Development of Spherical Crystals of Acetylsalicylic Acid for Direct Tablet-making

• Published in: Chemical & pharmaceutical bulletin Vol. 48; no. 12; pp. 1877 - 1881
• Main Authors: GOCZO, Hajnalka, SZABO-REVESZ, Piroska, FARKAS, Bela, HASZNOS-NEZDEI, Magdolna, SERWANIS, Serwanis Fahim, PINTYE-HODI, Klara, KASA, JR, EROS, Istvan, ANTAL, Istvan, MARTON, Sylvia
• Format: Journal Article
• Language: English
• Published: Tokyo The Pharmaceutical Society of Japan 01-12-2000; Maruzen; Japan Science and Technology Agency
• Subjects: acetylsalicylic acid; Aspirin - chemistry; Biological and medical sciences; Crystallization; diffuse reflectance; flowability; General pharmacology; Medical sciences; Particle Size; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; roundness; Solvents - chemistry; spherical crystallization; Tablets - chemistry; Particle size; Pharmaceutical technology; Ethanol; Diffuse reflection; Carbon tetrachloride; Crystallization; Acetylsalicylic acid; Compactibility; Non steroidal antiinflammatory agent; Flowability; Analgesic; Mixed solvent; Spherical crystals; Antipyretic; Spherical particle; Salicylates; Hydroorganic solvent
• ISSN: 0009-2363; 1347-5223
• DOI: 10.1248/cpb.48.1877

The production of spherical crystals has recently gained great attention due to the fact that the crystal habit (form, surface, size, etc.) can be modified during the crystallization process. Spherical crystals of ASA were developed by non-typical and typical spherical crystallization techniques. The non-typical spherical crystallization process (conventional stirred tank method) resulted in few monocrystals and non-spherical crystal agglomerates. The typical spherical crystallization process was carried out by the three solvent-system (ethanol-water-carbon tetrachloride). The products were qualified by morphological study, NIR investigation, salicylic acid content, dissolution rate, studies on flowability, compactibility, cohesivity and tablettability. The results demonstrate that only typical spherical crystallization can be recommended for the production of spherical crystals of ASA. Only product made by this technique shows excellent flow properties and favourable compactibility, cohesiveness and tablettability values.