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1- Introduction about herbal and animal drugs and their
preparations:
Crud drugs are vegetable or animal drugs that consist of natural
substances that have undergone only the processes of collection
and drying.
Natural substances:
1- Plant origin: leaves, flowers, seeds and barks. Or vegetable
saps, extracts and secretions.
2- Animal origin: whole animals, glands or organs, extracts
and secretions.
Animal drugs are produced from wild animals (similar to wild
plants) or domesticated animals (similar to cultivated plants).
Wild animals must be:
1- Hunted e.g., musk deer.
2- Fished for cod liver oil
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Domesticated animals:
I- When drugs consist of insects, the drugs are either:
A- Collected from wild insects (cantharides) or
B- Definite attempts are made to cultivate them to:
1- Furnish the insects with food and
2- Shelter
To maintain optimum conditions for their propagation e.g.,
(honey bee).
II- When drugs consist of animals:
- Drugs such as hormones, endocrine products and some
enzymes are obtained from domesticated hogs, sheep or cattle.
- The slaughter house is the usual source of glandular products
and enzymes.
I- Cantharides:
Source: cantharides are the dried beatles Lytta vesicatoria,
Meloide.
Constituents: cantharides contain cantharidine.
Uses: cantharides are an irritant and rubefacient.
1- If taken orally: it is excreted by kidney and irritates the
urinary tract (aphrodisiac).
2- Topical application of solution containing cantharidine: it is
effective in the removal of warts.
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3- Now D/C, used only in veterinary (toxic).
II- Cochineal or coccus:
Source: It consists of dried female insects, Dactylopius coccus.
Constituents: it contains 10% glycosidic coloring principle
“carminic acid” which is anthraquinone derivative.
Uses: coloring agent in tooth pastes.
Source: musk is the dried distilled secretion from the preputial
follicles of the small, male, musk deer animal found in china
and himalaya.
Constituents: The distilled musk yields 1.4% of the dark brown
volatile oil muskone.
Uses: high class perfumes.
Source: cleaned, dried and powdered thyroid gland obtained
from domesticated animals e.g., Ox.
Constituents: thyroids contains 0.17% - 0.23% of iodine.
Uses: thyroid is used in goiter and obesity.
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Source: pepsin is a substance containing a proteolytic enzyme
obtained from glandular layer of the fresh stomach of the hog.
Constituent: Pepsin is prepared by digesting the minced
stomach lining with HCl. This solution is clarified and
evaporated in vacuum.
Uses: pepsin is used to assist gastric digestion.
Vegetable drugs are arranged for study as:
1- Alphabetic: The drugs are arranged in alphabetical order.
2- Taxonomic: The drugs are arranged according to the plant
source. Phyla, families, genera, species, variety (botanical
classification).
3- Morphological: The drugs are divided into:
Organized drugs:
Leaves, flowers, fruits, seeds, herbs and entire organisms,
woods, barks, rhizomes and roots.
Unorganized drugs:
Dried lattices, gums, resins, oils, fats and waxes.
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4- Pharmacologic or therapeutic: Grouping of drugs
according to the pharmacological action or therapeutic use.
5- Chemical: the drugs are divided into groups according to
their most important constituent:
1- Carbohydrate: e.g., starch, agar, pectin.
2- Glycosides: vanillin, barbaloin.
3- Lipids:
a- Fixed oils and fats are glyceryl esters of fatty acids
that are saponified by alkali: olive oil, peanut oil,
sesame oil, caster oil.
b- Waxes are esters of fatty acids with high molecular
weight monohydric alcohol e.g., bees wax.
4-Volatile oils (essential oils) e.g., peppermint oil, clove oil,
cinnamon oil, anise oil, rose oil that responsible of odor of
plants.
5- Steroids: are derivatives of cyclopentanophenanthrene
e.g., estrogens, androgens, cholesterol, ergosterol.
6- Alkaloids: they are nitrogenous, crystalline or oily
compounds. Usually basic in nature e.g., atropine,
morphine, quinine, cocaine and reserpine.
7- Peptide hormones: these are active principles secreted by
certain endocrine glands e.g., glucagons, insulin and
oxytocin.
8- Enzymes: organic catalysts that are produced by living
organisms e.g., pepsin, pancreatin, rennin.
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9- Vitamins: chemical compounds that are necessary for
normal growth and function of animals e.g., thiamine,
riboflavin, ascorbic acid, vitamin E.
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Antibiotics:
chemical
compounds
produced
biosynthetically that cause kill or inhibit microorganisms
e.g., penicillin, tetracycline, erythromycin…..
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Biologics:
A- Antigens or antibody preparations are capable of
developing a state of immunity in the patient e.g., hepatitis B
vaccine, IG, diphtheria antitoxin.
B- Biologics related to human food e.g., human albumin,
anti-heamophilic factor.
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Allergens substances that causes unusual responses
called hypersensitivity in individuals, e.g., pollen grains,
mold, spores, feathers, animal dander.
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Poisonous plants: some higher plants and fungi
produce toxic effects when introduced into the human
body e.g., nightshade, water hemlock, amanita.
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Pharmacopoeias:
They
are
books
recognized
by
the
governments as the legal authority for standard of drugs. The
united states pharmacopoeia is revised and reprinted every five
years.
Official drug: is one that listed and described as definite
therapeutic agent in pharmacopoeia.
Unofficial drug: is one that have not recognized in
pharmacopoeia. They are listed in unofficial books e.g., British
pharmaceutical codex.
The descriptive material pertaining to any of the drugs in the
pharmacopoeia is known as the monograph.
In the monograph of a crude drug, the following information
are generally covered:
1- Names English, Arabic, Italian, French.
2- Definition.
3- Description
4- Special conditions of collection or preparation for the
market.
5- Identity test.
6- Tests for adulterant.
7- Method of assay.
8- Special storage requirements.
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9- dose
1- Endogenous plant:
Plant is growing in native country, e.g., Hyoscyamus in
Egypt, Cannabis sativa in India.
2- Naturalized plant:
Plants are cultivated in foreign land or in locality other than
their native countries, e.g., cotton is naturalized in Egypt and
endogenous to America.
3- Exotic plant:
Plant is used in countries where neither cultivated nor
growing wild, e.g., tea, digitalis.
4- Marine drug:
It is a pharmacological active compound of marine origin,
e.g., agar, carageenan, code liver oil.
5- Crude drug:
Drugs of animal or vegetable origin undergo processes of
collection and drying only.
6- Commercial origin:
It is refers to its production and its channels trade, e.g.,
Alexandrian senna is the product growing in Khartom but it
was shipped by way of Alexandria.
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To evaluate a crude drug:
Can be established by actual collection of the drug from plants
or animals origin → +ve identified.
How to determine the origin of the samples:
1- "Drug gardens' established by institutions engaged in
pharmacognostical research.
2- Comparing unknown sample with a- a published
description drug or b- with authentic drug samples.
It is refers to the intrinsic value of the drug, i.e., the amount of
medicinal principle or active constituents present.
How obtain high grade of quality?
I- Collection of the drug from the correct natural source at the
proper time and in proper manner.
e.g1.,
Opium
(morphine,
codeine,
papaverine…..etc).
Origin: Papaver somniferum (induce sleep).
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thebaine,
Time of collection: a- must collect from green unripe capsule
(fruit). Why?
b- 2-3 weeks after flowering. Why? Because at this time obtain
a maximum morphine content (active constituent). But before
this time, alkaloids content mainly thebaine which is inactive.
Proper manner: capsules must be incision slowly in the
morning, not deep and not allow aqueous juice to
contaminate latex.
e.g 2., clove:
Origin: Myristica fragrance (nice aroma).
Proper time: flower buds from clove tree. Because contain
high % of A.C.
Proper manner: absence of stalk. In official book say no
more than 5% of stalk and mother clove to obtain high grade of
quality.
II- Preparation of the collected drug by proper cleaning,
drying and garbling.
e.g., 1- Ox thyroid gland
2- Under ground organs roots, rhizomes, corms and tubers.
III- Proper preservation of the cleaned, dried, pure drugs
against contamination with dirt, moisture, fungi, filth and
insects.
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Occurrence on the market (commercial forms):
I- Entire crude drugs as:
A- Seeds (Coffee, fenugreek, nut meg, cardamom, caliber
beans).
B- Flowers as a- Bud (clove)
b- Chamomile
c- Santonica
d- Safflower
C- Fruits: Anise, cumen, coriander, fennel from family
Umbellifereae.
D- Leaves as tea, menthe, senna, digitalis, henna.
E- Roots and rhizomes as licorice, ipeca, ginger, gensing.
F- Bark as cinnamon, cascara, frangula, cinchona.
1- Cut, broken, sliced.
1- Pressed drugs together by hydraulic pressure as in
cannabis.
2- Powdered and then molded into forms as rhubarb.
3- Cinnamon bark, remove cork and cortex and packed in
double quill of cigar length.
4- Quillaia bark come to the market in large flat pieces.
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5- Sennoside (4 types which A.C. of Senna leave used as
laxative).
6- Lanatoside, lanoxin® from digitalis leave.
7- Digoxin® from digitalis leave.
8- Atropine SO4 injection from Atropa belladonna.
9- Pilocarpine eye drops.
10- Physostigmine eye drops from caliber beans.
II- A- Exudates: it is normal secretion or pathological
product of animal or plant (i.e., under microscope has no
cellular structure, so called unorganized drug).
Normal secretion:
a- Latex: milky juice which is present normally in capsules of
Papaver somniferum.
b- Juice: liquid juice from aloe.
c- Bee wax
Pathological product:
Underdone some special physical treatment e.g., gum, resin,
oleo resin, oleo gum resin (myrrh). They occur in
1- Tears, small round masses e.g., Acacia.
2- Cylindrical pieces e.g., Gamboge.
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B- Galinical preparation:
a- Extract ‫خالصه‬
Definition: concentrate preparation of liquid or dry or
moderate consistence obtained from animal or plant source. It
is prepared by masuration or percolation methods using any
suitable solvent.
Preparation
One part of extract is equivalent to one part of original dried
drug w/w, v/w.
Dry drug (1 gm of drug extract ≡ 1 gm of original).
Liquid (1 ml of drug extract ≡ 1 ml of original).
Maceration:
Herb reduced into pieces, add suitable solvent, allow to stand for
2-7 days in close container, decant the extract.
Percolation:
Herb reduced into pieces, add suitable solvent, allow to stand for
few hours in pestle (percolator), the percolate allow to flow
slowly through tap.
b-Tincture ‫صبغه‬
1/10 from extract.
Preparation
1 part of drug + 10 parts of extract solvent, macurate or
percolate, extract, evaporation, residue.
Potency:
1 ml tincture = 0.1 (1/10) weight of drug.
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c- Infusion ‫منقوع‬
Used in: 1- Volatile oil containing drug “thermolabile”.
2- Drug containing water soluble constituent.
Concentrate infusion: 1 volume of tea or coffee + 1 volume
of water in pestle for few minutes to 2 hours (max).
1- Cold water: cold infusion.
2- Hot water: hot infusion.
3- 25% alcohol (75% water): alcohol is help to prevent
putrefaction.
Dilute infusion:
1 volume of conc infusion + 10 volume of water in pestle for
12 hours (max). Should add preservative why?
1- A.C. in the mixture form:
Volatile oil of clove, anise, cinnamon, chamomile.
2- A.C. in the single form …why?
Bitter almond oil in benzaldehyde.
Black mustard oil in allylisothiocyanate
Winter green oil in methyl salicylate.
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The evaluation of a drug involves a number of methods:
Definition: The entire description of official crude drug
monographs.
= Organs of sense = Macroscopic appearance of drug.
1- Shape and size (for entire drugs not powdered).
Flowers:
Floral parts: stigmas, corollas, anther, ovary, receptacle.
Leaves and leaflets:
Length, width, apex, margin, base, venation, the texture of the
leaf and the hairs in upper and lower surface. The feel of the
surface described as soft, hairy smooth.
The bark:
i- The barks occur in three shapes:
1- Flat or curved pieces.
2- Single quills.
3- Double quills.
ii- Barks have two surfaces, an outer and inner.
iii- The inner surface is usually lighter in color than the outer
surface.
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2- Odor and taste.
Odor:
1- distinct
2- indistinct
[Depend on the amount of volatile constituents present in drug].
General terms used in describing odor are:
1-aromatic,
2-balsamic,
3- spicy,
4- comphoraceous.
Taste:
General terms used in describing taste are:
1- Acid (sour)
2- Saccharine (sweet): indicates sugar or sugar like substances
e.g., liquorice.
3- Saline (salty)
4- Alkaline
5- Bitter: indicates presence of substances such as bitter
principle, glycoside, alkaloids.
6- Tasteless (all substances insoluble in the salive).
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7- Distinctive sensations to the tongue:
a- mucilaginous and oily (soft feeling) e.g., linseed.
b- astringent (contraction of the tissues oh the mouth) indicates
presence of tannin.
c- pungent (warm biting sensation) e.g., ginger.
d- acrid (irritant sensation) e.g., Aconite, coca.
e- nauseous (those tending to excite vomiting), Ipeca.
3- Color and external markings.
May help in revealing the nature of the herb.
1- White: e.g., starch, flours, gums, talk)
2- Pale yellow (yellowish white) e.g., ginger, squill, white
pepper.
3- Deep yellow: e.g., peeled liquorice, calumba, hydrastis.
4- Light pale brown e.g., lupulin, nux vomica, fennel, coriander,
anise.
5- Dark brown: e.g., cloves.
6- Dark reddish brown: cinchona, nutmeg.
7- Red: Kamala.
8- Pale green e.g., lobelia.
9- Greenish brown: most of the leaf herbs.
4- Fracture and internal color.
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Dealing with microscopic
appearance of the herb in sectional
view and in powdered form.
Microscopical evaluation is useful in the study of:
1- Histologic elements of herbs.
2- Detection of adulterant.
3- Quantitative microanalysis of admixed or adulterated
powders.
Histology refers to the character and arrangement of these
tissues as they are present in the herb. Histologic studies are
made from very thin transverse (radial) or longitudinal
(tangential) sections (entire organ) properly mounted in
suitable stains, reagents or mounting media.
Powdered herbs posses very few macroscopic features of
identification
outside
of
color,
odor
and
taste.
Microscopically, the cells are broken, except those with
lignified walls, but the cell contents are scattered in the powder
and become very evident in the mounted specimen e.g., starch,
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calcium oxalate crystals, aleurone, phloem, glandular and
nonglandular hair, pollen grain.
For the identification of powdered crude drugs
1- leaves:
a- Trichomes (glandular and nonglandular)
b- Crystals of calcium oxalate
c- Stomata, resin.
d- Epidermis cells, palisade,
e- Vessels
2- flower:
a- Trichomes (glandular and nonglandular)
b- Epidermis, stigma, anther.
c- Pollen grain
d- Volatile oil
3- Fruits and seeds:
Starch
Aleurone
Sclerenchyma
Vitta
Endocarp
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Bark & wood:
Phloem, xylem
Trachedes, Parenchyma, wood Parenchyma
Fibers, medullary rays, cork, cambium.
In some cases, the drug may have the same diagnostic element,
they are known as closely related species. So, microscope is
not the method of choice.
It is used to identify closely related species.
1-Microscopical linear measurement
Used only in Root Rhizomes Bark
E.g1., Different between Cinnamon ‫ القرفه السيالنيه‬as quill and
Cassia ‫ القرفه الصينيه‬as flat [Both have same diagnostic
element].
So differentiate between both by:
Microscopical linear measurement
Cinnamon
Cassia
1- Diameter of starch granules
< 8 μm
> 10μm
2- Width of phloem fiber
30 μm
30-45 μm
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Active constituent
Cinnamon
Cassia
Volatile oil
0.7-1% v/w
1-2%v/w
Cinnamic aldehyde
60-75%
Not less than 85%
Phenolics
4-10%
-
Eugenol
10%
-
Tast
Astringent
More astringent
Cost
Cheap
Cheaper
E.g2., Ipecacuanha
Starch granule
Rio Ipecacuanha
15 μm
Cartagena Ipecacuanha
17-20 μm
Why we need to differentiate between Rio and Cartagena
Ipeca?
Because Rio Ipeca contains more emetine alkaloid.
E.g3.,
Contain clusters of CaOx
American podophyllum
60-100 μm
Indian podophyllum
30-40 μm
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If closely related species are leaves: We need to
2- Ratio value:
1- Palisade ratio.
2- Stomata index.
3- Vein islet number.
4- Vein islet terminate number
1- Palisade ratio:
Def: numbers of palisade cell under one epidermal cell
using four continuous epidermal cells for the count.
To do the ratio value is determined by “camera
lucida” can transfer the microscopic field to
microscopic stage by using mirror.
Surface preparation:
Take leave, T.S., count and draw 4 epidermal cells,
then count and draw palisade cells under 4 epidermal
cells.
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2- Stomatal index (%):
Def: it is the percentage of the number of stomata to the
total number of epidermal cells including the stomata,
each stoma being counted as one cell.
Stomatal index= S/E+S x 100
(S) Number of stomata per unit area
(E) Number of epidermal cells in the same unit area.
The figure obtained is constant for any species and can
be used for the differentiation between the closely related
species.
3- Vein islet number:
Def of vein islet: The small areas of green tissue outlined
by the veinlets are temrmed vein islet.
Def of vein islet number: is the number of vein islet per
mm2.
This value has been shown to be constant for any species
and unaffected by the age of the plant or the size of the
leaves.
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How to determined the mm2 ?
By using Eye-peice micrometer and stage micrometer.
4- Veinislet terminate number:
Def: it is the number of veinlet termination per mm2 of
leaf surface.
A veinlet termination is the ultimate free termination of a
veinlet or branch of a vienlet. It can be used to
distinguish between leaves of closely related species.
It is the study of active constituents by the application of
chemical and physical methods to small quantities (a few
milligrams) of the drug in powdered form or to histologic
sections of the drug. It offers a means by which
constituents of many drugs may be isolated and purified.
It includes steps:
I- Isolation of A.C.:
A- By chemical solvents:
1- Micro-extraction
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2- Micro-filtration
3- Micro-crystallization
B- By micro-sublimation
II- Identification of constituents:
1- By crystallography
2- By melting point determination
3- By confirmative test
1- Chemical test.
2- Physical test
Microextraction:
Def:
It is a separation of the constituents from a small quantity
of the drug and depends on the solubility of the
constituents in a solvent.
During microextraction procedures, various factors
must be considered, such as:
1- State of division of the drug (whole, broken,
powdered)
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2- Type of solvent used with increase polarity
[Pet.ether,
chloroform,
ethylacetate,
butanol,
ethanol, methanol, water].
3- Temperature: [increase temperature lead to increase
solubility between solvent and extract].
4- Nature of impurities e.g., if impurities soluble in
certain solvent do not used this solvent.
5- Nature of substances e.g., volatile oil, fixed oil,
sterol, triterpenes, anthracene, coumarin, flavonoids,
alkaloids, etc.
 If soluble in polar solvent means it is a polar
compounds.
 If soluble in non-polar solvent means it is a
non-polar compounds.
 All substances soluble in 90-95% alcohol.
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alcoholic extract [hydroalcoholic extract]
evaporation
residue
methanol : water (70-30%)
aqueoues
saponine
sugar
pet.ether
1- fixed oil
2- v.o.
3- sterol
butanol
1-saponine
2-sugar
chloroform
1- triterpenes
2- cardiac glycosides
ethylacetate
1- flavonoids
2- alkaloids
3- coumarin
4- all glycosides
Why we need to add dilute acid on the aqueous
extract?
Hydroalcoholic solution, evaporation, residue, soluble in
methanol:water (70-30%), add dilute acid.
1- To convert alkaloid to salts.
2- Ionized form of phenol (phenate) converted to
unionized form of phenate.
********************
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Why we add NH4OH instead of NaOH?
NaOH is very strong base and it is not used because:
1- It is hydrolyzed ester alkaloids e.g., vinca
alkaloids (vincrystine and vinblastine), atropine
alkaloid and coca alkaloids.
2- Can open lactone ring in some alkaloids such as
pilocarbine.
3- Form water soluble un-extracted phenate of
phenolic alkaloids as morphine & psychotrine,
emetine and cephaeline in Ipeca alkaloids.
4- Break down glycosydic linkage in glycoside
compounds.
To secure small quantities of the extracted substances in
a clear solution generally requires microfiltration
methods to obtain the extracted constituent in a pure
form necessitates crystallization and re-crystallization.
Micro-crystallization:
If substances is soluble in methanol and insoluble in
ethylacetate. How can be crystallization?
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Microsublimation:
1- It is refer to a method of obtaining a constituent of a
drug by heating the drug to vaporize its chief
constituent to a gaseous state and then condensing the
vapor back into a solid form.
2- This method is employed only when the drug or its
constituents are not decomposed by heat.
3- When the constituent condenses on a cool place, the
resulting crystals develop in a pure form.
4- Caffeine is sublimed from powdered Kola or from
powdered coffee.
II- Identification of constituents:
1- By crystallography: It is a science dealing with:
i- Classification of crystals
ii- Form
iii- Structure
iv- Properties of crystals e.g., crystal is:
 Isotropic
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 Anisotropic
 Uniaxial
 Biaxial
 Its type of extinction
 Optic sign
 Sign of elongation
 Refractory index
2- By melting point determination:
It is very important as a means of identifying pure
substances.
3- By confirmative test:
1- Chemical test.
2- Physical test
e.g., menthol is isolated from peppermint oil. It occurs as
colorless, hexagonal crystals, usually needle like. The
melting point of l-menthol from natural sources is
between 41 and 43 C. when l-menthol is triturated with
an equal weight of camphor, chloral hydrate or phenol,
the mixture liquefies, thus confirming the identity.
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