Sains Malaysiana 55(9)(2026): 1543-1555

http://doi.org/10.17576/jsm-2026-5509-11

 

Spherical Crystallisation of Piroxicam–Succinic Acid Multicomponent Particles: Solid-State, Particle, Dissolution and Tabletability Characteristics

(Penghabluran Sfera Zarah Pelbagai Komponen Asid Piroksikam–Suksinik: Pencirian Keadaan Pepejal, Zarah, Pelarutan dan Kebolehtabletan)

 

INDRA INDRA*, HILMA TAZKIYATUL FUADAH & FAJAR SETIAWAN

 

Pharmaceutics Group, Faculty of Pharmacy, Universitas Bakti Tunas Husada, Tasikmalaya, 46115, Indonesia

 

Diserahkan: 29 Jun 2026/Diterima: 3 September 2026

 

*Pengarang untuk surat-menyurat; email: indra@universitas-bth.ac.id

 

ABSTRACT

Piroxicam (PRX) is a poorly water-soluble drug with unfavourable powder properties that may limit dissolution and downstream processing. This study prepared spherical PRX–succinic acid (SUC) multicomponent crystalline particles (Sph-PRX–SUC) by spherical crystallisation and evaluated their solid-state, particle-level, and pharmaceutical properties. PXRD, ATR-FTIR, DSC, TGA, and hot-stage microscopy were complemented by assessments of morphology, particle size, micromeritic properties, wettability, aqueous solubility, intrinsic dissolution, and tabletability. Sph-PRX–SUC exhibited a diffraction profile distinct from PRX, SUC, their physical mixture, examined PRX polymorphs, and previously reported PRX–SUC phases, supporting the formation of a distinct PRX–SUC multicomponent crystalline phase. UV–Vis assay showed a PRX content of 75.11 ± 0.05% w/w across three independently prepared batches. Spherical crystallisation produced rounded millimetre-scale agglomerates with more favourable micromeritic properties and reduced the water contact angle from 92.40 ± 0.30° to 64.80 ± 0.30°. Apparent aqueous PRX solubility increased from 0.072 ± 0.016 to 0.312 ± 0.028 mg mL⁻¹, while IDR increased from 0.04634 ± 0.00063 to 0.21252 ± 0.00462 mg cm⁻² min⁻¹. At 200 MPa, tensile strength increased from 0.96 ± 0.16 to 3.54 ± 0.18 MPa. Overall, Sph-PRX–SUC exhibited distinct solid-state and particle characteristics associated with improved dissolution-related and compaction performance.

Keywords: Multicomponent crystalline particles; piroxicam; spherical crystallisation; succinic acid; tabletability

 

Abstrak

Piroksikam (PRX) ialah ubat yang sukar larut dalam air dan mempunyai sifat serbuk yang kurang menggalakkan, yang boleh mengehadkan prestasi pelarutan dan pemprosesan hiliran. Kajian ini menyediakan zarah kristal multikomponen PRX–asid suksinik (SUC) berbentuk sfera (Sph-PRX–SUC) melalui penghabluran sfera dan menilai sifat keadaan pepejal, ciri zarah serta sifat farmaseutikalnya. PXRD, ATR-FTIR, DSC, TGA dan mikroskopi pentas panas digunakan bersama penilaian morfologi, saiz zarah, sifat mikromeritik, kebolehbasahan, keterlarutan akueus, pelarutan intrinsik dan kebolehtabletan. Sph-PRX–SUC menunjukkan profil pembelauan yang berbeza daripada PRX, SUC, campuran fizikalnya, polimorf PRX yang dinilai serta fasa PRX–SUC yang telah dilaporkan, sekali gus menyokong pembentukan fasa kristal multikomponen PRX–SUC yang berbeza. Penentuan kandungan menggunakan UV–Vis menunjukkan kandungan PRX sebanyak 75.11 ± 0.05% w/w merentas tiga kelompok yang disediakan secara bebas. Penghabluran sfera menghasilkan aglomerat bersaiz milimeter yang membulat dengan sifat mikromeritik yang lebih menggalakkan serta mengurangkan sudut sentuhan air daripada 92.40 ± 0.30° kepada 64.80 ± 0.30°. Keterlarutan akueus PRX yang diukur meningkat daripada 0.072 ± 0.016 kepada 0.312 ± 0.028 mg mL⁻¹, manakala kadar pelarutan intrinsik (IDR) meningkat daripada 0.04634 ± 0.00063 kepada 0.21252 ± 0.00462 mg cm⁻² min⁻¹. Pada tekanan mampatan 200 MPa, kekuatan tegangan meningkat daripada 0.96 ± 0.16 kepada 3.54 ± 0.18 MPa. Secara keseluruhan, Sph-PRX–SUC menunjukkan ciri keadaan pepejal dan zarah yang berbeza serta dikaitkan dengan peningkatan prestasi berkaitan pelarutan dan pemampatan.

Kata kunci: Asid suksinik; kebolehtabletan; penghabluran sfera; piroksikam; zarah kristal multikomponen

 

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