LECTURE 13 – Phytopharmaceuticals for external use, dermatologics – PART 1 Dr. Ivana Daňková Dept. of Natural Drugs, Faculty of Pharmacy, VFU Brno PHYTOPHARMACEUTICALS academic year 2018/19 DERMATOLOGICS 2  = preparations used topically  in case of skin diseases  for skin irritation, blood congestion (hyperaemia), induction a feeling of warm  for protection of health skin against external influences  Disinfectants, antiseptics, antibacterials, antivirals, antifungals  Antipruritics, antiseborrheic agents, antipsoriatics, antiscabietics  Astringents, antiphlogistics  Keratolytic, emollients  Preparations used for repairing wounds (re-epithelisation, re-granulation)  Preparations used to treat burns, frostbites,…  Preparations used to treat muscular injuries, contusions, external antirheumatics,… DERMATOLOGICS 3 SKIN DISEASES  are usually divided into two great classes – functional and organic  functional – affections of the skin, hair, sebaceous glands, sweat glands  organic – inflammations, infectious diseases, new formations and tumours, haemorrhages (bleeding),… DERMATOLOGICS 4 Topical dermatological formulations:  topical medications should be applied on the skin as a thin layer  contain an active ingredient and vehicle. Vehicle contains water, oil, fat, alcohol, propylene glycol,…  solutions  tinctures  lotions (emulsions), suspensions  ointments, creams, pastes  hydrocolloids, hydrogels  (talcum) powders  liquid powders  aerosol foams or sprays  adhesive plasters PHYTOPHARMACEUTICALS used forWOUND HEALING 5 WOUND  is defined as a breaking of cellular and anatomical or functional continuity of living tissue  there are four phases in the process of wound healing:  phase 1 – is the vascular response (blood coagulation)  phase 2 – is the inflammatory response that involves migration of neutrophils at margin of incision  phase 3 – is the proliferative phase which is characterized by angiogenesis, granulation (newly formed wound matrix, consisting of collagen, matrix proteins and proteoglycans), wound contraction, and epithelisation  phase 4 – is a remodelling phase involving continuous accumulation of collagen and proliferation of fibroblasts PHYTOPHARMACEUTICALS used forWOUND HEALING 6 Agents promoting wound healing:  astringents – they are able to precipitate proteins – „wound contracting“ ability. Antioxidant activity refers to the possible antibacterial activity.  disinfectants – act to disrupt significant cellular structures or processes in order to kill or eliminate microorganisms  antiphlogistic (anti-inflammatory) agents – are able to reduce inflammation  preparations promoting wound healing and repair, including re-epithelisation, and re-granulation ASTRINGENTS 7 TANNINS  polyphenolic compounds, they are composed of a very diverse group of oligomers and polymers; subdivided into two groups:  hydrolyzable tannins (gallotannins, ellagitannins)  condensed tannins (proanthocyanidines, catechins)  the main characteristic is that they bind and precipitate proteins = astringent effect  the word „tannin“ reflects a traditional technology „tanning“ (waterproofing and preserving) = transforming animal hides into leather  Biological effect:  astringent – externally: wounds healing, bleeding stop, treatment of burns, frostbites, oral cavity disorders,… ASTRINGENTS 8 GALLA Quercus infectoria (Q. lusitanica), Fagaceae, gall oak  native to Morocco, Portugal, Spain, Turkey,...  „nutgalls“ (Galla tinctoria, Turkish gall,…) are produced by the infection from the insect Cynips gallae tinctoriae  nutgalls are rich in the tannin content ASTRINGENTS 9 Plant drugs containing tannins very often from the family Rosaceae, e.g.:  Tormentillae rhizoma – Potentilla tormentilla (P. erecta), tormentil  Sanguisorbae radix – Sanguisorba officinalis, great burnet  Agrimoniae herba – Agrimonia eupatoria, agrimony  Alchemillae herba – Alchemilla vulgaris, lady´s mantle  Rubi idaei folium – Rubus idaeus, raspberry  Rubi fruticosi folium – Rubus fruticosus, blackberry (brambleberry)  Fragariae folium – Fragaria vesca, wild strawberry  Anserinae herba – Potentilla anserina ASTRINGENTS 10 Potentilla tormentilla rhizome Agrimonia eupatoria herb Rubus idaeus leaf Rubus fruticosus leaf Fragaria vesca leaf Sanguisorba officinalis root Alchemilla vulgaris herb ASTRINGENTS 11 Other plant drugs containing tannins:  Bistortae rhizoma – Polygonum bistorta (Bistorta major), Polygonaceae  Quercus cortex – Quercus robur, Q. petraea, Fagaceae  Ratanhiae radix – Krameria triandra, Krameriaceae  Juglandis folium – Juglans regia, Juglandaceae  Hamamelidis folium/cortex – Hamamelis virginiana, Hamamelidaceae  Hyperici herba – Hypericum perforatum, Hypericaceae  Myrtilli fructus/folium – Vaccinium myrtillus, Ericaceae  plants from the family Lamiaceae, e.g.:  Salviae officinalis folium – Salvia officinalis, sage ASTRINGENTS 12 Bistorta major rhizome Hamamelis virginiana leaf/bark Hypericum perforatum herb Juglans regia leaf Krameria triandra root Quercus robur Quercus petraea bark PHYTOPHARMACEUTICALS with ASTRINGENT EFFECT 13  AGRIMONY Herbal tea (Megafyt Pharma)  POR SPC 1X50GM  Agrimoniae herba Agrimonia eupatoria, Rosaceae  contains: tannins, flavonoids, small amount of essential oils  SUKL code: 0076589 Selected medicinal products  ATC: V11  it has healing effects (astringent, anti-inflammatory properties)  production: pour 500 mL of water over 2 spoons of the drug, boil briefly for 10 min and let stay another 15 min  decoction is used as a poultice (warm compress), bath, or for gargling PHYTOPHARMACEUTICALS with ASTRINGENT EFFECT 14 Astringent tincture:  Ratanhiae tinctura Gallarum tinctura Myrrhae tinctura  indication: as an astringent wash for the mucous membrane of the mouth, as a gargle in sore throat  Ratanhiae tinctura  production: 1 part of the drug and 5 parts of ethanol 70% (V/V)  tannin content is 1.0 % at least (expressed as pyrogallol)  Gallarum tinctura  production: 1 part of the galls and 6 parts of ethanol 60% (V/V), maceration, 3 days  tannin content is 1.5 % at least  Myrrhae tinctura  production: 1 part of the myrrh and 5 parts of ethanol 90% (V/V) PHYTOPHARMACEUTICALS used forWOUND HEALING 15 GUMMIRESINA MYRRHA, MYRRH  Commiphora abyssinica Commiphora molmol, Burseraceae  thorny trees native to Africa  contains: about 60 % polysaccharides and proteins, 25-40 % of resin, 3-10 % of essential oil, steroids,...  effects: anti-inflammatory, astringent, antibacterial, healing  indications: inflammation of the mucous membrane of the mouth (gingivitis, stomatitis), pharyngitis  usually as tincture (Myrrhae tinctura) or Myrrhae extractum spirituosum DISINFECTANT DRUGS 16  disinfectants – act to disrupt significant cellular structures or processes in order to kill or eliminate microorganisms  antimicrobial, antiviral, antifungal effect  synthetic drugs are predominantly used  plant drugs containing:  phenolic compounds  essential oils – usually with the free –OH group, e.g.: thymolterpinen-4-ol menthol eugenol DISINFECTANTS 17 Plants containing essential oils with disinfectant and usually also „counterirritant“ effect , e.g.:  Thymi herba – Thymus vulgaris, Lamiaceae  Menthae piperitae folium/herba – Mentha piperita, Lamiaceae  Salviae off. folium/herba – Salvia officinalis, Lamiaceae  Rosmarini herba – Rosmarinus officinalis, Lamiaceae  Juniperi fructus/lignum – Juniperus communis, Cupressaceae  Caryophylli flos – Syzygium aromaticum, Myrtaceae  Eucalypti folium – Eucalyptus globulus, Myrtaceae  Melaleucae folium – Melaleuca alternifolia, Myrtaceae (tea tree oil)  Pini pumilionis etheroleum – Pinus mugo var. pumilio, Pinaceae, (essential oil from the branches and needles of the tree) DISINFECTANTS 18 CARYOPHYLLI FLOS Caryophylli etheroleum  Syzygium aromaticum (Eugenia caryophyllus), Myrtaceae clove, clove oil  thorny trees native to Africa  contains: essential oil (contains 70-85 % eugenol, 10 % β-caryophyllene), tannins  effects: antibacterial, astringent, healing, anaesthetic  indications: topical preparations for treatment of small injuries and wounds, used usually in mouth infections and inflammation, in dentistry PHYTOPHARMACEUTICALS with HEALING EFFECT 19  Plant drugs with healing effects:  Matricariae flos – Matricaria recutia, Asteraceae  essential oil, containing mainly sesquiterpene compounds (bisabolol = levomenol, bisabolol oxides, chamazulene, guaiazulene), flavonoids, coumarins, polyacetylens, mucilage,…  Millefolii herba – Achillea millefolium, Asteraceae  similar composition, mainly azulenes PHYTOPHARMACEUTICALS with HEALING EFFECT 20  CHAMOMILE Herbal tea (Megafyt Pharma)  POR SPC 1X50GM  Matricariae flos  SUKL code: 0076578 Selected medicinal products  ATC: V11  CHAMOMILLA Teva SOL 1X25ML  Matricariae extractum fluidum = liquid extract of Matricariae flos  ammonium solution 10%, water and ethanol 96% (2.5 : 47.5 : 50)  SUKL code: 0162391, OTC  ATC: V11  external use: inflammatory diseases of skin and mucous membranes, poorly healing wounds, ulcers, burns… PHYTOPHARMACEUTICALS with HEALING EFFECT 21  DERMAZULEN (Zentiva) DRM UNG 1X30GM  in 30 g: Guaiazulenum 60 mg Matricariae etheroleum 30 mg  SUKL code: 0000843 OTC medicinal products  ATC: D03AX  OPHTALMO-AZULEN (Zentiva) OPH UNG 1X5GM  in 5 g: Guaiazulenum 7.5 mg  SUKL code: 0000874 OTC medicinal products  ATC: S01XA01 PHYTOPHARMACEUTICALS with HEALING EFFECT 22  Calendulae flos Calendula officinalis, Asteraceae, marigold  calendulosides (glycosides of oleanolic acid), essential oil (mono- and sesquiterpene compounds), flavonoids, triterpene alcohols, polyacetylenes, carotenes and xanthophylls,…  external preparations of the drug inhibit inflammation and promote the formation of granulation tissue  infusions, tinctures, ointments as a wound-healing remedy for inflammation of the skin and mucous membranes, for poorly healing wounds, bruises, ulcers, rashes… PHYTOPHARMACEUTICALS with HEALING EFFECT 23  MARIGOLD Preparations  ointments, creams, lotions  e. g. of Weleda, Galmed, Dr. Müller, Aromatica, Apotheke,…  suitable also for very small children  addition of other components:  Balsamum peruvianum  Propolis  Hippophae rhamnoides PHYTOPHARMACEUTICALS with HEALING EFFECT 24  Balsamum peruvianum Myroxylon balsamum var. pereirae Fabaceae  peru-balsam oleoresin, containing 45-70 % „cinnamein“ = mixture of cinnamic and benzoic acids benzylesters, and 6-8 % resin  used as antibacterial, antifungal, and antiparasitic agent in case of wounds, ulcerations, bedsores...; promotes re-epithelisation, and re-granulation of the tissue  a component of Balsamum Višněvski (Suspensio Višněvski cum balsamo peruviano) PHYTOPHARMACEUTICALS with HEALING EFFECT 25  Suspensio Višněvski cum balsamo peruviano  Bismuthi tribromphenolas basicum 5.0 g Balsamum peruvianum 20.0 g Ricini oleum virginale ad 100.0 g  Suspensio Višněvski cum pice liquida (HBF, Herbacos Recordati)  DRM SUS 1X100GM  Bismuthi tribromphenolas basicum 3.0 g Pix fagi seu Pix lithanthracis 5.0 g Ricini oleum virginale ad 100.0 g  SUKL code: 0054248  ATC group: D05AA PHYTOPHARMACEUTICALS with HEALING EFFECT 26 CICADERMA DRM UNG 1X30GM (Boiron)  composition in 100 g:  Extractum herbarum vaselinum 97.0 g Ledum palustre – tinctura basica a.u.h. 1.5 g Pulsatilla vulgaris – tinctura basica a.u.h. 1.5 g !!! (homeopathic mother tinctures)  SUKL code: 0097947 OTC medicinal product  ATC: V11 (Phytopharmaceuticals)  be careful of the St.John´s wort content (photosensibilization)  Extractum herbarum vaselinum pro CICADERMA  Calendulae herba recens 20.0 g Hyperici herba recens 10.0 g Millefolii herba recens 10.0 g Vaselinum album 100.0 g  promotes healing of smaller injuries on the skin surface (small cuts, cracks, abrasions), small burns, solar erythema, insect bites PHYTOPHARMACEUTICALS with HEALING EFFECT 27 HERBADENT GNG SOL 1X25ML (Herbadent)  composition in 25 mL:  Herbarum extractum fluidum 22.5 mL Acidum salicylicum 0.25 g Acidum boricum 0.25 g Acidum citricum monohydricum 0.125 g Benzocainum 0.0625 g Menthae pip. etheroleum 0.05 g Caryophylli floris etheroleum 0.05 g Foeniculi amari fr. etheroleum 0.025 g Ethanol 96 % (V/V)  SUKL code: 0191186 OTC medicinal product  ATC: V11 (Phytopharmaceuticals)  Herbarum extractum fluidum pro Herbadent:  Agrimoniae herba 5.0 g Matricariae flos 2.0 g Salviae off. herba 2.0 g Tormentillae rhizoma 1.0 g Ethanolum 96 % 77.0 g Aqua purificata 18.5 g  for treatment of oral cavity disorders. Antiphlogistic, astringent, mild anaesthetic properties.