Challenges in herbal formulation Steps in herbal drug formulation Types of conventional herbal formulations Liquid herbal dosage forms Solid herbal dosage forms Other herbal dosage forms Novel dosage form

1. HERBAL FORMULATIONS
Presented By:
Mahewash Sana A. Pathan

2. CONTENTS:
• Challenges in herbal formulation
• Steps in herbal drug formulation
• Types of conventional herbal formulations
• Liquid herbal dosage forms
• Solid herbal dosage forms
• Other herbal dosage forms
• Novel dosage form
2

3. CHALLENGES IN HERBAL FORMULATION
• According to WHO, herbal dosage forms are the physical form like
liquid, solid, semi-solid products produced from herbs, with or
without excipients, in a particular formulation (such as decoctions,
tablets, ointment, etc.)
• The toxicological, epidemiological & other data available regarding
herbal formulation is confusing.
• Authentication of herbal materials is difficult.
• Pharmacological, toxicological & clinical documentation is tedious
task.
• It is difficult to follow pharmacovigilance guidelines in case of
herbal formulations.
• There is need to study herb-drug interactions.
• Standardization, safety & efficacy are a big challenge.
• There is various hurdles in conduction of clinical trials of herbal
formulations.
3

4. STEPS IN HERBAL DRUG FORMULATION
Selection,
drying &
grinding of
herbal
drugs
Extraction
of plant
materials
Filtration
&
concentrat
ion of
extracts
Powdered
extract
Preparatio
n of
dosage
forms
4

5. TYPES OF CONVENTIONAL HERBAL
FORMULATIONS
Conventional
herbal dosage
forms
Liquids solids Others
5

6. Liquid Herbal dosage forms
1. DECOCTIONS:
Extract is cooled & filtered
Boiling of crude drug with
water for a specific time
Dosage: 3-4 times a day upto 500
ml per day.
Example: Sijunzi decoction
(chinese herbal remedy,
mixture of Panax Ginseng,
Poriacocos, Atractylodes
macrocephala & Glycyrrhiza
auralensis)
6

7. 2. INFUSIONS:
• These are made by using
cold or hot water for herbal
extraction are dilute
solutions.
• Should be stored in cold &
dry place
• Shelf life is upto 24 hrs.
Dosage: 3-4 times a day upto
500 ml per day.
• Example: Tea, coffee, lemon
infusions.
7

8. 3. TINCTURE
• It is an alcoholic or
hydroalcoholic extract of
herbal materials, by using 1
part of herb & 5-10 parts of
ethanol.
• Can be stored in cool, dry &
dark place for 2 yrs.
Dosage: 5ml diluted to 25 ml,
2-3 times a day.
• Example: Tincture of iodine,
Benzoin tincture, cannabis
tincture.
8

9. 4. SYRUP:-
• Syrups are viscous liquids
containing high amount of sugars
or other sweetening agents.
• May or may not contain medicine
& flavoring agents.
• Due to high sugar content, they
are susceptible to microbial
contamination so they contain
preservatives.
EVALUATION:
• Organoleptic characters
• pH
• Specific gravity
• Total solid content
• Viscosity
• Stability
Preparation:
Preservative, colorants, flavoring agent may be
added.
Plant decoction is mixed with simple syrup in 1:4
ratio.
Solution is filtered
Decoction of plant material is prepared by boiling in
water.
40 gm of sucrose is dissolved in sufficient water to
get 100 ml of conc. Simple syrup.
Dosage: 1-2 teaspoonful thrice a day.
Example: Hempushpa syrup, Brahmi
syrup, Cough syrup, Heart tonic syrup.
9

10. 5. ORAL EMULSIONS:
• These are liquid dosage forms
consisting of two immiscible
phases which are stabilized by
addition of emulsifying agent.
One liquid can be uniformly
dispersed in another
immiscible liquid in the form
of small droplets using
emulsification equipment such
as agitators, homogenizers,
colloid mills & ultrasonic
devices.
Example: Intralipid®
Perikabiven®
10

11. 6. AROMATIC WATERS:
• These are water based
formulations saturated with
essential oils.
• These are prepared by
mixing distilled water with
one part of essential oil &
ten parts of talcum powder.
• It is shaken well & then kept
aside for 12 hrs, & then
filtered & volume is
adjusted.
• It should be made in small
quantities to protect it from
decomposition.
• Example: cardamom water,
peppermint water, camphor
water.
11

12. 7. HERBAL GLYCERITES:
• These are tincture like
dosage forms which are
prepared by extracting
herbal drugs with 50-60% of
glycerine as extraction
medium.
• The shelf life of glycerites is
about 6 months to 2 years.
• This form is suitable for
preparation of pediatric
medicines.
• Glycerin cannot be used for
herbs containing gums or
resins.
• Examples: Goldenseal
extract, Echinacea herbal
extract, Rhodiola extract.
12

13. 8. OXYMELS:
• These are sweet & sour
formulations containing
honey & small amount of
vinegar as carrier.
• Example: Garlic, Cayenne,
lobelia oxymels.
13

14. SOLID HERBAL DOSAGE FORMS
1. HERBAL TEA BAGS:
• Herbal materials i.e. dried
roots or leaves or flowers
are packed into paper or
cloth bags. Bags should be
free from bleach, gluten &
dioxin.
• The boiling should be
poured on bags for making
infusion.
2. DRIED POWDER:
• Herbs are dried &
pulverized to make coarse
or fine powder.
• It can be administered
directly by mixing with
warm water & can be
available as capsule or
sachet form.
14

15. 3. DRY EXTRACT POWDER:
• These can be prepared by
spray drying or freeze drying
of fluid extract with or without
using an adsorbent, or made
by drying & milling to produce
a powder.
• It may contain excipients,
stabilizers & preservatives.dry
extracts can be incorporated in
capsules, tablets or granules.
4. HERBAL MIXTURES:
• These are combination of
two or more plants. Plants
are dried & pulverized &
mixed into specific
proportions to get herbal
mixtures.
15

16. 5. GRANULES:
• These are agglomerations of
small spherical particles made
from dried fluid extracts.
• Can be administered after
reconstitution with water as
solution or suspensions.
• Can be used to make tablets or
capsules.
• E.g. Vasawlehachurna
granules, chyavanprash
granules, Gastrobeet oral
dispersible granules.
6. PILLS:
• These are spherical dosage
forms larger than granules
made from herbal extracts.
• These are made by
triturating dried powdered
herbs or dry extract with
excipients to form mass.
• E.g. Madhunashinivati,
chandraprabhavati,
khadiradivati, etc.
16

17. 7. CAPSULES:
• These are solid dosage forms
containing drug & appropriate
filler enclosed in a gelatin
container.
Advantages:
• Mask unpleasant taste of
medicine.
• Provide uniformity of dosage.
• Release content rapidly than
tablets.
E.g. Fenugreek capsules, Chlorella
capsules, pudinhara, moringa
capsules, etc.
8. LOZENGES:
• These are solid dosage form
which slowly release
medication in mouth.
• Can give local or systemic
action.
• Herbal extract is boiled with
sucrose & water to make
lozenges.
17

18. 9. TABLETS:
• Tablets are solid dosage form
made up of herbal extract,
granule is blended with
excipients & compressed to
form a defined size & shape.
• Preparation methods:
1. Direct compression
2. Wet granulation
3. Dry granulation
Coating of tablets:
• it is done to mask undesirable
colour, odour, taste, to protect
from moisture.
• It is carried out by using pan
coating or press coating
method.
Evaluation:
• Pre-compression:
Bulk density, tapped density,
housner’s ratio, carr’s index,
angle of repose.
• Post compression;
Hardness, thickness, friability,
weight variation, content
uniformity, disintegration
time, dissolution time, etc.
18

19. OTHER HERBAL DOSAGE FORMS
1. OINTMENTS:
• These are semi-solid greasy
preparations containing
anhydrous immiscible base
generally used for skin, rectum or
nasal mucosa.
• The process of making ointment
involve heating of oil & aqueous
phase separately & then mixing
of both phases with constant
stirring until the mixture get
congealed.
• E.g. Calendula ointment,
Herboheal ointment, pilex, pain
care ointment.
2. HERBAL CREAMS:
• Creams are semisolid dosage
forms containing herb in
hydrophilic base.
• Prepared by mixing powdered
drug or extract in cream base.
• It has relatively short shelf life
as compared to ointment.
• E.g. herbal fairness cream,
baby cream, etc. 19

20. 3. HERBAL BALMS:
• These dosage forms are like
ointment used to relieve
pain.
• These are made by mixing
herbs with ointment base.
• E.g. tiger balm, herbal pain
balm, lip balm.
4. INHALATIONS:
• These preparations
intended to be used in
bronchial tubes or lungs in
the form of aerosols.
• They may be dry powder
inhalation or liquid
inhalation.
• E.g. Astha aid drops, karval
plus inhalation capsules.
20

21. 5. PLASTERS & PATCHES:
• These are made by
spreading soft or dry herbal
extract on support made up
of fabric or synthetic resin.
• Intended to use topically on
the skin & deliver the active
ingredient through the skin.
• E.g. capsicum patch, herbal
medicated plasters.
6. MEDICATED OIL:
• These are prepared by
mixing, macerating or
boiling herbal drug, extract
of fresh juice with suitable
fixed oils.
• E.g. indulekha oil, tea tree
oil, peppermint oil, etc.
21

22. 7. HERBAL SOAPS:
• These are prepared by
incorporating herbal drugs
having antifungal or
antimicrobial properties
with detergent base.
• E.g. neem & turmeric soap,
papaya skin whitening soap.
8. HERBAL PASTES:
• These are similar to
ointment which contain
50% of drug powder
incorporated in fatty base.
• E.g. Dantkanti toothpaste,
miswak, Aloe vera
toothpaste.
22

23. 9. HERBAL SUPPOSITORIES &
PESSARIES:
• Made by mixing finely
powdered herbs or extracts
with cocoa butter base.
• E.g. tea tree pessaries,
neem oil suppositories,
herbal vaginal pessaries.
10. Herbal liniments:
• Used in the treatment of
soreness in muscles &
ligaments & pain.
• Should not be applied on
cut or broken skin
• Prepared by using alcoholic
extract of heat producing
herbs.
• E.g. liniment plus, penil.
23

24. NOVEL DOSAGE FORM
• Novel drug delivery system (NDDS) means the approaches,
formulations, technologies, & systems to transport a
pharmaceutical compound in the body so that it can safely
achieve its desired therapeutic effects.
• NDDS is nothing but combination of advanced techniques &
new dosage forms in which drug is delivered by the system
other than conventional drug delivery system.
• Advantages of NDDS:
1. Solubility & bioavailability enhancement
2. Enhance distribution & pharmacological activity.
3. Drugs can be released at predetermined rate
4. Less toxicity
5. Improve stability
6. Easily administered
7. Sustained action
24

25. 1. LIPOSOMES:
• These are microparticulate or
colloidal carriers having 0.05-0.5
micrometer diameter.
• Liposomes are artificial
microscopic vescicles containing
one or more phospholipid layers
enclosing an aqueous core.
• They are used to convey vaccines,
drugs, enzymes, or other
substances to target cells or
organs.
• Advantages: Highly
biocompatible, Biodegradable,
non-immunogenic, Easy to
prepare, Pharmacokinetic
properties can be easily
modulated, Can produce
sustained or controlled release.
• Preparation:
• Examples:
1. Therapeutic efficacy of
anticancer drug, ampelopsin is
improved.
2. Catechins show improved
permeability in skin
3. Uric acid liposomes show
enhanced solubility.
Lipids are
isolated using
organic solvent
Lipids disperse
in aqueous
media
Drug is loaded
by active or
passive loading
technique
Purification &
evaluation of
liposomes.
25

26. 2. PHYTOSOMES
• Phyto- plant; soma- cell like.
• Phytosomes are NDDS of
standardized plant extract or
water soluble phytoconstituents
which are entrapped into
phospholipids to produce lipid
compatible molecular
complexes.
• Preparation:
• Example: silymarin phytosome
showed increased
bioavailability , quercetin
phytosome exhibit improved
hepato-protective action.
Purification & evaluation.
Isolation of phytosomal complex by
lyophilization or spray drying
Extract of phytoconstituents mixed
in above solution in 1:1 ratio
Phospholipids are dissolved in
organic solvent
26

27. 3. NANOPARTICLES
• These are nano-sized
particles, ranging from 10-
1000 nm, containing
synthetic or semisynthetic or
herbal drugs.
• Advantages: enhance
solubility, reduce doses, can
deliver drug to site of action
& improve absorbance.
• Preparation:
• Examples: Artemisinin nano-
capsules show sustained drug
release, improved bioavailability
of glycyrrhizic acid.
Purification & evaluation.
Techniques include nano-precipitation,
emulsification, solvent diffusion, salting
out, dialysis, SCF.
Dispersion of polymers by different
techniques
27

28. 4. Microsphere
• These are spherical micro
particles having diameter of 1-
1000 mm.
• Made up of biodegradable
polymers like polylactic acid,
glycolic acid, albumin dextran &
firinogen.
• Advantages: can be ingested or
injected, easy to get desired
release profile, do not affect
drug activity,
• Preparation: microspheres are
prepared by various
techmiques such as spray
drying, solvent evaporation,
single & double
emulasification, phase
seperation coacervation,
solvent extraction & quassi-
emulsion solvent diffusion.
• Examples: Rutin-alginate-
chitosan microcapsules able to
target cardiovascular or
cerebrovascular region,
camptothecin loaded
microspheres show prolong
drug action. 28

29. 5. ETHOSOMES
• Ethosomes are nano-vesicles
made up of phospholipids &
have high content of ethanol
i.e. 20-45%.
• Advantages:
1. Help to improve
transdermal permeation of
drug through skin.
2. Can be used for drug
delivery of variety of drug .
3. As it is in semi solid
,provide improved patient
compliance.
• Preparation: Cold method
,classic mechanical
dispersion method.
• E. g.
1. liquorice ethosome show
anti inflammatory activity
and sustained release
2. Cannabis ethosome show
improved skin permeation.
29

30. 6. TRANSFEROSOMES
• They are vesicular system
consisting of phospholipids,
10-25% surfactant and 3-
10% ethanol.
• Preparation: Thin film
hydration, modified hand
shaking, lipid film hydration
E.g.. Capsicum transferosome
show increased skin
permeation
30

31. 7. NIOSOME
• This are multilamellar vesicles similar to liposomes & made
up of non ionic surfactant & cholesterol.
31

32. 8. PRONIOSOME
• They are water soluble
carrier particles coated with
surfactant .
• Before use these are
hydrated to form niosome
by shaking. These are gel
formulation
• E. g. levonorgestrel
proniosome gel or
patch .
32

33. 9. TRANSDERMAL DRUG DELIVERY SYSTEM
(TDDS)
• It is NDDS in which drug is delivered in the form of patches
through the skin.
• Preparation: Basic component are polymer or drug
reservoir, drug, permeation enhancer, backing laminates,
release liner & excipients.
Following methods are used
1. Polymer membrane permeation controlled TDDS
2. Matrix diffusion controlled TDDS
3. Micro-reservoir controlled TDDS
33

34. 34