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21. Herbal Formulation

Colourants:
 Colourant/colouradditiveisasubstancethatisadded
orappliedinordertochangethecolourofamaterial orsurface.colourantscanbeusedformanypurposes includingfoods,formulations,printing,painting,and plastics.Colourantsworkbyabsorbingvaryingamounts oflightatdifferentwavelengths(orfrequencies)ofits spectrum,transmitting(iftranslucent)orreectingthe
remaining light in straight lines or scattered. In India,
thereare≥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civilisation and fora long-time,
mineral, plant and animal products were the main
sourcesofdrugs.
Examples:Jack fruit (Artocarpus heterophyllus Lam),
turmeric (Curcuma longa), Hina (Lawsonia inermis L), Saffron(Crocus sativus), Sappan wood (Caesalpinia
sappan), Indigo (Indigofera tinctoria),Safower(Carthamus tinctorius), Madder or manjistha or Rubia (Rubia tinctorum),Logwood (Haematoxylon compechianum),
onion (Allium cepa), tea waste (Camellia sinensis), Pomegranate rind (Punica granatum), Chestnut hulls (peach to brown), Catechu or Cutch tree (brown), etc.
 Justication: colouring agents are substances which
colourother substances that are devoid of colour (transparent,white,orgray)orchangethecolourofthe substancethatalreadyhasadifferentcolour.
Sweeteners
 Asugarsubstituteisafoodadditivethatprovidesasweet
tastelike that of sugar while containing signicantly lessfoodenergythansugar-basedsweeteners,making ita zerocalorie or low-calorie sweetener. 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.Datesarewonderfulsweeteners
loaded with K, copper, iron, manganese, metallic element and pyridoxal. The syrup is an excellent sweetener enriched in manganese, calcium, potassium, and Zn.
Examples: Honey, dates, sugar, coconut sugar, maple
syrup,molasses,agavenectar,etc.
 Justication:Sweetening agent excipients are substances
thatsweetenandmaskthetasteoffood,beveragesand
medications to make them palatable to the consumer.
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.Theycanalsogivevolumetolow activedosetablets.Commonlyusedinwetgranulation, binders are added to create a more effectiveand
predictablegranule formation. Binders are classied
according to their application.
Examples: Guar gum, locurt gum, potato starch, gelatin,
cellulose,cellulosederivatives,polyvinylpyrrolidone,
starch, sucrose, polyethylene glycol, etc.
 Justication:Binderexcipientsholdtheingredientsof
aformulationtogether.
Diluents
 Diluents act asfillers in pharmaceutical tablets to
increaseweight and improve content uniformity.
Natural diluents include starches, hydrolysed starches,
andpartiallypre-gelatinisedstarches.Commondiluents
include anhydrous lactose, lactose monohydrate, and sugar alcohols, such as sorbitol, xylitol, mannitol.
Diluentsprovide better tabletproperties such as improvedcohesionortopromoteow.Mannitolisone ofthecostliestdiluents,however,itisstilloftenuseddue tothesensationitprovideswhenitisusedinchewable tablets. Diluents mustbe nontoxic, commercially availablein acceptable grade, physiologically inert, andphysically and chemically stable by themselves aswellasincombination with active pharmaceutical
ingredients (APIs).
Examples: Microcrystalline cellulose, lactose, sucrose,
gelatin, glucose, anhydrous lactose, lactose monohydrate, sorbitol, xylitol and mannitol, etc.
 Justication:Diluents or llers arepharmaceutical
componentswhichdonothave any pharmacological effectbutarenecessaryforpharmaceuticalpreparations. Diluentsarechemicallyineffectiveexcipients,mostof whichareusedintheformulationupto80%tobuild upthenecessarybulkofthedosageform.
ViscosityBuilders
 Viscositymodiersaredesignedtochangethethickness
ortexture of pharmaceutical ingredients. Viscosity modierscan include such products asthickeners, texturizers,gelationagentsandstiffeningagents.Many viscosity modiers canbe used to convert liquids to gels,pastesorpowderstoaidformulatorsincreating theideal product forend users. A viscositymodier candecreasethethicknessofaliquidtoimprovepour
ability and ultimately make it more palatable.
Examples: Embrace algarroba bean gum, xanthan gum,
gelatin, etc.
 Justication: Variousthickeners are found in natureor
arederivatives of natural thickeners. These ingredients
are polymers that absorb water to expand and increase
viscosity.Polyosederivativeslikehydroxyethylcelluloseare oftenemployedinproductslikeshampooorbodywashes. Gumisanotherexampleofanaturallyderivedthickener.
Disintegrants
 Disintegrantsareaddedtooralsoliddosageformstoaid
intheir de-aggregation. Disintegrantsare formulated
Section 2 Pharmacognosy
329
tocause a rapidbreak-up of solid dosageforms when theycomeinto contactwithmoisture.Disintegrationis typicallyviewedastherststepinthedissolutionprocess.
Examples: Crosslinked polymers, including crosslinked
polyvinylpyrrolidone(crospovidone), crosslinked
sodium carboxymethyl cellulose (croscarmellose
sodium),and the modified starch, sodium starch,
glycolate, Lepidus sativum, Isapghula husk (Plantago ovata), Hibiscus rosa sinesis Linn.
 Justication:Disintegratingagentsconstitutesubstances
intabletandcertainformulationsofrigidcapsulesused tomake it easier for dissolution fluid to penetrate moistureanddispersedosageform.Anoralsolidform ofdosage should ideally be dispersedinto the core particlesfromwhichitwasmadeof.
Flavours and perfumes
 Flavouring materials are received from a numberof
sources,andmostlyfromplant,suchasfromower, leaf,stemorbark.Tobeemployedinfoodmerchandise, thematerials area unit typically extracted from the materialtoproduceanisolatethatissimplytheavour. Theseavouringagentshavegoodimportancewithin thebusinessofmedication,particularlyincamouaging withthe medicines by their indispensable avours. Thus,they are additionally referred to as “masking
agents” or “bitter blockers”.
Examples:Different essential oils of anise,clove,
caraway,pimento,eucalyptusandcitrusfruits,menthol,
nutmeg, thyme or cinnamon, etc.
 Justication:Substancesaddedtofoodsandmedicine
toimprovethequalityoftaste.
Preservatives
 Preservativesareusuallyusedtomaximisetheshelf-
lifeof several food products and pharmaceuticals. Preservativesare vital to avoid thealteration and degradationof microorganisms during storage,
particularly in those with greater water content.
Example: Cinnamon, cayenne pepper, turmeric, cumin
seeds,neemoil,cloveoil,etc.
 Justication:Apreservativeisasubstanceorachemical
thatis added to products, such as foodproducts, beverages,pharmaceutical drugs, paints, biological
samples, cosmetics, wood, and many other products
toprevent decomposition by microbialgrowthor by
undesirable chemical changes.
Solvents
 Organic solvents are entrapped within the
formulationeitherduringthecourseofmanufacture ofactive pharmaceutical ingredients or during coatingof formulation. Residuallevels of these organicsolventsintabletcoresand filmcoatsare
critical as beyond permissible limits they are likely
tocause undesirable side effects or alter some kindof physicochemical property of theactive
pharmaceutical ingredients.
Example: Methanol, isopropyl alcohol, acetone, toluene,
butanol, dichloromethane, etc.
 Justication:The substance, usually a liquid, in which
anothersubstance (the solute) is dissolvedto form a
solution.
Active Ingredient
 Anactiveingredientistheingredientinapharmaceutical
drugor pesticide that is biologicallyactive. The similarterms active pharmaceutical ingredient (also abbreviatedas API) andbulk active are also used in medicine,andthetermactivesubstancemaybeused fornaturalproducts.
Examples: Neemleaves powder, Shikakai powder,
Boswellia, Ashwagandha, Triphala [amla (Emblica ofcinalis, or Indian gooseberry), Bibhitaki (Terminalia bellirica), Haritaki (Terminalia chebula)], Brahmi, cumin, licorice root, Gotu kola, bitter melon, cardamom, iron (Loha Bhasma), copper (Tamra Bhasma), etc.
 Justication: Active ingredient means theclinically
activematerial(s) that provide(s) pharmacological activityin a pharmaceutical product (excluding formulationcomponents,suchascoatings,stabilisers, excipientsor solvents,adjuvantsorcontrolledrelease
technologies).
Section 2 Pharmacognosy
330
Classication of bioenhancers
NATURAL BIOENHANCERS AND THEIR MAIN MECHANISMS OF ACTION ON VARIOUS DRUGS
S. No. Natural bioenhancer Biological source Mechanism of action
1. Aloe Aloe vera Intercellular modulation
2. Caraway Carum carvi Local mucosal tissue modulation
3. Curcumin Curcuma longa Metabolism (UDP-glucuronyl transferase) inhibition
4. Gallic acid ester Gallnuts, tea leaves, oak bark
5. Genistein Pueraria lobata Efflux transporter (MRP) inhibition
6. Gokhru extract Tribulus terrestris Local mucosal tissue modulation
7. Grapefruit juice Citrus paradisi Efflux transporter (P-gp, MRP2); metabolism (CYP3A4)
8. Lycopene Carotenoid Plant (red fruits and vegetables)
9. Peppermint oil
(herbal) plant (peppermint)
10. Piperine (alkaloid) Piper longum and
11 Quercetin
(flavonoid) plant
Mentha pipertita Metabolism (CYP3A) inhibition
Piper nigrum
Citrus fruits, vegetables, leaves, grains
Metabolism (CYP3A) inhibition
inhibition; renal uptake transporter (OATP) inhibition Dual carotenoid/LDL receptor mechanism for targeted hepatic
delivery
Local mucosal tissue modulation; thermogenic activity.
Efflux transporter (P-gp) inhibition
HERBAL EXCIPIENTS
Excipientsweredenedasthesubstanceusedasamedium forgivinga medicament, that istosay with simply the functionsof an inert support ofthe active principle or
principles.
Pharmaceuticalexcipientscanbedenedasnon-active
ingredientsthataremixedwiththerapeuticallyactive compound(s)toformmedicines.Theingredientwhich isnotanactivecompoundisregardedasanexcipient.
Classication of excipients
Excipientsaffect the behaviourand effectiveness of thedrug product more and morefunctionality and signicantly.
Excipients are alsoderived from natural sources,
synthesised chemically, or prepared semisynthetically
startingfromnaturalsourcedmaterials.Theyrangefrom simple,usually well-characterised, organic or inorganic moleculesto highly complex materials that are difcult tofullycharacterise.
Section 2 Pharmacognosy
331
Signicance of herbal excipients
CLASSIFICATION OF HERBAL EXCIPIENTS
Classicationof excipients is based ontheir role in thepharmaceutical formulation, their interactions inuencingdrugdelivery,ortheirchemicalandphysico-
chemical properties.
Excipients are also sometimes used to bulk up
formulationsthatcontainverypotentactiveingredients, toallowforconvenientandaccuratedosage.Depending ontherouteofadministration,andformofmedication, differentexcipientsmaybeused.
CLASSIFICATION OF NATURAL EXCIPIENTS ACCORDING TO THEIR PHARMACOLOGICAL ACTION
S. No. Type Examples
1. Antioxidant Tocopherol, vitamin C, citric acid, lecithin
2. Antibacterial Neem, curcuma
3. Adsorbents Kaolin, pectin, magnesium oxide
4. Antiadherants Talc, magnesium sterate, corn starch
5. Binding agents Acacia, tragacanth, gelatin
6. Colourant Amarnath, caramel, chlorophyll
7. Disintegrating agents CMC, starch
8. Diluents Starch, sucrose, lactose, mannitol
9. Emulsifying agents Guar gum, agar and acacia
Section 2 Pharmacognosy
10. Flavours Vanilla, lemon oil, orange oil
332
Contd...
S. No. Type Examples
11. Glidants Aerosil, talc
12. Lubricants Stearic acid, cocoa butter
13. Sweetening agent Honey, glycyrrhiza
13. Thickening agent Methyl cellulose, tragacanth
CLASSIFICATION OF NATURAL EXCIPIENTS ACCORDING TO THEIR CHEMICAL NATURE
S.No. Chemical Nature Example
1. Carbohydrates Acacia, tragacanth, agar, honey, pectin, Guar gum, dextrin
2. Fixed oils Cod liver oil, castor oil, soya bean oil, almond oil
3. Fats and waxes Cocoa butter, coconut oil, lard, beeswax, carnauba wax, spermaceti
4. Volatile oil Eucalyptus oil, clove oil, peppermint oil, lavender oil
5. Enzymes Pancreatin, pepsin, papain
6. Tannins Myrobalan, amla, bahera
7. Protein Gelatin, casein
Natural colourants
Colourants are characterised by their ability to absorb
visible part of the electromagnetic spectrum (380-780 nm).Forgood colouring property it hastohave high enough absorption coefcient(10000 to 40000 Imol-1
cm-1).
Colourantscouldbedividedbytheircolour,chemical compositionorstructure,biologicalfunctioninplant/
organism, physical properties (solubility), etc.
Natural colourants and their types
Classication of natural colourants
Classication of natural colourants
Extraction and isolation of natural colourants
Section 2 Pharmacognosy
333
CLASSIFICATION OF NATURAL COLOURANTS
1. PolyeneColourants: Polyenes are hydrocarbons with
more conjugated double bonds in the chain mostly in
“trans”conguration.
 Examples: Crocin extractis the trade term for the
yellow, water-soluble foodcolourant obtained from cape jasmine (Gardenia jasminoidesL.) and from red stigmasofsaffron(Crocus sativusL.).Curcuministhe principalcolourpresentintherhizomeoftheturmeric
plant (Curcuma longa).
2. Chalcone colourants:Safower(Carthamus tinctoriusL.)
Formerlyasareddyestufffortextiles;andcurrentlyas aminorcolourantbythefoodindustry.
3. Anthraquinones:LacobtainedfromCoccus laccae as a
reddyestuffduetolaccaicacid.
4. Napthaquinones:HennaobtainedfromLawsonia alba
asorangedyestuffduetopresenceofLawsone.Walnut obtainedfromJuglans nigraasbrowndyestuffdueto
presenceofJuglone.
5. Carotenoids:CapsicumobtainedfromCapsicum annum
capsanthinwhichhasorange-redcolourshade.Saffron fromCrocus sativus contains crocin which isyellow-
orange dye.
6. Indole derivatives:Indigo (Indigofera tinctoria)
contains blue colour dye due to compound Indigotin.
7. Oxyindole glycosides: Beetroot from Beta vulgaris
contains betanin which is a red colour dye.
8. Diaryl heptanoids:TurmericobtainedfromCurcuma
longa contains Curcumin which is yellow colour dye.
9. Benzopyrones:Logwoodcontainshaematinisablack
colour dye.
Classification on the basis of their source:
1. Natural polymers: Starch, pregelatinised starch, gelatin,
acacia, tragacanth and gums.
2. Synthetic polymers: PVC, HPMC, methyl cellulose,
ethyl cellulose, PEG.
3. Sugars: Glucose, sucrose, and sorbitol.
NUTRACEUTICALS HERBAL-BASED FORMULATION
Anutraceuticalisanysubstanceconsideredasafood,
or its part which, in addition to its normal nutritional
valueprovideshealthbenetsincludingtheprevention ofdiseaseorpromotionofhealth, e.g. lycopene, beta-
carotene.
Anutraceuticalis“anynon-toxicfoodcomponentthat hasscientifically proven health benefits, including diseasetreatmentorprevention.”Thetermnutraceuticals wascoinedfrom“nutrition”and“pharmaceutical”by StephenDefelice MD, founder and chairman of the foundationforinnovationinmedicine(FIM),Cranford,
New Jersy, in 1989.
AccordingtoDefelice“nutraceuticalsarefoodorpartof afoodthatprovidemedicalorhealthbenetsincluding thepreventionand/or treatment of adisease.”Greek physicianHippocrates(knownasfatherofmedicines) said“letfoodbeyourmedicine”.Thephilosophybehind is“focus on prevention”. Other words used in the contextareDietarysupplements,functionalfood,multi­functionalfood,etc.Functionalfoodsareordinaryfoods thathave components, ingredients that incorporated intogive them a specic medicinalor health benet, moreover,nutritionaleffect.
Schematic representation of different forms of nutraceuticals
NATURAL SWEETENERS AND ITS TYPE
NATURAL BINDING AGENTS
Bindersare agents employed to impart cohesiveness to thegranules. Thisensuresthetabletremainsintactafter compressionaswell as improving theowqualities by theformulationofgranulesofderivedhardnessandsize. Thechoice of a suitable binder for a tablet formulation requiresextensiveknowledgeoftherelativeimportanceof
Section 2 Pharmacognosy
binderpropertiesforenhancingthestrengthofthetablet andalsooftheinteractionsbetweenthevariousmaterials
334
constituting a tablet.
According to dietary supplement, health and education
Act(DSHEA), dietary supplementsare products
intended to supplement the diet that bears or contains
oneor more of the followingdietary ingredients: Avitamin, a mineral, a herbor other botanical, an aminoacid, a dietary substance for use byman to
supplement the diet by increasing the total daily intake, or a concentrate, metabolite, constituent, extract, or
combinations of theseingredients. It may be taken inthe form of pill capsule,tablet, or liquid form. It isnotrepresented for use as aconventionalfoodor asthe sole item of ameal or diet. It islabeled as a “dietarysupplement.”UndertheDSHEA(1994),the manufacturerofadietarysupplementis responsible forensuringthatthedietarysupplementissafebefore itismarketed.Simply,thefunctionalfoodconceptcan bedenedasfoodproductstobetakenaspartofthe usualdietin order to have benecialeffectsthat go beyondbasicnutritionalfunction.
BENEFITS OF NUTRACEUTICALS
Avoidthesideeffect.
Mayincreasethehealthbenecialeffect.
Mayhavenaturallydietarysupplement,sodonothave unpleasantsideeffect.
Mayincrease the health value, our diet andimprove medicalconditionofhuman.
Mayeasilybeavailableandeconomicallyaffordable.
Nutritional therapy is a healing system using dietary therapeutics or nutraceuticals as a complementary therapy.
Thistherapyisbasedonthebeliefthatfoodscannotonly besourcesofnutrientsandenergybutcouldalsoprovide medicinalbenets.
CATEGORY OF NUTRACEUTICALS
Substanceswithestablishednutritionalfunctions,suchas vitamins,minerals,aminoacids,andfattyacids—nutrients.
Herbs or botanical products as concentrates or extracts—herbals.
Reagentsderived from other sources (e.g.,pyruvate,
chondroitin sulphate, steroid hormone precursors)
servingspecific functions, such as sportsnutrition, weight-losssupplements,fortiedconventionalfoods,
and meal replacements—dietary supplements.
Dietarysupplements are not intended to treat orcure
disease, whereas nutraceuticals more emphasise the
expectedresultsoftheseproducts,suchaspreventionor treatmentofdiseases.
Some of themost common ways of classifying nutraceuticalscanbebasedonfoodsources,mechanism ofaction,chemicalnature,etc.Thefoodsourcesusedas
nutraceuticals are all natural and can be categorised as:
1. Dietaryber.
2. Probiotics.
3. Prebiotics.
4. Polyunsaturatedfattyacids.
5. Antioxidantvitamins.
6. Polyphenols.
7. Spices.
Nutraceuticalscanbebroadlyclassiedintothefollowing twogroupsareasfollows.
1. Potential nutraceuticals
Section 2 Pharmacognosy
335
2. Established nutraceuticals
CLASSIFICATION OF NUTRACEUTICALS
Section 2 Pharmacognosy
336
Classes and Components of Phytonutrients
S. No. Class/components Sources Potential benefits
1. Fatty acids Milk and meat Improve body composition, reduce cancers
2. Polyphenols
1. Flavonone Citrus fruits Neutralises free radicals, reduce risk
2 Flavones Fruits, vegetables, soya bean
3. Catechins/ Tannin Tea, babul pods
4. Anthocyanidine Fruits
5. Pro-anthocyanidine Cocoa, chocolate, tea, rapeseed Reduce cardiovascular disorders
3. Saponins Soya beans, chick pea Lower cholesterol, anticancer
4. Probiotics/Prebiotics/Synbiotics
Lactobacillus Yogurt Improve GI health Fructo-oligosaccharides Whole grains, onions
5. Phytoestrogen
i) Daidzein, Zenistein Soya bean, flax, maize Reduce menopause symptoms,
ii) Lignans Flax, rye, vegetables Reduce cancer and heart diseases
6. Carotenoids
β-carotene Oat, maize fodder, carrots, vegetables
and fruits Luteine Vegetables Healthy vision Zeoxanthine Eggs, citrus, corn Lycopene Tomatoes Reduce prostate cancer
7. Dietary fiber Insoluble fiber Wheat bran Reduce breast, colon cancer β-glucan Oats Reduce cardiovascular disorders Whole grain Cereal grains
of cancer
maintain bone health
Neutralises free radicals
PHYTOPHARMACEUTICALS WITH THEIR MARKER CONSTITUENTS
Alkaloids are basically nitrogen bases (alkaline) and contain a secondary or tertiary amine function within a heterocyclic ring.
Plant name Marker Structure Biological activity
Adhatoda vasica Adhatodine
Vasicine
Bronchodilator
Bronchodilator
Contd...
Section 2 Pharmacognosy
337
Plant name Marker Structure Biological activity
Atropa belladonna Atropine
Berberis aristata Berberine
Strychnos nux-vomica Brucine
Mydriatic
Antiperodic
Local anaesthetic
Strychnine
Camellia sinensis Caffeine
Erythroxylon coca Cocaine
Convulsant
CNS stimulant
Anaesthetic
Section 2 Pharmacognosy
338
Contd...
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