Browsing by Subject "tabletointi"

Lactose is probably the most used tablet excipient in the field of pharmacy. Although lactose is thoroughly characterized and available in many different forms there is a need to find a replacer for lactose as a filler/binder in tablet formulations because it has some downsides. Melibiose is a relatively unknown disaccharide that has not been thoroughly characterized and not previously used as an excipient in tablets. Structurally melibiose is close to lactose as it is also formed from the same two monosaccharides, glucose and galactose. Aim of this research is to characterize and to study physicochemical properties of melibiose. Also the potential of melibiose to be used as pharmaceutical tablet excipient, even as a substitute for lactose is evaluated. Current knowledge about fundamentals of tableting and methods for determinating of deformation behavior and tabletability are reviewed. In this research Raman spectroscopy, X-ray powder diffraction (XRPD), near-infrared spectroscopy (NIR) and Fourier-transform infrared spectroscopy (FT-IR) were used to study differences between two melibiose batches purchased from two suppliers. In NIR and FT-IR measurements no difference between materials could be observed. XPRD and Raman however found differences between the two melibiose batches. Also the effects of moisture content and heating to material properties were studied and moisture content of materials seems to cause some differences. Thermal analytical methods, differential scanning calorimetry (DSC) and thermogravimetry (TG) were used to study thermal behaviour of melibiose and difference between materials was found. Other melibiose batch contains residual water which evaporates at higher temperatures causing the differences in thermal behaviour. Scanning electron microscopy images were used to evaluate particle size, particle shape and morphology. Bulk, tapped and true densities and flow properties of melibiose was measured. Particle size of the melibiose batches are quite different resulting causing differences in the flowability. Instrumented tableting machine and compression simulator were used to evaluate tableting properties of melbiose compared to α-lactose monohydrate. Heckel analysis and strain-rate sensitivity index were used to determine deformation mechanism of melibiose monohydrate in relation to α-lactose monohydrate during compaction. Melibiose seems to have similar deformation behaviour than α-lactose monohydrate. Melibiose is most likely fragmenting material. Melibiose has better compactibility than α - lactose monohydrate as it produces tablets with higher tensile strength with similar compression pressures. More compression studies are however needed to confirm these results because limitations of this study.

Microcrystalline cellulose is a compactable, versatile, and popular excipient in tableting. Microcrystalline cellulose is produced using acid hydrolysis where most of the amorphous areas are removed and the crystalline part is left. Particle size affects most on the functionality of microcrystalline cellulose and that can be altered by changing the duration of acid hydrolysis or the drying method. The aim of this Master’s thesis was to compare new microcrystalline materials produced using energy efficient methods, to commercial Avicel-powders. The used formulation consisted of microcrystalline cellulose, hydroxypropyl methylcellulose, magnesium stearate and dried colloidal silicon dioxide. Due to the small particle size of AaltoCell™ samples it was not possible to use it for direct compaction, but with wet granulation this was successful. The tablets were tested by the standards of European pharmacopoeia and the tablets from wet granulated Avicel PH-101, AaltoCell™ sample B and C passed all the tests. Probably the problem with the rejected formulations was poor flowability, which caused poor reproducibility in the experiments with direct compressed tablets. The wet granulated Avicel PH-101 produced the best tablets with the used formulation.

Tramadol products for cats are not commercially available. Problems may occur when dividing a tablet registered for humans due to uneven distribution of active ingredient within a tablet and bitter taste of tramadol. Minitablets have multiple benefits, including small size, better uniformity of content, coatability and fast administration, in comparison to a divided conventional tablet. The purpose of this study was to develop minitablets which are possible to coat with a taste masking coating. Physical and chemical properties of tramadol hydrochloride, such as water solubility, temperature behavior and hygroscopicity were studied. Additionally, compatibility of tramadol hydrochloride with excipients was studied by a 3-month stability exam. The pre-tests of granulation were carried out by using lactose or ascorbic acid as an active ingredient to model tramadol hydrochloride. The granulation was performed with high shear granulator and tableting with a rotary tablet press. The only variable factor between the granulation batches was the amount of granulation fluid. The impact of the amount of granulation fluid to the tableting properties was examined by determining particle size distribution, Carr index and Hausner ratio. Uniformity of mass, uniformity of content, hardness, disintegration time and dissolution were examined. The study revealed that tramadol hydrochloride did not have incompatibilities with the examined excipients. Tramadol hydrochloride was not hygroscopic even though it was found out to be freely soluble in water. Tablets with adequate hardness were successfully compressed of both granulated masses and the direct compression mass. However, the direct compression mass had more undesirable properties regarding the processes. Most batches fulfilled the requirements set for uniformity of mass and uniformity of content. Although the purpose of this study was to develop a tablet for veterinary medicine, the results in this study may be utilized in developing a formulation for pediatric medicine.