Optimization of composition and technology for tablets containing aspen bark extract

Summary. Influence of quantitativefactorsof basic quality parameters has been investigated for tabletscontainingextractofaspenbark, receivedbydirect pressingmethodand mathematicalplanningof experiment.To set the optimal composition of tablets containingaspen bark extract the proportion ofProsolv 90, Ludiflash and Polyplasdone XL 10 has been studied. The relationship between the studied factors and parameters of tablets’ regression models has been described. As a result tablets containing aspen bark extractwith mentioned above formula match necessary pharmaco-technological parameters of State Pharmacopoeia of Ukraine. Introduction.Peptic and duodenal ulcer are serious problems in modern medicine. According to statistics this disease is found in 12,83 % of the adult population in Ukraine [1]. Among the remedies for treatment and prevention of peptic ulcers we can find herbal medicines that may be used in the treatment of pre-peptic conditions and during an acute period as a means of adjuvant therapy in combination with strong remedies [2]. An antacid, cytoprotective, anti-inflammatory and reparative actions of aspen bark extract were proved by the researches of domestic and foreign scientists [3, 4]. Previously, we researched the mutual influence of excipients on the main indicators of quality of aspen bark extract tablets obtained by direct compression method. Due to these researches the best excipientshave been selected. It is necessary to establish the optimal quantitative proportion of excipients in order to obtain the tablets with suitable parameters that satisfy the requirements of the State Pharmacopoeia of Ukraine (SPU) [5, 6]. Rational selection of excipients requires wide range of studies to obtain the optimal composition of the tablets containing aspen bark extract. Using mathematical planning of the experiment gives the possibility to reduce the number of experiments and to obtain the most detailed results of researches about effects of excipients on the basic parameters of tablet quality. The aim of investigation.In the previous stages of the experiment, we studied the effect of quantitative factors on pharmaco-technological parameters of tablets. To further study were selected Prosolv 90, Ludiflash and Polyplasdone XL 10.The aim of investigation was to set and study the proportion of excipients selected for developing optimal formula of tablets containing aspen bark extract. Materials and methods.The tablets based on aspen bark extract, obtained by direct compression method, have beenselected as research object. In the development of technology and tablet form,dry aspen bark extract, obtained by the Department of Pharmacognosyof the National University of Pharmacy,has been used [7]. The dry aspen bark extract is hygroscopic fine powder with particles of anizodiametric shape.Namely, from the group of samples of microcrystalline cellulose (MCC) – Prosolv 90 (Silicified MCC, manufactured by JRS Pharma GMBH & Co KG., Germany), from the group structure-based substances sugars – Ludiflash (combination of mannitolCrospovidone, Povidone and polyvinyl acetate, manufactured by BASF Corp., USA) and from the group of disintegrants – Polyplasdone XL 10 (homopolymer of vinyl pyrrolidone, manufactured by manufactured by Ashland Inc., USA). At establishment of optimal composition of the tablets based on aspen bark extract three excipientsinfluence, and also their correlation in composition of tabletshas been studied [8]. Results and discussion.The optimal formula of selected excipients has been set and their proportions in tablet dosage form at the shorter intervals have beendetermined. The study of each researched factor has been carried out according to 5 levels. As a result of studies we found the optimal number of excipients for tablet formula: Prosolv 90 – 0,054 g, Ludiflash – 0,03 g, Polyplasdone XL 10 – 0,025 g, MCC 102 – 0,0835 g, magnesium stearate – 0,0025 g in one unit of dose medication. As a result tablets of aspen bark extract with mentioned above formula have necessary pharmaco-technological parameters that meet the requirements of SPU: resistance to crushing – 130 H, abrasion – 0,04 % mass uniformity of tablets – ± 2,85%, disintegration – 6 min [9]. Conclusions Due to mathematical planning the quantitative impact of significant excipients on pharmaco-technological parameters of tablets based on aspen bark extract: Prosolv 90, LudiflashтаPolyplasdone XLhave been studied. Due to the regression analysis optimal composition of tablets based on aspen bark extract : dry aspen bark extract – 0,05 g, Prosolv 90 – 0,054 g, Ludiflash – 0,03 g, Polyplasdone XL 10 – 0,025 g, MCC 102 – 0,0835 g,Neusilin US 2 – 0,0025 g, talc –0,0025 g, magnesium stearate – 0,0025 ghas been determined. As a result tablets of aspen bark extract with mentioned above formula have necessary pharmaco-technological parameters that meet the requirements of SPU