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Sains Malaysiana 51(10)(2022):
http://doi.org/10.17576/jsm-2022-5110-13
Physicochemical
and Pharmacokinetic Evaluation of Praziquantel Co-Crystals by Varying the
Spacer Group of Co-Crystal Formers
(Penilaian Fizikokimia dan Farmakokinetik Gabungan Hablur Praziquantel dengan Mempelbagaikan Kumpulan Penjarak
Pembentuk Gabungan Hablur)
MUHAMMAD
WASIM1,*, ABDUL MANNAN1, TABINDA
AZIM2, RASHID ALI KHAN3, GHALLAB ALOTAIBI4,
MUHAMMAD AMER5, MUHAMMAD SHAFIQUE4, MUHAMMAD ASGHAR KHAN6,
SUMAIRA GUL7 & IZHAR HUSSAIN1
1Department
of Pharmacy, COMSATS University Islamabad, Abbottabad Campus, Abbottabad 45550,
Pakistan
2Department
of Pharmacy, Iqra University Islamabad Campus,
Islamabad, Pakistan
3Shifa
College of Pharmaceutical Sciences, Shifa Tameer-e-Millat University, Islamabad, Pakistan
4Department
of Pharmaceutical Sciences, College of Pharmacy, Al-Dawadmi Campus, Shaqra University, Shaqra,
KSA
5Department
of Pharmacy, Abasyn University Islamabad Campus,
Islamabad, Pakistan
6Department
of Pharmacy, University of Malakand, Chakdara 18800,
Pakistan
7Department
of Pharmacy, Abdul Wali Khan University Mardan, 23200, Pakistan
Diserahkan: 18 Januari 2022/Diterima: 23 Mei 2022
Abstract
The
research work focuses on investigating the effects of spacer group (varying
aliphatic chain length=n) of co-crystal formers (oxalic acid (OA, n=0),
(malonic acid (MA, n=1), (succinic acid (SA, n=2), (glutaric acid (GA, n=3),
and (adipic acid (AA, n=4) on the physicochemical properties and oral
bioavailability of praziquantel (PZQ) co-crystals. For this purpose, different
co-crystals of PZQ with dicarboxylic acid co-crystal formers (OA, MA, SA, GA,
and AA) were synthesized. These co-crystals were characterized by powder X-ray
diffractometry (XRPD), differential scanning calorimetry (DSC), Fourier
transform infrared spectroscopy (FT-IR), and thermogravimetry (TG) techniques.
The in-vitro (solubility and
dissolution) and in-vivo pharmacokinetic (P.K) studies were performed for PZQ co-crystals. Additionally,
the effect of polymer hydroxypropyl cellulose (HPC) on the formation of PZQ
co-crystals was also investigated. According to the study results, PZQ-SA
co-crystal showed improved solubility, dissolution, and oral bioavailability.
Overall, the solubility, dissolution, and oral bioavailability are consistent
with each other. The order of improved solubility, dissolution, and oral
bioavailability is observed as consistent like PZQ-SA > PZQ-AA > PZQ-GA
> PZQ-OA > PZQ-MA > pure PZQ. Concerning HPC polymer effects, PZQ-OA,
PZQ-MA, PZQ-GA, and PZQ-AA co-crystals were formed successfully in the presence
of HPC polymer but the PZQ-SA co-crystal was inhibited.
Keywords:
Co-crystal; pharmacokinetic parameters; physicochemical properties; spacer
group
Abstrak
Penyelidikan ini memberi tumpuan kepada kajian kesan kumpulan penjarak (pelbagai panjang rantai alifatik=n) pembentuk gabungan hablur (asid oksalik (OA, n=0), (asid malonik (MA, n=1), (asid suksinik (SA, n=2), (asid glutarik (GA, n=3) dan (asid adipik (AA, n=4) pada sifat fizikokimia dan bioketersediaan oral bersama gabungan hablur praziquantel (PZQ). Untuk tujuan ini, gabungan hablur berbeza PZQ dengan pembentuk gabungan hablur asid dikarboksilik (OA, MA, SA,
GA dan AA) telah disintesis. Gabungan hablur ini dicirikan oleh difraktometri sinar-X serbuk (XRPD), kalorimetri pengimbasan pembezaan (DSC), teknik spektroskopi inframerah transformasi Fourier
(FT-IR) dan termogravimetri (TG). Kajian in-vitro (keterlarutan dan pelarutan)
dan farmakokinetik in-vivo (P.K) telah dilakukan untuk gabungan hablur PZQ. Selain itu, kesan polimer hidroksipropil selulosa (HPC) pada pembentukan gabungan hablur PZQ turut dikaji. Menurut hasil kajian, gabungan hablur PZQ-SA menunjukkan kebolehgunaan sol yang lebih baik, pembubaran dan bioketersediaan oral. Secara keseluruhan, keterlarutan, pembubaran dan bioketersediaan oral adalah konsisten antara satu sama lain. Urutan keterlarutan, pelarutan dan bioketersediaan oral yang lebih baik diperhatikan sebagai konsisten seperti PZQ-SA >
PZQ-AA > PZQ-GA > PZQ-OA > PZQ-MA > PZQ tulen. Mengenai kesan polimer HPC, gabungan hablur PZQ-OA, PZQ-MA, PZQ-GA dan PZQ-AA telah terbentuk dengan jayanya dengan kehadiran polimer HPC tetapi gabungan hablur PZQ-SA telah dihalang.
Kata kunci: Gabungan hablur; kumpulan penjarak; parameter farmakokinetik; sifat fizikokimia
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*Pengarang untuk surat-menyurat;
email: wassypharmacist@gmail.com
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