Formulation design of oral pediatric Acetazolamide suspension: dose uniformity and physico-chemical stability study.
BACKGROUND
The formulation of an active pharmaceutical ingredient (API) as oral solution or suspension in pediatrics is a habitual practice, due to the non-existence of many commercialized medicines in pediatric doses. It is also the simplest way to prepare and administer them to this vulnerable population. The design of a formulation that assures the dose and the system stability depends on the physico-chemical properties of the API.


OBJECTIVE
In this study, we formulate a class IV API, Acetazolamide (AZM) as suspension for oral administration to pediatric population. The suspension must comply attributes of quality, safety and efficacy for this route of administration.


METHODS
We use simple compounding procedures, as well as fewer pure excipients, as recommended for children. Mass and uniformity content assays and physical and chemical stability studies were performed. To quantify the API an UPLC method was used.


CONCLUSIONS
We verified the physico-chemical stability of the suspensions and that they passed the mass test of the European Pharmacopeia (EP), but not the dose uniformity test.


CONCLUSIONS
This reveals that AZM must be formulated as liquid forms with a more complex system of excipients (not usually indicated in pediatrics), or otherwise solid forms capable of assuring uniformity of mass and dose for every dosage unit.
a Departamento de Ingeniería Química y Tecnología Farmacéutica, Facultad de Farmacia , Universidad de La Laguna , Tenerife , Spain.
Ana
A
Santoveña
a Departamento de Ingeniería Química y Tecnología Farmacéutica, Facultad de Farmacia , Universidad de La Laguna , Tenerife , Spain.
Javier
J
Suárez-González
a Departamento de Ingeniería Química y Tecnología Farmacéutica, Facultad de Farmacia , Universidad de La Laguna , Tenerife , Spain.
Cristina
C
Martín-Rodríguez
a Departamento de Ingeniería Química y Tecnología Farmacéutica, Facultad de Farmacia , Universidad de La Laguna , Tenerife , Spain.
José B
JB
Fariña
D000086:Acetazolamide / Q000008:administration & dosage* / Q000737:chemistry*; D000284:Administration, Oral; D000927:Anticonvulsants / Q000008:administration & dosage* / Q000737:chemistry*; D002648:Child; D004339:Drug Compounding; D004355:Drug Stability; D005079:Excipients / Q000737:chemistry; D006801:Humans; D013535:Suspensions
D000927:Anticonvulsants; D005079:Excipients; D013535:Suspensions; D000086:Acetazolamide
Acetazolamide; BCS class IV; dose uniformity; pediatric oral suspension; physico-chemical stability