Mesoporous silica based macromolecules for dissolution enhancement of Irbesartan drug using pre-adjusted pH method

Khanfar, Mai; Fares, Mohammad M.; Salem, Mutaz S.; Qandil, Amjad M.

doi:10.1016/j.micromeso.2013.02.007

Cited by 13 publications

(9 citation statements)

References 30 publications

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“…S244FP carriers showed a stronger intensity band from 1300 to 900 cm −1 due to Si–O stretching of the silanol group [ 24 ]. The FTIR spectra of NS2 also showed a broad band from 1300 to 900 cm −1 of the Al–O–Si stretching group and a broad stretch band at 3700–3000 cm −1 of the O–H stretching of the silanol group [ 25 ]. For all of the IBU-loaded S244FP particles, the spectra in Figure 2 a showed the combined individual characteristic peaks of IBU and S244FP carriers, indicating that IBU was physically rather than chemically adsorbed on the outer surface of the porous silica particles.…”

Section: Resultsmentioning

confidence: 99%

Investigating the Effects of Loading Factors on the In Vitro Pharmaceutical Performance of Mesoporous Materials as Drug Carriers for Ibuprofen

et al. 2017

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The aim of the study was to investigate the effects of the loading factors, i.e., the initial drug loading concentration and the ratio of the drug to carriers, on the in vitro pharmaceutical performance of drug-loaded mesoporous systems. Ibuprofen (IBU) was used as a model drug, and two non-ordered mesoporous materials of commercial silica Syloid® 244FP (S244FP) and Neusilin® US2 (NS2) were selected in the study. The IBU-loaded mesoporous samples were prepared by a solvent immersion method with a rotary evaporation drying technique and characterized by polarized light microscopy (PLM), Fourier transform infrared (FTIR) spectroscopy, X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC). Dissolution experiments were performed in simulated gastric media at 37 °C under non-sink conditions. The concentration of IBU in solution was determined by HPLC. The study showed that the dissolution rate of IBU can be improved significantly using the mesoporous S224FP carriers due to the conversion of crystalline IBU into the amorphous form. Both of the loading factors affected the IBU dissolution kinetics. Due to the molecular interaction between the IBU and NS2 carriers, the loading factors had little effects on the drug release kinetics with incomplete drug desorption recovery and insignificant dissolution enhancement. Care and extensive evaluation must therefore be taken when mesoporous materials are chosen as carrier delivery systems.

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Section: Resultsmentioning

confidence: 99%

Investigating the Effects of Loading Factors on the In Vitro Pharmaceutical Performance of Mesoporous Materials as Drug Carriers for Ibuprofen

et al. 2017

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“…Krstić i saradnici su pokazali da brzina rastvaranja karbamazepina iz čvrstih disperzija, izrađenih metodom uparavanja etanola na sobnoj temperaturi, uz korišćenja Neusilin ® -a UFL2, zavisi od odnosa adsorpcioni nosač/karbamazepin i da sa povećanjem udela adsorbenta u formualciji raste i brzina oslobađanja karbamazepina (56). Khvanfar i saradnici su prilikom formulacije čvrstih disperzija Neusilin ® -a i irbesartana došli do sličnih zaključaka (61). Pokazali su da se sa povećanjem udela Neusilin ® -a u formulaciji čvrstih disperzija sa irbesartanom povećava i brzina rastvaranja lekovite supstance, što objašnjavaju visokom specifičnom površinom Neusilina (300 m 2 /g) na koju se adsorbuje lekovita supstanca.…”

Section: Tabela II Karakteristike Najčešće Ispitivanih Sintetskih Mezunclassified

Properties and potential application of modern adsorbents in formulation of solid drug delivery systems

Krstić¹,

Milović²,

Ibrić³

2016

Arh farmaciju

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Poslednjih godina veliki broj adsorpcionih nosača prirodnog i sintetskog porekla privlači sve više pažnje zbog svoje biokompatibilnosti, prihvatljivih ekoloških i toksikoloških osobina, velike mogućnosti za modifikaciju fizičkohemijskih osobina, jednostavnog dobijanja, visoke stabilnosti i relativno niske cene. Ovi nosači su slične hemijske strukture, najčešće na bazi silicijum-dioksida, magnezijum-aluminometasilikata i kalcijum-fosfata, a međusobno se razlikuju po poroznosti struktura, specifičnoj površini, veličini, zapremini i obliku pora kao i mogućnosti funkcionalizacije površine. Uređeni mezoporozni materijali kao što su MCM -41 i SBA -15, kao i porozni materijali iz grupe Neusilin ® -a i Sylysia ® -a predstavljaju najčešće ispitivane adsorbente sa ciljem da povećaju brzinu rastvaranja lekovite supstance, a samim tim i biološku raspoloživost, ali se koriste i u formulaciji preparata sa modifikovanim ili ciljanim oslobađanjem lekovite supstance u određeno tkivo. Takođe prirodni silika materijal jedinstvenih karakteristika, izolovan iz dijatomita, dijatomitne mikrokapsule, predstavlja relativno jeftin adsorbent za formulaciju nosača za peroralnu primenu lekovite supstance kao i primenu u obliku implanta. Savremeni adsorbenti najčešće se koriste u izradi čvrstih disperzija sa nisko rastvorljivom lekovitom supstancom, ili kao adsorbenti za različite lipidne formulacije. Jedna od mogućnosti primene savremenih nosača koja se poslednjih godina ispituje jeste i funkcionalizacija površine poroznih materijala u cilju postizanja usporenog ili signalinicirajućeg oslobađanja lekovite supstance.

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“…In the silicate family, Neusilin ® is an entirely synthetic MAS, insoluble in water, and available in 11 different grades as an amorphous white powder or granules with the empirical formula Al 2 O 3 •MgO•1.7SiO 2 •xH 2 O. It is prepared using the spray drying process, resulting in an extensive specific surface area (100-300 m 2 /g) [12], high absorption capacity (up to 3.4 mL/g), high porosity [13], and good flow [14] and compression properties [15,16]. In an aqueous medium, it does not form a gel [12].…”

Section: Introductionmentioning

confidence: 99%

Exploration of Neusilin® US2 as an Acceptable Filler in HPMC Matrix Systems—Comparison of Pharmacopoeial and Dynamic Biorelevant Dissolution Study

et al. 2022

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Modern pharmaceutical technology still seeks new excipients and investigates the further use in already known ones. An example is magnesium aluminometasilicate Neusilin® US2 (NEU), a commonly used inert filler with unique properties that are usable in various pharmaceutical fields of interest. We aimed to explore its application in hypromellose matrix systems (HPMC content 10–30%) compared to the traditionally used microcrystalline cellulose (MCC) PH 102. The properties of powder mixtures and directly compressed tablets containing individual fillers NEU or MCC, or their blend with ratios of 1.5:1, 1:1, and 0.5:1 were investigated. Besides the routine pharmaceutical testing, we have enriched the matrices’ evaluation with a biorelevant dynamic dissolution study and advanced statistical analysis. Under the USP apparatus 2 dissolution test, NEU, individually, did not provide advantages compared to MCC. The primary limitations were the burst effect increase followed by faster drug release at the 10–20% HPMC concentrations. However, the biorelevant dynamic dissolution study did not confirm these findings and showed similarities in dissolution profiles. It indicates the limitations of pharmacopoeial methods in matrix tablet development. Surprisingly, the NEU/MCC blend matrices at the same HPMC concentration showed technologically advantageous properties. Besides improved flowability, tablet hardness, and a positive impact on the in vitro drug dissolution profile toward zero-order kinetics, the USP 2 dissolution data of the samples N75M50 and N50M50 showed a similarity to those obtained from the dynamic biorelevant apparatus with multi-compartment structure. This finding demonstrates the more predictable in vivo behaviour of the developed matrix systems in human organisms.

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Mesoporous silica based macromolecules for dissolution enhancement of Irbesartan drug using pre-adjusted pH method

Cited by 13 publications

References 30 publications

Investigating the Effects of Loading Factors on the In Vitro Pharmaceutical Performance of Mesoporous Materials as Drug Carriers for Ibuprofen

Investigating the Effects of Loading Factors on the In Vitro Pharmaceutical Performance of Mesoporous Materials as Drug Carriers for Ibuprofen

Properties and potential application of modern adsorbents in formulation of solid drug delivery systems

Exploration of Neusilin® US2 as an Acceptable Filler in HPMC Matrix Systems—Comparison of Pharmacopoeial and Dynamic Biorelevant Dissolution Study

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