Preparation and biological evaluation of (99m)Tc-ropinirole as a novel radiopharmaceutical for brain imaging.

Noninvasive brain imaging is a process that allows scientists and physicians to view and monitor the areas of the brain. The aim of this study was to formulate a novel radiopharmaceutical for the detection of brain disorders at early stages in susceptible patients. (99m) Tc-ropinirole was prepared by the direct complexation of ropinirole with technetium-99m. The results showed that the radiochemical yield (99m) Tc-ropinirole was 92 ± 2.87% and the radiochemical yield was evaluated by paper chromatography and HPLC. In vitro studies showed that the formed complex was stable for up to 6 h. In vivo uptake of (99m) Tc-ropinirole in the brain was 4.87 ± 0.15% injected dose/g organ at 30 min post-injection, which cleared from the brain with time till it reaches 2.3% at 2 h post-injection indicating that the brain uptake of (99m) Tc-ropinirole is higher than that of the commercially available (99m) Tc-HMPAO, which is 2.25% at 30 min. Pre-dosing mice with cold ropinirole reduced the brain uptake to 0.26 ± 0.01% injected dose/g organ, so this confirms the high specificity and selectivity of this radiotracer for the assessment of the dopamine receptors.

In vitro evaluation of flutamide-carrier systems. Part 1: Preparation and evaluation of flutamide systems with polyvinyl pyrrolidone and polyethylene glycol 4000 and 6000.

Coprecipitates were prepared using different ratios of flutamide with polyvinyl pyrrolidine (PVP), polyethylene glycol (PEG) 4000 and 6000. Drug solubility in carrier solutions, thin layer chromatography (TLC), differential scanning calorimetry (DSC), infra-red spectroscopy (IR), uniformity of drug content, drug dissolution from its respective systems and effect of aging on the physico-chemical parameters of stored flutamide-polymer system were studied. PEG 6000 was found to be the most efficient polymer in increasing both the solubility and the release rate of flutamide. Interaction was found to be complete in certain ratios of drug/polymer systems. The dissolution pattern of flutamide from all the prepared systems appeared to fit a first order mechanism. Physico-chemical parameters of flutamide/carrier systems were not influenced by storage.

Biological availability of sulfamethoxypyridazine and sulfisomidine polymers.

Dissolution rates and apparent solubilities of forms I, II and III of Sulfamethoxypyridazine (1) and forms I and II of sulfisomidine (2) were determined in water at 37 degrees C. The ratios of apparent solubilities of I:II:III for 1 forms and I:II for 2 forms were 1:1.18:1.25 and 1:1.32 respectively. Upon long contact of 2 with water the ratio of II:I decreased. This has been attributed to gradual transformation of 2 from form II to I. Gastrointestinal absorption of form III of 1, in human volunteers, was studied in comparison with the more stable form I. The same study was carried out on forms I and II of 2. Data were correlated and expressed in availability rate constants (K1), applying the one compartment open: model. This and other parameters show that form III of 1 is 1.4 times as much absorbed as form I, and that the availability of the metastable form II of 2 is 1.2 times as much absorbed as the stable form I.

Solid dispersions of nitrofurantoin, ethotoin, and coumarin with polyethylene glycol 6000 and their coprecipitates with providone 25,000.

The influence of two linear polymers, polyethylene glycol 6000 and povidone 25,000, on the dissolution rate of three poorly soluble drugs, nitrofurantoin, ethotoin, and coumarin, was studied. Povidone 25,000 produced better drug solubilization than polyethylene glycol 6000 with the drug-polymer ratios studied, and an increase in the weight fraction of either polymer gave more rapid dissolution. TLC and IR studies ruled out any interaction between the drugs and polyethylene glycol 6000. IR spectrophotometry provided evidence that there was complex formation between nitrofurantoin and povidone 25,000, probably via hydrogen bonding.