LECTURE 9 – Preparations used to treat
diabetes. Hepatoprotective agents.
Dr. Ivana Daňková
Dept. of Natural Drugs, Faculty of Pharmacy, VFU Brno
PHYTOPHARMACEUTICALS
academic year 2018/19
PHYTOPHARMACEUTICALS
used to treat DIABETES MELLITUS
2
DIABETES MELLITUS
 a serious disease in which the body
cannot properly control the amount
of sugar in the blood → a high level
of sugar in the blood
 „Juvenile-onset“ diabetes (type 1)
– is caused by the destruction of
insulin-producing B cells in the
pancreas
 „Maturity-onset“ diabetes (type 2,
four subtypes)
– insulin resistance – increased
insulin requirement due to a loss of
insulin receptors on cell membranes.
PHYTOPHARMACEUTICALS
used to treat DIABETES MELLITUS
3
Type 1 diabetes
 = insulin-dependent diabetes →
necessity of insulin replacement
 insulin administration
(insulin pen, insulin pump)
 prevention of life-threatening
hyperglycaemic (diabetic) coma
 prevention of diabetic complications
 angiopathy with blindness, myocardial infarction, renal failure
 prevention of insulin over dosage leading to life-threatening
hypoglycaemic shock (CNS disturbance due to lack of glucose)
PHYTOPHARMACEUTICALS
used to treat DIABETES MELLITUS
4
Type 2 diabetes
 usually in overweight adults – diabetic metabolic condition
 there is a relative insulin deficiency – enhanced demand
cannot be met by a diminishing insulin secretion
 therapy of first choice is weight reduction!
 oral antidiabetics
 the sulfonylurea type antidiabetics
 biguanide derivatives
 alpha-glucosidase inhibitors
 incretin based therapies
 etc.
PHYTOPHARMACEUTICALS
used to treat DIABETES MELLITUS
5
Treatment of diabetes type 2:
 weight reduction – caloric restriction to restore body weight to
normal is associated with an increase in insulin receptor number
or cellular responsiveness. The releasable amount of insulin is
again adequate to maintain a normal metabolic rate.
 dietary management, physical activity
 blood glucose (glycaemic) control
 non-glucose sweeteners
 glucokinins and other natural compounds that are able to
decrease blood sugar
 prevention and treatment of microvascular complications
(retinopathy, nephropathy, neuropathy,…)
 prevention of macrovascular complications – treatment of
dyslipidaemia and hypertension
Herbal remedies for DIABETES
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 „glucokinins“
= compounds that are able to reduce blood-sugar level
 e.g. natural guanidine derivatives – are able
to low glycaemia by inhibiting absorption
and promoting metabolism of glucose
 chromium
 a component of the so-called glucose tolerance factor
– a low molecular weight chromium(III) complex
6
GUANIDINE
Herbal remedies for DIABETES
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Plant drugs containing „glucokinins“, chromium e.g.:
 Galegae herba – Galega officinalis, Fabaceae, goat's-rue
 galegine, the guanidine derivative, present in all parts; chromium salts
 Myrtilli folium/herba – Vaccinium myrtillus, Vacciniaceae, billberry
 neomyrtillin – a methoxylated glucoside of gallic acid; chromium salts
(chromium content about 9.0 ppm)
 Phaseoli fructus sine semine (Phaseoli pericarpium) – Phaseolus
vulgaris, Fabaceae, kidney-bean pods (without seeds)
 Foenugraeci semen – Trigonella foenum-graecum, Fabaceae,
fenugreek seeds
 Cinnamomi cortex – Cinnamomum zeylanicum, C. verum, Lauraceae
 (Salviae folium, Zingiberis rhizoma)
Herbal remedies for DIABETES
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Galega officinalis
herb
Vaccinium myrtillus
leaf/herb
Phaseolus vulgaris
pericarp (pods without seeds)
Trigonella foenum-
graecum
seeds
Cinnamomum
zeylanicum
bark
Herbal remedies for DIABETES
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Natural alternative sweeteners for diabetics
 they do not raise blood sugar levels
 sugar alcohols – xylitol and erythritol. They are absorbed into the
blood stream more slowly than sugar and are low in carbohydrate.
Rather than being stored in the body they are eliminated efficiently
in the urine.
 inulin
 Stevia leaf – Stevia rebaudiana, Asteraceae
 contains sweet-tasting substances – stevioside, rebaudiosides
(many times sweeter than sugar)
 helps bring down high blood sugar
Herbal remedies for DIABETES
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INULIN
 = fructan, a nondigestible polysaccharide of fructose units
(about 2 to 5 % of glucose)
 a storage carbohydrate found in many plants, especially in roots and
rhizomes of Asteraceae family plants (usually obtained from cichory
root), or in some fruits, seeds,... (e.g. banana, onion)
 as a food ingredient can decrease the blood sugar level
Herbal remedies for DIABETES
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Plant drugs containing inulin, e.g.:
 Cichorii radix – Cichorium intybus, Asteraceae
 Inulae radix – Inula helenium, Asteraceae
 Taraxaci radix – Taraxacum officinale, Asteraceae
 Bardanae radix – Arctium lappa, A. minor, A. tomentosum,
Asteraceae, burdock root – 27-45 % of inulin
 Yacon – Polymnia sonchifolia (Smallanthus sonchifolius),
Asteraceae – tubers (tuberous roots)
 Graminis rhizoma – Elymus (Agropyron) repens,
Poaceae – common couch
- contains „triticin“, a polysaccharide related to inulin
which on hydrolysis yields fructose
Plant drugs containing INULIN
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Cichorium intybus
root
Inula helenium
root
Polymnia sonchifolia
„yacón“ – tuberous roots
Arctium lappa
root
ANTIDIABETIC PREPARATIONS
Herbal teas
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 DIABETAN (Leros)
 POR SPC 20X1GM, 1X100GM
 composition, in 100 g:
Phaseoli fructus sine semine 17 g
Myrtilli herba 15 g
Salviae officinalis herba 15 g
Galegae herba 12 g
Polygoni avicularis herba 10 g
Taraxaci radix cum herba 8 g
Rubi fruticosi folium 8 g
Foeniculi amari fructus 8 g
Bardanae radix 5 g
Liquiritiae radix 2 g
 SUKL code: 0056234, 0001918
 ATC: V11
 It positively influences increased
blood sugar levels. It has diuretic,
antiseptic and slightly spasmolytic
effects.
 For diabetics, the tea is suitable
as a part of diet
 CI: Patients with gall bladder and
gall-duct ailments (especially with
bile stones), fresh peptic ulcers
 be careful in case of hypertension
(Liquiritiae radix)
ANTIDIABETIC PREPARATIONS
Herbal teas
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 Herbal tea for DIABETICS
(Megafyt Pharma)
 20 x 1.5 g
 Galegae herba
Phaseoli fructus sine semine
Myrtilli folium
Urticae folium
Salviae folium
Taraxaci radix
 Pavel VÁŇA DIABETIC TEA
 40 X 1.6 g
 Myrtilli herba
Galegae herba
Inulae radix
ANTIDIABETIC PREPARATIONS
Herbal teas
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 DIAHERB Herbal Tea
(Grešík)
 loose tea 50 g or tea bags
 Myrtilli folium
Phaseoli fructus sine semine
Urticae folium
Galegae herba
Cichorii radix
Graminis rhizoma
Bardanae radix
Salviae folium
Equiseti herba
 too many plant drugs!
 Diabetic tea with cinnamon
(Fytopharma, Slovakia)
 20 X 1.5 g
 Myrtilli herba
Cichorii radix
Cinnamomi cortex
Herbal remedies for DIABETES
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Gymnemae folium
 Gymnema sylvestre, Asclepiadaceae, „gurmar“
 a woody climbing plant native to the tropical
forests of southern and central India
 chewing the leaves suppresses the sensation
of sweet – „sugar-killer“
 has been used in Indian herbal medicine as
a treatment for diabetes for nearly 2.000 y.
 active principles: gymnemic acids
(oleanane-type triterpenoid saponins)
 inhibition of glucose absorption, stimulation
of insulin secretion (due to regeneration
of the pancreatic B cells), increase of glucose
utilization
ANTIDIABETIC PREPARATIONS
Herbal teas
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 Diabetic tea with gymnema (Leros)
 10 (20) tea bags x 1g
 Myrtilli herba 30 %
Galegae herba 15 %
Rooibos (Aspalathus linearis) 10 %
Phaseoli fructus sine semine 10 %
Myrtilli fructus 10 %
Polygoni avicularis herba 10 %
Salviae officinalis herba 5 %
Liquiritiae radix 5 %
Gymnemae folium 5 %
Herbal remedies for DIABETES
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 GURMAR tea (Nutraceutica)
 loose tea – 150 g
 drink warm; 2-3 cups per day
 Edenpharma GYMNEMA SYLVESTRE
(Medinterra)
 oral capsules
 350 mg of herbal extract (25%)
 GURMAR 50 cps. (Brainway Inc.)
 gelatine capsules
 200 mg of herbal extract in 1 capsule
 1-3 capsules per day
Herbal remedies for DIABETES
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 DIABEN
(Advance Nutraceutics)
 oral capsules
 Gymnema sylvestre, „gurmar“
 cinnamon – contains chromium
salts and polyphenolics that helps
to decrease blood sugar
 α-lipoic acid – antioxidant
properties (e.g. treatment
of diabetic neuropathy)
Active constituents Content in
1 capsule
Gurmar (75% extract of
Gymnema sylvestre)
200 mg
α-lipoic acid 100 mg
Cinnamomi cortex extract 100 mg
Gelatine capsules
α-lipoic acid
Herbal remedies for DIABETES
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 DIALEVEL
(Walmark)
 food supplement suitable for diabetics,
prediabetics with general preventive measures
(diets and exercising), for people with impaired
glucose tolerance and for overweight people
 α-lipoic acid 200 mg
Cinnamomum cassia extract 55.6 mg
Chromium(III) 60 µg
 use 1-2 tablets per day
α-lipoic acid
Herbal remedies for DIABETES
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 Stevia rebaudiana, Asteraceae
 commonly known as „sweet leaf“,
„sugar leaf“, „honey herb“, „yerba dulce“
 leaves contain sweet-tasting substances
that are 300 times sweeter than sugar
(sucrose)
 diterpene glycosides – mainly stevioside,
rebaudioside A
 used as a component of herbal teas and
other remedies for diabetes treatment;
as a dietary supplement and food additive
(but some countries restrict its use
as a sweetener)
stevioside
Herbal remedies for DIABETES
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 STEVIA
 natural sweetener – good solubility, nice taste
 suitable for diabetics, in diets
 available as tablets, in powder or liquid form
 one tablet contains usually about 7,5 mg of stevioside
 use maximally 2,5 mg of stevioside on each kg
of body weight per day
 as a sweetener in some phytomedicinal products, e.g.
Aromatica Herbal syrup with plantain leaf and stevia
 producers and brand names, e.g.:
 Advance Nutraceutics - Steviadiet
Dr. Popov – Fytostevin,
Naturprodukt – Additiva, Teekanne – Kandisin,…
HEPATOPROTECTIVE DRUGS
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LIVER = HEPAR
 a vital organ (gland) that performs essential
functions related to digestion, metabolism,
immunity and the storage of nutrients, e.g.:
 synthesis of proteins, hormones, enzymes,…
 production of biochemicals necessary for
digestion (e.g. bile)
 storage of glycogen, fatty acids, vitamins,
minerals,…
 decomposition of blood cells
 detoxification
 drug biotransformation and elimination
HEPATOPROTECTIVE DRUGS
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LIVER = HEPAR
 is necessary for survival;
without liver the tissues of the body
would quickly die from lack of energy
and nutrients
 the liver is the only human internal
organ capable of natural regeneration;
it has an incredible capacity for
regeneration of dead or damaged
tissues; it is capable of growing to
restore its normal size and function
 in case of irreversible liver failure
there is the only option of liver
transplantation
HEPATOPROTECTIVE DRUGS
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LIVER FAILURE
 acute liver diseases is less
common but more deadly (mortality 80 %)
 multi-organ failure, adult respiratory distress syndrome (ARDS),
acute renal failure, cirrhosis
 chronic hepatic disease
is the most common cause:
 chronic active hepatitis
 widespread necrosis from severe
damage of hepatocytes (due to
alcohol, poisonous mushrooms,
microorganisms, hepatotoxic
plants, medications,…)
HEPATOPROTECTIVE DRUGS
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LIVER PROTECTION
 high-quality diet – eat organic foods (be careful about pesticides),
use natural household products, limit harmful foods
 drink alcohol only in moderation (if at all)
 avoid smoking
 be careful with consumption of mushrooms and some plants
(e.g. from the family Asteraceae, Boraginaceae…)
 prevention of viral infections (hepatitis B, C – vaccination)
 be careful with medications – e.g. paracetamol (acetaminophen)
 do physical exercises
 detoxify your body regularly
 consider liver health supportive supplements
HEPATOPROTECTIVE DRUGS
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 Silybi mariani fructus
(Cardui mariae fructus)
Silybum marianum (Carduus marianus),
Asteraceae, milk-thistle herb
 1.5-3% silymarin, a mixture of various
flavanone derivatives (flavolignans) present
only in the fruit – the principal components are
silybin, silichrystin, silydianin, dehydrosilybin,
silybinomer
 as hepatoprotective agent – provides relief for
chronic liver problems; protects and promotes
the growth of liver cells, helps to reduce the
level of fat in the liver; antioxidative properties.
HEPATOPROTECTIVE PREPARATIONS
Herbal teas
28
 Milk thistle fruit
(Leros)
 loose tea, 150 g
 Boil 1 teaspoon of the drug for
5 minutes in ¼ L of water;
allow to steep for 10 minutes
in a covered container.
 Always prepare a fresh
serving.
 As a dietary supplement,
consume 1 cup per day.
 Milk thistle fruit
(Megafyt Pharma)
 loose tea, 130 g
 pour boiling water over the
crushed fruit; after 10-15 min
passed through a strainer
HEPATOPROTECTIVE PREPARATIONS
Herbal teas
29
 LIVER Herbal tea
(Megafyt Pharma)
 20 x 1.5 g
 Silybi mariani fructus
Coriandri fructus
Schisandrae fructus
Rooibos (Aspalathi herba)
Taraxaci radix cum herba
Menthae piperitae herba
Cynarae flos
Curcumae rhizoma
soluble silymarin (4 %)
 LIVER Herbal tea with
helichrysum (Apotheke)
 20 x 1.5 g
 Helichrysi flos (Stoechados flos)
Cardui benedicti herba
Agrimoniae herba
Taraxaci radix
Foeniculi fructus
Menthae piperitae herba
Cichorii radix
HEPATOPROTECTIVE PREPARATIONS
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 FLAVOBION
POR TBL FLM 50X70MG
(Takeda GmbH, Germany)
 Silymarinum 70 mg in one
coated tablet
 SUKL code: 0163138
OTC medicinal product
 ATC: A05BA03 (Silymarin)
 Indications: auxiliary treatment
of chronic persistent and active
hepatitis, liver cirrhosis, toxicmetabolic
liver injuries (liver
steatosis, poisoning,…)
 no evidence of toxicity – suitable
for long-term usage
 dosage: 1-2 tablets 3 times daily
 CI: hypersensitivity to any
component, not suitable for
children up to 5y.
HEPATOPROTECTIVE PREPARATIONS
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 LAGOSA
POR TBL FLM 50X150MG
(Wörwag Pharma, Germany)
 Cardui mariae fructus
extractum siccum (35-40:1)
204 mg (= 150 mg of silymarin)
 SUKL code: 0019570
 ATC: A05BA03
 on medical prescription only
 Indications: see FLAVOBION
 Dosage: depending on the severity
of the disease and the treatment
phase use 3 to 6 mg of silymarin/kg
of body weight per day – 1 tablet
twice (up to 3 times) per day. The
interval between doses should be at
least 4 hours. Treatment with the
initial dose lasts for 1-6 weeks, once
the condition is improved, the daily
dose may be reduced. The total
duration of treatment may last from
3 months to 1 year.
 The tablets are taken after a meal,
swallowed whole, not blown.
HEPATOPROTECTIVE PREPARATIONS
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 LIPOVITAN S tbl. (Herbacos-Bofarma)
 Silybum marianum fructus extract 80%
(140 mg of silymarin)
 maximal daily dose of silymarin = 420 mg
 LIPOVITAN Duo tbl. (Herbacos-Recordati)
 cholin 255 mg
SIM complex (silymarin 65 mg, inositol 50 mg,
L-methionin 25 mg)
B vitamins (B1, B2, B3, B5, B6, B12), vit. E
 SILYMARIN DUO (DaVinci Academia)
 oral capsules
 Silybum marianum fructus extract
Scutellaria baicalensis root extract
HEPATOPROTECTIVE PREPARATIONS
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 SILYMARIN 140 (Generica)
 60 capsules
 Cardui mariae fructus extractum 175 mg
(silymarinum 140 mg)
+ essential phospholipids 40 mg
 Dr. Theiss SILYMARIN forte (Generica)
 for liver and veins protection
 silymarin, blackcurrant seed oil, mixture
of ω-3 and ω-6 fatty acids
 Dr. Theiss SILYMARIN
 + yacon (Polymnia sonchifolia)
 + maca (Lepidium meyenii, Brassicaceae)
 + Selenium, + vit. D
HEPATOPROTECTIVE PREPARATIONS
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 LIVERAX
(Advance Nutraceutics)
 oral capsules
 Astragalus membranaceus
– used in Chinese traditional medicine for favourable activities on
immune system and liver
Active constituents Content in
1 capsule
Silybi mariani fructus
(content of silymarin 80 %)
200 mg
Astragalus membranaceus 50 mg
Cholin 50 mg
Curcuma 50 mg
α-lipoic acid 20 mg
HEPATOPROTECTIVE PREPARATIONS
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 ESSENTIALE FORTE N
POR CPS DUR
(Sanofi-Aventis)
 1 capsule contains:
phospholipida sojae praeparata
300 mg
 SUKL code: 0125752
OTC medicinal product
 ATC: A05BA
 essential soya phosholipids
 Indications: toxic-metabolic liver
damage, hepatitis. In the small
intestine, phospholipids are absorbed,
transformed into phosphatidylcholine,
which enters the liver through the
lymphatic and blood vessels.
Here it participates in regeneration
of damaged liver cells, restoration
of cell membranes.
 Dosage: 2 capsules 3 times a day
 KI: Hypersensitivity to soya, peanut,
or any other excipient
 Treatment with the product can not
prevent liver damage due to the use
of harmful substances (e.g. alcohol) !!