HERBAL EXCIPIENTS

Introduction:
• Substances other than the herb (drugs) which are used in the
preparation of a herbal dosage form are known as additives.
• Also called as adjuvants, pharmaceutical aids or excipients.
• Herbal excipients represents the non-active component in a drug
product.
• Excipients influence the performance of the active pharmaceutical
ingredient (API) and also help to maintain the efficacy and safety of
the drug product within the desired limits.
• Also considered to be important in the delivery of the active drug to its
site of action
Classification:
1. Binders/Binding Agents: E.gs: Sucrose, glucose, acacia, tragacanth, gelatin, starch, ethyl
cellulose, methyl cellulose etc.
2. Diluents: E.gs: Dextrose, lactose, mannitol, microcrystalline cellulose (MCC) sorbitol, starch,
sucrose etc.
3. Suspending : E.gs: Gelatin, sodium carboxymethyl cellulose, carbopol etc.
4. Emulsifying Agents: E.gs: Acacia, methyl cellulose (MC), amine soaps, bentonite, carbomer,
beeswax, cetrimide, polysorbates etc.
5. Viscosity Enhancers/Viscosity Builders: E.gs: Hydroxy ethyl cellulose, carbomer, povidone
etc.
6. Disintegrating Agents:E.gs: Sodium starch glycolate, cross povidone, calcium silicate,
microcrystalline cellulose (MCC), starch, alginic acid etc.
7. Antifrictional Agents:
(a) Lubricants: Sodium lauryl sulphate, PEG 4000, PEG 6000, calcium stearate, talc, mineral oil etc.
(b) Glidants: E.g: Corn starch etc.
(c) Antiadherants: E.gs: Starch, talc etc
8. Organoleptic Agents
(a) Colourants: E.gs: FD & C blue No. 2, FD & C red No. 2.2, FD & C
orange No. 4, FD & C red no 40, FD & C yellow No. 8.
(b) Flavours: E.gs: Vanilla, cherry, raspberry, peppermint oil, acacia
syrup, benzaldehyde etc.
(c) Sweetening Agents: E.gs: Aspartate, mannitol, sucrose, sorbitol,
fructose, glycerine, sodium saccharin etc.
9. Antioxidants: E.gs: Tocopherol, propyl gallate, butylated hydroxy
toluene (BHT), butylated hydroxy anisole (BHA) etc.
10. Preservatives: E.gs: Methyl paraben, propyl paraben, sodium
benzoate etc
Merits of Herbal Excipients:
1. Biocompatible and non-irritant in nature.
2. Economical and the cost involved in their production is relatively less than that for
synthetic excipients.
3. Easily available.
4. Most of the herbal excipients used are basically carbohydrates i.e., Are composed of
repeating units of monosaccharide sugars and therefore are devoid of any toxicity.
5. Considerably safer than synthetic excipients and hence do not produce any side effects.
Demerits of Herbal Excipients:
6. Being natural products, they are highly susceptible to microbial contamination.
7. Natural excipients may exhibit variations in characteristics due to the influence of both
environmental and physical factors.
8. Major demerit with natural excipients is their high probability being associated with heavy metal
contamination
 Colourants:
• Impart colour to the colourless ingredients and improve the appearance of the preparation.
• Help to mask any objectionable colour of the drug.
• Makes the final product visually appealing .
• Increases patient compatibility.
• Obtained from natural sources like plants and animals.
• Concentration of the colouring agent should lie within the range of 0.0005% - 0.001%.
• Do not require FD & C and D & C approval for their incorporation in the drug products.
• Compatibility with the active ingredients and other excipients should be considered.
Demerits
• Suffer from batch-to-batch colour variation and being unstable.
• Colour fading upon absorbing light and in the presence of metals, heat, oxidising and
reducing agents.
Sweetening Agents:
• Herbal sweeteners are required only in oral solutions, and in solutions used in the mouth and
throat.
• Improve the palatability of the preparation by imparting sweet taste and masking the objectionable
taste of the drug and the additives. E.Gs: sucrose, mannitol, sodium saccharin, honey, jaggery etc
Binders:
• Incorporated to produce cohesive bonding between the granules during the process of compaction to
form a tablet.
• Binder determines the granule size uniformity, appropriate hardness of granules, compression
force to be applied and general quality (such as hardness) of the tablet.
• Ideal binding agent should confer appropriate hardness to the tablet, should maintain its integrity
even after compression and should allow proper release of drug from the tablet after disintegration
• Types of Binding Agents
(a) Sugars:
• Sucrose and glucose are also used as binding agents in the concentrations between 50-74%.
• Low cost adhesives employed in both dry and wet granulation.
• Granules produced are slightly hard and give brittle compacts upon compression.
• Hydroalcoholic solution of sucrose give comparatively softer granules. Since the sugar solutions
are prone to microbial contamination, therefore highly concentrated forms are employed.
• In tablets containing iron salts such as ferrous sulphate, sucrose plays the dual role of a binder and also
prevents the oxidation of ferrous sulphate.
(b) Natural polymeric binders:
• Gums natural acacia and tragacanth are used as binders in concentration of 10-25%, either alone or
in combination in dry and wet forms.
• Much more effective when used in wet form than as dry powder.
• Acacia is a suitable binder when the drug concentration is high and where granulation is difficult
with drugs like mephenesin.
c) Gelatin:
• Natural protein, which is used alone or sometimes in combination with acacia.
• Compared to natural gums, gelatin is more consistent, easier to prepare in solution form and
forms tablets as hard as acacia and tragacanth.
• Disadvantage of gelatin is that it supports the growth of bacteria and molds.
• Replaced with synthetic polymeric binders like methylcellulose, polyvinyl pyrrolidone (PVP).
d) Starch:
• One of the most commonly used granulating agent. Various forms of starch are used for the
purpose of granulation
Diluents:
• Inert substances added to increase the bulk of the tablet.
• Highly potent drugs such as digoxin, clonidine hydrochloride etc., Exert their therapeutic effect in very low doses,
hence their bulk is increased by adding diluents.
Types of diluents:
(a) Organic diluents:
• Carbohydrates or their derivatives.
• Exhibit properties like compactibility, flowing ability, hygroscopicity, solubility stability,provide mechanical strength
and palatability to the tablet, are non-toxic and impart appropriate solubility profile.
i. Dextrose:
• White, odourless, sweet, crystalline powder which imparts a cool feel in the mouth.
• Free-flowing, water soluble diluent and is available in hydrous (dextrose monohydrate) and anhydrous forms.
• Anhydrous form of dextrose is used when low moisture is desired.
ii. Lactose (milk sugar):
• White, odourless powder, slightly sweet in taste.
• Low-cost diluent.
• Soluble in water (1g in 4.63 ml of water) and insoluble in alcohol
a) Mannitol:
• Odourless, white, crystalline powder with a slight sweet taste.
• Dissolves slowly and imparts a cool sensation in the mouth, hence is preferably used as a diluent in
chewable tablet.
• Inert and non-hygroscopic is used in vitamin formulations which are moisture sensitive.
• Formulations containing mannitol require large amount of lubricants due to its poor flow
characteristics.
b) Starch:
• White, water insoluble and odourless substance obtained from different sources like corn, potato,
wheat etc.
• Used as a diluent, binding agent, disintegrating agent and film-former.
c) Inorganic Diluents:
• Calcium and magnesium salts and exhibit properties like abrasiveness, absorbency, lubricity,
mechanical strength, ph and solubility
• .E.gs: Dibasic calcium phosphate (DCP), calcium carbonate etc
Viscosity Builders:
• Viscosity builders or the viscosifiers are used in low concentrations to enhance the viscosity of the
solution.
• Used in the preparation of aqueous-external solutions, because these preparations should provide
adequate viscosity so as to remain on the affected area of skin or eyes for extended periods.
E.gs:Pectin, xantham gum, tragacanth, hydroxyethyl cellulose, carbomer, povidone.
Flavours
• improve the palatability by masking the objectionable or unpleasant flavour of the drug and the
additives.
• Types of Flavouring Agents
1. Artificial Flavours: Flavouring agents include any substance which is not derived from natural
sources.
2.Natural Flavours: Flavouring agents include essential oils, oleoresins, essence or
extractive, distillate.
Perfumes:
• Some of the natural perfumery agents that are utilised in herbal cosmetics include sandalwood oil,
rose oil, jasmine oil, lavender oil, benzoin etc.
• Compatible with other ingredients used in the formulation and should be fragrant.
• Combination of perfumes can also be used to obtain the desired fragrance.
• Should retain its aroma for longer time periods.
• Should not affect the solubility and stability.