Phenylephrine Hydrochloride

= Registered trademark of BASF Ph. Eur., USP, JP, IP

Technical Information
November 2013
Supersedes issue dated August 2010
03_080301e-04/Page 1 of 4
03_080301e-04 November 2013 Page 2 of 4 Phenylephrine Hydrochloride
General information Phenylephrine is classied as a direct sympathomimetic substance. It is mainly
used as a decongestant, especially for topical use in reducing swelling of mucous
membranes.

Phenylephrine is characterized by a phenyl-2-amino-ethanol structure. The substance
is derived from adrenaline, the only difference being the absence of the 4-hydroxy
function.

Phenylephrine (as well as its salts) is used in nished pharmaceutical products.
Three different salt forms of Phenylephrine currently dominate the world market:
Phenylephrine Hydrochloride, Tartrate and Tannate. Of these, Phenylephrine
Hydrochloride is most commonly used in pharmaceutical formulations on the market.

In addition to our current product range, BASF offers Phenylephrine Hydrochloride,
which is a white to almost-white crystalline powder.
1. Medical indications
Applications Phenylephrine Hydrochloride is an active pharmaceutical ingredient, which is mainly
used for the following pharmaceutical formulations:

Topical preparations

Eye drops
Nose drops and sprays


Oral preparations

Tablets and flm tablets
Capsules
Granules and powder for liquid intake (sachets)
Syrups and liquids

Apart from the above-mentioned formulations, there are some less commonly
used preparations in the form of effervescent and chewable tablets, oral strips,
creams, ointments and gels, injectables, ophthalmic inlays, ear drops, suppositories,
and nebulizers.
Indications Phenylephrine Hydrochloride is mainly recommended for topical applications.

Classifed as a direct sympathomimetic substance, Phenylephrine Hydrochloride
is mainly used locally for reducing swelling of mucous membranes in the nose and
local vasoconstriction in the eyes.

Phenylephrine is applied in a low dosage for unspecic and allergic conjunctivitis and
sinusitis. Furthermore, Phenylephrine Hydrochloride is used at higher con centrations
in ophthalmic formulations for diagnostic mydriasis and also for immobilizing the iris
and ciliary body in intraocular infections.

In addition, Phenylephrine is used orally for the treatment of sinusitis and pharyngitis as
an ingredient in cough and cold medicines. However, due to its strong vaso constrictive
effects, certain groups of patients should be excluded (see contraindications).

Oral Phenylephrine application for children:
In several European countries, the oral application of Phenylephrine is restricted
to adults. However, in the US, Canada and several Latin-American countries, it is
widely used in oral preparations which are also considered safe for young children.

Oral pediatric formulations of Phenylephrine are also marketed in South Africa,
Australia, and several Asian countries.
03_080301e-04 November 2013 Page 3 of 4 Phenylephrine Hydrochloride
Contraindications Narrow-angle glaucoma and rhinitis sicca (atrophic rhinitis) are contraindications
for the local and oral application of Phenylephrine.

Patients suffering from hyperthyreosis should not be orally treated with Phenylephrine.
Patients diagnosed with high blood pressure and arrhythmia can only take this API
orally after a careful risk-benet analysis.

Careful dosage for local application is also necessary for patients suffering from
high blood pressure or hyperthyreosis.

Extremely cautious dosage is necessary when Phenylephrine is applied locally
to babies and very young children. This application is only possible in strongly
diluted solutions (no sprays) because of the risk of severe side effects, which may
be due to absorption processes.

Phenylephrine is not recommended to be given orally to babies and very young
children. The orally toxic dosage is described by the literature as 3 mg/kg body
weight for children, but 300 mg/kg body weight for adults.
Pharmacology Like Adrenaline, Phenylephrine is a direct sympathomimetic substance.

Phenylephrine belongs to the group of so-called direct a-sympathomimetic drugs,
which, when given in low concentrations, cause the mucous membranes to contract
(through the constriction of the skin blood vessels).

In high concentrations, all blood vessels contract, which can lead to an increase
in blood pressure.
Pharmacokinetics After oral application, the substance is absorbed quickly and completely. The
biological half-life is 2 3 hours. Phenylephrine is mainly excreted via the kidneys.
80 90% of the orally applied dosage is eliminated within 48 hours.

The therapeutic plasma concentration of Phenylephrine is described by the literature
as 0.04 0.1 g/ml.
2. Chemical information
Name Phenylephrine Hydrochloride
Chemical name (-)-(1R)-(3-Hydroxyphenyl)-2-(methylamino)ethanol Hydrochloride
CAS-No. 61-76-7
Structural formula
H
N
HO
HO
H
+
Cl
-

Empirical formula C
9
H
13
NO
2
HCl
BASF Nutrition & Health www.pharma-ingredients.basf.com
03_080301e-04 November 2013 Page 4 of 4 Phenylephrine Hydrochloride
Appearance White or almost-white crystalline powder, odorless and fully soluble in water.
3. Grades
PRD-No. Particle size
30458832 Not less than 95%
pass 0.500 mm sieve No. 35
Not more than 70%
pass 0.150 mm sieve No. 100
Phenylephrine Hydrochloride
25 kg
5 kg
0.1 kg (sample)
Retest period See separate documentation: Q&R PI (not for regulatory purposes) available at
BASFs WorldAccount: https://worldaccount.basf.com (registered access).
4. Specication See separate documentation: Q&R PI (not for regulatory purposes) available at
BASFs WorldAccount: https://worldaccount.basf.com (registered access).
5. Regulatory status Phenylephrine Hydrochloride meets the requirements of the following current
monographs:

Ph. Eur.
USP
JP
IP
6. Storage Phenylephrine Hydrochloride should be stored in the original, tightly sealed container.
It should be placed in a well-ventilated, cool room at temperatures not exceeding
25 C and protected from direct sunlight.

Generally, Phenylephrine Hydrochloride is known to be a stable substance. The
retest period applies to material stored in the original, unopened container and
according to our recommendations.
Note This document, or any answers or information provided herein by BASF, does not
constitute a legally binding obligation of BASF. While the descriptions, designs, data
and information contained herein are presented in good faith and believed to be
accurate, it is provided for your guidance only. Because many factors may affect
processing or application/use, we recommend that you make tests to determine
the suitability of a product for your particular purpose prior to use. It does not relieve
our customers from the obligation to perform a full inspection of the products upon
delivery or any other obligation. NO WARRANTIES OF ANY KIND, EITHER EXPRESS
OR IMPLIED, INCLUDING WARRANTIES OF MERCHANTABILITY OR FITNESS
FOR A PARTICULAR PURPOSE, ARE MADE REGARDING PRODUCTS DESCRIBED
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A PART OF OUR TERMS AND CONDITIONS OF SALE.

November 2013