The mechanochemical preparation of solid disperse systems of ibuprofen-polyethylene glycol

Шахтшнейдер, Т. П.; Vasiltchenko, M.A.; Politov, A. A.; Болдырев, В. В.

doi:10.1016/0378-5173(95)04244-x

Cited by 47 publications

(22 citation statements)

References 8 publications

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“…5. Several studies have reported eutectic systems formed between ibuprofen and carriers, typically with ibuprofen contents between 30 and 35% (Shakhtshneider et al, 1996;Passerini et al, 2002;Newa et al, 2007Newa et al, , 2008Ho et al, 2008), which are consistent with the results obtained in this study.…”

Section: Resultssupporting

confidence: 95%

“…Although ibuprofen exists as a dimer in both solid and liquid states, drug:carrier hydrogen bond formation has been investigated in several studies. Ibuprofen and, to a lesser extent, ketoprofen have both been used as model compounds in solid dispersions with a range of carriers including polyethylene glycols (Shakhtshneider et al, 1996;Khan and Jiabi, 1998) and polyvinylpyrrolidone (Lu et al, 2005;Xu et al, 2007). Typically the focus of these studies is on the production of amorphous or microcrystalline dispersions and consequent improvements in dissolution rate.…”

Section: Introductionmentioning

confidence: 98%

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Stochiometrically governed molecular interactions in drug: Poloxamer solid dispersions

Ali

Williams

Rawlinson

2010

International Journal of Pharmaceutics

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This study probes the molecular interactions between model drugs and poloxamers that facilitate dissolution rate improvements using solid dispersions. Ibuprofen and ketoprofen solid dispersions were prepared at different mole ratios using poloxamers 407 and 188. The carbonyl stretching vibration of the ibuprofen dimer shifted to higher wavenumber in the infrared spectra of 2:1 drug:carrier mole ratio solid dispersions, indicating disruption of the ibuprofen dimer concomitant with hydrogen bond formation between the drug and carrier. Solid dispersions with mole ratios >2:1 drug:carrier (up to 29:1) showed both ibuprofen hydrogen-bonded to the poloxamer, and excess drug present as dimers. X-ray diffraction studies confirmed these findings with no evidence of crystalline drug in 2:1 mole ratio systems whereas higher drug loadings retained crystalline ibuprofen. Similar results were found with ketoprofen-poloxamer solid dispersions. Thermal analysis of ibuprofen-poloxamer 407 solid dispersions and their resultant phase diagram suggested solid solutions and a eutectic system were formed, depending on drug loading. Dissolution studies showed fastest release from the solid solutions; dissolution rates from solid solutions were 12-fold greater than the dissolution of ibuprofen powder whereas the eutectic system gave a 6-fold improvement over the powder. When designing solid dispersions to improve the delivery of poorly-water soluble drugs, the nature of drug:carrier interactions, which are governed by the stochiometry of the composition, can affect the dissolution rate improvement.

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Section: Resultssupporting

confidence: 95%

Section: Introductionmentioning

confidence: 98%

Stochiometrically governed molecular interactions in drug: Poloxamer solid dispersions

Ali

Williams

Rawlinson

2010

International Journal of Pharmaceutics

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“…Amobarbital amorphized in the presence of a variety of excipients such as carbon black, ethyl cellulose, precipitated silica and activated charcoal (72). A variety of other excipients such as b-cyclodextrin, dextrans, chitin, chitosan, gelatin, polyethylene glycol, methyl cellulose, hydroxyl propyl cellulose, calcium silicate and silicon dioxide were used to amorpize structurally diverse drugs, resulting in various degrees of amorphization (67)(68)(69)(70)(71)(72)(73)(74)(75)(76)(77). More recently, Bahl et al (78) have shown that increasing the amount of Neusilin US2 with respect to indomethacin reduced the amorphization time (Fig.…”

Section: Solid State Amorphizationmentioning

confidence: 99%

Methods of amorphization and investigation of the amorphous state

Einfalt¹,

Planinšek²,

Hrovat³

2013

Acta Pharmaceutica

117

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.g., polymorphs) provides pharmaceutical scientists with an opportunity to select the preferred form of the material to be used in a formulation. This is very useful since critical properties, such as particle morphology and dissolution properties, are frequently different in the different physical forms of a material. The amorphous form of pharmacologically active materials has received considerable attention because, in theory, it represents the most energetic solid state of a material, and should thus provide the biggest advantages in terms of dissolution rate and bioavailability (1). However, the amorphous form also shows various disadvantages, such as lower physical stability compared to crystals.The structure of an amorphous solid is usually described as possessing a crystal--like short-range molecular arrangement, but lacking a long-range order. As illustrated by Fig. 1, the immediate environment of a molecule (m) in an amorphous solid may not differ significantly from that in a crystal (e.g., similar number of and distance to nearest neighbors), but an amorphous solid lacks any long-range transational-orientational symmetry that characterizes a crystal (1). However, this is only true when we are dealing The amorphous form of pharmaceutical materials represents the most energetic solid state of a material. It provides advantages in terms of dissolution rate and bioavailability. This review presents the methods of solid--state amorphization described in literature (supercooling of liquids, milling, lyophilization, spray drying, dehydration of crystalline hydrates), with the emphasis on milling. Furthermore, we describe how amorphous state of pharmaceuticals differ depending on the method of preparation and how these differences can be screened by a variety of spectroscopic (X-ray powder diffraction, solid state nuclear magnetic resonance, atomic pairwise distribution, infrared spectroscopy, terahertz spectroscopy) and calorimetry methods.

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“…[1][2][3] Currently, various pharmaceutical approaches for the preparation of SDs, including coprecipitation, lyophilization, spray drying, solvent evaporation, fusion and cogrinding methods, have been reported. [4][5][6] However, most of these methods require a large amount of organic solvent to dissolve the drug and a water-soluble polymer. This causes environmental pollution and toxicity due to the residual solvent, 7) and furthermore, in the common fusion method, tacky or glassy solids may cause undesirable processing problems.…”

mentioning

confidence: 99%

Preparation and Evaluation of Solid Dispersions of Nitrendipine Prepared with Fine Silica Particles Using the Melt-Mixing Method

Wang

Cui

Sunada

2006

CHEMICAL & PHARMACEUTICAL BULLETIN

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Solid dispersions (SD) of nitrendipine (NTD), a poorly water-soluble drug, were prepared using the meltmixing method with hydrophilic silica particles (Aerosil and Sylysia) with different particle size and specific surface areas as carriers. Powder X-ray diffraction and differential scanning calorimetry evaluation showed that NTD in the SDs treated with the melt-mixing method was dispersed in the amorphous state. FT-IR spectroscopy obtained with the SDs indicated the presence of hydrogen bonding between the secondary amine groups of NTD and silanol groups of silica particles. The dissolution property of NTD in the SDs was remarkably improved regardless of the grade of silica. At the end of the dissolution test (60 min) the concentrations of NTD for the SDs with Aerosil 200 and Sylysia 350 were 8.88 and 10.09 m mg/ml, corresponding to 28 and 31 times that of the original NTD crystals, respectively. The specific surface area and the adsorbed water amount of the SDs were also significantly improved. The rapid dissolution rate from the SDs was attributed to the amorphization of drug, improved specific surface area and wettability than the original drug crystals. In the stability test, powder X-ray diffraction pattern indicated that amorphous NTD in the SD with Aerosil 200 was stable for at least 1 month under the humid conditions (40°C/75% RH).

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The mechanochemical preparation of solid disperse systems of ibuprofen-polyethylene glycol

Cited by 47 publications

References 8 publications

Stochiometrically governed molecular interactions in drug: Poloxamer solid dispersions

Stochiometrically governed molecular interactions in drug: Poloxamer solid dispersions

Methods of amorphization and investigation of the amorphous state

Preparation and Evaluation of Solid Dispersions of Nitrendipine Prepared with Fine Silica Particles Using the Melt-Mixing Method

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