[en] Haloperidol was chosen as a model compound to determine whether the degradation products created by sterilizing dose of gamma radiation would contaminate an implantible delivery device and be hazardous to the health of the person using it. Acrolein, chlorobenzene, and several other products were identified among the degradation products. They were quantitated and evaluated as being potentially dangerous. It is recommended that the development protocol for a radiation-sterilized, implantible drug include the identification and evaluation of the degradation products. (author)

No abstract available

[en] Short communication

No abstract available

[en] We studied the influence of cationic hydrotrope aniline hydrochloride on the micellization behavior of cationic amphiphilic phenothiazine drug promazine hydrochloride in the presence and absence of 50mmol kg"-"1 NaCl. The experimental critical micelle concentration (CMC) values came out to be lower than ideal CMC (CMCid) values, signifying attractive interactions between the two components in mixed micelles. NaCl further decreases the CMC of pure PMZ and aniline hydrochloride as well as their mixture due to screening of the electrostatic repulsion among the polar head groups. The bulk properties of solution were examined by using different theoretical models for justification and comparison of results. The micellar mole fraction of aniline hydrochloride (X"R"u"b_, X"M_1, X"R"o"d_1 and X"i"d_1) was evaluated by different proposed models, showing greater contribution of hydrotrope in mixed micelle. The negative values of interaction parameter (β) indicate synergistic interactions and negative values of β further decrease by the addition of salt in mixed systems. From the CMC values as a function of temperature, various thermodynamic properties have been evaluated and discussed in detail.

[en] Short communication

[en] We compared measurement of plasma nortriptyline by a recently developed radioimmunoassay technique with values obtained by traditional gas chromatography. The coefficeint of correlation (r) was 0.98 for 84 samples from 21 controlled patients; for a separate series of 45 samples from 34 patients who were receiving in addition other medication, r was 0.96. Use of radioimmunoassay in the routine determination of plasma nortriptyline concentration is discussed

[en] The propylpiperazine side chain of prochlorperazine was labeled with two, four, or six deuterium atoms by lithium aluminum deuteride reduction of the appropriate amide. The isotopic purity of the products after correcting for chlorine isotopes was greater than 95.7%

[en] Benzodiazepine receptors in the ovine frontal cortex were present at 56 days gestation and developed slowly until 96 days when the number increased rapidly, reaching adult levels by 120 days gestation. Scatchard analysis of 3H-diazepam specifically bound to cortical membranes suggested high (KD approximately equal to 2.0 nM) and low (KD approximately equal to 20.0 nM) affinity benzodiazepine receptors at all stages of development. Whereas the affinity of these receptors for 3H-diazepam did not alter during development, the number of both high and low affinity receptors increased significantly between 56 and 120 days gestation. The number of low affinity receptors were higher in late gestation and early neonatal life than in adulthood. The functional state of these receptors as determined by sensitivity to GABA did not alter during development. However, in the adult, nitrazepam, flunitrazepam, midazolam, and 1-methylisoguanosine were more potent in displacing 3H-diazepam at the low affinity than the high affinity receptor, whereas chlordiazepoxide and diazepam had greater potency at the high affinity binding site. Development of the benzodiazepine receptor in the majority of other brain regions studied occurred primarily after 68 days gestation, as was the case in frontal cortex. In contrast, hindbrain and midbrain benzodiazepine receptors had reached adult levels by 68 days gestation

[en] The antipsychotic drug, thioridazine, differs from more classical antipsychotic drugs with respect to both some atypical psychopharmacological characteristics and to the critical involvement of active metabolites in its pharmacology. Tritium labelled thioridazine has been prepared in our laboratory by palladium catalyzed reduction of an aryl brominated precursor using carrier free tritium gas in THF. The product is labelled in the 3-position of the phenothiazine ring system and a specific activity of 12 Ci/mmole was obtained. (author)