Pharmaceutical

ingredients 6/01/2017

Pharmaceutical ingredients
1.

Menthol

Synonyms
: Racementhol
Chemical Name : , 2-isopropyl-5-methylcyclohexanol , 4isopropyl- 1-methylcyclohexan-3-ol,
3-p-menthanol; p-menthan-3-ol; dlmenthol,
mentholum racemicum ,
Menthomenthol, mentoli, mentolis,
Hexahydrothymol, peppermint camphor,
racemic menthol
Functional Category : Flavoring agent; therapeutic agent.
Applications in Pharmaceutical Formulation
- Flavoring agent or odor enhancer. In addition to its
characteristic peppermint flavor, l-menthol,
which occurs naturally, also exerts a cooling or refreshing
sensation that is exploited in many topical preparations
- Exerts a similar effect due to a negative heat of solution, lmenthol interacts directly with the
bodys coldness receptors. d-Menthol has no cooling effect, while
racemic menthol exerts an effect approximately half that of lmenthol.
- When used to flavor tablets, menthol is generally
dissolved in ethanol (95%) and sprayed onto
tablet granules and not used as a solid excipient.
- Menthol has been investigated as a skin-penetration
enhancer and is also used in perfumery,
tobacco products, chewing
- Applied to the skin, menthol dilates the blood vessels,
causing a sensation of coldness followed
by an analgesic effect. It relieves itching and is used in creams,
lotions, and ointments. When administered orally in small doses
menthol has a carminative action

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Description
Racemic menthol is a mixture of equal parts of the
(1R,2S,5R)- and (1S,2R,5S)-isomers of menthol. It is a free-flowing
or agglomerated crystalline powder, or colorless, prismatic, or
acicular shiny crystals,
or hexagonal or fused masses with a strong characteristic odor
and taste
Typical Properties
Boiling point 212 C
Melting point 34 C
Solubility Very soluble in ethanol (95%), chloroform, ether, fatty
oils and liquid paraffin; freely soluble in glacial acetic acid;
soluble in acetone and benzene; very slightly soluble in glycerin;
practically insoluble in water.
Incompatibilities
Incompatible with: butylchloral hydrate; camphor; chloral
hydrate; chromium trioxide; b-naphthol; phenol; potassium
permanganate; pyrogallol; resorcinol; and thymol.
Safety
Almost all toxicological data for menthol relate to its use as a
therapeutic agent rather than as an excipient. Inhalation or
ingestion of large quantities can result in serious adverse
reactions such as ataxia and CNS depression, hypersensitivity

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ingredients 6/01/2017
reactions, severe abdominal pain, nausea, vomiting, vertigo,
drowsiness, and
coma

2.

Podophylline

Synonyms
: Podophyllotoxin (PPT), also known as podofilox
Applications in Pharmaceutical Formulation
Treat genital warts and molluscum contagiosum
Safety
While podophyllin, the herbal extract from which
podophyllotoxin is derived, can cause enteritis and potentially
fatal CNS depression, podophyllotoxin has been shown to be safe,
with minimal toxicity even in large dose
The most common side effects near the application site are
skin reactions, including burning, redness, pain, itching, swelling.
Application can be immediately followed by burning or itching.
Small sores, itching and peeling skin can also follow.
Neither podophyllin resin nor podophyllotoxin lotions or gels
are used during pregnancy because these medications can be
harmful to the fetus

3.

Eugenol
Eugenia caryophyllata Thunb.
Eugenia caryophyllus (Spreng.) Bullock & Harrison,
Eugenia aromatica Kuntze
Clove, Clove tree

3, 4-dihydroxyphenethyl
alcohol 3, 4-dihydroxybenzoic acid

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ingredients 6/01/2017
(eugenol)


Chemical Name : member of the phenylpropanoids class
Applications in Pharmaceutical Formulation
- Perfumes, flavorings, and essential oils. It is also used as
a local antiseptic and anaesthetic
- Eugenol can be combined with zinc oxide to form zinc
oxide eugenol which
has restorative and prosthodontic applications
in dentistry. For example, zinc oxide eugenol is used for
root canal sealing
Description
colourless to pale yellow oily liquid extracted from
certain essential oils especially from clove
oil, nutmeg, cinnamon, basil and bay leaf. It is present in
concentrations of 8090% in clove bud oil and at 8288% in
clove leaf oil
Safety
Eugenol is hepatotoxic, meaning it may cause damage to
the liver.
Overdose is possible, causing a wide range of symptoms from
blood in the patient's urine,
to convulsions, diarrhea, nausea, unconsciousness, dizziness, or
rapid heartbeat.
According to a published 1993 report, a 2-year-old boy nearly
died after taking between 5 and 10 ml In context, this would
represent a toxic dose in the range of 500-1000mg/kg,
approximately one third that of table salt.
4.

Coal tar solutions

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ingredients 6/01/2017
Chemical Name : complex and variable mixtures
of phenols, polycyclic aromatic hydrocarbons (PAHs),
and heterocyclic compounds
Applications in Pharmaceutical Formulation
It can be used in medicated shampoo, soap and ointment, as
a treatment for dandruff and psoriasis, as well as being used to
kill and repel head lice. When used as a medication in the U.S.,
coal tar preparations are considered over-the-counter
drug pharmaceuticals and are subject to regulation by the FDA.
Named brands include Denorex, Balnetar, Psoriasin, Tegrin, T/Gel,
and Neutar. When used in the extemporaneous preparation of
topical medications, it is supplied in the form of coal tar topical
solution USP, which consists of a 20% w/v solution of coal tar
in alcohol, with an additional 5% w/v of polysorbate 80 USP; this
must then be diluted in an ointment base such as petrolatum.
Human Use, as an OTC treatment for "Dandruff/seborrheic
dermatitis/psoriasis"
Various phenolic coal tar derivatives have analgesic (pain-killer)
properties.
These included acetanilide, phenacetin, and paracetamol
(acetaminophen). Paracetamol is the only coal-tar derived
analgesic still in use today, but industrial phenol is now usually
synthesized from crude oil rather than coal tar.
Description
Brown or black liquid of extremely high viscosity
Safety
- More than five percent of crude coal tar are Group
1 carcinogens
- Coal tar causes increased sensitivity to sunlight,[16] so
skin treated with topical coal tar preparations should be
protected from sunlight.

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ingredients 6/01/2017

5.
Polyoxyethylene Sorbitan Fatty
Acid Esters
Synonyms : Polysorbate , TWEEN
Chemical Name :

Functional Category :
- Dispersing agent , emulsifying agent , nonionic
surfactant
- Solubilizing agent , suspending agent , wetting agent.

Applications in Pharmaceutical Formulation

Polysorbates containing 20 units of oxyethylene are hydrophilic
nonionic surfactants that are used widely as emulsifying agents in
the preparation of stable oil-in-water pharmaceutical emulsions.
They may also be used as solubilizing agents for a variety of
substances including essential oils and oil-soluble vitamins, and

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ingredients 6/01/2017
as wetting agents in the formulation of oral and parenteral
suspensions.
They have been found to be useful in improving the oral
bioavailability of drug molecules that are substrates for
Pglycoprotein.
Description
Polysorbates have a characteristic odor and a warm, somewhat
bitter taste. Their colors and physical forms at 25 C are shown in,
although it should be noted that the absolute color intensity of the
products may vary from batch to batch and from manufacturer to
manufacturer.
Typical Properties

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Incompatibilities
Discoloration and/or precipitation occur with various
substances, especially phenols, tannins, tars, and tarlike
materials.The antimicrobial activity of paraben preservatives is
reduced in the presence of polysorbates
Safety
Nontoxic and nonirritant materials. There have, however, been
occasional reports of hypersensitivity to
polysorbates following their topical and intramuscular use.
Polysorbates have also been associated with serious adverse
effects, including some deaths, in low-birthweight infants
intravenously administered a vitamin E preparation containing a
mixture of polysorbates 20 and 80 The WHO has set an estimated
acceptable daily intake for polysorbates 20, 40, 60, 65, and 80,
calculated as total polysorbate esters, at up to 25 mg/kg bodyweight.