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Advisor(s)
Abstract(s)
Os Inibidores das Bombas de Protões são uma classe de fármacos largamente prescrita
por médicos em todo o mundo, sendo que existem também algumas formulações não
sujeitas a receita médica, sendo, assim, mais facilitada a sua aquisição por parte dos
doentes.
Estes fármacos são responsáveis pela supressão ácida do estômago e,
consequentemente, pelo aumento do pH gástrico, estando descritas variadas interações
com diferentes classes de fármacos.
Este trabalho foca-se nas interações de absorção existentes entre os Inibidores das
Bombas de Protões e outros fármacos, quando ambos são tomados por via oral,
verificando-se uma relação entre a classe biofarmacêutica dos fármacos e a ocorrência
deste tipo de interações: os fármacos de classe biofarmacêutica II e IV são os que
possuem maior predisposição para interagirem com os Inibidores das Bombas de
Protões, por possuírem uma solubilidade baixa e várias vezes dependente do pH,
estando o trabalho focado em fármacos destas duas classes.
Além disso, são também descritas as estratégias da tecnologia farmacêutica que nos
permitem ultrapassar estes problemas, tais como a utilização de excipientes
modificadores de pH e a utilização de dispersões sólidas amorfas.
No final do trabalho é realizada uma análise sobre os estudos de bioequivalência, mais
concretamente sobre as condições em que estes normalmente são realizados, ou seja,
em indivíduos saudáveis, e é discutida a relevância de realizar estudos adicionais de
bioequivalência quando estamos perante populações que realizam tratamentos com
agente antiácidos como os Inibidores das Bombas de Protões ou, por exemplo, em
populações com acloridria, sendo que, em ambos os casos há que ter em conta que o
pH gástrico difere dos seus valores fisiológicos.
Com este trabalho foi assim possível explorar e compreender os mecanismos adjacentes
às interações de absorção oral entre Inibidores das Bombas de Protões e outros fármacos
e concluir que os estudos de bioquivalência em indivíduos saudáveis podem não ser
suficientes para garantir esta mesma bioequivalência em todos os indivíduos.
Proton Pump Inhibitors are a class of drugs that are widely prescribed by doctors all over the world, and there are also some non-prescription formulations that make it easier for patients to acquire them. These drugs are responsible for acid suppression in the stomach and, consequently, an increase in gastric pH, and various interactions with different classes of drugs have been described. This study focuses on the absorption interactions between Proton Pump Inhibitors and other drugs, when both are taken orally. There is a relationship between the biopharmaceutical class of the drugs and the occurrence of this type of interaction: biopharmaceutical class II and IV drugs are the most likely to interact with Proton Pump Inhibitors, as they have low solubility and are often pH-dependent, and the study focuses on drugs from these two classes. Strategies in pharmaceutical technology that allow us to overcome these problems are also described, such as the use of pH-modifying excipients and the use of amorphous solid dispersions. At the end of the paper, an analysis is made of bioequivalence studies, more specifically the conditions under which they are normally carried out, i.e. in healthy individuals, and the relevance of carrying out additional bioequivalence studies is discussed when we are dealing with populations undergoing treatment with antacid agents such as Proton Pump Inhibitors or, for example, in populations with achlorhydria, since in both cases it must be taken into account that gastric pH differs from their physiological values. This work has therefore made it possible to explore and understand the mechanisms involved in oral absorption interactions between Proton Pump Inhibitors and other drugs and to conclude that bioequivalence studies in healthy individuals may not be sufficient to guarantee the same bioequivalence in all individuals.
Proton Pump Inhibitors are a class of drugs that are widely prescribed by doctors all over the world, and there are also some non-prescription formulations that make it easier for patients to acquire them. These drugs are responsible for acid suppression in the stomach and, consequently, an increase in gastric pH, and various interactions with different classes of drugs have been described. This study focuses on the absorption interactions between Proton Pump Inhibitors and other drugs, when both are taken orally. There is a relationship between the biopharmaceutical class of the drugs and the occurrence of this type of interaction: biopharmaceutical class II and IV drugs are the most likely to interact with Proton Pump Inhibitors, as they have low solubility and are often pH-dependent, and the study focuses on drugs from these two classes. Strategies in pharmaceutical technology that allow us to overcome these problems are also described, such as the use of pH-modifying excipients and the use of amorphous solid dispersions. At the end of the paper, an analysis is made of bioequivalence studies, more specifically the conditions under which they are normally carried out, i.e. in healthy individuals, and the relevance of carrying out additional bioequivalence studies is discussed when we are dealing with populations undergoing treatment with antacid agents such as Proton Pump Inhibitors or, for example, in populations with achlorhydria, since in both cases it must be taken into account that gastric pH differs from their physiological values. This work has therefore made it possible to explore and understand the mechanisms involved in oral absorption interactions between Proton Pump Inhibitors and other drugs and to conclude that bioequivalence studies in healthy individuals may not be sufficient to guarantee the same bioequivalence in all individuals.
Description
Trabalho Final de Mestrado Integrado, Ciências Farmacêuticas, 2024, Universidade de Lisboa, Faculdade de Farmácia.
Keywords
Proton pump Inhibitors Oral absorption Interactions Bioequivalence Mestrado integrado - 2024