LECTURE 8 – Preparations used to treat
some disorders of digestive system - II
Dr. Ivana Daňková
Dept. of Natural Drugs, Faculty of Pharmacy, VFU Brno
PHYTOPHARMACEUTICALS
academic year 2018/19
PHYTOPHARMACEUTICALS
vs. Digestive system (GIT = Gastrointestinal tract)
2
Major disorders of GIT that can be treat by phytomedicines:
 digestive disorders
 damaged mucosa of GIT
 ulceration
 inflammation (pharyngitis,
gastroenteritis)
 diarrhea/constipation
 vomiting
 infection, intoxication
Treatment of PEPTIC ULCERS
3
 in the area of a gastric and duodenal peptic ulcer, the mucosa has
been attacked by digestive juices = „self-digestion“
 usually the acid concentration is too high, or the protective effect
of mucus on the mucosal surface is decreased
 other cause is Helicobacter pylori infection
 Therapeutic aims:
 relief of pain and acceleration
of healing to lessen the risk
of dangerous complications
 Two therapeutic approaches:
 reduction of H+ concentration
 mucosal protection
Treatment of PEPTIC ULCERS
4
 I. Drugs for lowering acid concentration
 Ia – Acid neutralization = antacid drugs – containing H+
binding groups
 sodium bicarbonate, calcium carbonate, magnesium hydroxide,
aluminium hydroxide
 nonabsorbable antacids are preferred
 Ib – Inhibition of acid production – acting on their
respective receptors
 II. Protective drugs
promotes the mucus production → coating of mucosal defects
 sucralfate, misoprostol, colloidal bismuth compounds
 carbenoxolone
 mucilaginous plant drugs
Treatment of PEPTIC ULCERS
5
 CARBENOXOLONE
 is a derivative of glycyrrhetinic acid
(Liquiritiae radix, Glycyrrhiza glabra,
Fabaceae – liquorice)
 stimulates mucus production
 it is practically obsolete in this
indication
 it has also aldosterone-like effect that
promotes renal reabsorption of NaCl
and water, therefore, exacerbate
hypertension, congestive heart failure,
or swellings (oedemas)
Treatment of PEPTIC ULCERS
6
 Plant drugs containing mucilage, e.g.:
 Althaeae radix/ folium – Althaea officinalis, Malvaceae,
marshmallow
 Malvae folium/ flos – Malva sylvestris, Malvaceae, common
mallow
 Farfarae folium flos– Tussilago farfara, Asteraceae, coltsfoot
 Plantaginis folium – Plantago lanceolata, Plantaginaceae,
plantain
 etc.
Treatment of PEPTIC ULCERS
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Althaea officinalis
leaf/root
Malva sylvestris
leaf/flower
Tussilago farfara
leaf/flower
Plantago lanceolata
leaf/seed coat
LAXATIVES
8
 = drugs that relieve constipation,
a symptom that refers to irregularly
passing stools due to decreased
bowel function or diet that doesn´t
include enough fluids and fiber
 Laxatives can increase bowel
movements, promote bowel
evacuation by acting locally to
 stimulate intestinal peristalsis
 to soften bowel content
 or both
LAXATIVES
9
 Classification of laxatives:
 Bulk laxatives – distention of the intestinal wall by bowel
contents (increased filling of the bowel) stimulates
propulsive movements of the gut musculature (peristalsis)
 Irritant laxatives – purgatives, cathartics – exert an irritant
action on the enteric mucosa. Consequently, less fluid is
absorbed than is secreted – increased filling of the bowel
promotes peristalsis. Excitation of sensory nerve endings
elicits enteral hyper motility.
 Lubricant laxatives – no absorbable liquids (e.g. glycerol)
make faeces softer and more easily passed
LAXATIVES
10
BULK LAXATIVES
 vegetable fibers – rich in cellulose (component of plant cell
walls) = indigestible polysaccharide that is resistant to
digestive enzymes
 e.g. bran = cereals pericarp
 hydrophilic colloids, bulk gels – insoluble and
nonabsorbable carbohydrate substances (polysaccharides)
that expand on taking up water in the bowel
 mucilage drugs
 osmotically active laxatives – soluble but nonabsorbable
particles that retain water in the bowel due to their osmotic
activity
 salts (e.g. Glauber´s salt – sodium sulphate), polyhydric
alcohols (mannitol, sorbitol), disaccharide lactulose
LAXATIVES
11
IRRITANT LAXATIVES (PURGATIVES, CATHARTICS)
 these laxatives are distinguished according to the site of
irritation
 the small bowel irritant
 ricinoleic acid – in Castor oil
 the large bowel irritant
 anthraquinone derivatives
 synthetic drugs
– diphenolmethane derivatives
LAXATIVES
12
 RICINI OLEUM = Castor oil
– the oil obtained from the first cold-pressing
of the seed of Ricinus communis,
Euphorbiaceae (castor bean)
 ricinoleic acid
– major component
 oral administration of 10-30 mL of castor oil
is followed within 0.5 to 3 hours by discharge
of water stool
 very strong, massive effect ! – castor oil is
hardly suitable to treat ordinary constipation
 it can be employed after oral ingestion of a
toxin in order to hasten elimination and to
reduce absorption of the toxin from the gut
LAXATIVES
13
 ANTHRAQUINONE DERIVATIVES
 compounds derived from anthracene
and have a variable degree of oxidation,
in plants usually present as glycosides
 in the colon, they are hydrolyzed
by the β-glucosidases of the intestinal
flora, and the free anthraquinones are
reduced into active form = anthrones
 anthrones increase the secretion
of electrolytes and water and affect
intestinal motility
 the latency between drug intake
and laxative effect is 6 to 12 hours.
 daily dose is max. 30 mg of hydroxyanthracene
derivatives
LAXATIVE HERBAL DRUGS
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Plant drugs containing anthraquinone derivatives, e.g.:
 Frangulae cortex – Rhamnus frangula (Frangula alnus),
Rhamnaceae, frangula
 Rhamni purshianae cortex – Rhamnus purshianus (Frangula
purshiana), Rhamnaceae, Cascara sagrada
 Rhamni cathartici fructus – Rhamnus catharticus, Rhamnaceae,
purging buckthorn
 Rhei radix – Rheum officinale and/or R. palmatum Polygonaceae,
rhubarb
 Sennae folium/fructus – Cassia senna (C. acutifolia) and/or
C. angustifolia, Fabaceae, Alexandrian or Tinnevely senna
 Aloe – Aloe barbadensis, A. capensis, Xanthorrhoeaceae, aloe
LAXATIVE HERBAL DRUGS
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Rhamnus catharticus
fruit
Rhamnus frangula, R. purshiana
bark
Rheum officinale
Rheum palmatum
root/rhizome
Cassia senna, C.angustifolia
leaves/fruits
Aloe barbadensis
Aloe capensis
leaves – juice
LAXATIVES
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 Contraindication of purgatives, irritant laxatives:
 intestinal congestion, sudden abdominal episodes,
inflammatory diseases of the colon, abdominal complaints of
unclear origin
 children up to 10 years of age
 pregnant and nursing women

Warning:
 persons with heart and kidney illnesses, accompanied by
swellings, should be careful
 chronic usage can lead to dependence (habit-forming
syndrome) which can cause fluid and electrolyte imbalance
LAXATIVE HERBAL DRUGS
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Plant drugs containing mucilage and gums, e.g.:
 Lini semen – Linum usitatissimum, Linaceae, flax
 Psyllii semen – Plantago afra (Plantago psyllium), Plantago indica (P.
arenaria), Plantaginaceae
 Plantaginis ovatae semen – Plantago ovata (P. ispaghula),
Plantaginaceae, blond plantain, Indian plantago
 Agar – obtained from red algae – Gelidium, Rhodophyta
 a vegetable gums produced mostly as an exudate of various plants:
Gummi arabicum, Acaciae gummi – Acacia senegal, Fabaceae
Tragacantha, gum tragacanth – Astragalus gummifer, Fabaceae
Guma guar – from the seeds of Cyamopsis tetragonoloba, Fabaceae
Karaya gummi – trees of the genus Sterculia, Malvaceae
LAXATIVE HERBAL DRUGS
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Psyllium afra (Plantago psyllium)
seed (seed coat)
Psyllium indica (P. arenaria)
seed (seed coat)
Plantago ovata (P. ispaghula)
seed (seed coat)
Linum usitatissimum
seed
Gelidium
„agar“
LAXATIVE PREPARATIONS
Herbal teas
19
 LAXATIVE Herbal Tea
(Megafyt Pharma)
 POR SPC 20X1.5GM
 Sennae folium 750 mg
Menthae pip. herba 300 mg
Foeniculi fructus 150 mg
Liquiritiae radix 150 mg
Millefolii herba 150 mg
in 1 tea bag (1.5 g)
 SUKL code 0084374
 ATC: V11
 laxative preparation, mild
antiphlogistic and carminative
effects
 one tea bag (1.5 g) contains
12.5 mg of hydroxyanthracene
derivatives, sennosides
(maximal daily dose = 30 mg)
 suitable for adults and children
over 12y.
LAXATIVE PREPARATIONS
20
 Bio PSYLLIUM –
ISPAGHULA
(Megafyt Pharma)
 150 g
 Plantago psyllium
Plantago ovata
– seed coat (testa)
 PSYLLIUM
– many producers, various
packages
LAXATIVE PREPARATIONS
21
 PSYLLIUM cps.
(Medicol, Dr. Popov,
PharmaLine...)
 LEPICOL (ASP Czech s.r.o.)
 various products – as loose powder
or in capsules
 a multi-fibre source product
containing gentle psyllium husk
 + inulin (fructooligosaccharides from
Cichorium intybus root)
 + probiotics (Lactobacillus sp.,
Bifidobacterium bifidum)
 + digestive enzymes
 suitable also for children
LAXATIVE PREPARATIONS
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 FRUCTOLAX
(ORTIS Laboratoires)
 chewing cubes, tablets, syrup
 Ficus carica
Rheum palmatum/R. officinale
Guma guar (Cyamopsis tetragonoloba)
Tamarindus indica pulp
Phoenix dactylifera concentrate
wheat syrup
LAXATIVE PREPARATIONS
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 LAXAFRUIT (Vaminter S.L.)
 chewing cubes
 in 100 g:
paste from Ficus carica 62.9 g
syrup from Agave 12.6 g
Psyllium Husk (from Plantago ovata) 10.5 g
Rheum rhabarbarum (leaf stalks) 4.2 g
Tamarindus indica – legume pulp 3.4 g
plums (Prunus domestica) 2.1 g
oat fibre (Avena sativa) 2.5 g
Anisi fructus 0.8 g
yoghurt powder 0.5 g
inulin 0.5 g
 dosage usually 1 cube a day,
wash down with 2 dL of water.
DIARRHEA, DIARRHOEA
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Causes Examples
Viral infections Rotavirus, Norwalk virus
Bacterial infections E. coli, Vibrio cholerae, Campylobacter, Shigella,
Salmonella
Parasites Giardia, Entamoeba
Helminths (intestinal worms) Strongyloides
Allergic Lactose intolerance, celiac sprue, medication
side effects
Autoimmune Ulcerative colitis, Crohn's disease
Malabsorptive Pancreatic deficiency, biliary disease
Nutritional Zinc deficiency, vitamin A deficiency, enteral
feedings consisting of liquid nutritional formulas
delivered straight to the bowels
Functional Irritable bowel syndrome, short bowel syndrome,
cancer
ANTIDIARRHEAL AGENTS
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 Causes of diarrhea – gastroenteritis:
 bacteria/viruses – invade the gut wall
cause inflammation characterized by
increased fluid secretion into the lumen.
The enteric musculature reacts with
increased peristalsis. Some bacterial
toxins (e.g. Vibrio cholerae) inhibit ability
of mucosal enterocytes to absorb sodium
(Na+) and water, and, at the same time,
stimulate mucosal secretory activity
 The aims of antidiarrheal therapy are:
 to prevent dehydration and electrolyte
depletion
 to prevent excessively high stool frequency
ANTIDIARRHEAL AGENTS
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 Classification:
 adsorbent powders – nonabsorbable material
with a large surface area. These binds different
substances including toxins, permitting them
to be inactivated and eliminated.
Medicinal charcoal – the recommended effective
dose is in the range of 4-8 g. Other absorbents:
kaolin (hydrated aluminium silicate), chalk.
 oral rehydration solution – solution containing
salts and glucose
 opioids – inhibition of propulsive peristalsis.
Opium tincture (CNS effects !) → synthetic
derivatives with peripheral action
 antibacterial drugs
 astringents – tannins – cause precipitation
of mucosa surface proteins, „sealing“ of mucosa
ANTIDIARRHEAL AGENTS
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Plant drugs containing tannins, e.g.:
 Tormentillae rhizoma – Potentilla erecta (P. tormentilla),
Rosaceae, tormentil
 Bistortae rhizoma – Polygonum bistorta (Bistorta major),
Polygonaceae, common bistort
 Quercus cortex – Quercus robur, Q. petraea, Fagaceae, oak
 Sanguisorbae radix – Sanguisorba officinalis, Rosaceae, great
burnet
 Agrimoniae herba – Agrimonia eupatoria, Rosaceae, agrimony
 Myrtilli fructus/folium – Vaccinium myrtillus, Ericaceae, bilberry
 Fragariae folium – Fragaria vesca, Rosaceae, wild strawberry
 Alchemillae herba – Alchemilla vulgaris, Rosaceae, lady´s mantle
ANTIDIARRHEAL AGENTS
28
Potentilla tormentilla
rhizome
Vaccinium
myrtillus
leaf/fruit
Bistorta major
rhizome
Quercus robur
Quercus petraea
bark
Alchemilla vugaris
herb
Sanguisorba officinalis
root
Agrimonia eupatoria
herb
ANTIDIARRHEAL AGENTS
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Plant drugs containing tannins, e.g.:
 Rubi idaei folium – Rubus idaeus, Rosaceae, bramble leaf
 Rubi fruticosi folium – Rubus fruticosus, Rosaceae, raspberry leaf
 Juglandis folium – Juglans regia, Juglandaceae, walnut leaf
 Hamamelidis folium/cortex – Hamamelis virginiana,
Hamamelidaceae, witch hazel leaf/bark
 Salviae officinalis folium – Salvia officinalis, Lamiaceae, sage
 Theae folium – Thea sinensis, Theaceae, fermented (black) tea
ANTIDIARRHEAL PREPARATIONS
Herbal teas
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 TORMENTAN
(Leros)
 POR SPC 20X1.5GM
 Myrtilli fructus 480 mg
Tormentillae rhizoma 300 mg
Sanguisorbae radix 300 mg
Matricariae flos 105 mg
Salviae officinalis folium 105 mg
Menthae piperitae herba 105 mg
Liquiritiae radix 105 mg
in 1 tea bag (1.5 g)
 SUKL code: 0043957
 ATC: V11
 do not allow the tea to boil
 drink warm and unsweetened
3 times a day after meals.
 traditional herbal preparation
for diarrhoeal ailments.
It has anti-inflammatory
properties, soothes flatulence
and relieves spasm.
 suitable for adults and
children over 12y.
ANTIDIARRHEAL PREPARATIONS
Preparations containing tannins
31
 TASECTAN
CPS 15x 500 MG or sachets 20x 250 MG
(Pharma Swiss/Ocean Healthcare, Ireland)
 contains gelatin tannate
 suitable for babies, children and adults
as well
 use every 6 hours until the symptoms
disappear. It is usually effective within
12 hours.
ANTIDIARRHEAL PREPARATIONS
Adsorbent powders
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 CARBO MEDICINALIS
POR TBL NOB 20X300MG
(Icn Polfa)
 SUKL code: 0057338
 ATC: A07BA01
 dosage:
- in case of mild disorders:
600-1500 mg (2-5 tbl.) 3-4 times
a day
- in case of serious diarrhoeal
ailments – 3000-3600 mg
(10-12 tbl.) 3-4 times a day
 CARBOSORB
POR TBL NOB 20X320MG
POR PLV 1X25GM
(Imuna Pharm)
 SUKL code: 0031951;
0000982
 ATC: A07BA01
ANTIDIARRHEAL PREPARATIONS
Oral solid forms
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 EUCARBON POR TBL NOB 30
(SEDICO/F. TRENKA, Austria)
 Sennae folium pulveratum 105 mg
Rhei extr. siccum normatum 25 mg
Carbo vegetalis 180 mg
(vegetable charcoal)
Sulfur depuratum 50 mg
Foeniculi etheroleum 0.5 mg
Menthae pip. etheroleum 0.5 mg
 SUKL code: 0049998
OTC medicinal product
 ATC: A06AB56 (Sennosides,
combinations)
 dosage: 1-2 tablets up to 3 times daily
 Eucarbon® is a mild laxative with
prominent regulatory properties
to the intestinal functions.
 charcoal adsorbs metabolic/
bacterial toxins
 the addition of Senna & rhubarb
hastens the elimination of the
charcoal-toxins complex, reduces
intestinal desorption of the drug.
 The essential oils relieve flatulence