WO2022219567A1 - Composition de naproxène nano-particulaire dans de l'huile végétale utile pour le traitement de l'inflammation et de la douleur - Google Patents

Composition de naproxène nano-particulaire dans de l'huile végétale utile pour le traitement de l'inflammation et de la douleur Download PDF

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Publication number
WO2022219567A1
WO2022219567A1 PCT/IB2022/053490 IB2022053490W WO2022219567A1 WO 2022219567 A1 WO2022219567 A1 WO 2022219567A1 IB 2022053490 W IB2022053490 W IB 2022053490W WO 2022219567 A1 WO2022219567 A1 WO 2022219567A1
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WO
WIPO (PCT)
Prior art keywords
oil
naproxen
pain
composition
composition according
Prior art date
Application number
PCT/IB2022/053490
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English (en)
Spanish (es)
Inventor
Oscar Alzate
Original Assignee
Oscar Alzate
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 Oscar Alzate filed Critical Oscar Alzate
Publication of WO2022219567A1 publication Critical patent/WO2022219567A1/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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • 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
    • 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
    • A61K47/24—Organic 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
    • 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
    • A61K47/44—Oils, 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
    • 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
    • A61K47/46—Ingredients of undetermined constitution or reaction products thereof, e.g. skin, bone, milk, cotton fibre, eggshell, oxgall or plant extracts
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Definitions

  • the development belongs to the chemical, pharmaceutical and medicine fields in general, particularly to a topical composition of nano-particulate naproxen in an oily vehicle, useful as an analgesic and anti-inflammatory agent.
  • Non-steroidal anti-inflammatory drugs constitute a family of mainly anti-inflammatory, analgesic and antipyretic compounds, which treat symptoms such as inflammation, pain and fever.
  • NSAIDs are widely consumed among the world's population as over-the-counter and prescription drugs, where the problem with this growing trend lies in the presence of side effects, such as gastrointestinal effects associated with their use.
  • mode of action as inhibitors of the activity of the enzyme cyclooxygenase (COX) that mediates the biosynthesis of prostaglandins, thromboxane and prostacyclins, while certain classes of prostaglandins have the property of protecting the gastrointestinal epithelium from a series of ulcerogenic conditions, therefore when blocked, the cytoprotective nature of these lipid mediators is also affected.
  • COX cyclooxygenase
  • patent US9351984 discloses a pharmaceutical composition comprising NSAIDs that are added directly to an oil containing phospholipids, such as lecithin or a bio-compatible oil to which a phospholipid has been added, to prepare a composition with low gastrointestinal toxicity and enhanced therapeutic activity to treat or prevent inflammation, pain, fever, platelet aggregation, tissue ulceration, and/or other tissue disorders.
  • an oil containing phospholipids such as lecithin or a bio-compatible oil to which a phospholipid has been added
  • compositions are in the form of a non-aqueous solution, paste, suspension, dispersion, colloidal suspension or in the form of an aqueous emulsion or microemulsion for internal, oral, direct or topical administration.
  • the compositions may be in the form of an ointment, paste, oil, emulsion, microemulsion, or mixtures or combinations thereof.
  • the compositions can be mixed with other ingredients commonly used in ointments and in the cosmetic industry.
  • patent US20110033545 discloses topical pharmaceutical preparations that comprise both a solution and a suspension of nanoparticles and methods for the treatment of acute and chronic pain that use said preparations.
  • the disclosed preparations comprise a therapeutically effective amount of a nano-sized NSAID drug and a pharmaceutically acceptable carrier suitable for topical administration.
  • the nonsteroidal anti-inflammatory drug is presented in the form of nanoparticles of less than 1000 nm, preferably 40 to 60 nm.
  • Pharmaceutical preparations are intended to be administered topically by any known means; for example, creams, gels, lotions, ointments and transdermal patches.
  • the administration of the pharmaceutical preparations must be local, so as to minimize, as much as possible, the undesired collateral effects that may arise with systemic administration.
  • authors such as Gaber D. [Gaber D. (2019). Nano-lipid particles of naproxen for topical application: In vitro / in vivo study.
  • lipid nanoparticle-based (NpxNps)-based naproxen gel formulations for the treatment of osteoarthritis.
  • This study evaluates the characterization of the NpxNps for application topical by its physical characteristics, as well as in vivo transdermal release and analgesic effect.
  • the average size of the particles is in the range between 203 ⁇ 10 nm and 228 ⁇ 30 nm, so the author mentions that lipid-based nanoparticles with a pattern of controlled drug release can be a useful technology to improve drug release.
  • naproxen through a transdermal delivery system since they have the advantage of being nanometric in size and lipophilic in nature. Additionally, they are considered a safe vehicle for drugs since they are composed of biocompatible and biodegradable components.
  • the present development refers to a topical composition comprising nano-particulate naproxen as an active ingredient arranged in an oily vehicle selected from one or more oils rich in terpenoids and pharmaceutically acceptable excipients. Additionally, the present development also refers to the method for preparing said compositions. In an additional aspect, the present development refers to the use of the nano-particulate naproxen composition as an anti-inflammatory and/or analgesic agent, for the treatment of diseases or conditions associated with inflammation and/or joint or muscle pain, rheumatoid arthritis , osteoarthritis, back pain, chronic pain, muscle pain, muscle pain associated with menstruation, tendonitis, dental pain, and bursitis, among others.
  • the present development corresponds to a topical composition of nanoparticulate naproxen as active ingredient, an oily vehicle that is selected from one or more oils rich in terpenoids and pharmaceutically acceptable excipients.
  • Nanoparticulate naproxen is understood as naproxen nanoparticles that have particle sizes that do not exceed 800 nm.
  • the naproxen nanoparticles have sizes between 200 and 500 nm and in another particular embodiment between 200 and 300 nm.
  • the concentration of nano-particulate naproxen is up to 20% by weight, between 0.5 and 15% by weight or between 7.5 and 10% by weight.
  • nano-particulate naproxen By incorporating the nano-particulate naproxen into the oily vehicle, unique structures such as micelles or vesicles are formed that allow the active ingredient to be transported through the skin.
  • this is a natural property of terpenoids, since its oily nature allows it to maintain the micelles or vesicles that encapsulate the nano-particulate naproxen and give it the ability to permeate the layers of the skin, releasing itself at the site of action.
  • the oils comprise terpenoid-rich eucalyptus oil, aromatic and flavonoid-rich cedar oil, and astragalin-rich moringa oil.
  • the pharmaceutically acceptable excipients can be of the hydrophilic or lipophilic type, such as diluents, solvents, lubricants, colorants, flavoring agents, antioxidants, stabilizers, thickeners, humectants, and antimicrobial agents.
  • excipients are incorporated into the composition to reduce the effects of environmental conditions on the stability of the active ingredient.
  • the excipients have aromatic properties that produce relaxing effects through aromatherapy.
  • the present development is also directed to the method of making a nano-particulate naproxen composition.
  • the preparation method of the composition comprises obtaining nanoparticles of naproxen, mixing the nanoparticles with one or more vegetable oils rich in terpenoids and adding pharmaceutically acceptable excipients, where an additional component selected from flavonoids of vegetable origin with beneficial properties can also be incorporated. anti-inflammatory, antioxidant, and/or antibacterial.
  • the size of the nanoparticles is determined using techniques known in the art, such as light scattering, Raman diffraction, microscopy, or atomic testing.
  • a vegetable oil rich in terpenoids is added, selected from, without limitation, moringa oil, eucalyptus oil, tea oil, sage oil, citrus tree oil, pine oil, of cedar, lavender oil, menthol oil, and/or camphor oil, at room temperature (23 °C), with constant low revolution stirring (approximately 30 to 50 rpm), in a proportion of 3 to 5 volumes of the oil to 1 volume of the nano-particulate, until a homogeneous mixture is obtained.
  • terpenoids and/or flavonoids are optionally added under the same conditions, selected from, but not limited to, quercetin, isoquercetin, chlorogenic acid, astragalin, or mixtures thereof.
  • the composition obtained in the present invention is useful as an analgesic and/or anti-inflammatory agent and in general for purposes of treating, curing, and/or rehabilitating a condition or disease associated with inflammation and/or pain, alone or as a complement to treatments. conventional in situations of intense pain.
  • the inflammation and/or pain is of a joint or muscular type, more preferably rheumatoid arthritis, osteoarthritis, back pain, chronic pain, muscular pain, muscular pain associated with menstruation, tendinitis, dental pain and bursitis.
  • the application of the composition on the skin guarantees a prolonged effect, which suggests that the composition of the present invention is suitable for the treatment of chronic pain.
  • Example 1 Composition of nano-particulate naproxen transported in a mixture of vegetable oils
  • composition C a moringa extract was prepared by heating the moringa leaf extract powder to boiling in water with 10% glycerin, followed by resuspension in various percentages of organics/water, and removal of the organics by consecutive washes in water.
  • the extracts were filtered through Whatman No. 10 filter paper, followed by drying at room temperature and dispersing this precipitate in 2.0 mL of mineral oil.

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Botany (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

La présente invention concerne une composition topique qui comprend du naproxène nano-particulaire comme principe actif, disposé sur un véhicule huileux qui est sélectionné parmi une ou plusieurs huiles riches en terpénoïdes, et des excipients pharmaceutiquement acceptables. La présente invention concerne également le procédé pour produire cette composition à travers les étapes d'obtention des nanoparticules de naproxène avec une taille de particule comprise entre 200 et 300 nm, de mélange des nanoparticules avec une ou plusieurs huiles végétales riches en terpénoïdes, d'ajout d'excipients pharmaceutiquement acceptables et éventuellement de composés additionnels tels que de la quercétine, de l'isoquercétine, de l'acide chlorogénique, de l'astragaline ou des mélanges de ceux-ci jusqu'à obtenir un mélange homogène. La composition de l'invention permet de véhiculer le naproxène de telle manière qu'il soit absorbé par la peau de manière efficace, tout en favorisant l'effet analgésique et/ou inflammatoire du naproxène, en garantissant l'absorption de l'actif au niveau du site d'action, en diminuant le temps d'action dû à son application et à son action locale et en diminuant les effets gastriques secondaires propres du mécanisme d'action de l'actif en comparaison avec les compositions commercialement connues.
PCT/IB2022/053490 2021-04-15 2022-04-13 Composition de naproxène nano-particulaire dans de l'huile végétale utile pour le traitement de l'inflammation et de la douleur WO2022219567A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CONC2021/0004783 2021-04-15
CONC2021/0004783A CO2021004783A1 (es) 2021-04-15 2021-04-15 Composición de naproxeno nano-particulado en aceitevegetal útil para el tratamiento de la inflamación y eldolor

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WO2022219567A1 true WO2022219567A1 (fr) 2022-10-20

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Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007148116A2 (fr) * 2006-06-23 2007-12-27 Aston University Formules pharmaceutiques locales
WO2010066047A1 (fr) * 2008-12-10 2010-06-17 Roch Lebel Composition moussante topique et procédé d'application
IN201621029815A (fr) * 2016-08-31 2016-09-16 Shripad Abhimanyu PANSARE
US10806790B1 (en) * 2013-11-12 2020-10-20 Scott Shapiro Pain therapy cream with deep tissue delivery system

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007148116A2 (fr) * 2006-06-23 2007-12-27 Aston University Formules pharmaceutiques locales
WO2010066047A1 (fr) * 2008-12-10 2010-06-17 Roch Lebel Composition moussante topique et procédé d'application
US10806790B1 (en) * 2013-11-12 2020-10-20 Scott Shapiro Pain therapy cream with deep tissue delivery system
IN201621029815A (fr) * 2016-08-31 2016-09-16 Shripad Abhimanyu PANSARE

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
ABD EMAN, NAMJOSHI SARIKA, MOHAMMED YOUSUF H., ROBERTS MICHAEL S., GRICE JEFFREY E.: "Synergistic Skin Penetration Enhancer and Nanoemulsion Formulations Promote the Human Epidermal Permeation of Caffeine and Naproxen", JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 105, no. 1, 2016, US , pages 212 - 220, XP009540681, ISSN: 0022-3549, DOI: 10.1002/jps.24699 *
ABDULLAH GHASSAN, ABDULKARIM MUTHANNA, SALMAN IBRAHEEM, AMEER O Z, YAM M F, MUTEE, CHITNENI, MAHDI ELRASHID SALEH, BASRI, SATTAR M: "In vitro permeation and in vivo anti-inflammatory and analgesic properties of nanoscaled emulsions containing ibuprofen for topical delivery", INTERNATIONAL JOURNAL OF NANOMEDICINE, vol. 6, 2011, pages 387 - 396, XP055982573, DOI: 10.2147/IJN.S14667 *
ANONYMOUS: "Ultrabengue Gel", PLM, 23 April 2018 (2018-04-23), pages 1 - 2, XP055982571, Retrieved from the Internet <URL:https://www.medicamentosplm.com/Home/productos/ultrabengue_gel/63/101/12401/66> [retrieved on 20220722] *
DAS, ASHA ET AL.: "Natural permeation enhancer for transdermal drug delivery system and permeation evaluation: A review", ASIAN JOURNAL OF PHARMACEUTICAL AND CLINICAL RESEARCH, vol. 10, no. 9, September 2017 (2017-09-01), pages 5 - 9, XP055723474, DOI: http-//dx.doi.org/l 0.221 59/ajpcr.201 7.v1Oi9.19389 *
JAIN VIKAS, THAKUR MONIKA: "Development and characterization naproxen gel bearing eucalyptus oil for topical delivery", APPLIED MEDICAL RESEARCH, vol. 1, no. 2, 2015, pages 48 - 52, XP055982558, DOI: 10.5455/amr. 20150308 022937 *

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