Contents

• Herbal excipients

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Herbal excipients

At the end of the session, student will be able to

• Explain the various binders, diluents and super-disintegrants used

for formulating cosmetics

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 Binders

• Binders are agents employed to impart cohesiveness to the granules - which ensures
the tablet remains intact after compression

• Binders are added to tablet formulation to impart plasticity and thus increase the
interparticulate bonding strength within the tablet

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Advantage: Natural binders

• Low toxicity, biodegradable, availability and low cost

• Can also modify the release of drug, thereby, influencing absorption and subsequent
bioavailability of the incorporated drug

• Increase stability, precision and accuracy of dosage form

• Improve the organoleptic properties of the drugs where necessary in order to enhance
patient adherence

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Disadvantage: Natural binders

• Over time they occasionally lead to tablet hardening and a decrease in dissolution
performance

• When polymer binders are chosen, the addition of strong disintegrants such as super
disintegrants is typically required but these are considerably expensive and have a
negative effect on product stability as well as film coating appearance of the finished
products

• E.g. Plant starch, pregelatinized starch, gelatin, Plant Gums: acacia, tragacanth

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Acacia

• Source: Dried gummy exudation from the stems and branches of Acacia arabica,
A. senegal etc,
• Family: Leguminosae
• English: Indian Gum, Hindi: Babul
• Description: White or yellowish- white thin flakes, spheroidal spheres (up to 32
mm in diameter), powder, granules, or spray-dried powder. Odourless and bland
taste
• Constituents: (-) arabinose, (+) galactose, (- rhamnose), (+glyceronic acid)
• Arabin-Ca, Mg, K salts of Arabic acid
• Enzymes - Oxidase and peroxidase 7
Tragacanth

• Source: Dried gummy exudate obtained from the stem of Astragalus gummifer, Leguminosae
• Nature:
 White or pale yellowish or brown
 Odorless
 Mucilagenous
 Thin, flattened ribbon or powder
Constituents:

• Tragacanthin

• Bassorin- Viscosity – 60% - (minimum 3.75 % of methoxy groups)

• Tragacanthic acid - galacturonic acid, galactose, xylose and fucose

• Neutral polysaccharide on hydrolysis yields arabinose and galactose

• Glycoside of sterol derivative

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Gelatin

• Syn: Gelfoam, Puragel, Gelatina

• Source: Protein obtained by partial hydrolysis of animal collagenous tissues like bone,
skin, tendon and ligaments. (Ox, Bos Taurus, the Sheep, Ovies aries; Bovidae)
• Description: Faintly yellow amber coloured solid with characteristic odour. Its available
in the form of flakes, sheets, shreds, powder or granules.
• Suitable for both wet granulation and direct compression as tablet binders
Chemical Constituents
– Glutin
– Free from chondrin, sulphur and tryptophan
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– Major amino acid - Lysine
Starch

• Source: Polysaccharide obtained from either rice (Oryza sativa), or maize (Zea mays) or of
wheat (Triticum aestivum) or from tubers of potato (Solanum tuberosum) (Graminae;
Solanaceae)
• Very fine powder, white or slightly yellowish powder
• 5-25% used Chemical constituents:
Amylose and amylopectin
Amylose - soluble in water, 250-300 glucose units
 Amylopectin - insoluble in water, gelatinizing property,
linear and branched, pasty nature, adhesive property 10
 Diluents

• Diluents are inert powders acting as fillers in the formulation of tablets, capsules and

powders for sachets

• Used to make up the volume of tablet if tablet is inadequate to produce the volume

• Provide better tablet property like improved cohesion and flow

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Diluent - Properties

• Non toxic
• Easily available
• Physically and chemically stable
• Inert

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Diluent

• Water insoluble diluents

Starch
Microcrystalline cellulose
calcium phosphate
• Water soluble diluents
Lactose
sucrose
Mannitol
Sorbitol

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Microcrystalline cellulose

• Refined wood pulp - excipient

• Used as a binder/diluent in oral tablet and capsule formulations, typically in dry

granulation, wet granulation, and direct compression processes.

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Lactose

• Natural disaccharide - milk of most mammals

• White or almost white crystalline powder

• Used as filler or diluent - tablet, capsule, infant feed formula and in dry powder

inhalation

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Sucrose

• Sugar obtained from Saccharum officinarum, Beta vulgaris

• Graminae, Chenopodiaceae

• White crystals

• Disaccharaide – non reducing – yield – glucose and fructose

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Mannitol

• Mannitol is industrially derived from the sugar fructose, and is roughly half as sweet as
sucrose.
• Mannitol is also found naturally in many species, including plants, bacteria, and fungi
• White, odorless, crystalline powder, or free-flowing granules – cooling sensation in
mouth
• In pharmaceutical preparations it is primarily used as a diluent (10–90% w/w) in tablet
formulations
• Since it is not hygroscopic and may thus be used with moisture-sensitive active
ingredients. 17
 Disintegrants

• Disintegrants and super disintegrants are used in tablets and capsules to ensure the rapid

break down into their primary particles, facilitating the dissolution or release of the

active ingredients

• Disintegrants are substances or mixture of substances added in drug formulations which

increases dispersion or breakup of tablets and capsules into smaller particles for fast

dissolution
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 Super-disintegrants

• The ease of availability and ease of use in direct compression process suggest that

super-disintegrants would be good alternative in orally dissolving tablets than

sophisticated and patented techniques.

• Super-disintegrants are super-absorbing materials with tailor-made swelling properties

• These materials not absorb large amounts of aqueous medium but they swell rapidly

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 Super-disintegrants

• Super-disintegrants are more effective at lower concentrations about 1-10% by weight

relative to the total weight of the dosage unit and have greater disintegrating efficiency
and mechanical strength.

• Super-disintegrants particles are small and porous which allows rapid tablet
disintegration in the mouth without any mouth-feel from large particles or gelling and
particles are compressible which improves tablet hardness and friability

• Effective super-disintegrants provide better compressibility, compatibility and no

negative impact on the mechanical strength of high-dose drugs
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Starch

• Source: Polysaccharide obtained from either rice(Oryza sativa), or maize (Zea mays) or of

wheat (Triticum aestivum) or from tubers of potato (Solanum tuberosum)

• Very fine powder, white or slightly yellowish powder

• Polysaccharide – amylose and amylopectin

• 5-25% used

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Gum Karaya

• Gum karaya is a vegetable gum produced as an exudate by trees of the genus Sterculia

• Chemically, gum karaya is an acid polysaccharide composed of the sugars galactose,

rhamnose, and galacturonic acid

• The high viscosity nature of gum limits its uses as disintegrant in the development of

conventional dosage form

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Gum Karaya

• Gum karaya can be utilized as an alternative super-disintegrant to commonly available

synthetic and semisynthetic super-disintegrants due to its low cost, biocompatibility as

well as facile availability

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Agar

• It is the dried gelatinous substance obtained from Gelidium amansii (Gelidanceae) and
several other species of red algae like Gracilaria (Gracilariaceae) and Pterocladia
(Gelidaceae).

• Agar is yellowish-gray or white to proximately colorless, inodorate with mucilaginous

taste and is available in the form of divests, sheet flakes, or coarse powder.

• Agar consists of two polysaccharides, agarose and agar pectin. Agarose is responsible
for gel vigor and agar pectin is responsible for the viscosity of agar solutions

• High gel vigor of agar makes it a potential candidate as a disintegrants

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Fenugreek Seed Mucilage

• Trigonella foenum-graceum commonly kenned as fenugreek, is an herbaceous plant of

the leguminous family. Fenugreek seeds contain a high percentage of mucilage (a
natural gummy substance present in the coatings of many seeds).

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Soy Polysaccharide

It is a natural super-disintegrants that does not contain any starch or sugar so can be

utilized in nutritional products.

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Others

Gellan Gum

Mango Peel Pectin

Lepidium sativum Mucilage

Plantago ovata Seed Mucilage

Locust Bean Gum

Ficus Indica Fruit Mucilage

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