No abstract

Patients tend to evade the occurrence of hypoglycemic episodes by excessive carbohydrate intake. Glucose pellets with delayed release in the time of the maximum effect of insulin can not only prevent hypoglycemia but also eliminate the preventive carbohydrate intake. The pellets can be administered in a mixture with semisolid food. The cores containing glucose in combination with osmotically active agents (croscarmellose sodium, carmellose sodium, polyethylene glycol, or carboxymethyl starch) were prepared by extrusion-spheronization and coated with 15% water ethylcellulose dispersion (Surelease® B NF) in Wurster column (Medipo, Havlíčkův Brod, Czech Republic) into four coating levels (12.5, 25, 35, and 50%). Mean particle size is 0.63-0.73 for cores and 0.82-0.98 for coated pellets. Cores and coated pellets have excellent or good flow properties according to Hausner ratio and Carr index. Aspect ratio ranges from 1.78 to 2.17 for cores and from 1.73 to 2.31 for coated pellets. Dissolution was performed using pH-independent method and method with continual change of pH. The suitable pH-independent release was achieved in the samples containing carboxymethyl starch or polyethylene glycol. Glucose release is enabled by a membrane rupture caused by core swelling. It can be, therefore, assumed that the glucose release profile will not be affected by food or transit time.

The aim of this study was to prepare tablets containing ground fruits of cornelian cherry (Cornus mas L.) with high antioxidant capacity. The experiment was planned and evaluated on Design of Experiment (DoE) principle using Multivariate Data Analysis (MVA) as modern tools used in Quality by Design (QbD) approach. Various tableting mixtures with three different particle sizes of the plant material (up to 800 μm, more than 800 μm and their mixture) and percentage of silicon dioxide (1, 3 and 5%) were prepared. Tablets with a diameter of 10 mm and mass of 400 mg were subsequently produced from these mixtures using two compression forces (C=7 kN and C=14 kN). Principal Component Analysis (PCA) and Multiple Linear Regression (MLR) with response surface methodology were used to find the influential process-formulation parameters and describe their optimal settings. Finally, it is possible to say that the increasing level of silicon dioxide and the decreasing particle size of ground cornelian cherry lead to prolongation of disintegration time and increase of radial hardness and abrasion loss. Maximal antioxidant activity was obtained using 5% amount of silicon dioxide, the largest particle size and the low compression force.

The aim of this study was to find the optimal tablet composition with maximum content of dried fruits (Cornus mas L.). The effect of three different concentrations (12.5, 25 and 50 %) of two types of microcrystalline cellulose (Avicel ® PH 101 and Avicel ® PH 200) and three different compression pressures (20, 60 and 100 MPa) on the physical properties of tablet blends and tablets was studied. Tablets containing 50 % Avicel ® PH 101 compressed under 100 MPa were found to have the best physical properties. This combination of composition and compression pressure resulted in stable tablets even after storage under accelerated stability conditions (6 months, 40 °C and 75 % RH).Keywords: Cornus mas, microcrystalline cellulose, direct compression, accelerated stability, principal component analysis Lifestyle diseases such as cancer, cardiovascular diseases or diabetes mellitus type 2 are gradually becoming the global centre of attention as both direct and indirect economic costs increase each year. Therefore, new approaches to preventing the onset and progression of these diseases are being implemented. Antioxidants represent a promising supplement group with proven positive effects in the prevention of lifestyle diseases (1). Less commonly used plants and herbal remedies are becoming more and more popular sources of such antioxidants (2).One of the most promising medicinal plants with a broad spectrum of antioxidants is Cornelian cherry (Cornus mas) whose medicinal effect has been known for years (3). Its antibacterial, astringent, antidiarrheal and hypolipidemic effect have been already studied (4-6). Moreover, the antidiabetic effect of Cornelian cherry, based on its antioxidant properties, has become a target of recent scientific studies (7). For these reasons, efforts have been made to process Cornelian cherry fruits into tablets without using extraction methods. A previously published work describes the main constituent substances and pharmacological effects of Cornelian cherry fruits and points to the ALEŠ FRANC 1

Patients tend to prevent hypoglycemia by excessive saccharide intake leading to poorer glycemic control with potentially fatal consequences. This problem could be resolved by means of pellets with glucose release delayed by 120-360 min as a compensation of the antidiabetic drug peak effect. No glucose is released before; hence there is no risk of hyperglycemia and secondary complications. The pellets contain glucose in combination with an osmotically active ingredient and are coated with an ethylcellulose dispersion, which forms an insoluble semipermeable membrane and ensures delayed release. The release of glucose was assessed using dissolution and high-performance liquid chromatography. Dissolution profiles indicated the possibility of achieving the requested lag time using a combination of adequate compositions and coating concentrations. Lag times of 60, 240 and 360 min were achieved. The sample containing carboxymethyl starch was found to be most suitable for the intent of this work.Keywords: hypoglycemia, diabetes mellitus, pellets, delayed release, glucose, pellet evaluation Hypoglycemia is a common, dangerous and usually unpredictable complication in diabetes mellitus therapy. It can be defined as the occurrence of a variety of symptoms associated with plasma glucose concentration lowered under 3.9 mmol/l (1, 2). If untreated, hypoglycemia can lead to seizures, coma, and death (3). Hypoglycemia frequently develops as a result of misbalance between the effect of insulin or peroral antidiabetics and food intake. Hypoglycemia during sport activities, nocturnal hypoglycemia and hypoglycemia caused by irregular diet are typical examples of such situations.Children and adolescent are more vulnerable to hypoglycemia than adults. Many factors induce the risk of hypoglycemia in young patients. Children and adolescent tend to eat erratically and perform physical activity irregularly, making it difficult to ensure optimal glucose levels during the day. Moreover, hypoglycemic symptoms may be difficult for children to recognize and verbalize, which can lead to longer delays in treatment and in-