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Dissolution Tablet Shape

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Impact of Tablet Geometry

on Dissolution Profiles

Pearl Pereira Nambiar


Jan 2023
Influence of tablet shape and size on drug release

Dose proportional formulations of multiple strengths differentiated by size or


shape, are expected to have comparable dissolution profiles.
Studies have shown Tablet geometry plays a key role in the drug release behavior
of tablets.
For immediate release tablets, study findings indicated the drug burst release
was significantly decreased by decreasing the size of tablets.
Studies have also shown the influence of tablet geometry on controlled release
formulations.
Pearl Pereira Nambiar Jan 2023
Influence of tablet shape and size on drug release

Surface area/volume (SA/V) is one of the key variables in controlling drug release
from controlled-release matrix tablets containing hydrophilic polymers like
hydroxypropyl methylcellulose (HPMC) and carbomer.
Tablets with larger SA/V typically had faster release profiles, regardless of the
dose or shape.
Studies on controlled release formulations have shown that it is always essential to
keep the SA/V constant to get constant drug release profiles in different strengths.

Pearl Pereira Nambiar Jan 2023


Case study 1: Domperidone tablets of different shapes

Pharm Bull. 2020 Sep;10(4):656-661. doi: 10.34172/apb.2020.079. Epub 2020 Aug 9. PMID: 33072542; PMCID: PMC7539314.
Molavi F, Hamishehkar H, Nokhodchi A. Impact of Tablet Shape on Drug Dissolution Rate Through Immediate Released Tablets. Adv
Figure 1: Domperidone tablets of different shapes (a) Round
#6 flat (b) Round #6 biconvex (c) Round #9 flat (d) Round #9
biconvex (e) Round #11 flat (f) Oblong #12 biconvex

Study findings: Drug burst release, critical to the


successful therapeutic performance of anti-vomiting
dosage forms like Domperidone, is significantly affected by
being flat or biconvex in larger tablets; initial drug burst Figure 2: Dissolution profiles for Domperidone tablets of
release is reduced with the decrease in tablet size. different shapes and sizes
Pearl Pereira Nambiar Jan 2023
Case study 2: Theophylline tablets of different shapes

https://doi.org/10.1016/S0014-827X(02)01297-1.
estimating drug release, Il Farmaco, Volume 57, Issue 11,2002, Pages 939-945, ISSN 0014-827X,
H.Yeşim Karasulu, Gökhan Ertan, Different geometric shaped hydrogel theophylline tablets: statistical approach for
Figure 3: Theophylline tablets of different shapes-
triangular, cylindrical and half-spherical hydrogel
matrix tablets

Study findings: The release rate of the theophylline


prepared in the different shapes but possessing the Figure 4: Dissolution profiles for Theophylline hydrogel
same formulation depends on the geometric shape
matrix tablets of different shapes and drug to polymer ratio
of the tablets.
Pearl Pereira Nambiar Jan 2023
Case study 3: Guaifenesin tablets of multiple strengths
and different SA/V ratio

Tablets, Lubrizol Advanced Materials, Inc., Cleveland, OH


E. Draganoiu, A. Stansbrey, H. Luo, Effect of Tablet Surface Area/Volume on Drug Release From Carbomer Matrix
Figure 5: Drug release for guaifenesin tablets of same Figure 6: Drug release for guaifenesin tablets of multiple
strength but different SA/V ratio and shape (R: round, C: strengths and different SA/V ratio and shape (R: round, C:
Capsule) Capsule)
Study findings: Carbomer based tablets with larger surface area/volume (SA/V) typically have faster release profiles,
regardless of the dose or shape
Pearl Pereira Nambiar Jan 2023
Case study 4: 3D printed tablets of different shapes
containing Pramipexole, Levodopa and Praziquantel

pharmaceutics13091453
Surface Area to Volume Ratio of Tablet Geometry. Pharmaceutics 2021, 13, 1453. https://doi.org/10.3390/
PWindolf, H.; Chamberlain, R.; Quodbach, J. Predicting Drug Release from 3D Printed Oral Medicines Based on the
Figure 7: Designed geometries (from left to right): cube 1 (Q1), cube 2
(Q2), cube 3 (Q3), hollow cylinder (HC), cylinder (C) and pyramid (P).

Study findings:
 Despite the different behaviour of the matrix systems, the solubility properties of the APIs and the resulting
differences in Mean dissolution time (MDT), a correlation of the SA/V ratio and the MDT can be established for
all three tested formulations containing Pramipexole, Levodopa (both BCS I) and Praziquantel (BCS II)

 With the help of this correlation, the release time of an existing geometry with a given SA/V ratio can be
predicted without having to waste material and perform dissolution tests.

 Similarly, the required SA/V ratio can be predicted for a desired MDT and the corresponding geometry can be
designed and printed on this basis.

Pearl Pereira Nambiar Jan 2023


Disclaimer
The contents of this post are for informational purposes only. Any opinions
expressed are solely my own and do not express the views or opinions of my
employer.

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