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.
Highlights
Neuroendocrine Tumours (NET) are rare human tumour arising from the cells of the diffuse neuroendocrine system located in various organs and tissues of the human body
According to the results of the preliminary investigations, a hypothalamic hormone somatostatin analogue cyphetrylin has been selected for a preclinical study
Blokhin NMRCO, potato starch, lactose, povidone, talc, microcrystalline cellulose, calcium stearate and magnesium stearate were purchased from different suppliers and conformed to PhEur requirements
Summary
Neuroendocrine Tumours (NET) are rare human tumour arising from the cells of the diffuse neuroendocrine system located in various organs and tissues of the human body (gastrointestinal tract, lungs, pituitary gland, etc.) This type of tumours is characterized by the presence of secondary symptoms caused by metabolically active substances hyperproduction and secretion [1, 2]. Biotherapy with Somatostatin Analogues (SSA) has a proven effect in the treatment of clinical syndromes (carcinoid syndrome, hypoglycemia syndrome, Zollinger-Ellison syndrome, etc.). The drugs in this group (most widely used three SSA are as follows: octreotide, lanreotide and pasireotide) suppress clinical symptoms and reduce the level of biochemical tumour markers and have useful anti-proliferative activity [3, 4]. Cyphetrylin is pentapeptide (Boc-Cys(Thp)-Phe-D-Trp-Lys(Z)-ThrOMe) with noncyclic structure [5]
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