Evaluation of the impact of age-specific bile salt differences on the dissolution behavior of voriconazole using biorelevant media

N.A.

Makale detayları

Evaluation of the impact of age-specific bile salt differences on the dissolution behavior of voriconazole using biorelevant media

Yazarlar:

N.A.

Yayıncı:

Marmara University

Ana Başlıklar:

Pharmacology and Pharmaceutical Sciences (Other)

Dergi:

Journal of Research in Pharmacy Vol.27 Issue 6, pp.2535-2547

Belge Tipi:

Makale

Yayın Tarihi:

6/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001346317

pISSN:

2630-6344

Anahtar kelimeler:

Özet:

 Voriconazole is a well-accepted and effective antifungal agent belonging to BCS class II. Voriconazole is a highly intriguing drug with considerably variable pharmacokinetics among adults and children primarily attributed to the drug-metabolizing enzymes. Additionally, bile salts enhance the absorption of lipophilic drugs in the GI fluids. Since voriconazole has limited solubility, age-related fluctuations in bile salts may affect the drugs pharmacokinetics. Therefore, the purpose of this study is to assess whether age-associated changes in the GI fluid composition and fluid volume may play a role in affecting the dissolution behavior of voriconazole. Based on that, the solubility and in-vitro dissolution studies of voriconazole were carried out in biorelevant media using 900 ml and 500 ml as GI volumes for adults and pediatrics respectively. Additionally, employing variations in the bile salt concentrations for the dissolution medium to act as a surrogate representing various age-specific cohorts. The results demonstrated that changes in GI volume had a negligible impact on the in-vitro dissolution profiles of voriconazole. However, as anticipated, there were some notable impacts of bile salt changes on the in-vitro dissolution profiles of voriconazole. Furthermore, it can be inferred that other factors, such as variations in the expression and maturation of enzymes, may have a comparatively profound impact on the disparate pharmacokinetics of voriconazole in adults and children besides bile salts alone. Since pharmacopoeial buffers are unable to mimic actual in-vivo conditions, leading to misinterpretation of the results. Therefore, in-vitro dissolution investigations carried out in biorelevant media are preferable.

 Voriconazole is a well-accepted and effective antifungal agent belonging to BCS class II. Voriconazole is a highly intriguing drug with considerably variable pharmacokinetics among adults and children primarily attributed to the drug-metabolizing enzymes. Additionally, bile salts enhance the absorption of lipophilic drugs in the GI fluids. Since voriconazole has limited solubility, age-related fluctuations in bile salts may affect the drugs pharmacokinetics. Therefore, the purpose of this study is to assess whether age-associated changes in the GI fluid composition and fluid volume may play a role in affecting the dissolution behavior of voriconazole. Based on that, the solubility and in-vitro dissolution studies of voriconazole were carried out in biorelevant media using 900 ml and 500 ml as GI volumes for adults and pediatrics respectively. Additionally, employing variations in the bile salt concentrations for the dissolution medium to act as a surrogate representing various age-specific cohorts. The results demonstrated that changes in GI volume had a negligible impact on the in-vitro dissolution profiles of voriconazole. However, as anticipated, there were some notable impacts of bile salt changes on the in-vitro dissolution profiles of voriconazole. Furthermore, it can be inferred that other factors, such as variations in the expression and maturation of enzymes, may have a comparatively profound impact on the disparate pharmacokinetics of voriconazole in adults and children besides bile salts alone. Since pharmacopoeial buffers are unable to mimic actual in-vivo conditions, leading to misinterpretation of the results. Therefore, in-vitro dissolution investigations carried out in biorelevant media are preferable.

 Voriconazole is a well-accepted and effective antifungal agent belonging to BCS class II. Voriconazole is a highly intriguing drug with considerably variable pharmacokinetics among adults and children primarily attributed to the drug-metabolizing enzymes. Additionally, bile salts enhance the absorption of lipophilic drugs in the GI fluids. Since voriconazole has limited solubility, age-related fluctuations in bile salts may affect the drugs pharmacokinetics. Therefore, the purpose of this study is to assess whether age-associated changes in the GI fluid composition and fluid volume may play a role in affecting the dissolution behavior of voriconazole. Based on that, the solubility and in-vitro dissolution studies of voriconazole were carried out in biorelevant media using 900 ml and 500 ml as GI volumes for adults and pediatrics respectively. Additionally, employing variations in the bile salt concentrations for the dissolution medium to act as a surrogate representing various age-specific cohorts. The results demonstrated that changes in GI volume had a negligible impact on the in-vitro dissolution profiles of voriconazole. However, as anticipated, there were some notable impacts of bile salt changes on the in-vitro dissolution profiles of voriconazole. Furthermore, it can be inferred that other factors, such as variations in the expression and maturation of enzymes, may have a comparatively profound impact on the disparate pharmacokinetics of voriconazole in adults and children besides bile salts alone. Since pharmacopoeial buffers are unable to mimic actual in-vivo conditions, leading to misinterpretation of the results. Therefore, in-vitro dissolution investigations carried out in biorelevant media are preferable.

 Voriconazole is a well-accepted and effective antifungal agent belonging to BCS class II. Voriconazole is a highly intriguing drug with considerably variable pharmacokinetics among adults and children primarily attributed to the drug-metabolizing enzymes. Additionally, bile salts enhance the absorption of lipophilic drugs in the GI fluids. Since voriconazole has limited solubility, age-related fluctuations in bile salts may affect the drugs pharmacokinetics. Therefore, the purpose of this study is to assess whether age-associated changes in the GI fluid composition and fluid volume may play a role in affecting the dissolution behavior of voriconazole. Based on that, the solubility and in-vitro dissolution studies of voriconazole were carried out in biorelevant media using 900 ml and 500 ml as GI volumes for adults and pediatrics respectively. Additionally, employing variations in the bile salt concentrations for the dissolution medium to act as a surrogate representing various age-specific cohorts. The results demonstrated that changes in GI volume had a negligible impact on the in-vitro dissolution profiles of voriconazole. However, as anticipated, there were some notable impacts of bile salt changes on the in-vitro dissolution profiles of voriconazole. Furthermore, it can be inferred that other factors, such as variations in the expression and maturation of enzymes, may have a comparatively profound impact on the disparate pharmacokinetics of voriconazole in adults and children besides bile salts alone. Since pharmacopoeial buffers are unable to mimic actual in-vivo conditions, leading to misinterpretation of the results. Therefore, in-vitro dissolution investigations carried out in biorelevant media are preferable.

Makale detayları

Evaluation of the impact of age-specific bile salt differences on the dissolution behavior of voriconazole using biorelevant media

Yazarlar:

N.A.

Yayıncı:

Marmara University

Ana Başlıklar:

Pharmacology and Pharmaceutical Sciences (Other)

Dergi:

Journal of Research in Pharmacy Vol.27 Issue 6, pp.2535-2547

Belge Tipi:

Makale

Yayın Tarihi:

6/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001346317

pISSN:

2630-6344

Age-specific differences

bile salts

biorelevant media

in-vitro dissolution

voriconazole

Sayı

Makale detayları

Evaluation of the impact of age-specific bile salt differences on the dissolution behavior of voriconazole using biorelevant media

Yazarlar: N.A.

Yayıncı: Marmara University

Ana Başlıklar: Pharmacology and Pharmaceutical Sciences (Other)

Dergi: Journal of Research in Pharmacy Vol.27 Issue 6, pp.2535-2547

Belge Tipi: Makale

Yayın Tarihi: 6/2025

Belge Dili: İngilizce

Document ID (Org No.): 2001346317

pISSN: 2630-6344

Age-specific differences

bile salts

biorelevant media

in-vitro dissolution

voriconazole

Sayı

Yazarlar:

N.A.

Yayıncı:

Marmara University

Ana Başlıklar:

Pharmacology and Pharmaceutical Sciences (Other)

Dergi:

Journal of Research in Pharmacy Vol.27 Issue 6, pp.2535-2547

Belge Tipi:

Makale

Yayın Tarihi:

6/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001346317

pISSN:

2630-6344