Abstract
Itraconazole (ITZ) is an antifungal drug (BCSII) used for the treatment of local and systemic fungal infections. Furthermore, ITZ used as an antifungal prophylaxis for immunocompromised patients.
 The objective of the study is to overcome the two problems of low and pH dependent solubility of ITZ by its preparation as floating microparticles.
 Firstly, pH-dependent floating microparticles were prepared using oil in water solvent evaporation method, from which the best one (F7) selected as a best pH-dependent formula with composition of ITZ (200mg),EC (800mg), HPMC 15cps (200mg) and safflower oil (2ml) .Then, F7 was compared with the selected Relatively pH-independent ITZ floating microparticles formula with composition of ITZ(200mg), a first coat of HPMC15cps (200mg), a second coat of EC (800mg), HPMC 15cps (200mg) and safflower oil (2ml) which prepared by a dual coating solvent evaporation method using a first coat which provides relatively pH-independent solubility, while the second coat applied as a bouncy producing agents. Polyvinyl alcohol (PVA) was used as a surfactant in both cases.
 The prepared floating microparticles were subjected to various evaluation parameters such as yield percent, drug loading and drug entrapment efficiency (EE), particle size analysis, in- vitro bouncy, drug release, Fourier Transforms Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC) and X-ray Diffractometry (XRD) studies.
Highlights
Oral drug administration is the most common route to get a systemic effect due to its numerous advantages like safety, noninvasive, painless, does not require assistance, more convenient for chronic drugs administration and the medicament not need to be sterile.[1]several factors can affect the oral bioavailability, including water solubility and pH-dependent solubility
Microparticles defined as solid particles with gastric acidity is essential for adequate dissolution, and its oral bioavailability increased when taken with food since gastric pH decrease after food intake[9].Firstly the pH of the stomach is variable and impossible to remain below1.2 value, secondly there are cases that raise stomach pH value lead to decrease of ITZ solubility, and bioavailability include fasting state, patients taking gastric acid-reducing agents such as protein pump inhibitors(PPI) and H2-blockers and patients with AIDS who complain from Hypochlorhydria.[10]
The objective of this study is to overcome both low water solubility and pH-dependent solubility of Itraconazole by formulating it as floating microparticles and one with a relatively pHindependent floating microparticles and compared between them to improve the solubility at variable pH values and prolong the release of the ITZ in stomach, which may lead to increase in ITZ bioavailability
Summary
Oral drug administration is the most common route to get a systemic effect due to its numerous advantages like safety, noninvasive, painless, does not require assistance, more convenient for chronic drugs administration and the medicament not need to be sterile.[1]several factors can affect the oral bioavailability, including water solubility and pH-dependent solubility. Several techniques have been used to overcome these challenges include a reduction of the particle size that solves just water solubility problem(not the pH-dependent problem) such as micronisation or nanonisation, use of surfactants and conversion of crystalline to amorphous forms[2]. Oil in water solvent evaporation method is most straight forward method for microencapsulation, widely used in pharmaceutical industries and costeffective. This directly modified technique can be used to overcome many drugs physicochemical problems including both water solubility and pHdependent solubility using specific coating materials [3]. The objective of this study is to overcome both low water solubility and pH-dependent solubility of Itraconazole by formulating it as floating microparticles and one with a relatively pHindependent floating microparticles and compared between them to improve the solubility at variable pH values and prolong the release of the ITZ in stomach, which may lead to increase in ITZ bioavailability
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Schedule a callMore From: Iraqi Journal of Pharmaceutical Sciences ( P-ISSN: 1683 - 3597 , E-ISSN : 2521 - 3512)
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