Determination of the in vitro disintegration profile of rapidly disintegrating tablets and correlation with oral disintegration

• Published in: International journal of pharmaceutics Vol. 292; no. 1; pp. 29 - 41
• Main Authors: Abdelbary, G., Eouani, C., Prinderre, P., Joachim, J., Reynier, Jp, Piccerelle, Ph
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier B.V 23.03.2005; Elsevier
• Subjects: Administration, Oral; Biological and medical sciences; Drug Evaluation, Preclinical - methods; General pharmacology; Hot Temperature; Humans; In vitro disintegration profile; Medical sciences; Oral disintegration; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Pharmacopoeias as Topic - standards; Rapidly disintegrating tablets; Saliva; Solubility; Tablets - analysis; Tablets - chemical synthesis; Technology, Pharmaceutical - methods; Technology, Pharmaceutical - standards; Texture analyser; Time Factors; Water; Oral disintegration; In vitro disintegration profile; Rapidly disintegrating tablets; Texture analyser; Correlation; Pharmaceutical technology; Disintegration; Oral administration; In vitro; Texture; Dosage form; Tablet; Quantitative analysis
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2004.08.019

The assessment of the in vitro disintegration profile of rapidly disintegrating tablets (RDT) is very important in the evaluation and the development of new formulations of this type. So far neither the US Pharmacopoeia nor the European Pharmacopoeia has defined a specific disintegration test for RDT; currently, it is only possible to refer to the tests on dispersible or effervescent tablets for the evaluation of RDT's disintegration capacity. In the present study, we have evaluated the disintegration profile of RDT manufactured by main commercialised technologies, using the texture analyser (TA). In order to simulate as much as possible the oral disintegration of these dosage forms, a new operating structure was developed. This structure mimics the situation in the patient's mouth and provides a gradual elimination of the detached particles during the disintegration process. The obtained time–distance profiles or disintegration profiles enabled the calculation of certain quantitative values as the disintegration onset ( t 1) and the total disintegration time ( t 2). These values were used in the characterisation of the effect of test variables as the disintegration medium and temperature on the disintegration time of RDT. Moreover, the oral disintegration time of the same products was evaluated by 14 healthy volunteers. Results obtained when artificial saliva at 37 °C was employed as disintegration medium were used to correlate the in vitro ( t 2) and oral disintegration times. Excellent correlation was found and in addition, we were able to achieve a qualitative measure of the mouthfeel by comparing the thickness of the tablets and the penetration distance obtained from the disintegration profile. This method also permitted the discrimination between different RDT, where differences in the disintegration mechanism were reflected on the disintegration profile achieved for each tablet.