Twelve chronic hemiparetic outpatients with pronounced lower limb extensor spasticity were injected with 400 units of botulinum toxin A, EMG guided into the soleus, tibialis posterior, and both heads of the gastrocnemius muscles. Botulinum toxin A caused a definite reduction of plantar flexor spasticity, in 10 patients two weeks after the injection, as assessed by the Ashworth scale. Four of the patients were able to achieve active dorsiflexion of their affected ankle. Gait analysis including the measurement of vertical ground reaction forces showed a statistically significant (p < 0.01) improvement in velocity, stride length, stance symmetry, and the length of the force point of action under the affected foot. Qualitative improvements on the force diagrams indicated a better loading, advancement of the body, and push off of the affected limb in seven patients. Eight weeks after the injection the effects waned.
Co-ground powders of the poorly water-soluble drug nifedipine and a hydrophilic carrier, [partially hydrolyzed gelatin (PHG), polyvinylpyrrolidone (PVP), sodium dodecyl sulfate (SDS), hydroxypropyl methylcellulose (HPMC), polyethylene glycol (PEG), urea or Pluronic F108] were prepared in order to improve the dissolution rate of nifedipine. The effects of type of grinding equipment, grinding time, and type of hydrophilic carrier on the crystallinity of nifedipine (x-ray diffraction and differential scanning calorimetry) on the interaction between drug and carriers (differential scanning calorimetry), on the particle size and appearance (scanning electron microscopy), on the wettability (contact angle measurements), and on the drug release were investigated. Grinding nifedipine together with these carriers improved the dissolution rate. PHG-ground mixtures resulted in the fastest dissolution rate followed by PVP, SDS, HPMC, Pluronic, urea, and PEG. This effect was not only due to particle size reduction, which increased in the order PHG
The IN VITRO and IN VIVO condensation of endogenous (or administered) reactive amines and carbonyl compounds is reported, leading to alkaloid-type heterocycles. The spectrum of the presented "mammalian alkaloids" ranges from isoquinoline derivatives, via beta-carbolines, through to thiazolidines, arising from vitamin B (6), chloral, and glyoxylic acid, respectively. Formation of these compounds may occur accidentally, but might also be induced intentionally, as a therapy for metabolic diseases.
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