[e-drug] Paediatric drug formulations

E-DRUG: Paediatric drug formulations
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Dear e-drug community,

I am a Ph D student at Ghent University, involving with the technological contribution to the lack of paediatric formulations.

Reading different messages about paediatric drug formulations and especially the case of HIV, tuberculosis and malaria (quinine syrup), I decided to share knowledge with everybody by posting the following ideas and I will need anybody’s contribution to the problems encountered:

As in addition to the parenteral and rectal route, oral administration of drugs is a dominant principle in giving medicines to children and many drugs that are administered to children are not exclusively designed for children and further more do not always come in the appropriate strength, it is frequently necessary to split tablets, often in thirds or fourths as the paediatric doses are expressed on a milligram per kilogram basis.

Some studies have been undertaken to assess the accuracy of tablet splitting.
The authors concluded that tablet splitting resulted in an unacceptable weight variation and that the inequality of fragments may produce clinically important outcomes or risks of adverse effects, depending on the dose-response curve and therapeutic window of the particular drug.

From the above studies, it is not yet clearly defined at which level the reported mass unconformity compromise the therapeutic efficacy of the drug.

Malaria is a public health problem in over 100 countries worldwide, mine included (RWANDA). Especially in tropical Africa where it kills around a million people a year and 75% of them being children under 5 years of age, in many areas it accounts for around a quarter of all deaths in this age group.

The increasing spread of resistance to chloroquine an SP has been responsible for the drug combination use and the re-emergence of quinine as an important drug in the treatment of multiple-drug resistant Plasmodium falciparum malaria.

For children, a dose of 10 mg of quinine salt per kg body-weight given every 8 hours for 7 days is recommended. As for per oral way, quinine sulphate is only commercially available in a dose of 200 or 300 mg per tablets; the drug regimens are used to adapt the dose to body weight (WHO/FCH/CAH/00.1)

The study was conducted to evaluate the impact of breaking quinine sulphate tablets into halves and quarters, on the accuracy of doses for paediatric population.
We found that some halves deviated more than 25% from the expected mean weight.
For the quarters none of the studied tablet types comply with the requirements of Eur. Pharm and for tablets without breaking mark the deviation of more than 35% was found.
With such weight variability, in addition to the drug liberation profile which can differ between manufacturers, individual physiological factors, the change of the patient volume of distribution during malaria illness, regional quinine P. falciparum sensibility, the efficacy of tablet splitting practice is hazardous.

Pellets being small spheres (500-8005m in my case), as each particle contains a known quantity of the drug, can be an alternative solution to overcome the liquid formulation availability and cost problem. They offer many advantages such possibility of manufacturing of controlled or sustained release system, introduction of more than one drug in the final single dosage form, quick dissolution thus absorption, possibility to be filled in hard gelatine capsules or be compressed into tablets, good compliance as they can be sprinkled to the child food.

However, the problem is how to dose them!!

Any idea is welcomed.

Lombe Kasonde any idea through your masters study?

Does anybody have information to the quinine solution stability and better taste?

Which quinine paediatric formulations already on the market?

Davids Woods, kindly let me know more about the study on the access to paediatric formulation in developing countries.

Best regards,

Pierre Kayumba
Rwanda (studying in Belgium)
Pierre.Kayumba@UGent.be

E-DRUG: Re: Paediatric drug formulations (cont'd)

Dear Pierre Kayumba,

Fantastic write up indeed.
In Zambia we receive Quinine syrup formulations from various Pharmaceutical
Companies in India. As I reply, in front of me I have a Quinine Sulphate
Suspension 60 mls, each 5 mls contains Quninie Sulphate IP 150 mg, Flavoured
base qs, Colour: Sunset Yellow FCF: QSM-trade mark, by Leben Laboratories
PVT Ltd, India.

I just hope these supplies undergo quality analysis in view of causing
possible resistance.

[I would think other aspects of quality were more important than resistance. KM]

Kind regards

Dr. Mulenga Joseph
Medical Practitoner
Private Practice

E-DRUG: Re: Paediatric drug formulations (cont'd)

Thank you for giving some Scientific insight into what might be going on in this arena. When I started to raise the issue of lack of appropriate paediatric formulations in the year 2000 in various fora, the silence was defeaning! Later on, there were voices in favor of reformulating adult formulations.

However, what we need now is scientists like you to give us some backing in terms of such studies. As a quick concern, why is it that malaria deaths in children in Africa are not on the decline despite the availability of medicines for prevention and treatment? Could resistance to these medicines be emerging out of underdosing due to the pill splitting practices?

Regarding Quinine, from my memory of formulations, it is one of those medicines that really gets compacted when tableted. Most tablets fail dissolution tests (they come out in "sheets" rather than dissolve). I am also not certain about the uniformity of distribution of active ingredient in a tablet that is not designed for splitting.

I hope your studies shed some light into this so that we Policy makers and advocates can put "evidence" to our voices

Atieno Ojoo
Boston University School of Public Health

E-DRUG: Paediatric drug formulations (cont'd)
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Dear Atieno

< However, what we need now is scientists like you to give us some
backing in terms of such studies. As a quick concern, why is it that
malaria deaths in children in Africa are not on the decline despite
the availability of medicines for prevention and treatment? Could
resistance to these medicines be emerging out of underdosing due to
the pill splitting practices? >

I wonder whether it is worth raising again the issue aired in the
Essential Drugs Monitor 33 by Hilbrand Haak in his review of the
study by Maponga and Ondari: The quality of antimalarials: A study
in selected African Countries. WHO/EDM/PAR/2003.4. The problem
with poor quality products was exposed leading to confusion about
whether resistance was responsible for treatment failure or whether
insufficient ingredients in the products were the cause.

Beverley

Beverley Snell
Centre for International Health
Macfarlane Burnet Institute for Medical Research & Public Health
GPO Box 2284, Melbourne 3001 Australia
http://www.burnet.internationalhealth.edu.au

Telephone 613 9282 2115 / 9282 2275
Fax 61 3 9282 2144 or 9282 2100
Time zone: 11 hours ahead of GMT.
email <bev@burnet.edu.au>

Site: Alfred Medical Research & Education Precinct (AMREP),
corner Punt & Commercial Roads, Prahran 3181

E-DRUG: Paediatric drug formulations (cont'd)
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To ED,

I would like to reason that drug resistance would also come about more
likely due to underdosing arising from poor quality drugs than pill
splitting. In my environment even where the dosing, according to the drug
concentration e.g syrups/suspension and injectables, is correct we have a
similar situation. I would like to cite a situation of Chloroquine that was
in use for a long time until when its manufacturing was "liberalized".

regards

Dr. Mulenga Joseph
Zambia
docmulengajo@zamtel.zm