Gas chromatographic analysis of acetophenone oxime and its metabolites

A gas-liquid chromatographic (GLC) method has been developed for monitoring the metabolic reduction of acetophenone oxime or oxidative metabolism of the corresponding amine, alpha-methylbenzylamine in liver homogenates. The oxime, amine, n-hydroxy-alpha-methylbenzylamine and acetophenone are quantitatively determined after GLC separation of components with temperature programming on an SP-2401-DB-coated column. The first three compounds were silylated with N,O-bis(trimethylsilyl)-acetamide prior to chromatographic analysis to enhance the stability and improve the chromatographic properties of these components. The effluent gas was monitored with flame ionization detection, and permitted quantitation of components at sub-microgram/ml levels with reproducibility between injections of +/-2%. The optimal composition of enantiomeric mixtures of (R,S)-alpha-methylbenzylamines formed during metabolic reduction of acetophenone oximes were determined by conversion to diastereomeric amides and subsequent GLC analysis.     

Formulation and characterization of formaldehyde cross-linked degradable starch microspheres containing terbutaline sulfate

Preparation of starch microspheres using epichlorohydrin is a time consuming method and requires around 18 hr for cross-linking reaction. To reduce reaction time, terbutaline sulfate (TBS) loaded degradable starch microspheres (DSM) were prepared using formaldehyde as the cross-linking agent. All microspheres were spherical in shape and had a porous, rough surface with a mean particle size of 18-24 microm. Whatever the cross-linking time, it was seen that the release of the TBS was not complete during the release experiments. The influence of enzyme on the degradation of microspheres was moderate. Following intravenous administration, initial uptake of microspheres by the lung was higher than those of other organs.     

Formulation and in vitro evaluation of bisphosphonate loaded microspheres for implantation in osteolysis

Chitosan and poly(lactide-co-glycolide) acid (PLGA) microspheres loaded with alendronate sodium (AS) were prepared for orthopedic as well as dental applications. In orthopedics the aim was to make the total joint prostheses stay in the body for a long time without causing bone tissue loss, while in dentistry it was aimed to treat the alveolar bone resorption caused by periodontitis and also to make the dental treatment using implants easier by reducing the bone loss in patients with osteoporosis. Solvent evaporation method was used to prepare AS loaded PLGA microspheres and emulsion polimerization method was used to prepare AS loaded chitosan microspheres. Particle size, loading efficacy, surface characteristics, and in vitro release characteristics were examined on prepared formulations. After the examination of the scanning electron microscopy photographs of microspheres, chitosan microspheres were observed to have spherical structure and smooth surface characteristics while PLGA microspheres were observed to have spherical porous surface structure. Loading efficacy was found to be 3.30% for chitosan microspheres and 7.70% for PLGA microspheres. It was observed that 85% of AS had been released at the end of the third day from chitosan microspheres whereas 58% was released at the end of the fifth day from PLGA microspheres. It was found that chitosan microspheres gave first order release while PLGA microspheres gave zero order release.     

Influence of hydroxypropyl beta-cyclodextrin on the corneal permeation of pilocarpine

The influence of hydroxypropyl β-cyclodextrin (HPβCD) on the corneal permeation of pilocarpine nitrate was investigated by an in vitro permeability study using isolated rabbit cornea. Pupillary-response pattern to pilocarpine nitrate with and without HPβCD was examined in rabbit eye. Corneal permeation of pilocarpine nitrate was found to be four times higher after adding HPβCD into the formulation. The reduction of pupil diameter (miosis) by pilocarpine nitrate was significantly increased as a result of HPβCD addition into the simple aqueous solution of the active substance. The highest miotic response was obtained with the formulation prepared in a vehicle of Carbopol® 940. It is suggested that ocular bioavailability of pilocarpine nitrate could be improved by the addition of HPβCD.     

In vitro release properties of caffeine. I. effect of concentration and type of ointment base

Caffeine has recently been found to cure atopic dermatitis, presumably by increasing skin levels of cAMP.In the light of these findings, its release from different ointment bases at varying concentrations was investigated in vitro. The ointment bases used were a petrolatum (named as petrolatum A), a PEG ointment (USP XVIII), a hydrophilic ointment (USP XVIII), and a w/o type emulsifying ointment. It was incorporated into ointment bases at 1,5,10,20 and 30% (w/w) concentrations, by simple trituration technique.

Release experiments were carried out at 37°C, with diffusion cells which were placed in distilled water filled beakers.

For all caffeine concentrations used, the release was highest from the PEG ointment. It decreased with the hydrophilic ointment, the emulsifying ointment, and petrolatum A, in that order. From both petrolatum base and the PEG ointment, release of caffeine increased significantly with increasing concentrations. As for the hydrophilic and emulsifying ointments, release patterns were found to be independent of concentration for some percentages of caffeine.     

In vitro studies on enhancing effect of sodium glycocholate on transbuccal permeation of morphine hydrochloride

BACKGROUND: Poliovirus (PV) is the etiologic agent of paralytic poliomyelitis, which is sometimes followed, after decades of clinical stability, by new symptoms, including progressive muscular atrophy, collectively known as the post-polio syndrome. This raises the question of possible PV persistence in post polio patients. OBJECTIVE: To test the capacity of PV to establish persistent infections in human cells, three models were developed. STUDY DESIGN: This review focuses on the viral and cellular parameters involved in persistent PV infection. RESULTS: Many PV strains, which are generally lytic in primate cell lines, are able to establish persistent infections in human neuroblastoma cells. During persistent infection, PV mutants (PVpi) are consistently selected, and several of their capsid substitutions occur at positions known to be involved in PV-PV receptor interactions. PVpi have a particular property: they can establish persistent infections in non-neural HEp-2 cells. PV can also persistently infect primary cultures of human fetal brain cells and the majority of cells which survive infection belong to the neuronal lineage. CONCLUSIONS: The results obtained with the three models of persistent PV infection in human cells suggest that several mechanisms are used by PV to establish and maintain persistent infections in neural and non-neural cells. The interactions of the virus with its receptor seem to be a key-step in all cases. In the future, the elucidation of the etiology of the post-polio syndrome will require the characterization of PV sequences having persisted for decades in post-polio patients.     

Formulation and In Vitro Evaluation of Bisphosphonate Loaded Microspheres for Implantation in Osteolysis

ABSTRACT

Chitosan and poly(lactide-co-glycolide) acid (PLGA) microspheres loaded with alendronate sodium (AS) were prepared for orthopedic as well as dental applications. In orthopedics the aim was to make the total joint prostheses stay in the body for a long time without causing bone tissue loss, while in dentistry it was aimed to treat the alveolar bone resorption caused by periodontitis and also to make the dental treatment using implants easier by reducing the bone loss in patients with osteoporosis. Solvent evaporation method was used to prepare AS loaded PLGA microspheres and emulsion polimerization method was used to prepare AS loaded chitosan microspheres. Particle size, loading efficacy, surface characteristics, and in vitro release characteristics were examined on prepared formulations. After the examination of the scanning electron microscopy photographs of microspheres, chitosan microspheres were observed to have spherical structure and smooth surface characteristics while PLGA microspheres were observed to have spherical porous surface structure. Loading efficacy was found to be 3.30% for chitosan microspheres and 7.70% for PLGA microspheres. It was observed that 85% of AS had been released at the end of the third day from chitosan microspheres whereas 58% was released at the end of the fifth day from PLGA microspheres. It was found that chitosan microspheres gave first order release while PLGA microspheres gave zero order release.     

Antifungal Activity of Undecylenic Acid Emulsions by Microbiological Methods

Two nonionic surfactants (Simulsol 98 and Simulsol OL 50) alone and I:I mixtures, corn oil-undecylenic acid and water formed emulsions, oily isotropic liquid phases, lamellar and hexagonal liquid crystal phases. The optimum release of undecylenic acid from these phases were controlled microbiologically. The active ingredient undecylenic acid, is released more from emulsion systems containing liquid crystals than only liquid crystalline and oily isotropic liquid phases.     

Measurement of Small Discharges in Open Channels by Slit Weir

A rectangular slit weir is designed for measurement of small (<0.005 m3/s) discharges. The discharge coefficient is determined experimentally using the measured discharges and the corresponding heads over the weir. The relationship between the discharge coefficient and all relevant dimensionless parameters is investigated. It is concluded that the discharge coefficient can be represented solely as a function of Reynolds number.