• Publication type
• Meeting Abstract MeSH

Ternary phase diagrams are used for the cocrystal synthesis because they allow to conveniently choose the coformer and to define optimal process conditions. This article deals with the construction of predicted and experimental ternary phase diagrams of trospium chloride as the active substance. At first, the pre-selected co-crystals of trospium chloride with salicylic acid and trospium chloride with oxalic acid were prepared. Subsequently, the solubilities of the individual components and the co-crystals were measured. Values obtained were used for the prediction of cocrystals from ternary phase diagrams in two solvents (propan-1-ol and butan-1-ol). Experimental construction of diagrams was based on the detailed analysis of prepared suspensions of well-defined composition. Solid phases of suspensions were analyzed by X-ray powder diffraction, the liquid phases by UV-Vis spectrophotometry and gravimetry. In this way, diagrams for the co-crystal of trospium chloride with salicylic acid were created. Finally, predicted and experimental constructions were compared and the benefits and differences discussed.

• Keywords
• trospium chlorid, kokrystaly, ternární fázové diagramy,
• MeSH
• Muscarinic Antagonists chemistry   MeSH
• Benzilates MeSH
• Biological Availability MeSH
• Technology, Pharmaceutical MeSH
• Nortropanes MeSH
• Parasympatholytics * chemistry   MeSH
• Solubility * MeSH
• Spectrophotometry MeSH
• Urological Agents chemistry   MeSH
• Research MeSH
• Publication type
• Chart MeSH
• Research Support, Non-U.S. Gov't MeSH

Tenofovir disoproxil fumarate (TDF, form I) is an orally delivered pharmaceutical salt used for the treatment of HIV and chronic hepatitis, which acts as an inhibitor of nucleotide reverse transcriptase. There are many solid forms of TDF described in the literature; 2 of them were identified in the drug products: form I and form A. It seems that during formulation, the active pharmaceutical ingredient undergoes partial to total conversion of TDF form I to TDF form A. The goals of this study were to investigate when and why did the conversion occur and whether the conversion could be avoided and how. The influence of pH and possible interaction with excipients were studied. The conditions enabling using wet granulation in technology while preventing the undesired conversion were found. The stabilization was achieved either by replacement of used disintegrants or by acid addition to the current composition of formulation.

• MeSH
• X-Ray Diffraction methods   MeSH
• Hydrogen-Ion Concentration MeSH
• Anti-HIV Agents chemistry   metabolism   MeSH
• Excipients chemistry   metabolism   MeSH
• Drug Compounding methods   MeSH
• Drug Stability MeSH
• Tenofovir chemistry   metabolism   MeSH
• Publication type
• Journal Article MeSH
• Research Support, Non-U.S. Gov't MeSH

Chemie a fyzika pevných léčiv je nově se profilující předmět, který je speciálním zaměřením chemie a fyziky pevných látek na farmaceutické materiály. Náplní předmětu je získání základních znalostí o struktuře a vlastnostech farmaceutických substancí od molekulární úrovně až po úroveň mikrostruktury pevného stavu. Vychází ze základních krystatalografických pojmů, které jsou aplikovány na farmaceutické molekuly. Zabývá se především fenoménem polymorfismu chemických entit, dále problematikou rozpustnosti, krystalizace, chemickými a fyzikálními typy krystalických a amorfních substancí, degradacemi a stabilitou a v neposlední řadě i patentovou politikou farmaceutických firem. Kromě toho napomáhá k pochopení lékopisných pojmů a seznamuje studenty s rutinními analýzami pevné fáze.

• MeSH
• Copyright MeSH
• Physics MeSH
• Chemistry, Physical MeSH
• Pharmaceutical Preparations chemistry   MeSH
• Particulate Matter MeSH

• Conspectus
• Farmacie. Farmakologie
• Učební osnovy. Vyučovací předměty. Učebnice
• NML Fields
• farmacie a farmakologie
• chemie, klinická chemie
• fyzika, biofyzika
• NML Publication type
• učebnice vysokých škol