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Drug Extraction and Phytochemistry


Percolation
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A method of extraction achieved by the downward displacement of soluble extractive by a suitable solvent through a suitably comminuted
drug plant
STEPS:
1. Comminution
Particle size reduction
TOO FINE: may lead to the formation of a solid cake which will affect the downward flow of menstruum and will later
on lead to the formation of dry pockets within the body material which will escape extraction
TOO COARSE: may lead to formation of interstices which produces an incomplete extraction and will require excessive
volumes of menstruum to exhaust the marc
Degree of comminution depends on the composition of the crude drugs

LEAVES and PETALS: easily penetrated by the solvent; requires less degree of comminution

HARD and WOODY SUBSTANCE: require greater reduction in size


2. Selection of Suitable Solvent
Used to remove a solid, either in part or in its entirety
CHARACTERISTICS OF A SUITABLE SOLVENT
1. Display low toxicity to higher life forms
2. Inactive and does not destroy the extract (through complexation or dissociation)
3. Have preservative properties
4. Promote rapid physiologic absorption of the extract
5. Easily evaporated at a low heat
3. Imbibition
Comminuted drug is moistened with a portion of the menstruum in a lidded container of a suitable size (able to
accommodate the expansion of the drug)
Moistened drug is allowed to stand for a minimum period of four hours to allow the drug to imbibe the menstruum and
thereby swell to its maximum capacity
4. Packing
Drug is tranferred to a percolation vessel in portions
Each portion must be firmly packed to exclude any air pockets but not so firmly that the menstruum is forced from the
drug
CHECKING THE PACKING OF COMMINUTED DRUG
1. LOOSELY PACKED: Menstruum drips through the stopcock in less than 10 minutes
2. TOO TIGHTLY PACKED: First drop of menstruum takes 25 minutes or more
5. Maceration
Sufficient amount of menstruum is poured to leave a layer of 1 to 2 cm deep over the drug
The percolator is covered and left to macerate for a period of 24-48 hours in a warm, dark place at a temperature not
exceeding 25C

Phytochemistry
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Knowledge of the biologic origin or natural origin of drugs


Study of chemicals derived from plants and their biologic activities
Aims at studying inactive principles and classifying plant drugs using chemical and pharmacologic approach

Primary and Secondary Metabolites


Primary Metabolites
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Organic compounds that are directly involved in the normal processes of growth, development and functioning of the plant
Ex: carbohydrates, proteins, lipids

Secondary Metabolites
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Produced from primary metabolites and are not directly involved in the growth, development or reproduction of organisms
Physiologically active substances; absence does not result in immediate death, but rather in long-term impairment of the organisms
survivability, or aesthetics or no significant change at all
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Often restricted to a narrow set of species within a phylogenetic group


Ex: alkaloids, tannins, saponins

Systematic Phytochemical Investigation


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Authentication and extraction of the plant material


Separation and isolation of constituents
Characterization of isolated compounds
Investigation of biosynthetic pathways
Quantitative evaluation

Preparation of Plant for Screening


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Should be properly identified and authenticated by an acknowledged authority


Can either be fresh or dried
Extracted with the use of a suitable method
Properly stored

Phytochemical Screening for Plant Metabolites


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Preliminary Tests to Detect Primary Plant Metabolites: Carbohydrates, Proteins, Oils


Alkaloids
Basic nitrogenous compounds that make up the largest class of secondary metabolites
Usually have a bitter taste and are known to be physiologically active and may elicit several effects on the body
Occur in plants as water-soluble salts
Saponins
Steroid or terpenoid glycosides that are characterized by their ability to froth when the aqueous solution is agitated
Plants containing saponins have been used for their detergent properties
Exert a powerful haemolytic action on the red blood cells and are toxic when injected into the bloodstream
Flavonoids
Phenolic plant pigments containing gamma-benzopyrone nucleus
Steroids: Cardenolides and Bufadienolides
Steroidal aglycones that are referred to as cardiac glycosides because of their dramatic effects on the heart muscle
Tannins and Polyphenols
Have the ability to react with and precipitate proteins, forming stable water-insoluble copolymers
Used pharmaceutically for their astringent action
Contain an alcohol and an acid group
Further divided into two main groups: hydrolysable tannins and condensed tannins
Anthraquinones
Largest group of naturally-occurring quinine pigments
Commonly used as dyes, cathartics and purgatives
Contain the anthracene nucleus and often give orange-red compounds soluble in water and dilute alcohol
Give a characteristic red, violet, green or purple when reacted with a base
Cyanogenic Glycosides
Widely distributed in various plant families usually together with hydrolytic enzymes
Release hydrocyanic acid upon enzymatic hydrolysis
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ASSIGNMENT:
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Search for the complete botanical sources of the plants given to you last Friday.
Outline the procedure done in phytochemical screening of your plant samples.
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