Manufacture and Performance Evaluation of a Stable Amorphous Complex of an Acidic Drug Molecule and Neusilin

Maclean, Jenifer; Medina, César; Daurio, Dominick; Alvarez‐Núñez, Fernando; Jona, Janan; Munson, Eric J.; Nagapudi, Karthik

doi:10.1002/jps.22583

Cited by 39 publications

(26 citation statements)

References 30 publications

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“…Physical mixtures of crystalline compounds and a mesoporous material at suitable proportions were coground at room temperature. Amorphization was reported for several crystalline drugs such as ketoprofen,93 naproxen,93 progesterone,93 indomethacin,94 and sulindac 95…”

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

194

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

194

132

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“…3. Black square solubility of crystalline prednisone, red circle solubility of co-grinded 1:7 drug-Neusilin complex crystal form could be evaluated (14). Results of particle size and surface area measurements were listed in Table II.…”

Section: Surface Area and Particle Size Measurementsmentioning

confidence: 99%

“…In order to stabilize amorphous molecules during the storage and dissolution process, preparing solid dispersion is one approach and various polymers such as polyvinylpyrrolidone, polyethylene glycol, or cellulose derivatives have been widely used as dispersants (11,12). In contrast to organic polymers, Neusilin can also function as a carrier to keep drug in amorphous state (13,14). Neusilin® US 2 is a porous granule of amorphous magnesium aluminosilicate which retains a tremendous surface area (around 300 m 2 /g).…”

Section: Introductionmentioning

confidence: 99%

“…The surface of Neusilin contains a large amount of silanol functional groups which facilitate the formation of hydrogen bonds (15)(16)(17). After cogrinding a drug with Neusilin® US 2 , an amorphous drug-Neusilin complex is formed (13,14,18). One possible mechanism for the formation of amorphous complex is linked to the crystalline structure disruption which is caused by the force of mechanical shearing during milling then followed by the adherence of amorphous pieces into Nuesilin® US 2 surfaces by hydrogen bonds or salt bridge formation (15).…”

Section: Introductionmentioning

confidence: 99%

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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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“…Similar acid-base reactions have been reported in previous interaction studies. [24][25][26] In the case of N 1 SM 1 , prepared by freeze-drying after the wet-state equilibration of drug and SMCC in 1:1 ratio, the vibrations at 1727 cm −1 and 1685 cm −1 appeared slightly shifted and broadened and with decreased intensity when compared to that of the pure drug. In addition, the absence of the carboxylate peak in the spectra indicates partial amorphization of the drug and absence of any acid-base interaction.…”

Section: Physicochemical Analysismentioning

confidence: 97%

Interaction of naproxen with calcium carbonate: physicochemical characterization and in vitro drug release studies

Paroha¹,

Dubey²,

Mallick³

2014

Quím. Nova

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Interaction and physicochemical characterization of dispersions of naproxen in calcium carbonate after freeze-drying the wet-state equilibrated mixture have been investigated by analytical methods. The FT-IR study revealed the acid-base reaction between naproxen and calcium carbonate. The DSC study indicated physical interaction and significantly diminished crystallinity of naproxen in the formulation containing higher quantities of calcium carbonate. Furthermore, the SEM study showed the reduced particle size and loss of crystalline morphology in the same sample. Drug release increased with the increase of calcium carbonate in the formulations. Formulation of naproxen with calcium carbonate in 1:2 ratio allowed its dissolution to the greatest extent (94.96%) while other compositions, 1:0.5 and 1:1, showed 80.86% and 78.30% release, respectively.

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Manufacture and Performance Evaluation of a Stable Amorphous Complex of an Acidic Drug Molecule and Neusilin

Cited by 39 publications

References 30 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

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

Interaction of naproxen with calcium carbonate: physicochemical characterization and in vitro drug release studies

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