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WO1997002040A1 - Produit pharmaceutique a base de terpene - Google Patents

Produit pharmaceutique a base de terpene Download PDF

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Publication number
WO1997002040A1
WO1997002040A1 PCT/EP1996/002824 EP9602824W WO9702040A1 WO 1997002040 A1 WO1997002040 A1 WO 1997002040A1 EP 9602824 W EP9602824 W EP 9602824W WO 9702040 A1 WO9702040 A1 WO 9702040A1
Authority
WO
WIPO (PCT)
Prior art keywords
pharmaceutical product
product according
propolis
preparation
combination
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.)
Ceased
Application number
PCT/EP1996/002824
Other languages
English (en)
Inventor
Matteo Bevilacqua
Carlo Alberto Zaccagna
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
BEVILACQUA MARIA
Original Assignee
BEVILACQUA MARIA
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
Priority claimed from IT95PD000133A external-priority patent/ITPD950133A1/it
Priority claimed from IT95PD000134A external-priority patent/ITPD950134A1/it
Priority claimed from IT96PD000038A external-priority patent/ITPD960038A1/it
Application filed by BEVILACQUA MARIA filed Critical BEVILACQUA MARIA
Priority to EP96922041A priority Critical patent/EP0836478A1/fr
Priority to AU63058/96A priority patent/AU6305896A/en
Publication of WO1997002040A1 publication Critical patent/WO1997002040A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/32—Burseraceae (Frankincense family)
    • A61K36/324—Boswellia, e.g. frankincense
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/32—Burseraceae (Frankincense family)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/32—Burseraceae (Frankincense family)
    • A61K36/328—Commiphora, e.g. mecca myrrh or balm of Gilead

Definitions

  • the present invention relates to a terpene-based pharmaceutical product.
  • Olibanum is a substance commonly known as incense and available in nature in several varieties. It is a hardened gum-resin that flows out from cuts in the bark of various species of plants that are present in the regions between the equator and the tropics, particularly of India, Somalia, Eritrea, Saudi Arabia, and Guinea. They are mainly small plants, usually shrubs, or frutice ⁇ , which grow sparsely in the savanna on dry gypseous calcareous soils and belong to the Burseraceae family and the Boswellia species; they produce a gummy oleoresin that is collected in small receptacles inside the plant which are supplied by the schizogenous ducts.
  • Olibanum is known for its balsamic and anti- fermentative properties and has been used since antiquity in the treatment of colitides, parasitose ⁇ , and eye diseases. In popular medicine, olibanum is used for treating disorders of the respiratory system.
  • Patents are also directed to an active principle of olibanum, namely boswellic acid, and relate to usual forms of administration, such as ampoules, tablets, suppositories, ointments, and aerosols.
  • composition of olibanum varies according to the species of the plants that produce it; chemical research has shown the presence of cyclic monoterpenes, bicyclic terpenes, and sesquiterpenes, triterpenes (the only ones to which anti-inflammatory therapeutic properties have been attributed) .
  • Boswellia The main feature of incense obtained from plants of the genus Boswellia has been the presence of tetracyclic and pentacyclic triterpenes, the parent substances whereof are boswellic acid and alpha-amyrin, having a distinctly anti-inflammatory action.
  • Alcoholic extracts of Boswellia plants contain both active principles with their derivatives and have an evident anti-inflammatory activity; it is therefore implicit to admit that there is a synergy in their combined action.
  • the height of these trees can exceed twenty meters and they are scattered individually or in small groups and have a very abundant foliage.
  • the resinous substance that is produced is substantially different from the ordinary Boswellia incense and it has a series of interesting pharmacological properties that are unknown to the local population: — it has a considerable anti-inflammatory power; — it has a considerable antimycotic power; — it has a considerable anti-cryptogenic activity;
  • a principal aim of the present invention is to provide a pharmaceutical product based on olibanum that increases its therapeutic effects.
  • an important object is to provide a pharmaceutical product composed of natural substances, particularly substances of vegetable origin, and therapeutically particularly effective.
  • Another important aim is to provide a pharmaceutical product use whereof i ⁇ ⁇ ubstantially harmless.
  • Another aim is to provide a very inexpensive pharmaceutical product.
  • a pharmaceutical product characterized in that it is the combination of one or more terpene-containing substances and of propolis.
  • the pharmaceutical product consists of the combination of natural olibanum or derivatives thereof and propolis.
  • Propolis is a mixture of resinous, gummy, and balsamic substances collected by bees on the buds of various trees to reinforce their honeycombs, line the entry walls, and close the openings of the hive.
  • composition varies according to the local flora and the flowers that are present, the climate, the availability of resins on the buds, the gathering period, and the inclusion of contaminants such as wax.
  • propolis generally produces a bacteriostatic effect and, at high concentrations, al ⁇ o a bactericidal effect.
  • the antibiotic action is equal to that of sulfonamides and is one third or one quarter of the antibiotic action of streptomycin.
  • propolis The antibacterial activity of propolis is attributed to acids and aromatic ester ⁇ , with a predominantly bactericidal action, and to flavonoid ⁇ , with a predominantly bacterio ⁇ tatic action.
  • Propoli ⁇ also has an antiviral, antifungal, antiparasitic, and anticancer activity.
  • Propolis is considered to be a very different substance with respect to incense, the difference being supported most of all by the difference of the plants from which these substances are extracted by man or by bees.
  • the product can be provided in the form of tablets, pastilles, capsules, solutions, emulsions, ointments, creams, preparation ⁇ for inhalations, aerosol ⁇ , suppositories, and pessaries.
  • a preferred pharmaceutical product uses a powder of diluted natural propolis and olibanum and said compound is applied in the form of a cataplasm, preferably at the sick organ or on its nearest skin projection.
  • olibanum and propolis are used as whole product ⁇ (resins, oils, terpenes, gums), reduced to powder or microgranules beforehand and stored away from light and possibly in vacuum or in any case not in contact with the air.
  • the product is combined with a water-alcohol solvent or with an alcohol derivative or an ether.
  • a water-alcohol solvent or with an alcohol derivative or an ether.
  • the powder of olibanum and propolis is spread on a lap of cotton and is then wet with a 35-40% water-alcohol solution.
  • Said cataplasm is then applied at the sick organ or on its nearest skin projection by means of adhesive patches or inert self-adhesive systems.
  • the retention period of the product thus applied may vary from a few days to a few weeks.
  • the oily solution is kept in place with inert liquid- tight and self-adhesive material.
  • the oily solution can also be obtained by using particular fractions of oils, particularly omega-3 polyunsaturated fatty acids, in view of the synergy that increases the anti-inflammatory action of the resins and of said acids.
  • the product can be packaged as dry powder on a medium to be wet, or it can be a pre-packaged product that is kept in vacuum until it is applied.
  • Transdermal application can be performed in all skin regions, particularly the paranasal sinuse ⁇ , the entire spine, articular regions, chest and back regions, and abdominal regions.
  • Percutaneous absorption of the cataplasm in an oily solution is good, in view of the solubility of the components of olibanum and of propolis in fat ⁇ , and therefore al ⁇ o in the lipids constituting the sebaceous secretion layer that covers the horny skin layer and the cell membranes, and in view of the presence of terpenes.
  • the cataplasm activated by the solvent, causes its active principles, absorbed transdermally, to arrive directly in the sick organ at maximum concentration without being metabolized first.
  • the possibilities of use of the product are all those in which disorders occur that have an inflammatory, bacterial, and dystrophic a ⁇ pect, of varying etiology, both post-traumatic and not; as a main or secondary event, acute, chronic, in remission, or with effusion, even those that are resistant to ordinary steroid therapy and to FANS, both for human disea ⁇ es and for veterinary diseases.
  • the product can therefore be used in the field of affections: a) of the respiratory system:
  • rhinitides sinusitides, tonsillitides, pharyngitides, laryngitides; — acute, chronic, and recurring, specific or nonspecific pulmonary diseases, in particular on the basis of altered reactivity, such as asthma, asth oid bronchitis, chronic obstructive pulmonary disease; b) of the muscles, the skeleton, and the connective tissue, the pathogenesis whereof is predominantly: -- inflammatory (rheumatoid arthritis, goneitis, epicondylitis);
  • d) of the teeth and mouth periodontitides, carie ⁇ , gingivitides, herpetic manifestations, pharyngitis caused by beta-hemolytic streptococcus, by coagulase-positive staphylococcus, and by Candida albicans
  • e) of the gastrointestinal system oesophagitide ⁇ , gastritides, peptic ulcer, affections of the intestinal bacterial flora, regional enteritis, ulcerative colitis, hae orrhoides
  • f) of the liver and the biliary tract chronic hepatitis, cholecystitides
  • g) of the genitourinary tract vulvovaginitides, salpingitises, inflammations of the kidney and of the urinary tract, Coli and Proteus infections, phlogosis of the male genital tract
  • h) of the eye and ear blepharitis, conjunctivitides, inflammation of the lach
  • a prolonged action duration is furthermore provided with low administration frequency and a low daily total dose of the drug, with high terpene absorption. It should al ⁇ be noted that the preparation i ⁇ well- accepted, inexpensive, and easily u ⁇ able even by the patient.
  • Another terpene-ba ⁇ ed pharmaceutical product according to the invention i ⁇ the combination of myrrh with at least one other resin.
  • Myrrh is a fragrant resinou ⁇ ⁇ ubstance produced by most of the specie ⁇ of Commiphora (Bal ⁇ amodendron) , such as C. mukul, C. incisa, C. myrrha, C. molmol, C. africana, gileadensis, erkeri, which are pre ⁇ ent mainly in northwestern Africa and constitute the ⁇ o-called "myrrh family" .
  • the ⁇ e are bushes, rarely small trees, of two to seven meters, typical of rocky, calcareous or gypseous soils, more rarely on alluvial soil or consolidated dunes, usually without leaves, flowers, and fruits, which appear only as a consequence of rain.
  • the gum-resin known as myrrh exudes from the tree spontaneou ⁇ ly or through cuts in the bark, hardens in air into drops or lumps, softens without melting at approximately 100° Celsius, and melts at approximately 120° Celsius.
  • Myrrh has a remarkable antimicrobial, disinfectant, insect-repellent, and insecticidal power.
  • Myrrh also has a considerable analgesic, antispasmodic, and sedative activity with respect to the central and vegetative nervous system, probably to be ascribed to sesquiterpenes, some whereof have recently been isolated (furaneudesma-1,3-diene and curzarene), the analgesic action whereof has been attributed to a mechanism of interaction with brain opioids.
  • myrrh is preferable to use of its individual components, due to synergy with enhancement and to the wide range of therapeutic properties that are harmoniously blended and make it a product that has been known since antiquity both for its therapeutic properties and for its harmlessnes ⁇ .
  • myrrh is combined, in an original way, with another resin, which can be the mentioned Dacryoides Klaineana resin, propolis, or common incenses.
  • Said Dacryoides Klaineana resin has shown affinity in composition and pharmacological action with respect to myrrh since it contains terpenes (it has a particular content of sesquiterpenes, approximately 51.8%), so that its combination with myrrh has shown a considerable enhancement of effects and extension of activities, which include analgesic activities and the neuroendocrine sy ⁇ tem.
  • the Dacryoide ⁇ re ⁇ in is furthermore characterized in that it has a low rubber content (23%), softens without melting at approximately 80° Celsius, melts around 90° Celsius, and is only slightly aromatic.
  • Propolis too, has shown affinity in composition and pharmacological action with respect to myrrh and its combination with myrrh has shown an enhanced effect and an extended activity range.
  • the product obtained from the combination of myrrh with Dacryoides Klaineana resin and/or with propolis and/or common incenses can be provided in the form of tablets, pills, capsules, solutions, emulsions, ointments, creams, preparations for inhalation ⁇ , aero ⁇ ols, suppo ⁇ itorie ⁇ , and pe ⁇ saries.
  • vaporization or sublimation by constant ( thermo ⁇ tat-controlled ) heating to temperatures between 90° and 120° Celsius is particularly interesting.
  • the product is the combination of myrrh with Dacryoides Klaineana resin
  • the optimum temperature i ⁇ between 90° and 120° Celsius; for myrrh combined with Boswellia incense, between 100° and 120° Celsius; for propolis combined with myrrh, between 90° and 120° Celsiu ⁇ .
  • the po ⁇ ibilitie ⁇ of use of the product are all those in which it is necessary to provide an anti-inflammatory, antimycotic, antimicrobial, and particularly antifungal, antibacterial, insect-repellent, insecticide, anti- cryptogenic, analgesic, anti-anxiety, antidepres ⁇ ant action. From the above description it is evident that the intended aim and obj ects of the present invention have been achieved .

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  • Health & Medical Sciences (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Biotechnology (AREA)
  • Botany (AREA)
  • Medical Informatics (AREA)
  • Medicinal Chemistry (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Preparation (AREA)

Abstract

Produit pharmaceutique qui est une association d'une ou plusieurs substances contenant du terpène avec de la propolis, de préférence une association d'oliban naturel ou de ses dérivés avec de la propolis.
PCT/EP1996/002824 1995-07-03 1996-06-27 Produit pharmaceutique a base de terpene Ceased WO1997002040A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
EP96922041A EP0836478A1 (fr) 1995-07-03 1996-06-27 Produit pharmaceutique a base de terpene
AU63058/96A AU6305896A (en) 1995-07-03 1996-06-27 Terpene-based pharmaceutical product

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
IT95PD000133A ITPD950133A1 (it) 1995-07-03 1995-07-03 Preparazione ed uso di un prodotto farmaceutico a base di olibanum e propoli
ITPD95A000133 1995-07-03
IT95PD000134A ITPD950134A1 (it) 1995-07-03 1995-07-03 Prodotto farmaceutico a base terpenica
ITPD95A000134 1995-07-03
ITPD96A000038 1996-02-20
IT96PD000038A ITPD960038A1 (it) 1996-02-20 1996-02-20 Prodotto farmaceutico a base di mirra

Publications (1)

Publication Number Publication Date
WO1997002040A1 true WO1997002040A1 (fr) 1997-01-23

Family

ID=27274137

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1996/002824 Ceased WO1997002040A1 (fr) 1995-07-03 1996-06-27 Produit pharmaceutique a base de terpene

Country Status (3)

Country Link
EP (1) EP0836478A1 (fr)
AU (1) AU6305896A (fr)
WO (1) WO1997002040A1 (fr)

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2767062A1 (fr) * 1997-08-11 1999-02-12 Andre Pierre Morice Composition comprenant de la propolis
WO2000062751A3 (fr) * 1999-04-16 2001-01-18 Quest Int Compositions contenant des extraits de boswellia
WO2002056879A1 (fr) * 2001-01-03 2002-07-25 Medpharma Plc Utilisation de terpenes dans le traitement des infections du tube digestif
WO2002062362A3 (fr) * 2001-02-06 2003-11-20 Theodore Cherbuliez Composition antivirale et antibacterienne comprenant de la propolis
DE102005014334A1 (de) * 2005-03-24 2006-09-28 Franz Udo Willerscheidt SOPORUS Hypnotika/Sedativa und Psychopharmaka/Antidepressiva/Anxiolytika
WO2006128634A1 (fr) * 2005-05-28 2006-12-07 Hans-Ulrich Jabs Extrait d'oliban (resine d'oliban) se presentant sous la forme de nanoparticules, et son utilisation
WO2008017280A1 (fr) * 2006-08-10 2008-02-14 Franz Udo Willerscheidt Soporus; sédatif comprenant de la myrrhe et de la réglisse
CN102579625A (zh) * 2012-03-07 2012-07-18 南京同仁堂药业有限责任公司 一种治疗风湿性关节炎的中药滴丸的制备方法
ITPD20120343A1 (it) * 2012-11-13 2014-05-14 Matteo Bevilacqua Composto in particolare per la cura della depressione e dell'ansia
ITUB20151928A1 (it) * 2015-07-06 2017-01-06 Lampugnani Farm S P A Composizioni comprendenti estratti di propoli ed estratti di boswellia

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH01245058A (ja) * 1988-03-25 1989-09-29 Soken:Kk 樹脂組成物
AU7715491A (en) * 1990-06-12 1991-12-19 Cathy Palou A therapeutic preparation containing myrrh for treating skin disorders
RO108643B1 (ro) * 1994-01-12 1994-07-29 Felician Titus Stoica Unguent pentru tratamentul arsurilor

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH01245058A (ja) * 1988-03-25 1989-09-29 Soken:Kk 樹脂組成物
AU7715491A (en) * 1990-06-12 1991-12-19 Cathy Palou A therapeutic preparation containing myrrh for treating skin disorders
RO108643B1 (ro) * 1994-01-12 1994-07-29 Felician Titus Stoica Unguent pentru tratamentul arsurilor

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
DATABASE WPI Section Ch Week 8946, Derwent World Patents Index; Class A60, AN 89-335017, XP002020077 *
DATABASE WPI Section Ch Week 9525, Derwent World Patents Index; Class B04, AN 95-191942, XP002020076 *
MICHIE C A; COOPER E: "FRANKINCENSE AND MYRRH AS REMEDIES IN CHILDREN", JOURNAL OF THE ROYAL SOCIETY OF MEDICINE 84 (10). 1991. 602-605., XP000610910 *

Cited By (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6680074B1 (en) 1997-08-11 2004-01-20 Andre Pierre Morice Composition comprising propolis and at least an essential oil
WO1999007396A1 (fr) * 1997-08-11 1999-02-18 Morice Andre Pierre Composition comprenant de la propolis et au moins une huile essentielle
FR2767062A1 (fr) * 1997-08-11 1999-02-12 Andre Pierre Morice Composition comprenant de la propolis
CN1094361C (zh) * 1997-08-11 2002-11-20 安德烈·皮埃尔·莫里斯 含有蜂胶和香精油的组合物
WO2000062751A3 (fr) * 1999-04-16 2001-01-18 Quest Int Compositions contenant des extraits de boswellia
WO2002056879A1 (fr) * 2001-01-03 2002-07-25 Medpharma Plc Utilisation de terpenes dans le traitement des infections du tube digestif
WO2002062362A3 (fr) * 2001-02-06 2003-11-20 Theodore Cherbuliez Composition antivirale et antibacterienne comprenant de la propolis
DE102005014334A1 (de) * 2005-03-24 2006-09-28 Franz Udo Willerscheidt SOPORUS Hypnotika/Sedativa und Psychopharmaka/Antidepressiva/Anxiolytika
DE102005014334B4 (de) * 2005-03-24 2009-06-10 Franz Udo Willerscheidt Sedativum umfassend Myrrhe, Süßholzwurzel und Wein
WO2006128634A1 (fr) * 2005-05-28 2006-12-07 Hans-Ulrich Jabs Extrait d'oliban (resine d'oliban) se presentant sous la forme de nanoparticules, et son utilisation
WO2008017280A1 (fr) * 2006-08-10 2008-02-14 Franz Udo Willerscheidt Soporus; sédatif comprenant de la myrrhe et de la réglisse
CN102579625A (zh) * 2012-03-07 2012-07-18 南京同仁堂药业有限责任公司 一种治疗风湿性关节炎的中药滴丸的制备方法
ITPD20120343A1 (it) * 2012-11-13 2014-05-14 Matteo Bevilacqua Composto in particolare per la cura della depressione e dell'ansia
WO2014076643A1 (fr) * 2012-11-13 2014-05-22 ZAGGIA, Guerrino Composé particulièrement utile pour le traitement de la dépression et de l'anxiété
ITUB20151928A1 (it) * 2015-07-06 2017-01-06 Lampugnani Farm S P A Composizioni comprendenti estratti di propoli ed estratti di boswellia

Also Published As

Publication number Publication date
EP0836478A1 (fr) 1998-04-22
AU6305896A (en) 1997-02-05

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