phytopharmaceutical technology
TRANSCRIPT
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NATURAL MEDICINESNATURAL MEDICINES
TRADITIONAL Necessity of PRACTICAL INCREASING USAGE STOCK USAGE EFFECTIVENESS FRESH DRIED EXTRACT- ACTIVE PLANT PLANT PURIFIED CHEMICAL MATERIALS MATERIALS EXTRACT CONSTITUENTS
DIRECTLY INFUSION PHARMA- PHARMA- CONSUMED (DI GODOG) GEUTICAL CEUTICAL (Lalapan) (DI REBUS) DOSAGE DOSAGE JUICES (DI SEDUH) FORMS FORMS JAMU GENDONG
INSTABLE INPRACTICAL HYGROSCOPIC CONVENTIONAL VOLUMINOUS VOLUMINOUS INSOLUBLE DRUG
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EXTRACTEXTRACTCONCENTRED PREPARATIONCONCENTRED PREPARATIONOBTAINED BY EXTRACTING ACTIVE CHEMICAL CONSTITUENTOBTAINED BY EXTRACTING ACTIVE CHEMICAL CONSTITUENTFROM PLANT OR ANIMAL MATERIALSFROM PLANT OR ANIMAL MATERIALSUSING APPROPRIATE SOLVENTUSING APPROPRIATE SOLVENTFOLLOWED BY EVAPORATION OF SOLVENTFOLLOWED BY EVAPORATION OF SOLVENTAND THE RESIDUAL MATERIAL ARE REEXTRACTEDAND THE RESIDUAL MATERIAL ARE REEXTRACTEDSO THAT THE COMBINED EXTRACT ACHIEVE REQUIRED STANDARDSO THAT THE COMBINED EXTRACT ACHIEVE REQUIRED STANDARD
STEPS OF EXTRACT PRODUCTION 1. PREPARATION OF STARTING MATERIALS2. EXTRACTION3. SEPARATION OF MENSTRUM FROM RESIDUAL MATERIAL4. CONCENTRATION OF MENSTRUM5. DRYING PROCESS
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PREPARATION OFOFPREPARATION OFOF STARTING MATERIALSSTARTING MATERIALS
DRYING PROCESSDRYING PROCESS
LIVING PLANT HARVESTED ORGAN DRIED MATERIAL PHOTOSYNTHESIS DISCONTINOUS OF < 10% WATER BIOSYNTHESIS NUTRITIONAL SUPLY CONTENT
NATURAL > 10% WATER CONTENT DENATURATION ENZYMATIC ENZYME STILL ACTIVE OF ENZYME REACTION INHIBITION OF MICROBES CHEMICAL AND DECOMPOSITION OF STABILITY OF PHYSICAL ACT. CHEM. CONST. ACT. CHEM.CONST. STABILITY AND MICROBIAL AND PHYSICAL CONTAMINATION PROPERTIES
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PULVERIZATIONPULVERIZATION
BORDER PHASE DISTANCEBORDER PHASE DISTANCE((TEBAL LAPISAN BATASTEBAL LAPISAN BATAS))
Required distaince of solvent penetration to achieve active Required distaince of solvent penetration to achieve active chemical constituents in the cells of powderchemical constituents in the cells of powder
FINER IS THE POWDER SHORTER IS THE BORDER PHASE DISTANCE
EASIER IS THE SOLVENT PENETRATION
IN ACHIEVING ACTIVE CHEMICAL CONSTITUENTS
MORE EFFECTIVE IS THE EXTRACTION PROCESS
IN REALITY
IT IS NOT ALWAYS THE CASE
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SOME DISADVANTAGES OF TOO FINESS POWDERSOME DISADVANTAGES OF TOO FINESS POWDEROF PLANT MATERIALOF PLANT MATERIAL
1. EVAPORATION OF VOLATILE OIL DUE TO BROKEN CELLS In THE POWDER
2. INSOLUBLE BALLAST SUBSTANCES DISCHARGE THE MENSTRUM
WATER INSOLUBLE SUBSTANCES : LIPIDS
CHLOROPHYL
RESINS
ETHANOL INSOLUBLE SUBSTANCES : CARBOHYDRATES
PROTEINS
3. VERY FINE INTERCELLULAR SPACE CAUSES CLOGGING IN PERCOLATION PROCESS
4. RHIZOMES AND SEEDS CONTAINING STARCH WILL GELATINIZE IN THE PRESENT OF WARM WATER =>
THE MIXTURE BECOME STICKY AND FORMS PORRIDGE
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STEPS OF EXTRACTIONSTEPS OF EXTRACTION
1. SOLVENT PENETRATION INTO CELLS
Border phase distance – Powder finess
Hardness of cells – Leaves, flowers, rhizomes Soft
Woods, certain fruits Hard
Solvent – Biger is the percentage of OH group,
stronger is the penetration capability of solvent
Water > Glycerol > Methanol > Ethanol > Eter
2. DEVELOPMENT OF INTRA AND INTERCELLULAR SPACE
3. CONTACT BETWEEN SOLVENT AND ACTIVE CHEMICAL CONSTITUENTS
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STEP OF EXTRACTION (Continued)STEP OF EXTRACTION (Continued)
4. DISSOLUTION OF ACTIVE CHEMICAL CONSTITUENTS Polarity of solvent and active chemical constituents – Like and Dislike Solvent saturation – Percolation (supply of new solvent) > Maceration Heating process – Decrease viscosity of solvent – Increase capability in dissolving active chemical constituents Stirring and shaking - Increase dissolution of active chemical
constituents
5. DIFFUSION OF ACTIVE CHEMICAL CONSTITUENTS TO OUTSIDE CELLS
Different concentration of solute in solvent between outside and inside cells – Concentration equilibrium – Percolation > Maceration
Pressure – Percolation (liquid flow of addition solvent) > Maceration Created by addition of pressure or vacum
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SOLVENTS SOLVENTS DISSOLVED CHEMICAL CONSTITUENT GROUPSDISSOLVED CHEMICAL CONSTITUENT GROUPS
HEXANE Terpenoids (volatile oil), Triterpenes, Steroids, Coumarins, Benzene, Toluene Polymethoxy flavones, Lipid, Resin, Chlorophylls, Xanthophylls
CHLOROFORM All above mentioned groups, Anthraquinones, Free alkaloids, Dichloromethane Curcuminoids, Free phenols
DIETHYL ETHER All above mentioned groups, Flavonoid aglycones, Phenolic acids
ETHYL ACETATE All above mentioned groups, Flavonoid monoglycosides, Acetone Quasinoids, Other glycosides
ETHANOL All above mentioned groups, Flavonoid diglycosides, Tannin, And other alcohols
HOT WATER All above mentioned groups starting from those dissolved in diethyl ether, Alkaloid salts, Flavonoid polyglycosides, Mono- and Disaccharides, Amino acids and Proteins
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STABILITY OF ACTIVE CONSTITUENTSSTABILITY OF ACTIVE CONSTITUENTSEsters : Methyl salicylate Gaultheria fragrantissima Wall Counter irritant Hydrolysis : Methanol and
Salicylic acid Benzyl acetate Jasminum officinale L. Aromatherapy Hydrolysis : Benzyl alcohol and Acetic acid
OC
OH3C
C
O
OCH3
OH
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Ethyl p-methoxy cinnamate
Kaempferia galanga L.
Expectorant and Analgesic
Hydrolysis : Etanol and
p -Methoxy cinnamic acid
Linalyl acetate
Ocimum basilicum L.
Aromaterapi
Hydrolysis : Linalyl alcohol and
Acetic acid
O
C CH3
O
OCH3
C CH
CO
OC2H5
H
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GLYCOSIDEGLYCOSIDE
Apium graveolens L.
Apigenin-7-O-apiosyl-glucoside
Apiin Apigenin
Polar Semi polar
Water soluble Ethanol soluble
Apiosil-glukosil-O O
O
OH
OH
O
O
OH
OH
HO
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POLYSACCHARIDESPOLYSACCHARIDES
Plantago major L. seedsGuazuma ulmifolia Lamk. leavesPOLYSACCHARIDE MONO/DISACCHARIDE- Water soluble fiber - Glucose, galactose- Mucilage - Sucrose, lactose- Big molecule - Small molecule - Difficult to be absorbed - Easy to be absorbed
- Facilitating defecation - Source of energy - Decrease appetite - Increase body weight - Slimmer
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OXIDATION & POLYMERIZATIONOXIDATION & POLYMERIZATION
Mono and sesqui terpene
(component of volatile oils)
oxydation
Become darker
polymerization
Resin
Insoluble
Increase toxicity
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ULTRAVIOLET LIGHTULTRAVIOLET LIGHT
Azulene - Curcuma aeruginosaChamazulene – Matricaria chamomilla Unsaturated sesquiterpene Blackish blue color Decoloration by UV lightCurcuminoid or Diarylheptanoid Indirect exposure of UV light Prohibited disinfection by radiation
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HEATING FACTORHEATING FACTOR
Volatile oils- Terpenoid hydrocarbon with low boiling point
evaporated, disappear- Sesquiterpene lacton - thermolabile
Poly unsaturated compounds- Carotenes- Curcuminoid- Poly unsaturated fatty acid (PUFA)
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pH FACTORpH FACTOR
Inactivation of enzyme by boiling of Curcuma
rhizomes in water containing Calcium Bright
brownish yellow
Big mistake
Disappearance of Volatile oil by water steam
Decomposition of Curcumin to become ferulic
acid
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NECESSITY OF STANDARDIZATIONNECESSITY OF STANDARDIZATION
CHEMICAL CONSTITUENTS : - Active chemical constituents – Dose influencing
therapeutic effect
- Ballast substances- carbohydrate, protein, lipid, chlorophyll, resin, tannin - Saturation of extract Influence the solubility of active constituents - Influence absorption of active constituents
- Starting materials, extracts, and products must be standardized
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PRODUCTION OF PURIFIED EXTRACTPRODUCTION OF PURIFIED EXTRACT
- DELIPIDATION and FRACTIONATION
- SAPONIFICATION
- RESIN ELIMINATION
- DISTILLATION
- PRECIPITATION BY :
- Different solvent polarities
- Heavy metal – Poly phenol reaction
- Protein – Tannin reaction
- ALKALOID SEPARATION
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DELIPIDATION AND FRACTIONATIONDELIPIDATION AND FRACTIONATION
PLANT POWDER PLANT POWDER PETROLEUM ETHANOL ETHER RESIDUE EXTRACTNON POLAR RESIDUE ETHANOLSUBSTANCES Chloroform Evaporation; /Ether + Hot Water
SUSPENSIONRESIDUE EXTRACT CHCl3 Ether: Ethanol /ETHER Ethyl acetate: Butanol
EXTRACT ETHANOL DIFFERENT FRACTIONS
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SAPONIFICATIONSAPONIFICATION
NON POLAR / LIPID EXTRACT KOH Solution
SOAP WATER FRACTION
Ether
WATER ETHER FRACTION FRACTION (TRITERPENE
STEROID CAROTENOID)
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RESIN ELIMINATIONRESIN ELIMINATION
ETHANOLIC EXTRACT ETHANOLIC EXTRACT
Petroleum ether KOH ethanolic
/Hexane
PE/Hexanic INSOLUBLE PRECIPITATE SOLUBLE
FRACTION FRACTION (RESIN) FRACTION
CURCUMIN PIPERINE
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DISTILLATIONDISTILLATION
NON POLAR/ LIPID EXTRACT
+ WATER DISTILLATION
ESSENTIAL OIL NON VOLATILE FRACTION