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Incorporation of herbal actives in
pharmaceuticals
Presented By:
AVITASHRI SAGAR PATIL
M. Pharm First Year [Dept. of Pharmaceutics]
Rajarambapu College of Pharmacy, Kasegaon.
Rajarambapu College of Pharmacy, Kasegaon.
1
Introduction:-
‱ Plants produce many chemicals that are biologically active, not
just in themselves, but also in other organisms.
‱ The use of herbal products, especially plants for healing is as
ancient and universal as medicine itself.
‱ Hippocrates, one of the ancient authors who described medicinal
natural products of plant and animal origins, listed approximately
400 different plant species for medicinal purposes.
‱ World Health Organisation (WHO),some 3.4 billion people in the
developing world depends on plant based traditional medicines.
Rajarambapu College of Pharmacy, Kasegaon.
2
‱ An impressive number of modern drugs have been derived from
natural sources. Over the last century, a number of top selling drugs
have been developed from natural products.
‱ Nature has been a potential source of therapeutic agents for
thousands of years.
‱ Example :-
‱ Anticancer drug vincristine from Vinca rosea, Narcotic analgesic
drug Morphine from Papaver somniferum, Antimalarial drug
artemisinin from Artemisia annua, Anticancer drug Taxol from Taxus
brevifolia and Antibiotic drug Penicillin from penicillium .
Rajarambapu College of Pharmacy, Kasegaon.
3
Advantages:-
 Biodegradable
 Biocompatible and nontoxic
 Economic
 Safe and devoid of side effect
 Easy availability
Rajarambapu College of Pharmacy, Kasegaon.
4
Disadvantages :-
 Microbial contamination
 Variation
 The uncontrolled rate of hydration
 Slow process
 Heavy metal contamination
Rajarambapu College of Pharmacy, Kasegaon.
5
Several examples of herbal active ingredients
that provide medicinal uses for human being
1. Alkaloids:-
This group is comprised of a wide variety of plants that contain
nitrogen-bearing molecules that makes them very active. many of these
plants have been used to create well-known drugs used for medicinal
purposes.
Example:- Vincristine, which was derived from periwinkle is used to treat
cancer.
2. Bitters:-
This group is comprised of a variety of plants that are lumped
together because of their very bitter taste. This bitterness causes
stimulation of the salivary glands and digestive organs. As such, bitters can
be used to improve appetite and strengthen the digestive system.
Example:- wormwood and hops.
Rajarambapu College of Pharmacy, Kasegaon.
6
3. Cardiac glycosides:-
These compounds are found in various medicinal plants
and have strong direct action on the heart. Cardiac glycoside such as
digitoxin, digoxin ,and convallotoxin support heart strength and rates
of contraction when failing. These compounds also have a diuretic
effect that stimulates urine production and aids in removal of fluid
from tissues and the circulatory system.
Example:- Foxglove, Lily.
4. Cyanogenic Glycosides:-
These glycocides are based upon cyanide, a very deadly poison, but
in small doses, they can serve as a muscle relaxant. The bark of wild
cherry and the leaves of elderberry (Sambucus racemosa) contain
cyanogenic glycocides, which can be used to suppress and soothe dry
coughs.
Rajarambapu College of Pharmacy, Kasegaon. 7
5. Flavonoids:-
Flavonoids are found widely throughout the plant world and they
have a wide range of medicinal uses and actions. They often act as
pigments giving a yellow or white color to flowers and fruits. Some
flavonoids have anti-viral and anti-inflammatory properties. Flavonoids
found in many plants like lemon and buckwheat are known to strengthen
capillaries and prevent leakage into tissues.
6. Minerals:-
Many plants have high levels of minerals because they can draw
minerals from the soil and can convert them into a form that is more
easily used by the human body. Mineral content is often the key factor in
a plant’s effectiveness as a medicine. One example of a plant high in
minerals is horsetail. The high silica content in horsetail plants is used
for arthritis because it supports the repair of connective tissue.
Rajarambapu College of Pharmacy, Kasegaon.
8
7. Phenols:-
Phenols are plant compounds that are thought to be produced to
protect against infection and herbivory by insects. They are often anti-
inflammatory and antiseptic and can have anti-viral properties. Phenols
vary in structure and range from salicylic acid (similar to aspirin) to
complex sugar-containing phenolic acids. Wintergreen and willow
contain salicylates. Members of the mint family often contain phenols.
8. Polysaccharides:-
Polysaccharides are found in all plants and comprised of multiple
units of sugar molecules linked together. For medicinal purposes, the
“sticky” polysaccharides produce mucilage or gums that are commonly
found in bark, roots, leaves, and seeds. These sticky polysaccharides
are able to soak up large quantities of water and form jelly like masses
that can be used to treat dry or irritated tissues such as skin and
mucous membranes.
Rajarambapu College of Pharmacy, Kasegaon.
9
9. Proanthocyanins:-
These compounds are pigments, which give fruits and flowers
red, purple, or blue hues and are closely related to tannins and
flavonoids. These compounds have been documented to be valuable
in protection of circulation specifically in the heart, eyes, and feet.
Red grapes, blackberries, and hawthorn berries all have high levels of
proanthocyanins.
10. Saponins:-
This group of active compounds obtains its name from the fact
that like soap, they produce lather when placed in water. There are
two main forms of saponins: steroidal and triterpenoid. Steroidal
saponins are very similar to the chemical structures of many of the
human body’s hormones including estrogen and cortisol. Examples
plants containing saponins include agave, wild yam, and several
members of the lily family. Several native plants are used in a process
to produce synthetic hormones for humans.
Rajarambapu College of Pharmacy, Kasegaon.
10
11. Tannins:-
Most plants produce tannins. Tannins serve as a deterrent to
herbivory by insects and grazing animals given that that they provide
a harsh unpalatable flavor. Tannins are also useful in curing leather
because of their tendency to contract and astringe tissues by binding
with precipitating proteins. Examples of plants high in tannins include
oak bark and black catechu.
12. Volatile oils:-
Volatile oils are extracted from plants and are used to produce
essential oils that play a very important role in medicinal botany.
These oils are often very complex and can be comprised of 100 or
more compounds. These oils have many uses. For example, tea tree
oil is a strong antiseptic. Resins and gums are often linked with
essential oils, however these are not volatile.
Rajarambapu College of Pharmacy, Kasegaon.
11
13. Vitamins:-
Many plants contain high levels of useful vitamins. Many well-
known fruits and vegetables have high levels of vitamin C and beta-
carotene. Lesser-known vitamin containing plants like watercress, rose
hips, and sea buckthorn have high levels of vitamins B, C, and E.
Herbal excipients:-
1. Colorants:-
In India, there are more than 450 plants that can yield dyes. In
addition to their dye-yielding characteristics, some of these plants also
possess medicinal value. The use of natural products together with their
therapeutic properties is as ancient as human civilization.
Example:- Natural dyes obtained from plants - Berry, flower, bark, leaf,
seed etc. (e.g. Catechu,
Indigofera, Myrobalan and Pomegranate).
Rajarambapu College of Pharmacy, Kasegaon.
12
2. Sweeteners:-
Artificial sweeteners may be derived through manufacturing of
plant extracts or processed by chemical synthesis. Sugar alcohols such
as erythritol, xylitol, and sorbitol are derived from sugars. In 2017,
sucralose was the most common sugar substitute used in the
manufacture of foods and beverages.
Example:-Stevia is used in many parts of the world as a non-caloric
sweetener. Along with sweetness, a bitter taste is also felt in humans.
3. Binders:-
Binder excipients are formulated to act as an adhesive to
literally “bind together” powders, granules and other dry ingredients
to impart to the product the necessary mechanical strength.
Example:- Gelatine , cellulose, cellulose derivatives, polyvinyl
pyrrolidone , starch, sucrose and polyethylene glycol.
Rajarambapu College of Pharmacy, Kasegaon.
13
4. Diluents :-
Diluents act as fillers in pharmaceutical tablets to increase
weight and improve content uniformity. Natural diluents include
starches, hydrolyzed starches, and partially pre-gelatinized starches.
Example:- anhydrous lactose, lactose monohydrate, and sugar alcohols
such as sorbitol, xylitol and mannitol.
5. Viscosity builders :-
Viscosity modifiers are designed to change the thickness or texture
of pharmaceutical ingredients. . A viscosity modifier can decrease the
thickness of a liquid to improve pour ability and ultimately make it
more palatable.
Example:- Gum, xanthan gum, and gelatin.
Rajarambapu College of Pharmacy, Kasegaon.
14
6. Disintegrants :-
Disintegrants are added to oral solid dosage forms to aid in
their de-aggregation. Disintegrants are formulated to cause a rapid
break-up of solids dosage forms when they come into contact with
moisture.
Example:- Lepidium sativum known as asaliyo and widely used as herbal
medicine and pharmaceutical excipient as disintegrating agent.
7. Flavors & perfumes :-
Flavoring materials are received from a number of sources, and
mostly from plants such as from flower, leaf, stem or bark. These
Flavoring agents have good importance within the business of
medication, they are additionally referred to as “masking agents” or
“bitter blockers”.
Example:- peppermint, clove, eucalyptus and citrus fruits, menthol,
nutmeg, cinnamon.
Rajarambapu College of Pharmacy, Kasegaon.
15
Rajarambapu College of Pharmacy, Kasegaon.
16

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Incorporation of herbal actives in pharmaceuticals

  • 1. Incorporation of herbal actives in pharmaceuticals Presented By: AVITASHRI SAGAR PATIL M. Pharm First Year [Dept. of Pharmaceutics] Rajarambapu College of Pharmacy, Kasegaon. Rajarambapu College of Pharmacy, Kasegaon. 1
  • 2. Introduction:- ‱ Plants produce many chemicals that are biologically active, not just in themselves, but also in other organisms. ‱ The use of herbal products, especially plants for healing is as ancient and universal as medicine itself. ‱ Hippocrates, one of the ancient authors who described medicinal natural products of plant and animal origins, listed approximately 400 different plant species for medicinal purposes. ‱ World Health Organisation (WHO),some 3.4 billion people in the developing world depends on plant based traditional medicines. Rajarambapu College of Pharmacy, Kasegaon. 2
  • 3. ‱ An impressive number of modern drugs have been derived from natural sources. Over the last century, a number of top selling drugs have been developed from natural products. ‱ Nature has been a potential source of therapeutic agents for thousands of years. ‱ Example :- ‱ Anticancer drug vincristine from Vinca rosea, Narcotic analgesic drug Morphine from Papaver somniferum, Antimalarial drug artemisinin from Artemisia annua, Anticancer drug Taxol from Taxus brevifolia and Antibiotic drug Penicillin from penicillium . Rajarambapu College of Pharmacy, Kasegaon. 3
  • 4. Advantages:-  Biodegradable  Biocompatible and nontoxic  Economic  Safe and devoid of side effect  Easy availability Rajarambapu College of Pharmacy, Kasegaon. 4
  • 5. Disadvantages :-  Microbial contamination  Variation  The uncontrolled rate of hydration  Slow process  Heavy metal contamination Rajarambapu College of Pharmacy, Kasegaon. 5
  • 6. Several examples of herbal active ingredients that provide medicinal uses for human being 1. Alkaloids:- This group is comprised of a wide variety of plants that contain nitrogen-bearing molecules that makes them very active. many of these plants have been used to create well-known drugs used for medicinal purposes. Example:- Vincristine, which was derived from periwinkle is used to treat cancer. 2. Bitters:- This group is comprised of a variety of plants that are lumped together because of their very bitter taste. This bitterness causes stimulation of the salivary glands and digestive organs. As such, bitters can be used to improve appetite and strengthen the digestive system. Example:- wormwood and hops. Rajarambapu College of Pharmacy, Kasegaon. 6
  • 7. 3. Cardiac glycosides:- These compounds are found in various medicinal plants and have strong direct action on the heart. Cardiac glycoside such as digitoxin, digoxin ,and convallotoxin support heart strength and rates of contraction when failing. These compounds also have a diuretic effect that stimulates urine production and aids in removal of fluid from tissues and the circulatory system. Example:- Foxglove, Lily. 4. Cyanogenic Glycosides:- These glycocides are based upon cyanide, a very deadly poison, but in small doses, they can serve as a muscle relaxant. The bark of wild cherry and the leaves of elderberry (Sambucus racemosa) contain cyanogenic glycocides, which can be used to suppress and soothe dry coughs. Rajarambapu College of Pharmacy, Kasegaon. 7
  • 8. 5. Flavonoids:- Flavonoids are found widely throughout the plant world and they have a wide range of medicinal uses and actions. They often act as pigments giving a yellow or white color to flowers and fruits. Some flavonoids have anti-viral and anti-inflammatory properties. Flavonoids found in many plants like lemon and buckwheat are known to strengthen capillaries and prevent leakage into tissues. 6. Minerals:- Many plants have high levels of minerals because they can draw minerals from the soil and can convert them into a form that is more easily used by the human body. Mineral content is often the key factor in a plant’s effectiveness as a medicine. One example of a plant high in minerals is horsetail. The high silica content in horsetail plants is used for arthritis because it supports the repair of connective tissue. Rajarambapu College of Pharmacy, Kasegaon. 8
  • 9. 7. Phenols:- Phenols are plant compounds that are thought to be produced to protect against infection and herbivory by insects. They are often anti- inflammatory and antiseptic and can have anti-viral properties. Phenols vary in structure and range from salicylic acid (similar to aspirin) to complex sugar-containing phenolic acids. Wintergreen and willow contain salicylates. Members of the mint family often contain phenols. 8. Polysaccharides:- Polysaccharides are found in all plants and comprised of multiple units of sugar molecules linked together. For medicinal purposes, the “sticky” polysaccharides produce mucilage or gums that are commonly found in bark, roots, leaves, and seeds. These sticky polysaccharides are able to soak up large quantities of water and form jelly like masses that can be used to treat dry or irritated tissues such as skin and mucous membranes. Rajarambapu College of Pharmacy, Kasegaon. 9
  • 10. 9. Proanthocyanins:- These compounds are pigments, which give fruits and flowers red, purple, or blue hues and are closely related to tannins and flavonoids. These compounds have been documented to be valuable in protection of circulation specifically in the heart, eyes, and feet. Red grapes, blackberries, and hawthorn berries all have high levels of proanthocyanins. 10. Saponins:- This group of active compounds obtains its name from the fact that like soap, they produce lather when placed in water. There are two main forms of saponins: steroidal and triterpenoid. Steroidal saponins are very similar to the chemical structures of many of the human body’s hormones including estrogen and cortisol. Examples plants containing saponins include agave, wild yam, and several members of the lily family. Several native plants are used in a process to produce synthetic hormones for humans. Rajarambapu College of Pharmacy, Kasegaon. 10
  • 11. 11. Tannins:- Most plants produce tannins. Tannins serve as a deterrent to herbivory by insects and grazing animals given that that they provide a harsh unpalatable flavor. Tannins are also useful in curing leather because of their tendency to contract and astringe tissues by binding with precipitating proteins. Examples of plants high in tannins include oak bark and black catechu. 12. Volatile oils:- Volatile oils are extracted from plants and are used to produce essential oils that play a very important role in medicinal botany. These oils are often very complex and can be comprised of 100 or more compounds. These oils have many uses. For example, tea tree oil is a strong antiseptic. Resins and gums are often linked with essential oils, however these are not volatile. Rajarambapu College of Pharmacy, Kasegaon. 11
  • 12. 13. Vitamins:- Many plants contain high levels of useful vitamins. Many well- known fruits and vegetables have high levels of vitamin C and beta- carotene. Lesser-known vitamin containing plants like watercress, rose hips, and sea buckthorn have high levels of vitamins B, C, and E. Herbal excipients:- 1. Colorants:- In India, there are more than 450 plants that can yield dyes. In addition to their dye-yielding characteristics, some of these plants also possess medicinal value. The use of natural products together with their therapeutic properties is as ancient as human civilization. Example:- Natural dyes obtained from plants - Berry, flower, bark, leaf, seed etc. (e.g. Catechu, Indigofera, Myrobalan and Pomegranate). Rajarambapu College of Pharmacy, Kasegaon. 12
  • 13. 2. Sweeteners:- Artificial sweeteners may be derived through manufacturing of plant extracts or processed by chemical synthesis. Sugar alcohols such as erythritol, xylitol, and sorbitol are derived from sugars. In 2017, sucralose was the most common sugar substitute used in the manufacture of foods and beverages. Example:-Stevia is used in many parts of the world as a non-caloric sweetener. Along with sweetness, a bitter taste is also felt in humans. 3. Binders:- Binder excipients are formulated to act as an adhesive to literally “bind together” powders, granules and other dry ingredients to impart to the product the necessary mechanical strength. Example:- Gelatine , cellulose, cellulose derivatives, polyvinyl pyrrolidone , starch, sucrose and polyethylene glycol. Rajarambapu College of Pharmacy, Kasegaon. 13
  • 14. 4. Diluents :- Diluents act as fillers in pharmaceutical tablets to increase weight and improve content uniformity. Natural diluents include starches, hydrolyzed starches, and partially pre-gelatinized starches. Example:- anhydrous lactose, lactose monohydrate, and sugar alcohols such as sorbitol, xylitol and mannitol. 5. Viscosity builders :- Viscosity modifiers are designed to change the thickness or texture of pharmaceutical ingredients. . A viscosity modifier can decrease the thickness of a liquid to improve pour ability and ultimately make it more palatable. Example:- Gum, xanthan gum, and gelatin. Rajarambapu College of Pharmacy, Kasegaon. 14
  • 15. 6. Disintegrants :- Disintegrants are added to oral solid dosage forms to aid in their de-aggregation. Disintegrants are formulated to cause a rapid break-up of solids dosage forms when they come into contact with moisture. Example:- Lepidium sativum known as asaliyo and widely used as herbal medicine and pharmaceutical excipient as disintegrating agent. 7. Flavors & perfumes :- Flavoring materials are received from a number of sources, and mostly from plants such as from flower, leaf, stem or bark. These Flavoring agents have good importance within the business of medication, they are additionally referred to as “masking agents” or “bitter blockers”. Example:- peppermint, clove, eucalyptus and citrus fruits, menthol, nutmeg, cinnamon. Rajarambapu College of Pharmacy, Kasegaon. 15
  • 16. Rajarambapu College of Pharmacy, Kasegaon. 16