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Pharma Ingredients

& Services
Caffeine Anhydrous
Technical Information
January 2010
Supersedes issue dated October 2009
03_030708e-10/Page 1 of 12
= Registered trademark of BASF group Ph. Eur., USP, JP
1. Medical indication Caffeine is a methylxanthine (like theophylline or theobromine), a natural substance
derived from the purine found in various plant families worldwide. Well-known
examples of plants in which Caffeine is found include coffea arabica (coffee), thea
sinensis (black tea), ilex paraguayensis (mate) and cola vera (cola nuts). These have
been used as stimulants since ancient times.

In terms of pharmacology and therapy, methylxanthines belong to the group of
psychoanaleptics. Methylxanthines affect the central nervous system, the cardio-
vascular system, the skin, the kidneys and also act as phosphor diesterase inhibitors.

Caffeine is mostly used in combination with analgesics and antihistamines, but it
is also used in the treatment of apnoea in newborns, in skin care products and in
the food and beverage industry.
Pharmacology Among the methylxanthines, Caffeine has the most distinctive central effect. It
primarily acts on the cerebral cortex and stimulates psychic and sensory functions.
Caffeine increases mental receptivity and efciency and reduces fatigue. Only high
doses stimulate the autonomic nervous system.

The effects of Caffeine on the cardiovascular system, especially in acute circulatory
failure, are based on the stimulation of vasomotor centres and, in part, on the excitation
of the myocardium.

Various peripheral vessels in the kidneys and other areas innervated by the splanchnic
nerve as well as the coronaries are dilated by Caffeine. However, blood pressure
is generally not affected.

The tone of the cerebral vessels is raised and the cerebrospinal pressure reduced.
Caffeines effect on vascular headaches is attributed to this factor.

At relatively high doses, Caffeine and theophylline inhibit phosphodiesterase, an
enzyme that degrades cyclic adenosine monophosphate (cAMP) to the inactive
adenosine monophosphate. This leads to an increase in cAMP concentrations,
affects smooth muscle spasmolysis and promotes glycogenolysis and lipolysis.
The lipolytic effect is seen in increasing plasma concentrations of free fatty acids
after oral ingestion of Caffeine. The high concentration of cAMP activates a specic
enzyme that hydrolyses the triglycerides to fatty acids and glycerol.

This lipolytic effect can also be used in the cosmetics industry in the management
of cellulites.

Other pharmacological properties of caffeine, such as suppression of fatigue by
increasing the amount of oxygen in the CNS cells, are explained by its competitive
inhibition of adenosine receptors. By promoting the release of noradrenaline,
adrenaline and especially dopamine, Caffeine also has a positive effect in the
treatment or prevention of Parkinsons disease.
Pharmacokinetics Caffeine is almost completely absorbed. Peak plasma levels are reached within
30 minutes. The apparent distribution volume is between 0.35 1.1 l/kg.

The substance is excreted with the urine. Its biological half-life is about 3 5 hours.
Smokers eliminate Caffeine twice as fast as non-smokers because of enzyme
induction.
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2. Chemical Information
Name Caffeine
Trade name Caffeine Anhydrous
Chemical name 1,3,7-Trimethylxanthine
CAS-No. 58-08-2
EINECS-No. 200-362-1
Structural formula
Empirical formula C
8
H
10
N
4
O
2
Molecular weight 194.19 g/mol
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3. Grades
PRD-No. Particle size
30057897 Not less than 95%
pass 0.300 mm sieve (No. 50)
Caffeine Anhydrous Powder
50 kg
1 kg (sample)
0.05 kg (sample)
30057886 Not less than 97%
pass 0.150 mm sieve (No. 100)
Caffeine Anhydrous Fine
Powder
50 kg
0.05 kg (sample)
30057889 Not less than 100%
pass 0.500 mm sieve (No. 35)
Not more than 29%
pass 0.150 mm sieve (No. 100)
10 29%
pass 0.075 mm sieve (No. 200)
Caffeine Anhydrous Granular
0.07/0.5
50 kg
0.5 kg (sample)
0.05 kg (sample)
30057887 Not less than 97%
pass 0.500 mm sieve (No. 35)
Not more than 10%
pass 0.212 mm sieve (No. 70)
Caffeine Anhydrous Granular
0.2/0.5
100 kg
50 kg
1 kg (sample)
0.05 kg (sample)
30057315 Not less than 90%
pass 0.710 mm sieve (No. 25)
Not more than 10%
pass 0.212 mm sieve (No. 70)
Caffeine Anhydrous Granular
0.2/0.7
50 kg
0.05 kg (sample)
30057892 Not less than 95%
pass 1.005 mm sieve (No. 30)
Not more than 60%
pass 0.600 mm sieve (No. 30)
Not more than 30%
pass 0.500 mm sieve (No. 35)
Not more than 5%
pass 0.063 mm sieve (No. 230)
Caffeine Anhydrous Granular
0.5/1.0
50 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. Physical and chemical
properties
Solubility: Water: sparingly soluble
Ethanol: slightly soluble
Ether: slightly soluble
5. Regulatory status
Caffeine Anhydrous meets current Ph. Eur., USP, and JP monographs.

EDMF, US-DMF, JDMF, and CEP (CoS) are available upon request and when
necessary.

6. Specications
See separate document: Standard Specication (not for regulatory purposes)
available via BASFs WorldAccount: https://worldaccount.basf.com (registered
access).
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7. Particle characterization The following data strongly depend on the operator and method employed and
may vary from lab to lab.
7.1 Caffeine Anhydrous Powder
Particle size specication Not less than 95% pass 0.300 mm sieve (No. 50)
Volume Loose bulk volume approx. 2.3 ml/g
Bulk volume approx. 2.1 ml/g
Tapped volume approx. 1.5 ml/g
SEM photographs


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7.2 Caffeine Anhydrous Fine Powder
Particle size specication Not less than 97% pass 0.150 mm sieve (No. 100)
Volume Loose bulk volume approx. 2.8 ml/g
Bulk volume approx. 2.6 ml/g
Tapped volume approx. 2.0 ml/g
SEM photographs


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7.3 Caffeine Anhydrous Granulated
0.07/0.5
Particle size specication Not less than 100% pass 0.500 mm sieve (No. 35)
Not more than 29% pass 0.150 mm sieve (No. 100)
10 29% pass 0.075 mm sieve (No. 200)
Volume Loose bulk volume approx. 1.7 ml/g
Bulk volume approx. 1.6 ml/g
Tapped volume approx. 1.4 ml/g
SEM photographs

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7.4 Caffeine Anhydrous Granulated
0.2/0.5
Particle size specication Not less than 97% pass 0.500 mm sieve (No. 35)
Not more than 10% pass 0.212 mm sieve (No. 70)
Volume Bulk volume approx. 1.6 ml/g
Tapped volume approx. 1.5 ml/g
SEM photographs


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7.5 Caffeine Anhydrous Granulated
0.2/0.7
Particle size specication Not less than 90% pass 0.710 mm sieve (No. 25)
Not more than 10% pass 0.212 mm sieve (No. 70)
Volume Loose bulk volume approx. 1.7 ml/g
Bulk volume approx. 1.6 ml/g
Tapped volume approx. 1.5 ml/g
SEM photographs


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7.6 Caffeine Anhydrous Granulated
0.5/1.0
Particle size specication Not less than 95% pass 1.005 mm sieve (No. 30)
Not more than 60% pass 0.600 mm sieve (No. 30)
Not more than 30% pass 0.500 mm sieve (No. 35)
Not more than 5% pass 0.063 mm sieve (No. 230)
Volume Bulk volume approx. 1.6 ml/g
Tapped volume approx. 1.5 ml/g
SEM photographs

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BASF SE - Care Chemicals Division - Pharma Ingredients & Services - 67117 Limburgerhof - www.pharma-ingredients.basf.com
8. Formulations Besides its use in pharmaceutical and skin care products, the largest amount of
Caffeine is used for soft drinks such as colas and energy drinks.
Pharmaceutical applications In the pharmaceutical industry, and especially in the United States, Caffeine is often
sold in pill form intended to keep the taker awake. However, Caffeine is mostly used
in combination products with painkillers such as paracetamol, acetyl salicylic acid
or ibuprofen. Caffeine has an additive effect in combination with these active
substances.
Caffeine tablets Caffeine, ne powder 50 mg
Avicel PH 200 40 mg
Kollidon

VA 64 4 mg
Kollidon CL 5 mg
Magnesium stearate 0.5 mg
Aerosol 200 0.5 mg
Mix all ingredients and compress in 6 mm round tablets.
Compression force 2.5 kN
Hardness 92 N
Disintegration within 1 min
Dissolution more than 80% after 10 min
General information for tableting: small grades result in higher hardness at low
compression forces.
In most cases, caffeine may be added as a dry powder (without prior granulation)
to painkiller formulations, and compressed into tablets.
Cosmetic applications Caffeine is often used in skin care products such as creams or gels. When applied
on the skin, there is a widening of the small blood vessels in the skin. As a result,
the skin can appear fresher and there may be a reduction of small wrinkles.
High content caffeine gel Caffeine, powder 200 7.0%
Carbopol 971 0.5%
Deionized water 64.5%
Ethanol 28.0%
Caffeine is dissolved in a water/ethanol mixture at 50 C. After cooling to about
20 C, carbopol is added and dissolved and the pH value adjusted to 6.5 6.8 using
0.1 mol NaOH. Tetraethylene diamine may be used instead of NaOH. The resulting
gel takes several hours to form.
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
OR DESIGNS, DATA OR INFORMATION SET FORTH, OR THAT THE PRODUCTS,
DESIGNS, DATA OR INFORMATION MAY BE USED WITHOUT INFRINGING THE
INTELLECTUAL PROPERTY RIGHTS OF OTHERS. IN NO CASE SHALL THE
DESCRIPTIONS, INFORMATION, DATA OR DESIGNS PROVIDED BE CONSIDERED
A PART OF OUR TERMS AND CONDITIONS OF SALE.

January 2010
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