HERBAL EXCIPIENTS herbal drug technology
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Colourants Sweeteners Binders Diluents, Viscosity builders, Disintegrants, Flavours Perfumes.
HERBAL EXCIPIENTS herbal drug technology
- 1. HERBAL EXCIPIENTS Miss Poonam Pardhi Assistant Professor Adarsh Institute of Pharmacy, Nagpur
- 2. HERBAL EXCIPIENTS • WHO defines Excipient as the substance other than active ingredients which have been appropriated evaluated for safety and or included in a drug delivery system. • Excipients can be defined as non active ingredients that are mixed with therapeutically active compounds to form medicines. • Excipients are substances which are used as a medium for giving a medicament. • These substances helps in the processing of the drug delivery system during its manufacturing, protects, support or enhance stability, bioavailability or patient acceptability, • Assist in product identification, or enhance any other attribute of the overall safety, effectiveness and delivery of the drug during storage 2
- 3. ADVANTAGE OF HERBAL EXCIPIENTS • Biodegradable – Naturally occurring polymers produced by all living organisms. The show no adverse effects on the environment or human being. • Biocompatible and non-toxic- Chemically, nearly all of these plant materials an carbohydrates in nature and composed of repeating monosaccharide units. Hence the are non-toxic. • Economic - They are cheaper and their production cost is less than synthetic material • Safe and devoid of side effects - They are from a natural source and hence, safe and with out side effects. • Easy availability - In many countries, they are produced due to their application in many industries 3
- 4. DISADVANTAGES OF HERBAL EXCIPIENTS • Microbial contamination During production, they are exposed to external environment andhence, there are chances of microbial contamination. • Variation- Synthetic manufacturing is controlled procedure with fixed quantities of ingredients while production of natural polymers is dependent on environment and various physical factors. • The uncontrolled rate of hydration- Due to differences in the collection of natural materials at different times, as well as differences in region, species, and climate conditions the percentage of chemical constituents present in a given material may vary. • Slow Process- As the production rate is depends upon the environment and many otherfactors, it can't be changed. So natural polymers have a slow rate of production. • Heavy metal contamination - There are chances of Heavy metal contamination often associated with herbal excipients. 4
- 5. SomeexamplesofHerbalExcipientswiththeirSourcesandUses EXCIPIENT SOURCE USES Agar Gelidium amansii (Gelidiaceae) • Laxative • suspending agent • emulsifying agent • gelling agent in suppositories Gum Ghatti Anogeissus latifolia (Combretaceae) • Binder • emulsifier • Suspending agent Aloe mucilage Aloe species (Liliaceae) • Gelling agent • sustained release agent Gum acacia Acacia arabica (Combretaceae) • Suspending agent • emulsifying agent • binder in tablets • emollient in cosmetics. Tamarind seed Tamarindus indica (Leguminosae) Binding agent and emulsifier Shatavari mucilage Asparagus racemosus (Apocynaceae) Binding agent and sustaining agent in tablet 5
- 6. SIGNIFICANCE OF SUBSTANCES OF NATURAL ORIGIN AS EXCIPIENTS The following excipients of natural origin and their significance are discussed below: 1) Colourants 2) Sweeteners 3) Binders 4) Diluents 5) Viscosity builders 6) Disintegrants 7) Flavours 8) Perfumes 6
- 7. COLOURANTS • Many natural coloured substances are found in plants and animals. • The difference between a dye and a pigment is that - • Dye gets absorbed by the material when applied to fibres and impart a permanent colour while, the pigments is only applied to the surface. • The coloured compounds are called chromogen, and has a chromophore group and/or auxochrome, which appear as coloured substance by absorbing light in the near UV region. 7
- 8. IDEALPROPERTIESOFACOLOURANT • It should be non-toxic. • It should be physiologically inactive. • It should be free from harmful impurities. • It should have a high tinctorial (colouring) power so that only small • quantities are required. • It should be stable on storage, and resistant to light, tropical temperatures, • hydrolysis and microorganisms. • It should be compatible with medicaments. • It should be readily soluble in water ; however, oil-soluble and spirit –soluble colours are also required. • It should not have unacceptable taste and odour. • It should be easily available and economical. 8
- 10. TURMERIC • Turmeric is a spice which provides yellow colour to the curry. • In India, it is in use for thousands of years as a spice as well as a medicinal herb. • Curcuma is the dried and fresh rhizomes of Curcuma longa Linn. (C. domestica) (and belongs to family Zingiberaceae) . • C. amada , C. angustifo lia, C. aromatica , C. caesia , C.zedoaria, and C. longa are some other varieties of curcuma. 10
- 11. • Curcuma is a genus having around 70 species of rhizomatous herbs. • It is found to be growing widely distributed in South -East Asia, especially in India, China, Thailand, Italy, Malaysia, Archipelago, and N. Australia. • India cultivates around 90% of the total output of turmeric in the world. • Mainly cultivated in Tamil Nadu and Andhra Pradesh & Kerala • Curcuma consists of volatile oil (1 -6.5%), resin, numerous zingiberaceous starch grains, and curcuminoids (yellow coloured substances). • Curcumin (50-60%) is the major constituent of curcuminoids 11
- 12. Turmeric has the following morphological properties: • Colour: Yellowish-brown. • Odour: Characteristic. • Taste: Slightly bitter. • Shape: Round rhizomes are oblong, while long varieties are cylindrical and short branched. • Surface: Root scars and annulations are present. • Fracture: Horny and internal surface is orange. Turmeric has the following uses: • It is used as a colouring agent for ointments and creams. • It is used for the detection of boric acid. • It is used as an anti-inflammatory. • In China, C. wenyjuin (C. aromatica) is used for cervical cancer. • It is used as an anti-arthritic agent, which has been isolated from • C. aromatic species. 12
- 13. ANNATTO • Seeds of achiote tree yield an orange-red coloured pigment, called annatto, which is used as a colouring agent in food and condiments. • It is used in food for imparting yellow or orange coloration. • Annatto consists of the dried seeds of the plant Bixa orellana L. (and belongs to family Bixaceae). • The plant is cultivated in Peru, Jamaica, Mexico, Kenya, India, and Brazil. 13
- 14. Annatto has the following morphological properties: Fruits: Spherical or broadly elongated, 2-4.5cm, flattened, 2 valved, densely covered with long bristles, and green, greenish-brown or red when mature. Capsules: Sub-globose or ovoid, 2 -4.5cm, slightly laterally compressed,densely purple-brown spiny, and rarely smooth. Spines: 1-2 cm long. Seeds: Numerous, bright orange-red fleshy coats, obovoid -angular, 4- 5 mm, and smooth. • The seeds of annatto contain bixin dye and are covered with aril. • The content of seeds includes 12% of annatto oleo resin. • 50% of this resin is water -soluble. • 4-5% of pigment and 0.3 -0.8% of volatile oil are also present. • Bixin is the monomethyl ester derivative of a dicarboxylic acid, norbixin 14
- 15. Bixin has the following uses: • Bixin possesses antioxidant properties. • It acts as a filter for UV radiation. • It has hepato protective properties. • Annatto is mainly used as colouring agent in foods, cosmetics, alcoholic and non-alcoholic beverages, dairy desserts, fats and oils and in margarine. 15
- 16. SWEETENERS • Sweeteners are agents which either impart a sweet taste or increase the perception of sweet taste. • Due to the adverse effects of synthetic sweeteners, the natural sweetening agents are preferred. • Sweetening agents are of two types: 1. Natural sweeteners of plant origin, and 2. Chemically synthesised artificial or synthetic sweeteners. • Natural sweetening agents are non -saccharides. • They are of low calories, still excessively sweet (100 -10,000 times sweeter than sugar), non-toxic, and can overcome the problems of sucrose and synthetic sweeteners. • In plants, the active sweet principles are stored as terpenoids, steroidal saponins, proteins,volatile oils, etc 16
- 18. STEVIA • Stevia rebaudiana is a shrub of up to 30 cm height. • It has composite wrapped flowers with 3-4 cm long sessile leaves. • Stevia is found in Paraguay where it is known by the names of sweetleaf or sugarleaf. • The Stevia plant is intensely sweet and its active ingredients are diterpene glucosides, particularly stevioside (4-10%), rebaudioside (2 - 4%). 18
- 19. • Other chemical constituents of stevia are volatile oils (e.g., nerolidol and caryophyllene); and flavonoids (e.g., quercetin, apigenin, austroinulin). • Stevia rebaudiana has a high sweetening index as stevioside is 200- 300 times sweeter than sucrose Stevia has the following uses: 1. It is used as a mild osmotic laxative. 2. It is slightly hypoglycaemic. 3. It is used as a hypotensive and antibacterial. 4. It is used for treating constipation. 5. It is a sugar substitute for diabetics. 19
- 20. BINDERS • Binders are agents used to impart cohesiveness to the granules so that the tablets remain intact after compression • Binders are used to hold various powders together during tablet formation. • The wet binder is the most important ingredient in wet granulation. • Binders are generally hydrophilic and soluble in water. Advantages 1. They are less toxic, biodegradable, easily available, and economic. 2. They can affect the release of drug, thereby, influence the absorption and bioavailability of the incorporated drug. Disadvantages 3. Sometimes, they cause tablet hardening and consequently decrease the dissolution performance. 4. If polymer binders are used, strong disintegrants (such as super disintegrants) need to be added, which are costly and also exert a negative effect on product stability as well as film coating appearance of the finished products 20
- 21. ACACIA • According to the USP, acacia is the dried gummy exudation obtained from the stems and branches of Acacia senegal (L.) Willd. or other African species of Acacia. • It is also found in the stems and branches of Acacia arabica, Willd. (and belongs to family Leguminosae). 21
- 22. • It is also found throughout the vast area from Senegal to the Red sea and to eastern India. • It extends southwards to northern Nigeria, Uganda, Kenya, Tanzania, and southern Africa. • In India, A. arabica (babul tree) grows wildly in Punjab, Rajasthan and on Western Ghats Acacia has the following uses: 1. Its mucilage is a demulcent. 2. It is an essential pharmaceutical aid for emulsification and to be used as a thickening agent. 3. It is used as a binding agent in tablet formulations. 4. It is used in making candies and other food products. 5. It is used in manufacturing spray -dried fixed flavours which are powdered flavours used in packaging of dry-mix products (puddings, desserts, and cake mixes). 22
- 23. DILUENTS Diluents are used in tablet formulation to provide properties which make the tablets better like: • To improve cohesion, • To allow direct compression manufacturing, • To increase flow, and • To adjust weight of tablet as per the capacity. Ideal Characteristics of a Diluent 1. It should neither support microbiological growth nor contribute to microbiological load in the dosage form. 2. It should neither adversely affect the product dissolution nor interfere with the bioavailability of active therapeutic ingredient. 3. It should be colourless. 4. It should be inert and not react with the drug substance. 5. It should not exhibit its own physiological or pharmacological activity. 6. It should have constant physical and chemical properties. 23
- 24. LACTOSE • Lactose is a natural disaccharide containing galactose and glucose. • It is obtained from the milk of most mammals. • It is a white or almost white crystalline powder having no odour and a faintly sweet taste. • It is stable in air but readily absorbs odours. Lactose has the following uses: 1. It is used as a filler or diluent in tablets and capsules. 2. It is also used in infant feed formulae and in dry powder inhalations. 3. It is used with sucrose to prepare sugar coating solutions. 24
- 25. VISCOSITY BUILDERS • Viscosity builders are added to mixture to increase the viscosity without modifying other properties like taste, odour , etc. • These agents also increase thestability of the preparation . • They are also added to provide or improve palatability or pourability to the dosage form. • Ideal Characteristics of a Viscosity Builder It should provide a structured vehicle. It should exhibit yield stress. It should be compatible with other excipients. It should be non-toxic. It should impart viscosity that should not get affected by tepmerature or ageing. 25
- 26. Advantages • High viscosity of a pharmaceutical preparation: • Inhibits crystal growth, • Enhances the physical stability • Prevents the transformation of metastable crystal to a stable crystal. Disadvantages • High viscosity of a pharmaceutical preparation: • Hinders the re-dispersibility of the sediments, • Reduces the absorption of drug, and • Creates problems in handling of material during manufacturing. 26
- 27. XANTHAN GUM • Xanthan gum is a polysaccharide gum produced by the bacterium , Xanthomonas campestris on some specific carbohydrates. • The chief chemical constituents of xanthan gum are D-glucosyl, D – mannosyl and D-glucosyluronic acid residues , and variant quantum of O -acetyl and pyruvic acid acetal. 27
- 28. Xanthan gum has the following properties: • It is a yellowish-white, odourless, and free-flowing powder. • It gets swiftly dissolved in water on shaking and turns into a highly viscous solution at relatively low concentrations. • On evaporation of its aqueous solutions, it forms a strong film. • It is fairly stable and resistant to thermal degradation. • Its viscosity does not depend on temperature ranging between 10- 70oC. • It is compatible with various salts. Xanthan gum has the following uses: • It is used to enhance oil recovery. • Due to the pseudoplastic property of its aqueous solutions, it is used in toothpastes and ointments to enable them to hold their shape and also to spread readily. • Due to its excellent suspending and emulsifying nature, it is used in pharmaceutical preparations 28
- 29. DISINTEGRANTS • The agents added to tablets, capsules, and some encapsulated formulations to promote their breakdown into smaller fragments in an aqueous environment are termed disintegrants. • Thus, disintegrants increase the available surface area and promote rapid release of drug particles. • Swelling, porosity and capillary action, and deformation are the three mechanisms and factors affecting tablet disintegration. 29
- 30. Ideal Characteristics of a Disintegrant • It should strongly interact with water to exert its disintegrating action. • It should act via combining of swelling and/or wicking and/or deformation mechanisms. • Super disintegrants give significant improvements over starch. Advantages • They are effective even in low concentrations. • They impart a less effect on compressibility and flow ability of the granules or powder. • They are more effective in intra-granular form. • Disadvantages • 1) They are more hygroscopic, therefore cannot be used with moisture- sensitive drugs. 30
- 31. GUAR GUM • Guar gum is the powder of the endosperm of the seeds of Cyamopsis tetragonolobus Linn. (and belongs to family Leguminosae). • Guar gum powder is obtained from the Guar seed undergoing multiple industrial processes. • Guar gum attains uniformity and very high viscosity at low concentrations by getting rapidly hydrated in cold water. • Being colloidal in nature, it provides excellent thickening to the solution. • The plant from which guar gum is obtained is an annual shrub either growing wildly or cultivated in dry climate. • In India, it is cultivated in Maharashtra, Gujarat, Karnataka, and Rajasthan. • The plant is also grown in Pakistan. 31
- 32. • Galactomannan (guaran) is the major constituent of guar gum. This substance hydrolyses to yield galactose and mannose. Guar gum has the following morphological properties: Colour: Colourless or pale yellowish-white. Odour: Characteristic. Taste: Mucilaginous. Solubility: Completely soluble in cold and hot water; insoluble in alcohol; practically insoluble in oils, greases, hydrocarbons, ketones, and esters. Extra Features: Solutions of guar gum in water are tasteless, odourless, non-toxic, neutral, heat stable, and possess 5 -8 times thickening power than starch. In water, guar gum forms a thick colloidal solution and swells rapidly 32
- 33. Guar gum has the following uses: • It is used as a bulk laxative. • Since its thickening power is 5 -8 times more than starch, it is used as a thickener. • It is used in treating peptic ulcer. • It is an appetite depressant. • It is used as a binding and disintegrating agent in tablet manufacturing. • It is widely used as film -forming agent for cheese, salad dressing, ice –cream and soups. • It is used pharmaceutically to produce jelly. • It is used in suspensions, emulsions, lotions, creams, and toothpastes. 33
- 34. FLAVOURS • Flavours or flavouring agents are the excipients added to enhance the palatability of pharmaceutical preparations. • Some of the commonly used natural flavours are fruit, nut seafood, spice blends, vegetables , and wine. Natural Flavour s or Natural Flavouring Agents: • These agents areacceptable for human consumption. • They are obtained by physical processing of natural resources like vegetables, fruits, etc. Nature-Identical Flavouring Agents: • These agents are either chemically obtained from aromatic raw materials or synthetically obtained. • Their chemical composition is similar to substances present in natural products meant for human consumption, either processed or not. Artificial Flavouring Agents: • These agents are synthesised chemically and have not been intended for human consumption either processed or not 34
- 35. CARDAMOM OIL • Cardamom is the dried ripe fruits of Elettaria cardamomum (and belongs to family Zingiberaceae). • Cardamom grows wildly in Sri Lanka , Myanmar, • Malaysia, and Malabar hills. In India it is grown in Karnataka, Tamil Nadu, and Kerala. • Guatemala is the largest producer of cardamom in the world. 35
- 36. Cardamom has the following morphological properties: Cardamom Fruit (Capsule) Colour: Pale green or cream. Odour: Characteristic and aromatic. Taste: Characteristic and aromatic. Size: Length 1-2cm. Shape: Ovoid or oblong. Seed Colour: Ripe seeds are dark red-brown; unripe seeds are pale red. Odour: Strongly aromatic. Taste: Pleasantly aromatic with a sensation of pungency. Size: Length 4mm and width 3mm. Shape: Angular Cardamom Oil Colour: Pale yellow liquid. Odour: Balsamic. Taste: Sweet and aromatic. Viscosity: Watery. 36
- 37. • The chemical constituents of cardamom fruits are volatile oil (2.8- 6.2%), starch (50%), fixed oil (1-10%), and calcium oxalate. • The principal constituents of oil are α-pinene, β –pinene, limonene, α- terpineol, methyl eugenol, myrcene, sabinene, α-phellandrene Cardamom has the following uses: 1. It is a stimulant and carminative. 2. It is used for treating indigestion, constipation, and flatulence. 3. In India, green cardamom ( A. subulatum) is used for treating teeth and gum infections. 4. It is used for preventing and treating throat troubles, congestion of lungs, and pulmonary tuberculosis. 5. It is used in inflammation of eyelids. 6. It is used as an antidote for snake as well as scorpion venom. 7. It is used as a breath-freshener. 8. It is used in nausea (even the nausea related to pregnancy) and heartburn. 37
- 38. PERFUMES • Perfumes are used to enhance the odour of the formulation. Generally, perfumes include an active ingredient or enhancer and one or more adjuvants (such as extenders, antioxidants, fixatives, etc.). • The aroma or odour is imparted by the active ingredient that enhances or augments the aroma of an existing perfume Composition • Other ingredients of the perfumes are fixatives and extenders. • The fixative agents are used to slow down the evaporation rate of perfume by reducing the volatility, whereas an extender is added to enhance the volume of the perfume composition without diluting or reducing the aroma. 38
- 39. SANDALWOOD OIL • Sandalwood oil is an essential oil steam-distilled from the chips and billets cut from the heartwoods of many species of sandalwood trees. • Sandalwood oil is distilled from the heartwood of the plant Santalum album Linn. (and belongs to family Santalaceae). • Sandalwood tree is an evergreen plant of India and Malaysia. • It is about 10-12m in height and is grown largely in the parts of India. • Such plants are cultivated exclusively in the forests of Karnataka, Tamil Nadu, and Kerala. 39
- 40. Sandalwood has the following morphological properties: Colour: The oil is pale yellow to colourless, while the wood is yellow or pale red in colour. Odour: Characteristic and persistent. Taste: Unpleasant. Solubility: Soluble in water (very slightly), alcohol, and chloroform. Texture: Darker and higher zones. • Sandalwood oil contains 95% of two isomeric sesqui-terpene alcohols, i.e., α- santalol and β-santalol. • The other constituents are aldehyde santalol (C16H22O), santene, santenone, teresantol, santalone, and santalene. • The oil is only present in the woody part of the plant, and not in the secretory cells or glands 40
- 41. Sandalwood has the following uses: • It is used as a perfumery in cosmetics and incense sticks preparations. • The sandalwood paste has been used since ancient times to comfort headache and reduce fever. • Sweating can also be controlled by applying a mixture of dry sandalwood powder and rose water over the affected area. • The paste is also used to cure skin inflammation. • Since ancient times, the wood and its oil act as an expectorant, diuretic, and diaphoretic. • It also guards against harmful infect ions caused by pathogenicmicroorganisms, i.e., Eberthella typhosa and Escherichia coli. 41
- 42. 42 THANK YOU