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INDUSTRIAL PRODUCTION,
ESTIMATION AND UTILIZATION OF
PHYTOCONSTITUENTS
Presented By:
Mahewash Sana A. Pathan.
Department of Pharmaceutics,
R. P. College of Pharmacy, Osmanabad.
FORSKOLIN
Biological Source: Labdane diterpenoid
extracted from roots of Coleus forskohlii,
family- Lamiaceae.
2
 Industrial Production:
3
1
• Roots & bark powder extracted
with toluene at 60˚C for 2 hours.
2
• Filtrate collected & concentrated at
temperature not exceeding 40˚C.
3
• Concentrated extract mixed with n-
hexane, yields crude forskolin in
the form of brown ppt.
4
• Purified using column
chromatography.
FORSKOLIN
 Estimation:
TLC & HPTLC
Mobile phase – Toluene: ethyl acetate ( 8.5:
1.5 v/v)
Stationary phase- Silica gel F254
Visualizing agent- 5% vanillin in glacial acetic
acid and 10% sulphuric acid in water.
 Utilization:
1. Antidepressant
2. Vasodilating
3. Antiobesity
4. In glaucoma
5. Antiasthmatic 4
FORSKOLIN
SENNOSIDES
 Source: Dianthrone glycosides, leaflets
of Cassia angustifolia (Indian senna) &
C. acutifolia ( Alexandrian senna).
Family- Leguminosae.
5
 Industrial production:
6
1
• Dried senna leaves powder extracted with
benzene for 2-3 hrs.
2
• Marc is dried and extracted with methanol for
4-6 hrs.
3
• Mix both the extracts and concentrated .
4
• pH of extract adjusted to 3.2 by HCl.
5
• Extract is mixed with hydrous calcium chloride
in 25 ml denatured spirit.
6
• pH adjusted to 8 using ammonia & set aside
for 2hrs, results into ppt of sennosides.
SENNOSIDES
 Estimation:
Column- C18
Mobile phase- 1% acetic acid in water:
Acetonitrile (82:18)
Flow rate- 1ml/min
Detection- 350 nm
 Utilization:
1. Treatment of constipation
2. In skin diseases
3. As an anthelmintic
4. Useful in loss of appetite, dysentry,
indigestion, malaria, jaundice, gout,
rheumatism & anaemia.
7
SENNOSIDES
ARTEMISININ
 Source: sesquiterpene lactone obtained
from the leaves & unexpanded flower heads
of Artemisia annua.
Family- Asteraceae.
8
 Industrial production:
9
1
• Fresh leaves are dried below 60˚C, powder is
extracted with methanol by maceration.
2
• Methanol extract partitioned with hexane
3
• The hydro alcoholic extract partitioned with
ethyl acetate until the colourless.
4
• Contentrated at controlled temperature at 40˚C
under vacuum.
5
• Artemisinin obtained as fine white crystals after
recrystallization with cyclohexane.
ARTEMISININ
 Estimation:
HPLC & HPTLC method
Mobile phase- n-hexane : ethyl acetate ( 7.5:
2.5 v/v)
Stationary phase- silica gel F254
Visulazing agent- anisaldehyde sulphuric acid
reagent followed by heating to 110˚C.
 Utilization:
1. Antimalarial
2. In gastric infections
3. Suppress inflamatory immune reactions
4. Anticancer
10
ARTEMISININ
DIOSGENIN
 Source: Aglycone obtained after the
hydrolysis of steroidal saponin glycoside
dioscin present in Dioscorea deltoidea, D.
composite.
Family- Dioscoreaceae.
11
 Industrial production:
12
1
• Dried powder hydrolyzed with 2.5N
H2SO4 by reflux or autoclave.
2
• Marc washed with 10% sod.
Bicarbonate to neutralize acid.
3
• Hydrolyzed powder extracted with
benzene for 6-8 hrs.
4
• Benzene extract is filtered, residue
dissolve in chloroform and
concentrated by recystallization.
DIOSGENIN
 Estimation:
HPTLC method
Mob. Phase- toluene: ethyl acetate: formic acid
(5:4:1)
St. phase- Silica gel F 254
 Utilization:
1. As a precursor for steroidal synthesis
2. In preparation of oral contraceptives
3. In treatment of rheumatism.
13
DIOSGENIN
DIGOXIN
 Source: Cardiac glycoside obtained from
leaves of Digitalis lanata.
Family- Scrophulariaceae.
14
 Industrial production:
15
1
• Fresh leaves made into
paste & treated with neutral
salt.
2
• Paste is defatted with
benzene & followed by
extraction with ethyl
acetate
3
• Extract contain lanatoside
C, which after hydrolysis
yields digoxin.
DIGOXIN
DIGOXIN
 Estimation:
Assay- 40 mg test & std solution of digoxin
dissolve in sufficient ethanol.
5 ml of resulting solution, add 3ml picric acid
solution.
Measure absorbance at 495 nm.
 Utilization:
treatment of cardiac disorders.
16
ATROPINE
 Source: tropane alkaloid, flowering tops of
Atropa belladonna, Datura stramonium &
Hyoscyamus niger.
 Family- Solanaceae.
17
ATROPINE
 Industrial production:
18
1
• Powdered drug extracted with
ether or benzene
2
• Concentrate the non-polar extract
& partitioned with acetic acid.
3
• Add sodium bicarbonate leading to
ppt alkaloid
4
• Dry the ppt & crystallized by
dissolving in solvent ether
 Estimation:
Assay- sulphate salt of atropine titrated against
0.1 N perchloric acid.
 Utilization:
1. As preanesthetic medication
2. Antispasmodic
19
ATROPINE
PODOPHYLLOTOXIN
 Source: resin, roots & rhizomes of
Podophyllum hexandrum, P. emodi & P.
peltatum.
 Family- Berberidaceae.
20
PODOPHYLLOTOXIN
 Industrial production:
21
1
• Dried roots & rhizomes
extracted with methanol
2
• Evaporate the filtrate to
semisolid mass
3
• Dissolve in acidic water
results into pptn of
podophyllotoxin
 Estimation:
HPLC
Mob. Phase- methanol: water ( 62: 38 v/v)
Detector wavelength- 280nm.
 Utilization:
1. Antitumour
2. Purgative
3. Emetic
4. Treatment of warts
22
PODOPHYLLOTOXIN
CAFFEINE
 Source: xanthine alkaloid, leaves of
Camellia sinesis (Theaceae), seeds of
Coffea arabica (Rubiaceae).
23
CAFFEINE
 Production:
24
1
• Leaflet powder boiled with 2%
sodium carbonate water for 10 min
& filtered.
2
• Evaporate & partitioned with
dichloromethane
3
• Evaporate to get crystals of caffeine.
4
• Purified by recystallization from hot
ethanol.
 Estimation:
HPLC method
Mob. Phase- methanol: acetonitrile ( 65: 35
v/v)
Column- C18
 Utilization:
Stimulant
25
CAFFEINE
TAXOL
 Source: nitrogen containing subs, bark of
Taxus brevifolia, fam- taxaceae.
26
TAXOL
 Production:
27
1
• Powdered bark extracted with
methanol, filtered & evaporated
to dryness.
2
• Partition with the mixture of
carbon tetrachloride & water,
filter & evaporated.
3
• Dried CCl4 fraction again
extracted with CCl4 : methanol,
evaporate to obtain crude taxol.
 Estimation:
HPTLC method
Mob phase- chloroform:methanol (7:1v/v)
Visualizing agent- vanillin sulphuric acid.
 Utilization:
1. Treatment of ovarian, lung, bladder,
esophageal & other types of cancers.
2. Antiproliferative agent.
28
TAXOL
VINCRISTINE & VINBLASTINE
 Source: Indole alkaloid, Vica rosea, family-
Apocynaceae.
29
VINCRISTINE &
VINBLASTINE
 Production: Plant tissue culture technique.
 Estimation: HPLC method
Mob phase- acetonitrile: 0.1 M phosphate
buffer.
Wavelength- 254nm.
 Utilization:
1. In chemotherapy regimens
2. Childhood leukemia
3. immunosuppressant
30
THANK YOU
31

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Industrial production, estimation and utilization of phytoconstituents

  • 1. INDUSTRIAL PRODUCTION, ESTIMATION AND UTILIZATION OF PHYTOCONSTITUENTS Presented By: Mahewash Sana A. Pathan. Department of Pharmaceutics, R. P. College of Pharmacy, Osmanabad.
  • 2. FORSKOLIN Biological Source: Labdane diterpenoid extracted from roots of Coleus forskohlii, family- Lamiaceae. 2
  • 3.  Industrial Production: 3 1 • Roots & bark powder extracted with toluene at 60˚C for 2 hours. 2 • Filtrate collected & concentrated at temperature not exceeding 40˚C. 3 • Concentrated extract mixed with n- hexane, yields crude forskolin in the form of brown ppt. 4 • Purified using column chromatography. FORSKOLIN
  • 4.  Estimation: TLC & HPTLC Mobile phase – Toluene: ethyl acetate ( 8.5: 1.5 v/v) Stationary phase- Silica gel F254 Visualizing agent- 5% vanillin in glacial acetic acid and 10% sulphuric acid in water.  Utilization: 1. Antidepressant 2. Vasodilating 3. Antiobesity 4. In glaucoma 5. Antiasthmatic 4 FORSKOLIN
  • 5. SENNOSIDES  Source: Dianthrone glycosides, leaflets of Cassia angustifolia (Indian senna) & C. acutifolia ( Alexandrian senna). Family- Leguminosae. 5
  • 6.  Industrial production: 6 1 • Dried senna leaves powder extracted with benzene for 2-3 hrs. 2 • Marc is dried and extracted with methanol for 4-6 hrs. 3 • Mix both the extracts and concentrated . 4 • pH of extract adjusted to 3.2 by HCl. 5 • Extract is mixed with hydrous calcium chloride in 25 ml denatured spirit. 6 • pH adjusted to 8 using ammonia & set aside for 2hrs, results into ppt of sennosides. SENNOSIDES
  • 7.  Estimation: Column- C18 Mobile phase- 1% acetic acid in water: Acetonitrile (82:18) Flow rate- 1ml/min Detection- 350 nm  Utilization: 1. Treatment of constipation 2. In skin diseases 3. As an anthelmintic 4. Useful in loss of appetite, dysentry, indigestion, malaria, jaundice, gout, rheumatism & anaemia. 7 SENNOSIDES
  • 8. ARTEMISININ  Source: sesquiterpene lactone obtained from the leaves & unexpanded flower heads of Artemisia annua. Family- Asteraceae. 8
  • 9.  Industrial production: 9 1 • Fresh leaves are dried below 60˚C, powder is extracted with methanol by maceration. 2 • Methanol extract partitioned with hexane 3 • The hydro alcoholic extract partitioned with ethyl acetate until the colourless. 4 • Contentrated at controlled temperature at 40˚C under vacuum. 5 • Artemisinin obtained as fine white crystals after recrystallization with cyclohexane. ARTEMISININ
  • 10.  Estimation: HPLC & HPTLC method Mobile phase- n-hexane : ethyl acetate ( 7.5: 2.5 v/v) Stationary phase- silica gel F254 Visulazing agent- anisaldehyde sulphuric acid reagent followed by heating to 110˚C.  Utilization: 1. Antimalarial 2. In gastric infections 3. Suppress inflamatory immune reactions 4. Anticancer 10 ARTEMISININ
  • 11. DIOSGENIN  Source: Aglycone obtained after the hydrolysis of steroidal saponin glycoside dioscin present in Dioscorea deltoidea, D. composite. Family- Dioscoreaceae. 11
  • 12.  Industrial production: 12 1 • Dried powder hydrolyzed with 2.5N H2SO4 by reflux or autoclave. 2 • Marc washed with 10% sod. Bicarbonate to neutralize acid. 3 • Hydrolyzed powder extracted with benzene for 6-8 hrs. 4 • Benzene extract is filtered, residue dissolve in chloroform and concentrated by recystallization. DIOSGENIN
  • 13.  Estimation: HPTLC method Mob. Phase- toluene: ethyl acetate: formic acid (5:4:1) St. phase- Silica gel F 254  Utilization: 1. As a precursor for steroidal synthesis 2. In preparation of oral contraceptives 3. In treatment of rheumatism. 13 DIOSGENIN
  • 14. DIGOXIN  Source: Cardiac glycoside obtained from leaves of Digitalis lanata. Family- Scrophulariaceae. 14
  • 15.  Industrial production: 15 1 • Fresh leaves made into paste & treated with neutral salt. 2 • Paste is defatted with benzene & followed by extraction with ethyl acetate 3 • Extract contain lanatoside C, which after hydrolysis yields digoxin. DIGOXIN
  • 16. DIGOXIN  Estimation: Assay- 40 mg test & std solution of digoxin dissolve in sufficient ethanol. 5 ml of resulting solution, add 3ml picric acid solution. Measure absorbance at 495 nm.  Utilization: treatment of cardiac disorders. 16
  • 17. ATROPINE  Source: tropane alkaloid, flowering tops of Atropa belladonna, Datura stramonium & Hyoscyamus niger.  Family- Solanaceae. 17
  • 18. ATROPINE  Industrial production: 18 1 • Powdered drug extracted with ether or benzene 2 • Concentrate the non-polar extract & partitioned with acetic acid. 3 • Add sodium bicarbonate leading to ppt alkaloid 4 • Dry the ppt & crystallized by dissolving in solvent ether
  • 19.  Estimation: Assay- sulphate salt of atropine titrated against 0.1 N perchloric acid.  Utilization: 1. As preanesthetic medication 2. Antispasmodic 19 ATROPINE
  • 20. PODOPHYLLOTOXIN  Source: resin, roots & rhizomes of Podophyllum hexandrum, P. emodi & P. peltatum.  Family- Berberidaceae. 20
  • 21. PODOPHYLLOTOXIN  Industrial production: 21 1 • Dried roots & rhizomes extracted with methanol 2 • Evaporate the filtrate to semisolid mass 3 • Dissolve in acidic water results into pptn of podophyllotoxin
  • 22.  Estimation: HPLC Mob. Phase- methanol: water ( 62: 38 v/v) Detector wavelength- 280nm.  Utilization: 1. Antitumour 2. Purgative 3. Emetic 4. Treatment of warts 22 PODOPHYLLOTOXIN
  • 23. CAFFEINE  Source: xanthine alkaloid, leaves of Camellia sinesis (Theaceae), seeds of Coffea arabica (Rubiaceae). 23
  • 24. CAFFEINE  Production: 24 1 • Leaflet powder boiled with 2% sodium carbonate water for 10 min & filtered. 2 • Evaporate & partitioned with dichloromethane 3 • Evaporate to get crystals of caffeine. 4 • Purified by recystallization from hot ethanol.
  • 25.  Estimation: HPLC method Mob. Phase- methanol: acetonitrile ( 65: 35 v/v) Column- C18  Utilization: Stimulant 25 CAFFEINE
  • 26. TAXOL  Source: nitrogen containing subs, bark of Taxus brevifolia, fam- taxaceae. 26
  • 27. TAXOL  Production: 27 1 • Powdered bark extracted with methanol, filtered & evaporated to dryness. 2 • Partition with the mixture of carbon tetrachloride & water, filter & evaporated. 3 • Dried CCl4 fraction again extracted with CCl4 : methanol, evaporate to obtain crude taxol.
  • 28.  Estimation: HPTLC method Mob phase- chloroform:methanol (7:1v/v) Visualizing agent- vanillin sulphuric acid.  Utilization: 1. Treatment of ovarian, lung, bladder, esophageal & other types of cancers. 2. Antiproliferative agent. 28 TAXOL
  • 29. VINCRISTINE & VINBLASTINE  Source: Indole alkaloid, Vica rosea, family- Apocynaceae. 29
  • 30. VINCRISTINE & VINBLASTINE  Production: Plant tissue culture technique.  Estimation: HPLC method Mob phase- acetonitrile: 0.1 M phosphate buffer. Wavelength- 254nm.  Utilization: 1. In chemotherapy regimens 2. Childhood leukemia 3. immunosuppressant 30