Formulation and Evaluation of Somatostatin Analogue Tablets

Abstract

Objective: This study was undertaken with the aim of the formulation and evaluation of hypothalamic hormone somatostatin analogue tablets, which are intended for neuroendocrine tumours treatment.
 Methods: Tablets were prepared by using the wet granulation method and evaluated for weight variation, resistance to crushing, friability, disintegration time, content and content uniformity. Stability tests have been performed.
 Results: Characteristics of somatostatin analogue cyphetrylin powder have been investigated, and the wet granulation method has been chosen to prepare tablets. Technical pharmaceutical properties of formulations of different compositions and obtained tablets were estimated and the best formulation CF11 has been established with appropriate characteristics: disintegration time less than 15 min, resistance to crushing more than 30 kg·m·s−2, weight variation ˂7.5 %, active substance content closed to the nominal quantity and consistent cyphetrylin distribution in the batch. Performed examinations showed cyphetrylin tablets stability in the long-term study.
 Conclusion: Because of somatostatin analogue cyphetrylin powder properties tablets were prepared by the wet granulation method with starch, lactose, povidone, talc, microcrystalline cellulose, calcium stearate and magnesium stearate as excipients. The best formulation including povidone has characteristics corresponding to requirements of European Pharmacopoeia (PhEur) and State Pharmacopoeia of the Russian Federation (PhRu). Examination of cyphetrylin tablets showed its quality and stability within the time of observation–12 mo.

Test Dissolution for quality control of water-insoluble somatostatine analog

“…Н. Н. Блохина» Минздрава России разработана ЛФ -таблетки, содержащие 6 мг цифетрилина. Клиническое исследование I фазы показало необходимость увеличения количества ДВ в таблетке до 60 мг [16][17][18].…”