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.

4- Pharmacologic or therapeutic: Grouping of drugs

according to the pharmacological action or therapeutic use.

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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.

10- Antibiotics: chemical compounds produced

biosynthetically that cause kill or inhibit microorganisms

e.g., penicillin, tetracycline, erythromycin…..

11- 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.

12- Allergens substances that causes unusual responses

called hypersensitivity in individuals, e.g., pollen grains,

mold, spores, feathers, animal dander.

13- 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. 9- dose

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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, thebaine,

papaverine…..etc).

Origin: Papaver somniferum (induce sleep).

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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- Infusionمنقوع

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.

The evaluation of a drug involves a number of methods:

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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.

2- Odor and taste.

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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).

7- Distinctive sensations to the tongue:

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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,

calcium oxalate crystals, aleurone, phloem, glandular and

nonglandular hair, pollen grain.

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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

Bark & wood:

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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 السيالنيه as القرفه

quill and Cassia الصينيه as flat [Both have same القرفه

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 Cartagena Ipecacuanha 15 μm 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 CaOxAmerican podophyllum Indian podophyllum60-100 μm 30-40 μm

If closely related species are leaves: We need to

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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.

2- Stomatal index (%):

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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

2- Micro-filtration

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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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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.

********************

Why we add NH4OH instead of NaOH?

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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?

Microsublimation:

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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

Anisotropic

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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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