Prilling of API/fatty acid suspensions: processability and characterisation

E. De Coninck; V. Vanhoorne; A. Elmahdy; M. Boone; G. Van Assche; D. Markl; B. G. De Geest; T. De Beer; C. Vervaet

doi:10.1016/j.ijpharm.2019.118756

Prilling of API/fatty acid suspensions: processability and characterisation

E. De Coninck, V. Vanhoorne, A. Elmahdy, M. Boone, G. Van Assche, D. Markl, B. G. De Geest, T. De Beer, C. Vervaet^*

^*Corresponding author for this work

Strathclyde Institute Of Pharmacy And Biomedical Sciences

Research output: Contribution to journal › Article › peer-review

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Abstract

Current study evaluated the processability and characteristics of prills made of an active pharmaceutical ingredient/fatty acid (API/FA) suspension instead of previously studied API/FA solutions to enlarge the application field of prilling. Metformin hydrochloride (MET) and paracetamol (PAR) were used as model APIs while both the effect of drug load (10–40%) and FA chain length (C14–C22) were evaluated. API/FA suspensions were processable on lab-scale prilling equipment without thermal degradation, nozzle obstruction or sedimentation in function of processing time. The collected prills were spherical (AR ≥ 0.898) with a smooth surface (sphericity ≥ 0.914) and a particle size of ±2.3 mm and 2.4 mm for MET and PAR prills, respectively, independent of drug load and/or FA chain length. In vitro drug release evaluation revealed a faster drug release at higher drug load, higher API water solubility and shorter FA chain length. Solid state characterisation via XRD and Raman spectroscopy showed that API and FA crystallinity was maintained after thermal processing via prilling and during storage. Evaluation of the similarity factor indicated a stable drug release (f₂ > 50) from MET and PAR prills after 6 months storage at 25 °C or 40 °C.

Original language	English
Article number	118756
Journal	International Journal of Pharmaceutics
Volume	572
Early online date	21 Oct 2019
DOIs	https://doi.org/10.1016/j.ijpharm.2019.118756
Publication status	Published - 15 Dec 2019

Keywords

controlled release
fatty acids
Metformin hydrochloride
multiparticulate dosage forms
paracetamol
prilling

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10.1016/j.ijpharm.2019.118756

De-Coninck-etal-IJP-2019-Prilling-of-API-fatty-acid-suspensions-processability-and-characterisationAccepted author manuscript, 1.15 MBLicence: CC BY-NC-ND 4.0

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title = "Prilling of API/fatty acid suspensions: processability and characterisation",

abstract = "Current study evaluated the processability and characteristics of prills made of an active pharmaceutical ingredient/fatty acid (API/FA) suspension instead of previously studied API/FA solutions to enlarge the application field of prilling. Metformin hydrochloride (MET) and paracetamol (PAR) were used as model APIs while both the effect of drug load (10–40%) and FA chain length (C14–C22) were evaluated. API/FA suspensions were processable on lab-scale prilling equipment without thermal degradation, nozzle obstruction or sedimentation in function of processing time. The collected prills were spherical (AR ≥ 0.898) with a smooth surface (sphericity ≥ 0.914) and a particle size of ±2.3 mm and 2.4 mm for MET and PAR prills, respectively, independent of drug load and/or FA chain length. In vitro drug release evaluation revealed a faster drug release at higher drug load, higher API water solubility and shorter FA chain length. Solid state characterisation via XRD and Raman spectroscopy showed that API and FA crystallinity was maintained after thermal processing via prilling and during storage. Evaluation of the similarity factor indicated a stable drug release (f2 > 50) from MET and PAR prills after 6 months storage at 25 °C or 40 °C.",

keywords = "controlled release, fatty acids, Metformin hydrochloride, multiparticulate dosage forms, paracetamol, prilling",

author = "{De Coninck}, E. and V. Vanhoorne and A. Elmahdy and M. Boone and {Van Assche}, G. and D. Markl and {De Geest}, {B. G.} and {De Beer}, T. and C. Vervaet",

year = "2019",

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doi = "10.1016/j.ijpharm.2019.118756",

language = "English",

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TY - JOUR

T1 - Prilling of API/fatty acid suspensions

T2 - processability and characterisation

AU - De Coninck, E.

AU - Vanhoorne, V.

AU - Elmahdy, A.

AU - Boone, M.

AU - Van Assche, G.

AU - Markl, D.

AU - De Geest, B. G.

AU - De Beer, T.

AU - Vervaet, C.

PY - 2019/12/15

Y1 - 2019/12/15

N2 - Current study evaluated the processability and characteristics of prills made of an active pharmaceutical ingredient/fatty acid (API/FA) suspension instead of previously studied API/FA solutions to enlarge the application field of prilling. Metformin hydrochloride (MET) and paracetamol (PAR) were used as model APIs while both the effect of drug load (10–40%) and FA chain length (C14–C22) were evaluated. API/FA suspensions were processable on lab-scale prilling equipment without thermal degradation, nozzle obstruction or sedimentation in function of processing time. The collected prills were spherical (AR ≥ 0.898) with a smooth surface (sphericity ≥ 0.914) and a particle size of ±2.3 mm and 2.4 mm for MET and PAR prills, respectively, independent of drug load and/or FA chain length. In vitro drug release evaluation revealed a faster drug release at higher drug load, higher API water solubility and shorter FA chain length. Solid state characterisation via XRD and Raman spectroscopy showed that API and FA crystallinity was maintained after thermal processing via prilling and during storage. Evaluation of the similarity factor indicated a stable drug release (f2 > 50) from MET and PAR prills after 6 months storage at 25 °C or 40 °C.

AB - Current study evaluated the processability and characteristics of prills made of an active pharmaceutical ingredient/fatty acid (API/FA) suspension instead of previously studied API/FA solutions to enlarge the application field of prilling. Metformin hydrochloride (MET) and paracetamol (PAR) were used as model APIs while both the effect of drug load (10–40%) and FA chain length (C14–C22) were evaluated. API/FA suspensions were processable on lab-scale prilling equipment without thermal degradation, nozzle obstruction or sedimentation in function of processing time. The collected prills were spherical (AR ≥ 0.898) with a smooth surface (sphericity ≥ 0.914) and a particle size of ±2.3 mm and 2.4 mm for MET and PAR prills, respectively, independent of drug load and/or FA chain length. In vitro drug release evaluation revealed a faster drug release at higher drug load, higher API water solubility and shorter FA chain length. Solid state characterisation via XRD and Raman spectroscopy showed that API and FA crystallinity was maintained after thermal processing via prilling and during storage. Evaluation of the similarity factor indicated a stable drug release (f2 > 50) from MET and PAR prills after 6 months storage at 25 °C or 40 °C.

KW - controlled release

KW - fatty acids

KW - Metformin hydrochloride

KW - multiparticulate dosage forms

KW - paracetamol

KW - prilling

UR - https://www.sciencedirect.com/journal/international-journal-of-pharmaceutics

U2 - 10.1016/j.ijpharm.2019.118756

DO - 10.1016/j.ijpharm.2019.118756

M3 - Article

C2 - 31648017

AN - SCOPUS:85074768108

SN - 0378-5173

VL - 572

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

M1 - 118756

ER -

Prilling of API/fatty acid suspensions: processability and characterisation

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