thinner when the temperature is high in summer, and it looks watery after extrusion; when the temperature is low in winter, the ointment base It is hard and not easy to squeeze out of the ointment tube, which makes the active ingredient API in mupirocin ointment unevenly distributed in the matrix, which affects the patient's experience and efficacy.
  • the present application proposes a mupirocin ointment and a preparation method thereof.
  • the active ingredients of the present application are uniformly distributed, have a suitable consistency, are easy to apply, and are convenient for patients to use.
  • This application proposes a mupirocin ointment. Its raw materials include 20-100 parts by weight of mupirocin, 500-700 parts of polyethylene glycol 3350, 400-600 parts of polyethylene glycol 400, 1- 2 parts vitamin E, 39-58 parts propylene glycol.
  • the content of mupirocin is 2-10%.
  • This application also discloses a method for preparing the above mupirocin ointment, which includes the following steps: taking polyethylene glycol 400, adding polyethylene glycol 3350, and propylene glycol to mix to obtain solution A; taking polyethylene glycol 400, and then adding mopi Mix Luoxing and Vitamin E to obtain suspension B; mix Solution A and Suspension B at 55-65°C, then cool to 35-45°C, grind, cool to room temperature, and canned.
  • the above mupirocin ointment is 5-10g/stick.
  • the weight ratio of polyethylene glycol 400 in solution A to polyethylene glycol 400 in suspension B is 4-7:3-6.
  • the solution A and the suspension B are stirred for 15-25 minutes and mixed evenly.
  • vitamin E is added to increase the stability of mupirocin, and the ratio of polyethylene glycol 3350, polyethylene glycol 400 and propylene glycol is adjusted to reduce the proportion of polyethylene glycol 400 to improve the summer temperature.
  • the problem of ointment base is relatively thin, and by adding appropriate amount of propylene glycol, polyethylene glycol 3350, polyethylene glycol 400 to improve the problem of hard ointment base when the temperature is low in winter; and in the preparation process, the polyethylene glycol 3350.
  • a mupirocin ointment its raw materials include 20 parts by weight of mupirocin, 520 parts of polyethylene glycol 3350, 420 parts of polyethylene glycol 400, 1 part of vitamin E, and 39 parts of propylene glycol.
  • the preparation method of the above mupirocin ointment includes the following steps:
  • suspension B includes lotion;
  • a mupirocin ointment its raw materials include 100 parts by weight of mupirocin, 700 parts of polyethylene glycol 3350, 600 parts of polyethylene glycol 400, 2 parts of vitamin E, and 58 parts of propylene glycol.
  • the preparation method of the above mupirocin ointment includes the following steps:
  • suspension B includes lotion;
  • a mupirocin ointment, its raw materials include 50 parts by weight of mupirocin, 500 parts of polyethylene glycol 3350, 400 parts of polyethylene glycol 400, 1 part of vitamin E, and 49 parts of propylene glycol.
  • the preparation method of the above mupirocin ointment includes the following steps:
  • suspension B includes lotion;
  • a mupirocin ointment, its raw materials include 50 parts by weight of mupirocin, 500 parts of polyethylene glycol 3350, and 450 parts of polyethylene glycol 400.
  • Example 3 three batches of mupirocin ointment were produced, and the batch numbers were 190601, 190602, and 190603.
  • a batch of mupirocin ointment was produced according to the comparative example, and the batch number was 190501.
  • the batch numbers are 18100585, 18100240, 19040148, 8D9G (British import batch numbers); the performance tests of the above samples were carried out, and the results are as follows:
  • the kinematic viscosity of the paste was measured with a viscosity-temperature control integrated meter, and the apparent viscosity of the above samples was compared with the same instrument and rotor under the same measurement conditions.
  • a DHR-1 rheometer was used to detect the rheology of the paste.
  • the same instrument and a 25mm rotor were used to compare the apparent viscosity of the above samples under the same measurement conditions.
  • the measurement method For the measurement method, first select a 25mm clamp and perform zero calibration, take an appropriate amount of mupirocin ointment sample to the center of the clamp, touch Bearing lock to lock the bearing, and then touch Trim gap to wait for intermittent closing to the trimming gap, use a suitable scraping tool Remove the excess sample spilling to the periphery of the fixture. Click the Go to Geometry gap button and wait for the completion of setting the test gap to start the test. In the test, the linear viscoelastic region of the sample is measured at a strain of 0.01-100% under the oscillation mode, and the rheological curve of the sample is measured at 0.01-100s-1 under the flow test.

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

Abstract

La présente invention concerne un onguent de mupirocine. Les matières premières correspondantes comprennent, en poids : 20-100 parties de mupirocine, 500-700 parties de polyéthylèneglycol 3350, 400-600 parties de polyéthylèneglycol 400, 1-2 parties de vitamine E et 39-58 parties de propylèneglycol. La présente invention concerne en outre un procédé de préparation de l'onguent de mupirocine décrit, comprenant les étapes suivantes, consistant à : prendre du polyéthylèneglycol 400, ajouter du polyéthylèneglycol 3350 et du propylèneglycol et les mélanger uniformément, de manière à obtenir une solution A ; prendre du polyéthylèneglycol 400, puis ajouter de la mupirocine et de la vitamine E et les mélanger uniformément, de manière à obtenir une suspension B ; mélanger la solution A et la suspension B uniformément à 55-65°C, puis abaisser la température à 35-45°C, broyer, refroidir à température ambiante et mettre en boîte, de manière à obtenir un produit. L'onguent de mupirocine obtenu présente une distribution uniforme de principe actif, une consistance appropriée, une application aisée et une utilisation pratique pour des patients.
PCT/CN2019/128624 2019-12-17 2019-12-26 Onguent de mupirocine et procédé de préparation associé WO2021120268A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201911302071.6A CN110787128A (zh) 2019-12-17 2019-12-17 一种莫匹罗星软膏及其制备方法
CN201911302071.6 2019-12-17

Publications (1)

Publication Number Publication Date
WO2021120268A1 true WO2021120268A1 (fr) 2021-06-24

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PCT/CN2019/128624 WO2021120268A1 (fr) 2019-12-17 2019-12-26 Onguent de mupirocine et procédé de préparation associé

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CN (1) CN110787128A (fr)
WO (1) WO2021120268A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
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CN114053210A (zh) * 2021-10-26 2022-02-18 海南全星制药有限公司 一种莫匹罗星软膏及其制备方法

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113520994B (zh) * 2021-08-12 2024-06-14 福元药业有限公司 一种莫匹罗星软膏制剂
CN116270433B (zh) * 2023-03-14 2023-09-01 郑州大学第一附属医院 一种莫匹罗星软膏、制备方法及用途

Citations (7)

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EP1174133B1 (fr) * 2000-07-18 2005-03-23 Agis Industries (1983) Ltd Composition pharmaceutiques contenant de mupirocine amorphe
WO2009047788A2 (fr) * 2007-08-06 2009-04-16 Glenmark Pharmaceuticals Limited Combinaison topique contenant une combinaison de mupirocine et de béclométhasone
CN102335122A (zh) * 2011-06-21 2012-02-01 北京协和药厂 一种莫匹罗星软膏及其制备方法
CN102871955A (zh) * 2012-10-29 2013-01-16 杭州朱养心药业有限公司 包含莫匹罗星的软膏药物组合物
CN102885763A (zh) * 2012-10-29 2013-01-23 杭州朱养心药业有限公司 一种新颖的莫匹罗星软膏剂药物组合物
CN105412000A (zh) * 2015-11-23 2016-03-23 安徽新和成皖南药业有限公司 一种莫匹罗星软膏的制备方法
US20170196823A1 (en) * 2016-01-07 2017-07-13 Cmpd Licensing, Llc Urea Cream Formulations

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* Cited by examiner, † Cited by third party
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CN108348453B (zh) * 2015-08-05 2021-09-03 罗切斯特大学 包含莫匹罗星及新霉素的抗微生物组合物
US9717748B2 (en) * 2015-12-18 2017-08-01 Cmpd Licensing, Llc Compositions and methods for treating an infection

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1174133B1 (fr) * 2000-07-18 2005-03-23 Agis Industries (1983) Ltd Composition pharmaceutiques contenant de mupirocine amorphe
WO2009047788A2 (fr) * 2007-08-06 2009-04-16 Glenmark Pharmaceuticals Limited Combinaison topique contenant une combinaison de mupirocine et de béclométhasone
CN102335122A (zh) * 2011-06-21 2012-02-01 北京协和药厂 一种莫匹罗星软膏及其制备方法
CN102871955A (zh) * 2012-10-29 2013-01-16 杭州朱养心药业有限公司 包含莫匹罗星的软膏药物组合物
CN102885763A (zh) * 2012-10-29 2013-01-23 杭州朱养心药业有限公司 一种新颖的莫匹罗星软膏剂药物组合物
CN105412000A (zh) * 2015-11-23 2016-03-23 安徽新和成皖南药业有限公司 一种莫匹罗星软膏的制备方法
US20170196823A1 (en) * 2016-01-07 2017-07-13 Cmpd Licensing, Llc Urea Cream Formulations

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114053210A (zh) * 2021-10-26 2022-02-18 海南全星制药有限公司 一种莫匹罗星软膏及其制备方法
CN114053210B (zh) * 2021-10-26 2023-09-29 海南全星制药有限公司 一种莫匹罗星软膏及其制备方法

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