Herbal excipients

Definition, Functions of excipients, Ideal properties, Advantages, Disadvantages of herbal excipients, Classification of excipients
Natural colorants, Natural sweeteners, Natural binders, Natural diluents, Viscosity builders, Disintegrating agents, Natural perfumes & flavoring agents

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

2. Contents: Definition Functions of excipients Ideal properties Advantages, Disadvantages of herbal excipients Classification of excipients Natural colorants Natural sweeteners Natural binders Natural diluents Viscosity builders Disintegrating agents Natural perfumes & flavoring agents 2

3. PHARMACEUTICAL EXCIPIENTS: According to International Pharmaceutical Excipients Council- “substance other than the active drug substance which has been appropriately evaluated for safety & are included in a drug delivery system to either aid the processing of the drug delivery system during its manufacture, protect, support or enhance stability, bioavailability, assist in product identification, or enhance any other attributes of the overall safety & effectiveness of the drug delivery system during storage or use.” Pharmaceutical excipients are inactive substances added to medicinally active compounds to formulate dosage form. 3

4. FUNCTIONS OF EXCIPIENTS Add bulk to the formulation During manufacturing, helps to handle API. Assist in drug administration Enhance patient compliance Enhance drug solubility & bioavailability. Avoid drug degradation Give robust & reproducible result of formulation Modify the pH & osmolarity of liquid dosage form. Helps in particle dispersion Helps to mask unpleasant taste, odor, color. Helps to maintain stability. 4

5. 5

6. IDEAL PROPERTIES OF EXCIPIENTS They can be used practically. They should be non toxic & nonirritant Should be non volatile in nature. Should not be affected by temperature, light & hydrolysis. Should be easily available & cheap. Should not have specific color, odor & taste. Should possess good water & lipid solubility. Should be compatible with active ingredient in the preparation Should be pharmacologically inert. 6

7. 7

8. ADVANTAGES OF HERBAL EXCIPIENTS : Natural excipients are Biocompatible, economic, easily available, less toxic, have soothing action & nonirritant, safe & biodegradable, and can be chemically modified. DISADVANTAGES OF HERBAL EXCIPIENTS: they are prone to microbial contamination, yield & chemical composition of natural excipients vary in different conditions, there are possibilities of heavy metal contamination. 8

9. CLASSIFICATION OF HERBAL EXCIPIENTS Based on regulatory aspects- 9

10. CLASSIFICATION OF HERBAL EXCIPIENTS Based on Source - 10

11. CLASSIFICATION OF HERBAL EXCIPIENTS Based on Chemical nature - 11

12. CLASSIFICATION OF HERBAL EXCIPIENTS Based on Application of excipients - 12

13. NATURAL COLOURANTS Natural colorants are highly colored compound capable to impart colour to fabric, leather, drugs, cosmetics, & plastic. Advantages of natural colorants: Natural colourants are soft, lustrous and soothing. Wide ranges are available. They are usually renewable. Eco-friendly & stable. Non hazardous to human health. Show some medicinal properties. 13

14. 1. HENNA Synonym : Egyptian private, Mignonnette , Mahendi . B/S : Dried leaves of Lawsonia inermis , Family- Lythraceae . G/S : North Africa, India, Srilanka . C/C : Lawsone (2,5-Dihydroxy-1,4- naphthoquinone ), phenolic glycosides, coumarians , xanthene,flavonoides , fats,resine , tannins. Chemical test : on addition of acid in decoction of henna, orange red colour vanishes. On addition of alkali colour darkens. Application : as hairdye , colourant in other cosmetics. 14

15. 2. TURMERIC Synonym : Haldi , Indian saffron. B/S : Dried, fresh rhizomes of plant Curcuma longa, family- Zingiberaceae. G/S : India, china, Malaysia, Italy & Australia. C/C : 5% volatile oils, resin & diaryl heptanoid yellow couring substance called as Curcuminoids . Other phytoconstituents are atlantone , demethoxycurcumine , tumerone , sugars, minerals, etc. Chemical test : Curcumin gives crimson red colour with sulphuric acid. Application: As a colourant in various phrmaceutical dosage forms, cosmetics & food products. 15

16. 3. ANNATO Synonym : chiote tree, lipstick tree B/S : dried seeds of Bixa orellana , fam - Bixaceae . G/S : Central & South America, India. Description : Bixin occurs as orange yellow crystals or dark red brown to red-purple powder. Chemical test : annatto dissolved in acetone shows absorbance maxima at about 425, 475 & 487 nm. Applications : Colouring & coating agent for solid & liquid pharmaceutical dosage forms. In manufacture of wood stains & varnishes & for silk dyeing. 16

17. 4. INDIGO Synonym : Neel, indigo B/S : Leaves of Indigo tinctoria , I. suffruticosa , family- Leguminoseae . G/S : India, America, Europe, Africa. Description : dye occurs as dark blue crystalline powder. Dye is insoluble in water, alcohol or ether but soluble in DMSO, chloroform, nitrobenzene. C/C : glycoside Indican , rotenoids deglelin , dehydrodeguelin , rotenol , rotenone, tephrosin & sumatrol . Application : colourant in pharmaceutical & food industry, dyeing of jeans, etc. 17

18. NATURAL SWEETENERS These are the substances which are added to drug formulation to mask bitter taste & can be used by diabetic patients also. Natural sweeteners are sacharide & non- saccharide type. Non- saccharide sweeteners are of various types such as terpenoids, dihydrochalcones , dihydrocoumarins , sweet proteins, & steroidal saponins. Advantages: They are non-calorific in nature. Have less possible side effects. Quality & quantity can be improved by modern technologies. Economic No rise in blood sugar level Avoid decay of teeth. 18

19. 1. STEVIA Synonym : honey leaf, sugar leaf B/S : extracted from plant S tevia rebaudiana , Family- Compositae . G/S: Paraguay, South brazil, Japan, South east Asia, USA, etc. C/C: diterpene glycoside, Stevioside . Application: natural calorie free sweetener in liquid or solid foods, beverages. Substituent for conventional sugars. Sweetening agent of choice for diabetic patients . 19

20. 2. LIQUORICE Synonym : Yashtimadha , mulethi , Liquorice root. B/S: dried peeled, unpeeled roots & stolons of plant Glycyrrhiza glabra , Fam - Leguminoseae . G/S : mediterranean region & china, france , italy , spain , USA, england , Asia & India. C/C : pentacyclic triterpenoid saponin , Glycyrrhizin. Chemical test : with 80% sulphuric acid, it shows deep yellow colour. Application : sweetener, flavouring agent, foam stabilizer . 20

21. 3. SERENDIPITY BERRY Synonym: Monellins B/S: F ruits of plant Dioscoreophyllum volkensii , family- Menispermaceae . G/S : Tropical Africa Description: R eadily soluble in water, denatures at higher temperature. C/C : Sweet protein, Monellin . Use : As table top sweetener. 21

22. 4. THAUMATIN Synonym : Talin , Katemafe fruit B/S : arils of fruits of the tropical plant Thaumatococcus daneilli , Fam - Marantaceae . G/S : West Africa C/C : Thaumatin protein. Description: 2000-10000 times sweeter than sucrose. Water & dilute alcohol soluble. Use : low caloric sweetener & flavouring agent. 22

23. NATURAL BINDERS Binders are excipient which binds all ingredients used in formulation to form suitable dosage form. Natural binders are less toxic, can be degraded naturally, economic, available easily & abundantly & enhance stability & texture to dosage form. 23

24. 1. ACACIA Synonym : Indian gum, Babul. B/S : it is dried gummy exudation from the stems & branches of Acacia arabica , A. senegal , Fam - Leguminoseae . Description : it occurs as yellowish white or white flakes, spherical spheres, powder, granules, or spray dried powder. C/C : Arabinose , galactose , rhamnose , & glycuronic acid. Chemical test : When acacia powder is treated with lead sub acetate, it gelatinizes the aqueous solution. Use: As a natural binder for tablets, suspending agent, emulsifying agent, thickener. As base in pastilles & lozenges. 24

25. 2. TRAGACANTH Synonym : Gum tragacanth , Persian tragacanth . B/S : dried gum obtained from plant Astragalus gummifer , Fam - Fabaceae . G/S : Iraq, Iran, Syria, Turkey, Afghanistan, Pakistan & Russia. Description : Tragacanth has flat, lamellated , curved fragments, or straight or spirally twisted linear pieces. It is white to yellowish in colour, translucent, odourless with mucilagenous taste. C/C : water soluble & water insoluble polysacharides . Bassorin , cellulose, starch, protein & ash. Chemical test : when strong iodine solution is added to tragacanth , it developes olive green colour. Use : used to make various pharmaceutical formulations like creams, gels, & emulsions. 25

26. 3. STARCH Synonym : Amido , Amidon , Amylum B/S: it is polysaccharide obtained from grains like corn ( Zea mays ) Fam - Gramineae , potato ( S olanum tuberosum ) Fam - Solanaveae , wheat ( Triticum aestivum ) & rice ( Oryza sativa ), fam - Poaceae . Description : odourless , tasteless, fine white coloured powder. Practically insoluble in cold ethanol & in cold water. C/C: Amylose & amylopectin & α -glucose. Chemical test: starch solution is heated with HCl & then neutralized by NaOH, the solution is heated with Fehling’s solution, brick red ppt is produced. Use: it is a binder of choice in wet granulation & tablet formulation. Has wide applications in nasal, oral, periodontal novel drug delivery system & to get site specific drug delivery. 26

27. 4. GELATIN Synonym : Byco , Cryogel , Instagel , Solugel B/S : it is a protein obtained by partial acid or alkaline hydrolysis of animal collagen tissues like bone, skin, tendon & ligaments. Description: faintly yellow amber coloured vitreous, brittle solid. Odourless & tasteless. Practically insoluble in water, most of organic solvents, fixed oils & volatile oils. soluble in hot water, glycerol, & acetic acid. C/C : Glycine (25-27%), alanine, glutamic acid, proline , arginine , aspartic acid, hydroxy proline , isoleucine , leucine , phenyl alanine & tryptophan. Chemical test : gelatin powder, when heated with soda lime, evolves ammonia gas. Use: used in implantable delivery systems, mainly hard & soft gelatin capsule. In formulation of suppositories, pastilles, pessaries , pastes. Absorbable gelatin sponge acts as haemostatic agent.also used in food industry & in photographic emulsion. 27

28. NATURAL DILUENTS Natural fillers or diluents are the substances which enhance the bulk of solid dosage form or may dilute liquid formulations. They are biodegradable, do not have toxicity, economic & eco-friendly in nature. They provide proper structural form & assure proper weight for easy administration. 28

29. 1. CELLULOSE Synonym : Arbocel , E460, Elcema , Sanacel . B/S: It is a polysaccharide & is a structural compound found in the cells of plants, algae & few bacteria. Description; it is white, odorless, & tasteless powder varying particle sizes. Practically insoluble in water & most of the organic solvents. Chemical test: with Schulze reagent cellulose shows purple colour. Use: diluent for tablets, filler for hard gelatin capsule, helps in direct compression of granules, as a suspending agent, in manufacturing of pellets & in cosmetics & food industry. 29

30. 2. LACTOSE Synonym : milk sugar, Lactin , lactosum . B/S : It is a natural disaccharide of animal origin consisting of galactose & glucose & obtained from milk of most of mammals. Description : It is white crystalline powder, odorless, faintly sweet taste. It is hygroscopic at high relative humidity. Chemical test : when lactose is mixed with water & heated on water bath with 10M ammonia, it shows red colour. Use : as diluent in tablets, capsules, dry powder inhalations. As a coating agent with sucrose. Used to prepare lyophilized products. 30

31. 3. MANNITOL Synonym: Cordycepic acid, manna sugar, D- mannite , Mannogem B/S: It is exudation from the stem of Fraxinus ornus , fam - Oleaceae . Descriptoin : It is white, crystalline powder or free flowing granules. It is odourless , non-hygroscopic, & sweet powder. Soluble in alkalies , ethanol(95%), glycerin & water. insoluble in ether. Use: diluent for tablet formulations, helps in direct compression, acts as sweetening agent, in formulation of antacid preparations, acts as thickening agent, plasticizer in soft gelatin capsules. Therapeutically acts as osmotic diuretic, as diagnostic agent for kidney function, in treatment of acute renal failure, cerebral edema & to reduce intraocular pressure. 31

32. VISCOSITY BUILDERS These ar e the aqueous solutions to increase its viscosity without altering properties. The inhibit crystal growth, improve physical stability, prevent formation of stable crystal from metastable crystal. Types: Natural gums E.g. acacia, tragacanth , xanthan gum, etc. Cellulose derivatives E.g. Methyl cellulose, ethyl cellulose, CMC Chitosan Synthetic polymers E.g. carbomer, PVA Clays E.g. Magnesium aluminium silicates, bentonite , etc. 32

33. 1. XANTHAN GUM Synonym: corn sugar gum, Keltrol , Rhodigel . B/S: It is a polysaccharide produced by fermentation using the bacterium like Xanthomonas compestris . Description: It is a cream or white coloured , odourless , free flowing, fine powder. Practically insoluble in ethanol & ether, soluble in cold or warm water. in market, it is available in potassium & sodium salts. Chemical test : Xanthan gum is suspended in 0.1 N HCl, flask is closed with formation bulb containing barium hydroxide & heated. BaOH solution shows white turbidity. Use: It acts as good emulsifying agent, stabilizer & thickener, viscosity enhancer for oral & topical pharmaceutical formulations, cosmetics & foods. It can be added to sustained release matrix & ophthalmic liquid dosage forms. 33

34. Fig: Xanthan gum 34

35. 2. CARRAGEENAN Synonym: Chondrus extract, Irish moss extract. B/S: It is sulphated polysaccharide obtained from the red algae Chondrus crispus , family- Rhodophyllaceae . G/S: it is produced at North Atlantic coast of Europe, North America, France, Spain, Denmark & USA. Description: It is yellow-brown to white coloured , coarse to fine powder, without any taste. it is water soluble & stable at pH 9. C/C: It mainly consist of K, Na, ca, Mg, & ammonium sulfate esters of galactose & 3,6-anhydrogalactose copolymers. Chemical test: It becomes translucent & gelatinous when soaked in cold water. Use: In preparation of suspensions, emulsions, gels, creams, lotions, eye drops, suppositories, tablets, capsules, etc. It is excipient of choice for oral & buccal drug delivery. Also used for microencapsulation of proteins & probiotic bacteria. 35

36. Fig: Carrageenan 36

37. 3. GUAR GUM Synonym: Guaran , guar flour, Jaguar gum B/S: It is a galactomannan polysaccharide obtained from endosperm of the seeds of the guar plant, Cyamopsis tetragonoloba , family- fabaceae . G/S : India, Pakistan, U.S, Australia & Africa. Description : It is white to yellowish white powder, odorless, blend taste, insoluble in organic solvents. Chemical test : with 2% lead acetate, it gives precipitate. Use: As a binder, disintegrant , suspending, thickening, & stabilizing agent, in controlled release carrier dosage forms. Commonly used in food & cosmetic industry. 37

38. Fig: Guar gum 38

39. DISINTEGRATING AGENTS They help in dispersion or disintegration of tablets & release contents of capsules into small fragments. They act by various mechanism such as swelling , penetration, de formation & repelling. They are effective in low concentration, do not affect compressibility, more effective at intra-granular region. But, they have high cost, can cause side effects, have less patient compliance. 39

40. 1. CHITOSAN Synonym: D eacetylated chitin. B/S: it is natural polysaccharide obtained from crab and shrimp shells. Description: O dourles , white or creamy-whit powder or flakes, sparingly soluble in water & conc. Organic acids. Chemical tests : with iodine and 10% sulphuric acid, it forms deep violet colour Use: used in controlled drug delivery , mucoadhesive dosage forms rapid release, improved peptide delivery, colonic drug delivery systems, and for 40

41. 2. PREGELATINIZED STARCH Synonym: Compressible starch, Intastarch , Pharma-Gel, Prejel B/S: It is obtained from modification of potato starch. Description: It occurs as a moderately coarse to fine, white to off-white colored powder which is odourless & has characteristic taste. Practically soluble in organic solvents, slightly soluble in cold water. Composition: 5% free amylose , 15% amylopectin , 80% unmodified starch Chemical test : When solution is treated with iodine solution, it forms reddish violet to blue color. Use: as a disintegrants, binder & diluent in tablets & capsules. 41

42. 3. MICROCRYSTALLINE CELLULOSE Synonym: Avicel , Celex , Cellulose gel B/S: obtained from partial depolymerisation of cellulose. Description: white, odorless, tasteless, crystalline powder having porous particles. Slightly soluble in 5%w/v NaOH solution & practically insoluble in water, dilute acids & organic solvents. Chemical test: it is heated with phosphoric acid & catechol for 30 min, produce red color. Use: as a lubricant, disintegrating agent, binder or diluent in oral tablet & capsule formulations. 42

43. NATURAL PERFUMES & FLAVOURING AGENTS Natural perfume are the mixture of essential oils or aromatic compounds, fixatives, & solvents applied to the human body, animal, food objects, pharmaceutical products & living spaces. Flavours are taste masking agents used to mask the unpleasant taste or odour of dosage form & enhance the flavour of medicine & patient compliance. 43

44. 1. SANDAL WOOD OIL Synonym : Chandan B/S: it is volatile oil obtained by steam distillation of heartwood of Santalum album & S. spicatum , Family- Santalaceae . Description : colorless to golden yellow in color with pleasant woody odor. It is oily, viscous liquid, soluble in 5 vol of 70% alcohol. Use: in aromatherapy, in cosmetics, soap, perfue , to treat common cold, bronchitis, UTI & inflamation . 44

45. 2. ROSE OIL Synonym: Otto of rose, Attar of rose, Rose essence. B/S : It is volatile oil obtained by distillation of fresh flowers of Rosa damascena , R. centifolia , family- Rosaceae . Description: colourless or yellow liquid with characteristic odour of rose, rose oil is miscible in 1ml chloroform. Chemical test: rose oil is mixed with equal quantity of chloroform & 90% alcohol, At 20 °C, it deposits crystals within 5 min. Use: flavouring agent, perfume, hydrate dry skin, to treat acne, reduces signs of ageing, scars & to treat eczema. 45

46. 3. LEMON OIL Synonym : Limbu , oleum limonis B/S: obtained from fresh peel of the ripe fruits of Citrus lemon , Family- Rutaceae . Description: pale greenish-yellow in colour with sharp, fresh smell, bitter taste & has watery viscosity. Chemical test: solution of lemon oil with 3 vol of alcohol is neutral to slightly acidic in nature. Use: Flavouring agent, perfume, treat fever, throat infections, bronchitis, asthma, constipation, dyspepsia & flu. 46

47. 47