Preparation and evaluation of enteric-coated delayed-release pellets of duloxetine hydrochloride using a fluidized bed coater

Kim, Yong‐Il; Pradhan, Roshan; Paudel, Bijay K.; Choi, Jae Young; Im, Ho Taek; Kim, Jong Oh

doi:10.1007/s12272-015-0590-y

Cited by 8 publications

(5 citation statements)

References 28 publications

(26 reference statements)

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“…Bulk density was measured with 50 g of pellets, which were ( M ) weighed, placed in a 100 mL graduated glass cylinder and then dropped from 5 cm away from the table. 24 The occupied volume ( V ) by the pellets was read precisely, and the bulk density (d) was obtained with the formula d = M / V . Three batches of pellets were measured in parallel.…”

Section: Methodsmentioning

confidence: 99%

Orally Deliverable Dual-Targeted Pellets for the Synergistic Treatment of Ulcerative Colitis

Tang

Yang

et al. 2021

DDDT

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Purpose The effective treatment of ulcerative colitis (UC) poses substantial challenges, and the aetiopathogenesis of UC is closely related to infectious, immunological and environmental factors. Currently, there is a considerable need for the development of orally bioavailable dosage forms that enable the effective delivery of therapeutic drugs to local diseased lesions in the gastrointestinal tract. Methods Berberine (BBR) and Atractylodes macrocephala Koidz (AM) volatile oil, derived from the Chinese herbs Coptis chinensis Franch and Atractylodes macrocephala Koidz, have anti-inflammatory and immunomodulatory activities. In this study, we prepared colon-targeted pellets loaded with BBR and stomach-targeted pellets loaded with AM volatile oil for the synergistic treatment of UC. The Box–Behnken design and β-cyclodextrin inclusion technique were used to optimize the enteric coating formula and prepare volatile oil inclusion compounds. Results The two types of pellets were spherical and had satisfactory physical properties. The pharmacokinetic results showed that the AUC and MRT values of the dual-targeted (DPs) pellets were higher than those of the control pellets. In addition, in vivo animal imaging confirmed that the DPs could effectively deliver BBR to the colon. Moreover, compared with sulfasalazine and monotherapy, DPs exerted a more significant anti-inflammatory effect by inhibiting the expression of inflammatory factors including IL-1β, IL-4, IL-6, TNF-α and MPO both in serum and tissues and enhancing immunity by decreasing the production of IgA and IgG. Conclusion The DPs play a synergistic anti-UC effect by exerting systemic and local anti-inflammatory and provide an effective oral targeted preparation for the treatment of UC.

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Section: Methodsmentioning

confidence: 99%

Orally Deliverable Dual-Targeted Pellets for the Synergistic Treatment of Ulcerative Colitis

Tang

Yang

et al. 2021

DDDT

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“…There are different methods for the fabrication of MOPs, including freeze‐drying (Stange, Fuhrling, & Gieseler, ), centrifugal granulation (Peng et al, ), extrusion spheronization (Zoubari, Ali, & Dashevskiy, ), and fluidized bed granulation (Kim et al, ). However, freeze‐drying requires the use of organic solvents and is still far from industrialization (Alshetaili et al, ).…”

Section: Introductionmentioning

confidence: 99%

“…There are different methods for the fabrication of MOPs, including freeze-drying (Stange, Fuhrling, & Gieseler, 2013), centrifugal granulation (Peng et al, 2015), extrusion spheronization (Zoubari, Ali, & Dashevskiy, 2019), and fluidized bed granulation (Kim et al, 2015).…”

mentioning

confidence: 99%

Modified‐release oral pellets for duodenum delivery of doxycycline hyclate

Huang

et al. 2019

Drug Development Research

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To minimize the gastric and esophageal injury effect, a system to deliver doxycycline hyclate (DOXY) to the duodenum area is needed. DOXY‐containing modified‐release oral pellets (DMOP) coated with hydroxypropyl methylcellulose phthalate HP‐55 (HPMCP HP‐55) and hydroxypropyl methylcellulose E15 (HPMC E15) appear to be a reasonable choice. This coating layer dissolves at pH 5.5, which is the pH of the duodenum, but not at a gastric pH (1.2). The formulation and preparation of DMOP were optimized, and a scale‐up test was performed. The results showed that the production reproducibility was acceptable, and the quality of DMOP well met the standards of Chinese Pharmacopeia (Ch.P, 2015 edition). Notably, the accumulated DOXY release was lower than 50% at pH 1.2 (20 min) and higher than 85% at pH 5.5, which met the USP40‐NF35 standard for DOXY modified‐release formulations. Moreover, the storage stability of DMOP with different packages was investigated by stress testing, accelerated and long‐term testings. The stability of DMOP was maintained up to 12 months, in terms of DOXY content and in vitro release behavior. The results seem to suggest that DMOP could be a promising duodenum delivery system.

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“…Many pharmacokinetic parameters of prime signicance such as volume of distribution, mean residence time, clearance and bioavailability can be estimated using statistical moment analysis without the complicated nonlinear regression approach of compartmental analysis. [27][28][29] Previously, numerous explorations were conceded to characterize corneal permeability mechanism and predicted drug delivery rates to the eye. 30,31 Previously several models have been examined to explain drug transport kinetics 32,33 and many investigators have characterized in vitro and in vivo correlation employing statistical moment analysis.…”

Section: Introductionmentioning

confidence: 99%