Complex Effects of Drug/Silicate Ratio, Solid-State Equivalent pH, and Moisture on Chemical Stability of Amorphous Quinapril Hydrochloride Coground with Silicates

Hailu, Shumet A.; Bogner, Robin H.

doi:10.1002/jps.22387

Cited by 12 publications

(5 citation statements)

References 28 publications

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“…During the amorphization process, a drastic change in dynamics of drug molecules may arise as the molecules transition from crystal lattices to nanosized capillaries. The increase in molecular mobility discussed in the sections Thermodynamics and Dynamics of Naphthalene Confined in Mesopores and Dynamics of Ibuprofen Confined in Mesopores raises potential concern about the kinetics of chemical degradation of the drug in addition to the normal environmental stress such as moisture 116. Although there are no comprehensive studies reported, qualitative assessment can be made.…”

Section: Methods Of Preparing Amorphous Drug–silica Formulationsmentioning

confidence: 99%

Application of Mesoporous Silicon Dioxide and Silicate in Oral Amorphous Drug Delivery Systems

Qian

Bogner

2012

Journal of Pharmaceutical Sciences

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132

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Section: Methods Of Preparing Amorphous Drug–silica Formulationsmentioning

confidence: 99%

Application of Mesoporous Silicon Dioxide and Silicate in Oral Amorphous Drug Delivery Systems

Qian

Bogner

2012

Journal of Pharmaceutical Sciences

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132

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“…The reaction was initiated by blending the drug and the excipient at room temperature. Similarly, the beneficial effect of magnesium aluminometasilicates on the stability of amorphous quinapril hydrochloride after storage at high humidity has been reported ( 18 ). Several studies have also been carried out on the amorphization of crystalline drugs by co-grinding with silicates ( 19 ).…”

Section: Introductionmentioning

confidence: 73%

Preformulation Studies on Solid Self-Emulsifying Systems in Powder Form Containing Magnesium Aluminometasilicate as Porous Carrier

et al. 2014

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The influence of alkaline and the neutral grade of magnesium aluminometasilicate as a porous solid carrier for the liquid self-emulsifying formulation with ibuprofen is investigated. Ibuprofen is dissolved in Labrasol, then this solution is adsorbed on the silicates. The drug to the silicate ratio is 1:2, 1:4, and 1:6, respectively. The properties of formulations obtained are analyzed, using morphological, porosity, crystallinity, and dissolution studies. Three solid self-emulsifying (S-SE) formulations containing Neusilin SG2 and six consisting of Neusilin US2 are in the form of powder without agglomerates. The nitrogen adsorption method shows that the solid carriers are mesoporous but they differ in a specific surface area, pore area, and the volume of pores. The adsorption of liquid SE formulation on solid silicate particles results in a decrease in their porosity. If the neutral grade of magnesium aluminometasilicate is used, the smallest pores, below 10 nm, are completely filled with liquid formulation, but there is still a certain number of pores of 40–100 nm. Dissolution studies of liquid SEDDS carried out in pH = 1.2 show that Labrasol improves the dissolution of ibuprofen as compared to the pure drug. Ibuprofen dissolution from liquid SE formulations examined in pH of 7.2 is immediate. The adsorption of the liquid onto the particles of the silicate causes a decrease in the amount of the drug released. Finally, more ibuprofen is dissolved from S-SE that consist of the neutral grade of magnesium aluminometasilicate than from the formulations containing the alkaline silicate.

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“…In this study, three main factors that contribute to chemical degradation were investigated: temperature, relative humidity (% RH) and drug-carrier ratio (Hailu and Bogner, 2011). It can be deduced that hydrolytic degradation is predominant during the storage, in which the relative humidity (% RH) plays an important role in chemical instability of amorphous ART compared with the storage temperature.…”

Section: Chemical Stability Of Artmentioning

confidence: 99%

Enhanced dissolution and stability of artemisinin by nano-confinement in ordered mesoporous SBA-15 particles

Letchmanan

Shen

et al. 2015

Journal of Microencapsulation

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Dissolution of poorly water-soluble drug, Artemisinin (ART), was enhanced by encapsulating the drug particles inside pore channels of ordered mesoporous silica, SBA-15, via co-spray drying. The drug release profiles of ART were investigated by using flow-through cell (USP IV) and in vitro dissolution tester (USP II). The co-spray-dried ART/SBA-15 samples demonstrated significantly improved dissolution rates and supersaturation compared to the untreated ART. The low cytotoxicity effect of ART and SBA-15 on Caco-2 cells after 24 h incubation demonstrated the biocompatibility of ART/SBA-15. Finally, the storage stability of the samples was investigated for 6 months under five different storage conditions. Overall, the solid dispersions exhibited excellent physical stability; however, their chemical stability was affected by humidity regardless of storage temperatures. The formulation of solid dispersions of ART/SBA-15 is potentially safe and an effective approach to enhance the solubility of poorly water-soluble ART.

show abstract

Complex Effects of Drug/Silicate Ratio, Solid-State Equivalent pH, and Moisture on Chemical Stability of Amorphous Quinapril Hydrochloride Coground with Silicates

Cited by 12 publications

References 28 publications

Application of Mesoporous Silicon Dioxide and Silicate in Oral Amorphous Drug Delivery Systems

Application of Mesoporous Silicon Dioxide and Silicate in Oral Amorphous Drug Delivery Systems

Preformulation Studies on Solid Self-Emulsifying Systems in Powder Form Containing Magnesium Aluminometasilicate as Porous Carrier

Enhanced dissolution and stability of artemisinin by nano-confinement in ordered mesoporous SBA-15 particles

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