Inhibiting the Gastric Burst Release of Drugs from Enteric Microparticles: The Influence of Drug Molecular Mass and Solubility

Alhnan, Mohamed Albed; Cosi, Daniele; Murdan, Sudaxshina; Basit, Abdul W.

doi:10.1002/jps.22174

Cited by 22 publications

(13 citation statements)

References 16 publications

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“…This study was designed to decrease the irritation and to protect the drug in the acidic environment. To prepare CLA-loaded microspheres, the O/O (oil in oil) emulsion solvent evaporation technique was used according to early reports (Alhnan et al 2010;Mundargi et al 2011). Liquid paraffin was used as the dispersion medium or external phase because of the insolubility of CLA and Eudragit Ò L100 in liquid paraffin.…”

Section: Formulation Of Microspheresmentioning

confidence: 99%

Preparation, characterization and pharmacokinetics evaluation of clarithromycin-loaded Eudragit® L-100 microspheres

Liu

et al. 2015

Eur J Drug Metab Pharmacokinet

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The aim of this work was to prepare pH-dependent clarithromycin microsphere formulation by emulsion solvent evaporation method, employing Eudragit(®) L-100. Prepared microspheres were evaluated by carrying out in vitro release and in vivo pharmacokinetics studies. Drug-polymer interactions were studied by differential scanning calorimetry, X-ray diffractometry analyses and results showed that clarithromycin was molecularly dispersed in the polymer. The particle size distribution of microspheres was found over the range of 10~50 μm. The drug is hardly released in the HCl solution pH 1.2 in the first 2 h, but is rapidly released in phosphate buffer pH 7.2, and the cumulated release reached 98.1 % at 8 h. The pharmacokinetic profiles were conducted open, randomized, two-period crossover design with a 7-day interval between doses in healthy beagle dogs. The results indicated that the extent of absorption of the clarithromycin-load microspheres was the same as pure drug, but different in the rate of drug absorption in vivo.

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Section: Formulation Of Microspheresmentioning

confidence: 99%

Preparation, characterization and pharmacokinetics evaluation of clarithromycin-loaded Eudragit® L-100 microspheres

Liu

et al. 2015

Eur J Drug Metab Pharmacokinet

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“…Dual FDM 3D printer was employed with two different filaments; i) filament for enteric shell (Eudragit L100-55), and ii) filament for the core (API, PVP) processed through an HME compounder. Theophylline was used as a model drug to develop the enteric core structure due to its high solubility in acidic medium and small molecular weight, rendering it a major challenge for an enteric system(29).Unlike single FDM 3D printing of theophylline(18), frequent blocking of PVP filament (core) was encountered in dual FDM 3D printing. It is possible that whilst the first nozzle is printing, the filament in the second head remains at elevated temperature leading to material adherence to the inner wall of the nozzle head.…”

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confidence: 99%

Fabricating a Shell-Core Delayed Release Tablet Using Dual FDM 3D Printing for Patient-Centred Therapy

et al. 2016

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“…9A), and complied with USP criteria for oral dipyridamole products. (Convention, 2007) This might be attributed to rapid ionization of cationic chains of the methacrylate polymer in gastric medium as well as high solubility of dipyridamole in this medium (Alhnan et al, 2010;Paprskarova et al, 2016).…”

Section: Resultsmentioning

confidence: 99%

On demand manufacturing of patient-specific liquid capsules via co-ordinated 3D printing and liquid dispensing

Okwuosa

Soares

Gollwitzer

et al. 2018

European Journal of Pharmaceutical Sciences

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114

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A method for the production of liquid capsules with the potential of modifying drug dose and release is presented. For the first time, the co-ordinated use of fused deposition modelling (FDM), 3D printing and liquid dispensing to fabricate individualised dosage form on demand in a fully automated fashion has been demonstrated. Polymethacrylate shells (Eudragit EPO and RL) for immediate and extended release were fabricated using FDM 3D printing and simultaneously filled using a computer-controlled liquid dispenser loaded with model drug solution (theophylline) or suspension (dipyridamole). The impact of printing modes: simultaneous shell printing and filling (single-phase) or sequential 3D printing of shell bottom, filling and shell cap (multi-phase), nozzle size, syringe volume, and shell structure has been reported. The use of shell thickness of 1.6 mm, and concentric architecture allowed successful containment of liquid core whilst maintaining the release properties of the 3D printed liquid capsule. The linear relationship between the theoretical and the actual volumes from the dispenser reflected its potential for accurate dosing (R = 0.9985). Modifying the shell thickness of Eudragit RL capsule allowed a controlled extended drug release without the need for formulation change. Owing to its low cost and versatility, this approach can be adapted to wide spectrum of liquid formulations such as small and large molecule solutions and obviate the need for compatibility with the high temperature of FDM 3D printing process. In a clinical setting, health care staff will be able to instantly manufacture in small volumes liquid capsules with individualised dose contents and release pattern in response to specific patient's needs.

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Inhibiting the Gastric Burst Release of Drugs from Enteric Microparticles: The Influence of Drug Molecular Mass and Solubility

Cited by 22 publications

References 16 publications

Preparation, characterization and pharmacokinetics evaluation of clarithromycin-loaded Eudragit® L-100 microspheres

Preparation, characterization and pharmacokinetics evaluation of clarithromycin-loaded Eudragit® L-100 microspheres

Fabricating a Shell-Core Delayed Release Tablet Using Dual FDM 3D Printing for Patient-Centred Therapy

On demand manufacturing of patient-specific liquid capsules via co-ordinated 3D printing and liquid dispensing

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