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)
  • A61K36/28—Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
• • 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)
• • 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)
  • A61K36/81—Solanaceae (Potato family), e.g. tobacco, nightshade, tomato, belladonna, capsicum or jimsonweed
• • 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
  • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
  • A61K9/1682—Processes
• • 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
  • A61K9/20—Pills, tablets, discs, rods
  • A61K9/2095—Tabletting processes

Definitions

• the present invention is related to pharmaceutical compositions and to processes for its production. More specifically, the compositions of the present invention is oral and solid, and comprises as active principles dry artichoke extracts in association with other active ingredients. In a preferential embodiment of the invention, the composition comprises dry extracts of artichoke, boldo and jurubeba associated with magnesium sulphate and choline bitartrate, acting together as modulating agents of the gastrointestinal tract functions, including hepatic, biliary and gastrointestinal tract motility functions.
• the compositions of the present invention are stable and presented under the oral solid dosage form, overcoming difficulties of use, storage and production of the previously available compositions.
• the liver is an organ where several reactions occur, including the synthesis of many enzymes and reactions related to body detoxication.
• liver is very important to the health of the individual. Since the middle of the 16 th century, several books and scientific works about medicinal plants provide knowledge about innumerable useful plants which act as liver therapeutical agents, including boldo ⁇ Peumus boldus) and artichoke ⁇ Cynara scolymus).
• the artichoke In folk medicine, the artichoke is recommended for the treatment of indigestions caused by inadequate bile production, being also indicated as liver medicine and as cholagogue. It is generally used in aqueous alcoholic extract. The artichoke also provides significant diuresis, grounding its use as a dehydrating agent. On the other hand, artichoke leads to improved elimination of uric acid salts, grounding its use as an antirheumatic agent. In 1934, one of the first compounds having biological activity were isolated from artichoke leaves. In 1954, cynarine was identified and although absent from the extract it is produced during processing of the plant, when heated in aqueous environment. Some important composite classes present in the artichoke are flavonoids and caffeoylquinic acids.
• compositions were developed using generally basal leaves because they comprise higher levels of choleretic active principles.
• the composition of the present invention differs from the currently available artichoke compositions due to the fact that these compositions have artichoke associated with sorbitol (Miller), or artichoke associated with boldo (Vitamed/Herald's/Sim ⁇ es).
• composition of the present invention comprises as active principles dry extracts of artichoke, boldo and jurubeba associated with magnesium sulphate and choline bitartrate. This composition displayed very good results in clinical trial conducted at Grafee Guinle Hospital, in Rio de Janeiro, and filed in the Ministry of health (results not yet published). In addition, the composition of the present invention required the development of new excipients to enable direct compression.
• Document US 2003/044512 discloses a liver nutritional composition, containing vegetal extracts and adjuvants, such as amino acids and vitamins, which protects the liver against damages and promotes its regeneration, as well as improves its function.
• vegetal extracts and adjuvants such as amino acids and vitamins
• the composition described in this document neither discloses use the combination of dry artichoke extract with the associations of the present invention nor contains Magnesium Sulphate and Choline Birtartrate.
• Document WO 00/19973 describes compositions containing boldo extract to be used in cosmetic and/or dermatological preparations. However, such preparations don't aim any modulating action of the gastrointestinal tract activity and don't contemplate formulations such as the ones disclosed by the present invention.
• Document GB 912738 describes compositions with cholagogue and/or choleretic activities. However, such activity is due to cynnamic acid derivatives, and there isn't any mention neither to vegetal extracts nor to formulations such as the ones disclosed by the present invention
• compositions with the same purpose of those of the present invention are currently available, such compositions are different and present limitations: (i) the compositions in liquid form have several disadvantages related to stability and to difficulties in the production and use; and (II) the ones available in dry form don't use the dry artichoke extract in combination with the associations of the present invention, and don't comprise neither Magnesium Sulphate nor Choline Bitartrate, and also present many stability problems, like hygroscopicity, which makes the production difficult and its shelf-life smaller.
• compositions of the present invention were successfully overcome by the compositions of the present invention, and by its preparation process, in order to make available stable solid formulations containing vegetal extracts and chemical substances acting together as cholagogues, choleretics, hepatoprotectors, etc to modulate the gastrointestinal function.
• an oral solid pharmaceutical composition comprising as active principles dry artichoke extracts in association with selected ingredients of the group that consists of: hepatoprotector agents, cholagogues, laxatives, stimulants of the digestive function, lipotropic and/or gastrointestinal motility agents, or combinations thereof.
• the oral solid pharmaceutical composition comprises as active principles dry extracts of artichoke, boldo and jurubeba, in association with Magnesium Sulphate and Choline Bitartrate.
• an oral solid pharmaceutical composition endowed with improved stability.
• the present invention comprises pharmaceutical compositions containing modulator agents of the gastrointestinal tract functions.
• the expression "gastrointestinal tract functions" comprises the activities played by the liver, bile and the gastrointestinal motility. Many studies showed that some ingredients can play more than one role, acting, for example, as modulator of the biliary secretion and as hepatoprotector.
• the administration route normally is carried through oral liquids.
• the oral liquids can be presented in the form of extracts, dispersions and emulsions in which the active principle is diluted together with other pharmacologic excipients used in the formulation.
• This therapeutical administration method is widely used for pediatric or geriatric use, when the users may have difficulties on the medicine ingestion.
• the oral liquids present the disadvantage of the having a considerable volume, making its container difficult to be transported when there is necessity of user locomotion.
• the content has to be homogenized before the use and also has to be correctly dosed, using an appropriate and previously clean measuring device.
• the administration in the solid and/or dried form is efficient in many aspects, because it facilitates the ingestion of the medicine in different dosages without requiring volume measurements. Moreover, the solid and/or dried form provides the advantage of being compact and easy to transport, being able to be taken in the pocket.
• the solid and/or dried form of the present invention demonstrated a lower microbial growth susceptibility during the storage time, favoring the conservation of the medicine and its respective validity.
• the solid and/or dried form can be presented as a tablet containing a core with a composition based on the active ingredients, used individually or collectively with pharmaceutically acceptable and conventionally used ingredients, such as disintegrant excipients (sodium crosscarrnellose or another), lubricant (magnesium stearate or another), agglutinants (microcrystalline cellulose or another) and binders (povidone k-30 or another).
• disintegrant excipients sodium crosscarrnellose or another
• lubricant magnesium stearate or another
• agglutinants microcrystalline cellulose or another
• binders povidone k-30 or another
• the present invention comprises oral solid pharmaceutical compositions containing as active principles dry artichoke extracts in association with ingredients selected from the group consisting of: hepatoprotector agents, cholagogues, laxatives, stimulants of the digestive function, lipotropic and/or of gastrointestinal motility agents, or combinations thereof.
• Artichoke extracts (Cynara scolymus L) are known for its diuretic activities, promoting greater water elimination due to the increase of diuresis.
• the association of these extracts with the above-mentioned ingredients provides synergic effects, being the mechanism of action of the additional ingredients detailed below.
• the biliary secretion modulators are generally known as cholagogues, which are responsible for the increase of the bile and/or choleretic flow, that are responsible for the increase of the production of bile.
• Some examples of cholagogues generally used are the extracts of plants, such as, Achillea millefolium, Arctium lappa, Baptisia tintoria, Berberis vulgaris, Calendula officinalis, Chelidonium majus, Chionanthus virginicus, Curcuma Ionga, Cynara scolymus, Gentiana l ⁇ tea, Lavendula angustif ⁇ lia, Mentha piperita, Rheum officinalis, Rosmarius officinalis, Sanguinaria canadensia, Schisandra chinensis, Stillingia sylvatica, Taraxacum officinale, Verbena officinalis, Solanum paniculatum L.
• the gastrointestinal motility modulators can be subdivided in 2 classes: laxatives and producers of constipation.
• Laxatives are substances that increase the peristalsis, promoting the regular movement of excrements. Many substances can act in this way, such as alimentary fibers, fibers of Psyllium
• anticholinergic agents antipsychotic and antiparkinsonian
• cations containing agents aluminum, calcium, bismuth and iron salts, sucralfate
• others such as the calcium channel blockers, diuretics, anti-inflammatories, opioids substances, clonidine, ganglion blockers.
• Substances which protect the liver and stimulate cell regeneration include vegetal extracts such as extracts of Peumus boldo, Solanum paniculatum, Silybum marianum.
• Lipotropic agents help on the reduction of the cholesterol blood levels, stimulate lecithin production and reduce production of fat in the liver and rest of the body.
• Some lipotropic agents generally used are methionine and choline bitartrate.
• the oral solid composition comprises dry artichoke extracts, boldo and jurubeba, in association with Magnesium Sulphate and Choline Bitartrate.
• Table I presents the ingredients, their concentrations and their respective functions in the composition of the present invention. Table I - Fomulation
• compositions of the present invention can be prepared by a process that comprises the following steps:
• the dried and granulated material can be encapsulated by processes known in the state of the art.
• the dried and granulated material obtained at the previous step can be tabletted. Therefore, an additional step is required, adding magnesium stearate, sodium croscarmellose and silicon dioxide (additive of tabletting) to the dried and homogenized pellet of the previous step, of followed by complete homogenization; and

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• Health & Medical Sciences (AREA)
• Natural Medicines & Medicinal Plants (AREA)
• Life Sciences & Earth Sciences (AREA)
• Pharmacology & Pharmacy (AREA)
• Chemical & Material Sciences (AREA)
• Engineering & Computer Science (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Medicinal Chemistry (AREA)
• Animal Behavior & Ethology (AREA)
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• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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• 2005
  • 2005-09-14 BR BRPI0504985-7A patent/BRPI0504985A/pt not_active IP Right Cessation
• 2006
  • 2006-09-12 WO PCT/BR2006/000183 patent/WO2007030902A2/en not_active Ceased

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