Galenical formulations

Bioequivalence (e.g. equivalence of efficacy) of two different galenical formulations of the same compound as measured by maintained remission rates in schizophrenic patients after an oral or depot antipsychotic formulation. 

Tasset, C., Preat, V., and Roland, M. (1992). Galenical formulations of Amphoterid.nFBiarm. Belg., 47, 523-536. 

Complementary research activities deal with the development of suitable galenical formulations, the elaboration of analytical methods for monitoring cyclosporin levels, the study of pharmacokinetics and metabolism and, last but not least, the elucidation of the intriguing mechanism of action of cyclosporin A. 

Pancreatic lipase is rapidly inactivated at pH values less than 4 [25] (Figs. 3 and 5], which has important consequences in the development of galenic formulations for pancreatic enzyme replacement. 

When pancreatin is administered to patients in some galenic formulation, it mUy with the food mass and performs some digestion in the stomach. However, most... 

To about 10% of the normal pancreatic secretion, 100,000 FIP units of lipase are required per meal [80]. This means that in order to facilitate patient compliance, foe galenic formulation should contain the maximum amount of panoreatin possible per dose. Earlier studies suggest a minimum of 30,000 FIP units per meal [81], but in recent years higher amounts per meal have been recommended [80,82]. 

The stability and homogeneity3 of the radiolabeled compound should be tested also in the galenic formulation intended to be used. 

For small animals or dosing of a large number of animals, individual doses are determined by weighing the syringes containing the galenic formulation prior to and after each administration stability of radioactive concentration is determined on two aliquots before and after each series of administration. 

Certainly, every radiokinetic as well as any in vivo pharmacokinetic study depends on the galenic formulation used. Aqueous solutions, solutions with organic water-miscible components, solutions with surfactants, emulsions, micro emulsions or suspensions can be responsible for distinct differences of radiokinetics (pharmacokinetics). Therefore, a conscious choice of galenic vehicle and formulation procedure is critical ... 

Other conditions depend on the method of administration, delivery system, or galenic formulation of these enzymes. For parenteral administration, the toxicant... 

Cano, J.P., Soliva, M., Hartmann, D., Ziegler, W.H. and Amrein, R. (1977) Bioavailability from various galenic formulations of flunitrazepam. Arzneim Forsch, 27, 2383-2388. 

The bioavailability of molecules exclusively screened through in vitro assays can be low. Because of the polarity of the functional groups present in the molecule, they may be poorly absorbed or incorrectly distributed. They may also, as a result of their vulnerability, be the subject of early metabolic destructions, such as first-pass effects or any other kind of degradation leading to a short biological half-life. For such molecules, in vivo administration is limited to the parenteral route, and their clinical usefulness is thus restricted. Sometimes an adequate pharmaceutical formulation (micro-encapsulation, sustained-release or entero-soluble preparations) can overcome these drawbacks, but often the galenic formulation is inoperant, and a chemical... 

When pancreatin is administered to patients in some galenic formulation, it mixes with the food mass and performs some digestion in the stomach. However, most enzymic activities will be destroyed before reaching the duodenum [76]. Only therapeutic results can be expected in patients where the postprandial pH remains relatively high as a consequence of, for example, alcoholic gastritis or concomitant medication with inhibitors of gastric acid secretion. 

In short, drug design may be considered as an integrated whole approach which essentially involves various steps, namely chemical synthesis, evaluation for activity-spectrum, toxicological studies, metabolism of the drug, i.e., biotransformation and the study of the various metabolites formed, assay procedures, and lastly galenical formulation and biopharmaceutics. 

Harder, S. Siewert, M. Thurmann, P. Blume, H. Rietbrock, N. Siewert, B. Plasma concentrations of S-verapamil after single doses of two different galenic formulations of racemic verapamil. Arzneimittelforschung 1993, 43, 520-523. 

Pricker, G., B. Haeberlin, A. Meinzer, J. Vonderscher. 2006. Galenical formulations, US Patent 7025975-B2. 

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