Permeability of olmesartan medoxomil from lipid based and suspension formulations using an optimized HDM-PAMPA model
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Tarih
2022
Yazarlar
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Erişim Hakkı
info:eu-repo/semantics/closedAccess
Özet
Hexadecane membrane-parallel artificial membrane permeability assay (HDM-PAMPA) is based on an artificial hexadecane membrane that separates the two compartments (donor and acceptor compartment). This model is used to predict the permeability of drugs in gastrointestinal tract and to simulate the passive absorption. In vivo behaviour of the drugs can be estimated with these systems in drug development studies. In our study we optimized HDM-PAMPA model to determine permeability of olmesartan medoxomil (OM) lipid based drug delivery system (OM-LBDDS). In order to prove that LBDDS formulation facilitates the weak permeability of OM, permeation rates were compared with the OM suspension formula (containing 0.25% v/w CMC). The experiment was performed on a 96-well MultiScreen® PAMPA filter plate (MAIPN4510). The permeability of olmesartan formulations from the donor to acceptor compartment separated by a HDM membrane were determined by the previous validated HPLC method. We created positive control series without coating hexadecane membrane to present the LBDDS and suspension formulation permeability from uncoated plates. The effective permeability constant (Pe) was calculated by the formula and improvement of permeability of OM-LBDDS formulation from hexadecane membrane was confirmed. On the contrary there was no permeation of OM-Suspension in the hexadecane coated plates. As a result, the intestinal permeability of OM-LBDDS was calculated to be at least 100 times more than the suspension. OM-Suspension permeation was only observed in the hexadecane uncoated positive control plates. This was also manifestation of HDM-PAMPA mimicking permeability of intestines because of its lipidic construction.
Açıklama
Anahtar Kelimeler
Bioavailability, Permeability Efficiency, PAMPA, Hexadecane, LBDDS
Kaynak
Pharmaceutical Development and Technology
WoS Q Değeri
Q2
Scopus Q Değeri
Q2
Cilt
Sayı
Künye
Komesli, Y., Karasulu, E. (2022). Permeability of olmesartan medoxomil from lipid based and suspension formulations using an optimized HDM-PAMPA model. Pharmaceutical Development and Technology. 10.1080/10837450.2022.2114495
