Physical and chemical changes of medicinals in mixtures with adsorbents in the solid state. I. Effect of vapor pressure of the medicinals on changes in crystalline properties.

Konno, Tsutomu; Kinuno, Koji; Kataoka, Katsuo

doi:10.1248/cpb.34.301

Cited by 43 publications

(42 citation statements)

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“…A possible explanation for this phenomenon suggests that as the total surface area of Neusilin® US 2 increased, prednisone slices adhered and settled onto the surface of Neusilin® US 2 granules, thus inhibiting the reversion back to the ordered shape in the crystalline structure (15). It is worth noting that previous reports in the literature suggested that mixing Neusilin with volatile crystalline organic compounds may transform such compounds from crystalline state into amorphous state (24).…”

Section: Differential Scanning Calorimetry Studiesmentioning

confidence: 98%

Development of a Mini-Tablet of Co-Grinded Prednisone–Neusilin Complex for Pediatric Use

et al. 2013

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Abstract. The purpose of this study is to enhance the dissolution rate of prednisone by co-grinding with Neusilin to form a complex that can be incorporated into a mini-tablet formulation for pediatrics. Prednisone-Neusilin complex was co-grinded at various ratios (1:1, 1:3, 1:5, and 1:7). The physicochemical properties of the complex were characterized by various analytical techniques including: differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), scanning electron microscope (SEM), particle size, surface area, solubility, and dissolution rate. The co-grinded prednisone-Neusilin complex (1:7) was blended with other excipients and was formulated into a 2-mm diameter mini-tablet. The minitablets were further evaluated for thickness, weight, content uniformity, and dissolution rate. To improve taste masking and stability, mini-tablets were coated by dip coating with Eudragit® EPO solution. DSC and XRPD results showed that prednisone was transformed from crystalline state into amorphous state after co-grinding with Neusilin. Particle size, surface area, and SEM results confirmed that prednisone was adsorbed to Neusilin's surface. Co-grinded prednisone-Neusilin complex (1:7) had a solubility of 0.24 mg/ mL and 90% dissolved within 20 min as compared to crystalline prednisone which had a solubility of 0.117 mg/mL and 30% dissolved within 20 min. The mini-tablets containing co-grinded prednisoneNeusilin complex (1:7) exhibited acceptable physicochemical and mechanical properties including dissolution rate enhancement. These mini-tablets were successfully dip coated in Eudragit® EPO solution to mask the taste of the drug during swallowing. This work illustrates the potential use of co-grinded prednisone-Neusilin to enhance solubility and dissolution rate as well as incorporation into a mini-tablet formulation for pediatric use.

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Section: Differential Scanning Calorimetry Studiesmentioning

confidence: 98%

Development of a Mini-Tablet of Co-Grinded Prednisone–Neusilin Complex for Pediatric Use

et al. 2013

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“…Activated carbon, porous crystalline cellulose, and zeolites are examples of porous materials that have been used widely for pharmaceuticals. [9][10][11] Folded sheets mesoporous material (FSM-16) has been synthesized by an intercalation of quaternary ammonium surfactant as a template in a layered polysilicate kanemite, followed by calcination.12-16) FSM-16 is composed of hexagonal channels and has extremely large specific surface area and large pore volume. Due to its highly uniform porous structure with hexagonal arrays, FSM-16 is widely used as a reactor for catalytic reaction, as an adsorbent and as a host for the inclusion of large molecules.…”

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confidence: 99%

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confidence: 99%

Effect of Pore Size of FSM-16 on the Entrapment of Flurbiprofen in Mesoporous Structures

Tozuka

Wongmekiat

Kimura

et al. 2005

CHEMICAL & PHARMACEUTICAL BULLETIN

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The improvement of bioavailability of poorly water-soluble drugs is important for oral administration. Amorphization is one of the techniques that has been commonly used for solubility enhancement.1,2) Amorphous material of drug can be obtained by several methods, e.g., spray-drying, 3) solid dispersion, 4) co-grinding with cyclodextrins 5) or crystalline cellulose, 6) and mixing with porous materials. 7,8) Porous materials have a unique capacity to adsorb organic compounds due to their large specific surface area and porous structure. Activated carbon, porous crystalline cellulose, and zeolites are examples of porous materials that have been used widely for pharmaceuticals. [9][10][11] Folded sheets mesoporous material (FSM-16) has been synthesized by an intercalation of quaternary ammonium surfactant as a template in a layered polysilicate kanemite, followed by calcination.12-16) FSM-16 is composed of hexagonal channels and has extremely large specific surface area and large pore volume. Due to its highly uniform porous structure with hexagonal arrays, FSM-16 is widely used as a reactor for catalytic reaction, as an adsorbent and as a host for the inclusion of large molecules. 17,18) Itoh et al. 19) studied the photostability of chlorophyll a after adsorption into FSM-16. The enhancement of the photostability was attributable to the interactions between chlorophyll and FSM-16 to form chlorophyll-FSM conjugate, and also between two chlorophyll molecules to form a chlorophyll dimer within the pores of FSM-16.In the previous paper, we investigated the use of FSM-16 for pharmaceutical applications. We reported the change in molecular state of salicylamide from crystal to amorphous by adsorption into the FSM-16 channels during sealed-heating process. The amorphization of the drug accordingly resulted in enhanced dissolution of sealed-heated sample. 20) In the present study, three kinds of FSM-16 with different pore diameters [FSM-16(Oc), FSM-16(Do) and FSM-16(Doc)] were employed to investigate the molecular state of the drug and its interaction with FSM-16. Flurbiprofen (FBP), a poorly water-soluble non-steroidal anti-inflammatory drug, was used as a model compound. Changes in the molecular state of FBP were investigated using powder X-ray diffractometry, thermal analysis and FT-IR spectroscopy. The changes in pore diameter and specific surface area of samples prepared by various methods were investigated using small angle X-ray scattering and nitrogen gas adsorption BET method for understanding the effect of adsorption of FBP molecules on pore structure of FSM-16. ExperimentalMaterials Flurbiporfen (FBP) of reagent grade was kindly supplied by Kaken Pharmaceutical, Co. Ltd., Japan, and was used without further purification. Three kinds of mesoporous silica FSM-16, i.e., FSM-16(Oc), FSM-16(Do) and FSM-16(Doc), were kindly supplied by Toyota Central R&D Labs., Inc., Japan. Mean pore width and specific surface area of FSM-16(Oc), FSM-16(Do), FSM-16(Doc) were 16.0, 21.6, 45.0 Å and 700, 1250, 1040 m 2 /g, respectively...

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“…Recently, more and more novel production methods have been developed to control the size distribution and porous structure of final products. Drug molecules can be incorporated into mesoporous materials using various techniques, including, solvent deposition (Hu et al 2011), vapor-phase mediated mass transfer (Konno et al 1986), and mechanical activation (Limnell et al 2011). Mesoporous materials are known to stabilize amorphous drugs via several mechanisms.…”

Section: Mesoporous Silica-and Silicon-based Systemmentioning

confidence: 99%

Excipients That Facilitate Amorphous Drug Stabilization

Wei

Dattachowdhury

Vangara

et al. 2015

Excipient Applications in Formulation Design and Drug Delivery

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The importance of the amorphous state in studying bioavailability of poorly water-soluble drugs cannot be over-emphasized. The higher free energy and therefore the apparent high solubility of the amorphous phase are some of the advantages for promoting the amorphous phase, as compared to its crystalline counterpart. It is well known that the amorphous phase is thermodynamically unstable. This might result in the conversion of the metastable form to its stable crystalline form during storage. This conversion might also lead to product failure during storage owing to the poor dissolution properties of the crystalline form. Excipients can play a key role in preventing such a transformation during storage as well as maximizing the therapeutic efficacy of the amorphous material. This book chapter intends to highlight the delivery issues pertaining to amorphous drugs with a special emphasis on the most commonly used excipients in stabilizing amorphous drug substances in formulations.

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Physical and chemical changes of medicinals in mixtures with adsorbents in the solid state. I. Effect of vapor pressure of the medicinals on changes in crystalline properties.

Cited by 43 publications

References 0 publications

Development of a Mini-Tablet of Co-Grinded Prednisone–Neusilin Complex for Pediatric Use

Development of a Mini-Tablet of Co-Grinded Prednisone–Neusilin Complex for Pediatric Use

Effect of Pore Size of FSM-16 on the Entrapment of Flurbiprofen in Mesoporous Structures

Excipients That Facilitate Amorphous Drug Stabilization

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