The effect of particle size variation on tablet tensile strength for spray-dried lactose, Sta-Rx 1500 and Avicel PH-101 was investigated. Decreasing the particle size of spray-dried lactose and Sta-Rx 1500 resulted in stronger compacts whereas the tablet tensile strength of Avicel PH-101 was unaffected by particle size variation. The Heckel relationship, at two different contact times, was used to examine the predominant compaction mechanism. This was independent of the size fractions studied for all three materials. Angle of repose and Hausner ratio measurements indicated a correlation between the internal forces of friction and cohesion of the sized powders and the tensile strength of compacts formed from them.

This study has demonstrated greater efficacy of a new percutaneous amethocaine preparation relative to Eutectic Mixture of Local Anaesthetics (EMLA). Initially, a double-blinded trial was undertaken on each preparation individually against placebo, as the recommended method of application was different for EMLA (2.5 g applied for 60 min under an occlusive dressing) and the amethocaine formulation (0.5 g applied for 30 min). Thereafter, the two preparations were compared directly, in a double-blinded study using a standardized application for both formulations. The results indicated that both preparations provided significant (chi-square; P less than 0.001) percutaneous local anaesthesia when compared with placebo. The amethocaine preparation produced significant anaesthesia (chi-square, P less than 0.001) after 30 min application. Furthermore, the amethocaine formulation demonstrated both increased rapidity of action and increased duration of effect, as determined by a two-tailed unpaired t test, in comparison with EMLA when application times of both 30 and 60 min were used for each preparation. The results of this study indicate that the amethocaine preparation provided more rapid and prolonged anaesthesia than EMLA.

Taurolin, a non-antibiotic antimicrobial agent, significantly reduced the adherence of buccal and vaginal strains of Candida albicans blastospores and urine isolates of Escherichia coli and Staphylococcus saprophyticus to epithelial cells. Light microscopy and radio-isotopic counting methods were used to quantify the adherence of the micro-organisms to either uroepithelial or buccal epithelial cells. A maximum reduction in adherence of approximately 65% was obtained. The anti-adherence capacity was time-dependent, requiring a contact time of 30 min to achieve maximum effect. Taurolin at sub-minimum inhibitory concentrations (MIC) significantly reduced the adherence of Candida and E. coli. A concentration slightly higher than the MIC was required for Staph. saprophyticus. Treatment of either epithelial cells or micro-organisms with Taurolin resulted in reduced adherence of microorganisms.

1. The efficacy and safety of a novel percutaneous anaesthetic preparation based on amethocaine has been investigated in the paediatric clinical environment. 2. There were 1241 recorded applications on a named patient basis made to patients from infant to age 16 years. Of these, 88.7% had satisfactory anaesthesia to venepuncture challenge, rising to approximately 90% when the infant group was excluded. 3. A 30 min application time was found to be adequate for reliable topical anaesthesia. 4. There were no serious adverse reactions to the preparation. Of the total 6.9% recorded reactions, 6.3% were of a mild, transient erythema later identified as due to the vasodilator action of the drug. 5. A total of 123 patients received more than one application of the preparation. There was no evidence of sensitisation on subsequent exposure to the preparation. 6. The short application time required was found to be advantageous to ward and clinic routines.

We have used EMLA, 4% amethocaine gel and placebo for facial portwine stains, for a period of 1 h, in a double-blind study. After removal of the preparations from the skin surface, each area was treated with six pulses of the laser, each 5 mm in diameter. Any pain noted immediately after treatment was recorded using both visual analogue (VAS) and verbal rating (VRS) scores. Twenty nine patients completed the study and statistical analysis of the results indicated that both EMLA and 4% amethocaine gel were superior to placebo (P < 0.001). However, when EMLA and 4% amethocaine gel were compared, the amethocaine preparation was significantly better (P < 0.05, VAS; P < 0.005 VRS) than EMLA in reducing pain caused by the laser treatment.