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16 Cocrystals in Pharmaceutical Sciences
Table 1.2 Some commercial pharmaceutical cocrystals. (Continued)
Commercial
name Approval API Coformer Improved property Indic ation Manufacturer References
Dimenhydrinate USFDA
1982
(ANDA)
Diphenhydramine 8-Chlorotheophylline Enhanced
solubility an d
pharmacokinetics
Motion sickness Watson Laboratories
Inc., New Jersey,
USA
[37, 118]
Mobic
®
USFDA
2000
Meloxicam Aspirin Enhanced solubility,
improved
bioavailabilit y,
stabilized the API,
and provided
synergistic
therapeutic eects
Osteoarthritis
and
rheumatoid
arthritis.
Boehringer
Ingelheim
Pharmaceuticals
[37]
Zafatek
®
Japan 2015 Trelagliptin Succinic acid Improved solubil ity Diabetes Takeda
Pharmaceutical
Company
Limited, Tokyo,
Japan
Ibrutinib Te ntative
approval
Ibrutinib Fumaric acid Improved stability Anticancer-
chronic
lymphocytic
leukemia
Teva Pharmaceutical
Industries Ltd.,
Tel Aviv-Yafo,
Israel
[59]
Pharmaceutical Cocrystals 17
1.5 Marketed Products
e market acceptance of cocrystallized pharmaceuticals demonstrates the
eective implementation of cocrystallization in the pharmaceutical busi-
ness. Some of the marked products are presented in Table 1.2.
1.6 Future of Pharmaceutical Cocrystals
e research conducted over the previous decade has helped to shape
several elements of cocrystallization, including cocrystal screening, char-
acterization, manufacturing processes, and development. e versatility
of cocrystals oers opportunities beyond traditional pharmaceuticals.
Exploring their use in nutraceuticals, cosmetics, and agrochemicals can
open new markets and applications. Tailor-made cocrystals can nd appli-
cations in customized medicines for individual patients based on their
unique genetic and metabolic proles, improving personalized treatment
plans. Cocrystals could be used in precision medicine to create more pre-
cise dosing regimens and drug combinations, thereby optimizing thera-
peutic outcomes and minimizing side eects. It could also be used as a
multifunctional carrier that can deliver multiple drugs simultaneously,
improving treatment ecacy for complex diseases. ey can also be inte-
grated into advanced drug delivery systems like nanoparticles, liposomes,
and microspheres for targeted and controlled release.
In addition, the recent advances in green and sustainable chemistry can
be utilized to develop sustainable green and eco-friendly synthesis meth-
ods for cocrystals, thereby reducing the environmental impact of pharma-
ceutical manufacturing. ese innovative processes minimize waste and
energy consumption, contributing to a more sustainable pharmaceutical
industry.
While the potential of cocrystals is immense, regulatory hurdles and
market acceptance remain signicant challenges. A continuous dialog with
regulatory bodies and transparent clinical data can help mitigate these
challenges. e regulatory strategies from agencies (USFDA and EMA) on
medicinal cocrystals demonstrate their recognized signicance in the cre-
ation of better candidates with superior properties [59]. ere is a need to
establish comprehensive regulatory guidelines for the approval and com-
mercialization of cocrystals, thereby facilitating their entry into the market.
e pharmaceutical manufacturing and investigations of cocrystals
should also focus on the standardization of the synthetic procedures,
18 Cocrystals in Pharmaceutical Sciences
identication, and improvement of the properties that impact the quality
of cocrystals including the reproducibility, yield and purity, and integration
of cocrystal screening and research into the drug development process.
Technological advancements in crystallography, computational chemis-
try, and material science will continue to drive the evolution of cocrystals,
enabling more sophisticated and eective drug formulations. Cocrystals
have the potential to make a global impact by improving drug accessibility
and ecacy in developing regions. Addressing aordability and produc-
tion scalability will be crucial for this vision.
e future of cocrystals in pharmaceutical sciences is promising, with
the potential to revolutionize drug development and delivery. By embrac-
ing interdisciplinary collaboration, leveraging advanced technologies, and
addressing regulatory and market challenges, the pharmaceutical industry
can harness the full potential of cocrystals to improve patient outcomes
and create a more sustainable and innovative future in drug development.
1.7 Conclusion
Cocrystals exhibit promising outcomes in altering and enhancing the phys-
icochemical properties of API. Several cocrystal formation techniques are
available, ranging from lab-scale synthesis to continuous operations at the
industrial level. is article provides a brief overview of several approaches
for cocrystal formation, coformer selection, and cocrystal characteriza-
tion, along with appropriate examples. Cocrystals are gaining popularity
in the pharmaceutical industry owing to their enhanced physicochemical
qualities, as well as the availability of patent rights for cocrystals, which is
critical for huge pharma businesses to earn money. Pharmaceutical cocrys-
tals are projected to become a more common method of pharmaceutical
research once the way for their creation is established and their advantages
have been demonstrated.
Acknowledgment
e authors are very thankful to the Department of Pharmaceutics and
Industrial Pharmacy, University of Ibadan for providing infrastructural
and library facilities.
Pharmaceutical Cocrystals 19
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