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Pharmacognosy
PREPARED BY JOSE ALFONSO P. CANTOR, RPH.
Introduction and
History
Pharmacognosy
Study of drugs of biologic origin usually plants
A highly specialized science that deals with biochemical
and economic features of natural drugs and their
specific components
History
1.Papyrus Ebers
2.Pedianios Dioscorides
3.Claudius Galen
4.C.A Seydler
5.Fluckiger
6.Jonathan A Schmidt (J.A Schmidt)
7.Scientist who isolated compounds and other novel discoveries
Papyrus Ebers
Discovered in ancient Egypt in a tomb of a
mummy by George Ebers
Scrolls of paper with 600-700 citations of
drugs from plants and animals
Pedanios Dioscorides
Author of “De Materia Medica” (Medicinal
Materials) that contains 600 plants with
medicinal properties
Claudius Galen
Described method of preparing formula containing
plant and animal drugs in apothecaries
The Father of EXTEMPORANEOUS COMPOUNDING
Created Galen’s cerate or Cold cream
C.A Seydler
He coined the term “Pharmacognosy” in his
dissertation: Analetica Pharmacognostica
Pharmakon means: Drug/Poison
Gnosis means: Knowledge
Fluckiger
He wrote a comprehensive meaning of
Pharmacognosy
Definition is as follows: “Pharmacognosy is the
simultaneous application of various scientific
disciplines with the object of acquiring drugs from
every point of view”
J.A Schmidt
He is the one who first used the term
“Pharmacognosy” in his book:
Lerbuch de Materia Medica that contains
different medicinal plants and its properties
Prominent Scientists
1. Pelletier and Caventou – discovered Quinine (Anti-malarial
quinoline alkaloid)
2. Friedrich Serturner – isolated Morphine from Poppy
plant/Papaver somniferum
3. Pierre Robiquet – isolated Codeine (Anti-tussive and Narcotic
analgesic)
4. Claude Bernard – discovers the site of action of Tubocurarine
(Isoquinoline alkaloid)
Crude Drugs
Natural vs Synthetic
Drug Compounds
NATURAL SYNTHETIC
Extracted or obtained Created inside research
directly from plants or laboratory with the aid of
animals computers and scientists
Alkaloids and Penicillins Examples:
(P.chrysogenum and Fluoroquinolones
P.nonatum)
Crude Drugs
Vegetable or animal drugs that consists of natural substances that have
undergone only the processes of COLLECTION and DRYING
Step 2:Harvesting
gathering of cultivated sample for experiment by manual
or mechanical means
Preparation of Crude Drugs
Step3:Drying
removal of moisture to protect the plant from microbial spoilage.
Other benefits are
1.Fixes contituents
2.Facilitate comminution (reduction of particle size)
3.Reduces bulk
Curing (Special method of drying)
aims to enhance active constituents and inactivate toxic ones
Example: Cascara sagrada – used as laxative ; cured by MgO within 1 year
Preparation of Crude drugs
Final step:Garbling
Physical or mechanical removal of extraneous matter
(soil,dirt,and plant parts)
Optional step
Packaging,storing and Preservation –for protection from
environmental conditions and other purposes such as:
1.To enhance marketability
2.To preserve and prolong shelf life
Evaluation of Drugs and
Drug Adulteration
Evaluation of Drugs
It is used or utilized to identify the drug and determine
its intrinsic value and purity
Methods are the following:
1. Organoleptic
2. Microscopic
3. Biologic
4. Chemical
5. Physical
Methods of Drug Evaluation
1. Organoleptic
macroscopic analysis and evaluation using the 5 sense
2. Microscopic
identification of pure and powdered drug. Identifies shape of
powdered drug and 3D shape
3. Biologic
utilizes living organisms to determine the effect of the drug
Examples are: Pigeon – Digitalis
Sheep - Warfarin and Protamine
Oxytocin – Chicken
Dog - PTH
Methods of Drug Evaluation
4. Chemical
best method of determining the official potency (QC
assay)
5. Physical
application of physical constants to active drug
principles such as color, density, and melting point.
Drug Adulteration
debasement of an article or a drug product
Types of adulteration:
1.Inferiority
2.Spoilage
3.Deterioration
4.Admixture
5.Sophistication
6.Substitution
Types of Adulteration
1. Inferiority
any substandard drug or low quality regardless of cause
2. Spoilage
a drug which is unfit for consumption or can’t be used
due to microbial damage (bacteria or fungi)
3. Deterioration
destruction of active constituents via aging or bacteria;
still can be used
Types of Adulteration
4. Sophistication
the true kind of adulteration which is intentional
;partly replacing the product
5. Substitution
worst kind of substitution; total replacement and
intentional
Classification of Drugs
Classification of Drugs
1. Morphology
drugs are grouped according to the part used
2. Therapeutic
drugs are grouped as they are employed medicinally
3. Chemical constituents
based on the active principles; Most preferred
method of study
Classification of Drugs
Taxonomic/Zoological/Botanical
considers phylogeny (natural relationship among plant and animal)
OLD NAME NEW NAME OLD NAME NEW NAME
Labiatae Lamiaceae Palmae Arecaceae
Leguminosae Fabaceae Guttiferae Clussiaceae
Umbelliferae Apiaceae Graminae Poaceae
Compositae Asteraceae Cruciferae Brassicaceae
Brassicaceae or Cruciferous vegetables are CYP
inducers
10 Medicinal Plants of
DOH
COMMON NAME SCIENTIFIC NAME MEDICINAL USE
Akalpulko/Ringworm Cassia alata Anti-fungal
bush
Niyog-niyogan Quisqualis indica Anthelminthic
5.Stachyose
Glucose + Fructose + Galactose + Galactose
Polysaccharides
Functions of polysaccharides
1.Storage
2.Plant structure
Types of Polysaccharides
1.Homoglycan – made up of 1 sugar type only
2.Heteroglycan – made up of 2 or more types of sugar
Homoglycan
1.Starch (Glucosan)
Natural source: Corn (Zea mays) and Potato (Solanum
tuberosum)
Pharmaceutical use: Tablet diluent, binder, disintegrant
and antidote for Iodine
Mixture of 2 polysaccharides: Amylose and
Amylopectin
AMYLOPECTIN
AMYLOSE
(PASTE FORMING)
STRUCTURE Linear Branching
2.Agar/Japanese isinglas/Gulaman
Obtained from: Geladium cartilagineum and Gracilaria confervoides
use: stiffening agent in preparation of culture media; thickening
agent
Components: Agarose and Agaropectin
Marine Gums
3.Carageenan/Irish moss/Chondrus
Obtained from Red algae or seaweeds:
Chondrus crispus
Gigartina mamillosa
Nongelling, thickening
Nongelling agent Gelating agent
agent
Marine Gums
4.Danish agar/Furcellaran
from red algae (Furcellaria fastigiata)
Similar property to Kappa carrageenan
Forms mucilage similar to K-carrageenan
Microbial Gums
1. Xanthan Gum
High MW gum from the action of Xanthomonas campestris on a suitable
carbohydrate
Special characteristic: Pseudoplastic flow
Thickening, emulsifying, suspending agent
2. Dextran gum
From Leuconostoc mesenteroides (Transglucosylase enzyme)
Seed Gums
SOURCE NOTES
Plantago seed Spanish/French Psyllium Bulk forming laxative
Blonde/Indian Psyllium Gum swells
3. Apocynum
Black Indian hemp, dogbane (Apocynum
cannabinum)
Main constituent: Cymarin
Cardiac Glycosides
4. Adonis
Natural source: Pheasant’s eye (Adonis vernalis)
Main const.: Adonitoxin, cymarin, K-strophantin
5. Strophantum
Natural source: S. kombe, S. hispidus
Main constituents
K-strophanthin
G-strophanthin (Ouabain) –toxic form
used as arrow poison to induce cardiac arrest to animals in Africa
Cardiac Glycoside
6. Convallaria
Natural source: Lily of the Valley (Convallaria
majalis)
Main constituent: Convallatoxin
7. Cactus grandiflorus
Natural source: Stem of Night-blooming cereus
(Selenicereus grandifloras)
Cardiac Glycoside
8. Squill
Natural source: Mediterranean or White Squill (Urginea
maritima)
Main const.:Scillarenin
Use:Expectorant, emetic,carditonic, and diuretic
9. Oleander/Rose Bay
Natural source: Adelfa (Nerium oleander)
Main const.:Oleandrin
Anthraquinone Glycoside
Commonly used as cathartics except Chysarobin
(keratolytic)
Borntrager Test – test for anthraquinone glycosides
Derivatives are color orange
MOA: tone of smooth muscle in wall of large
intestines
S/E: Melanosis coli
Anthraquinone glycoside
5 types of anthraquinone glycoside
1.Anthracene – such as rhein and chrysophanol
5.Aloin/C-glycoside
Anthraquinone Glycoside
1.Cascara sagrada from Sacred bark (Rhamnus
purshiana)
Main constituents: Barbaloin and Chyrsaloin
Should be cured with MgO for 1yr. to reduce irritating properties
To reduce bitter taste take with: Licorice or Yerba santa
Curacao Aloe (A. barbadensis, A. vera) and Cape Aloe (A. spicata)
2. CITRUS BIOFLAVONOIDS
Hesperidin, hesperitin, diosmin, naringin
2.ETHYLVANILLIN
synthetic analog
Lactone Glycosides (Anti-coagulant)
1. Coumarin
lactone of hydroxycinnamic acid (use: Flavoring agent)
Natural source: Tonka beans (Dipteryx odorata) & Sweet
clover (Melilotus alba)
2. Dicoumarol/Bisdihydroxy coumarin
Natural source: Improperly cured leaves and flowering
tops of Melilotus officinalis
Lactone Glycosides (Anti-coagulant)
3.Cantharides/Blistering flies
Natural source: Dried insect (Cantharis vesicatoria)
Main constituent: Cantharides (Aphrodisiac S/E:
Priapism)
4.Psoralens (Ammi majus)
Main constituent: Methoxsalen and xanthotoxin
Use: Aid in repigmentation in vitiligo and management
for psoriasis
Phenol Glycosides
1. Bear berry/Uva ursi
Main constituent: Arbutin
Use: Astringent and Diuretic
2. Poison Ivy
Main constituent: Urushiol (Old antidote: Zirconium)
3. Hesperidin
Tannins
Tannins
Non-crystallizable hydrocolloid mixture of polyphenols
Forms colloidal solutions in water and with puckering taste
Use:
Astringent
Carcinogenic potential (Tannins in Areca catechu)
Converts animal hide to leather
Alkaloidal precipitant (Tannic acid)
Tannins
HYDROLYZABLE NONHYDROLYZABLE
Other name Pyrogallotannins Phlobatannins
Pyrogallol, phenolic
Hydrolyzation Phlobaphenes
acids
FeCl3 Test Bluish black ppt Greenish black ppt
Br Water No precipitate Precipitate
Lead Acetate Soluble Non soluble
Leather Type Bloom Tanner’s red
Tannins
TEST FOR PRESENCE OF TANNINS
1. Goldbeater Test (+) result: Brown or black coloration
2. Gelatin Test (+) result: Gelatin precipitation
Ester value
Milligram(mg) of KOH required to saponify the esters in 1g of substance
NO COCONUT OIL
Fixed Oils (SeCoCoPea)
4 Official Fixed Oils Used In Pharmacy Practice
NO COCONUT OIL
Fats
1.Lanolin
Natural source: Wool of Ovis aries (sheep)
Main Constituent: Cholesterol and isocholesterol
Hydrous lanolin: 25% water
Anhydrous lanolin/wool fat: 0.25% wayer
Use: Water absorbable ointment base and emollient
Fats
2.Cod liver oil – from Gadus morrhua
Note: THE ONLY LIQUID FAT
Use: Nutritional source of Vitamin A and D
Fatty Acids (From Hydrolysis Of Fat And Oil)
1. Stearic acid
Used as tablet diluent except Zinc stearate used as dusting powder
Sodium stearate – stiffening agent and emulsifier
Eleoptene
Liquid hydrocarbon portion
Eucalyptol, Methyl salicylate& Eugenol/Clove oil
Volatile Oils
May secreted in specialized secretory
structures:
1. Glandular hairs
2. Modified parenchymal cells
3. Oil tubes (vittae)
4. Lysigenous or schizogenous passages
Volatile Oils
Oil tubes / Vittae Apiaceae
Glandular hairs / trichomes Lamiaceae
3. Tolu balsam
component of Compound benzoin tincture
Main constituents: Toluresinnotannol cinnamate and Benzyl benzoate
4. Benzoin
component of Compound benzoin tincture
Alkaloids
Alkaloids
Organic nitrogenous plant secondary metabolites which are
pharmacologically active
Other properties
Bitter taste
Usually crystalline or amorphous
Alkaloid base – lipid soluble
Alkaloidal salts – water soluble
All alkaloids are solid except: Coniine, Arecoline, Nicotine & Sparteine
Alkaloidal Reagents
Reagent Composition Positive result
Mayer’s Potassium Mercuric Iodide Cream ppt
Alkaline Potassium Mercuric Brown ppt
Nessler’s
Iodide
Wagner’s Iodine In Potassium Iodide Reddish brown ppt
Dragendorf’s Potassium Bismuth Iodide Reddish brown ppt
Valser’s Mercuric Iodide White ppt
Marme’s Cadmium In KI Cream ppt
Sonnenchein’s Phosphomolybdic Acid Yellow ppt
Phosphotungstic Acid yellow to orange
Schiebler’s
ppt
Hager’s Saturated Picric Acid Yellow ppt
Alkaloids (Ring Structure)
1. Protalkaloids Or Non-heterocyclic Alkaloids
They contain nitrogen in a side chain and considered
as an alakaloid due to their pharmacological property
Other name: Alkaloidal amine
2. Heterocyclic Or Typical Alkaloids
The nitrogen is in a ring structure and chemically
considered as an alkaloid
Pyridine-piperidine Alkaloids
Source Use
Nicotine Nicotinia tabacum Smoking deterrent
2. Catharanthus/Vinca/Periwinkle (Catharanthus
roseus)
Constituent: Vincristine, Vinblastine, Vinorelbine
MOA: Arrest cell division at Metaphase
Use: Anti-CA (e.g. Hodgkin’s disease)
Indole Alkaloid
3. Nux vomica (seed of Strychnos nux vomica)
Constituents: Strychnine (central stimulant), Brucine (alcohol
denaturant)
4. Ignatia/St. Ignatius Bean (Strychnos ignatia)
commercial source of strychnine (vermin killer)
Indole Alkaloid
5. Physostigma/Calabar/Ordeal bean (Physostigma venenosum)
Constituent: Physostigmine for Glaucoma & Anti-
cholinergic poisoning
MOA: Acetylcholinesterase inhibition leading to increase
effects of ACh
Indole Alkaloid
6. Rye ergot/Ergot/Secale Cornutum
dried sclerotium of Claviceps purpurea on Rye bread
Main constituents:
Ergonovine/Ergometrine – oxytocic for postpartum
hemorrhage
Ergotamine – for migraine
Ergotoxine – lipid soluble mixture of Ergocristine,Ergocryptine
& Ergoconine
LSD – most potent hallucinogen
Indole Alkaloid
6. Rye Ergot/Ergot/Secale Cornutum
S/E:Ergotism
Two Types Of Ergotism
Gangrenous ergotism/St. Anthony’s fire – tissue
death due to excessive vasoconstriction
Convulsive ergotism- convulsion associated with
Vit.A deficiency
Imidazole Alkaloid (1 Only)
1. Pilocarpus/Jaborandi (Pilocarpus jaborandii)
Main constituent: Pilocarpine- direct muscarinic
agonist for glaucoma
Steroidal Alkaloid
1. Green hellebore (Veratrum viride)
insecticide
Effect: Slows down heartbeat leading to hypotension