Impact of the counterion on the solubility and physicochemical properties of salts of carboxylic acid drugs.

AIM: Salt formation is a widely used approach to improve the physicochemical and solid state properties of an active pharmaceutical ingredient. In order to better understand the relationships between the active drug, the selected counterion and the resultant salt form, crystalline salts were formed using four different carboxylic acid drugs and a closely related series of amine counterions. Thirty-six related crystalline salts were prepared, characterized and the relationship between solubility and dissolution behaviour and other properties of the salt and the counterion studied. METHODS: Salts of four model acid drugs, gemfibrozil, flurbiprofen, ibuprofen and etodolac were prepared using the counterions butylamine, hexylamine, octylamine, benzylamine, cyclohexylamine, tert-butylamine, 2-amino-2-methylpropan-1-ol, 2-amino-2-methylpropan-1,3-diol and tris(hydroxymethyl)aminomethane. Salt formation was confirmed, the salts were characterized and their corresponding solubilities determined and rationalized with respect to the counterions' properties. RESULTS AND CONCLUSION: The properties of the salt highly dependent on the nature of the counterion and, although there is considerable variation, some general conclusion can be drawn. For the alkyl amines series, increasing chain length leads to a reduction in solubility across all the acidic drugs studied and a reduction in melting point, thus contradicting simplistic relationships between solubility and melting point. Small, compact counterions consistently produce crystalline salts with high melting point accompanied with a modest improvement in solubility and the nature of hydrogen bonding between the ions has a major impact on the solubility.

Does enough quality of life-related discussion occur during dermatology outpatient consultations?

BACKGROUND: Dermatologists' assessments of how their patients' lives are affected by the skin disease are of importance for informing clinical decisions. However, there is no information about how often quality of life (QoL) issues are discussed in outpatient consultations. OBJECTIVE: To examine the relationship between the extent of QoL-related discussion during dermatology outpatient consultations, and the current impact of the disease on patients' lives. PATIENTS AND METHODS: A total of 238 consultations were observed in a teaching dermatology outpatient department for QoL-related discussion initiated by either the clinician or the patient. Following the consultation, all patients were posted a Dermatology Life Quality Index (DLQI) questionnaire to complete and return within 1 week. RESULTS: QoL discussion was absent in 40% of consultations. Consultants initiated the fewest QoL discussions with patients, and nurses the most (P < 0.0001). One hundred and twenty-eight (54%) patients returned the DLQI, 114 (48%) of which were evaluable. The mean score was 5.6, SD +/- 6.6, median 3, range 0-29. The mean DLQI score for the patients with whom there was no QoL discussion was 4.0 +/- 4.7, n = 55, compared with the mean DLQI score for patients with whom QoL was discussed 6.8 +/- 7.2, n = 59 (P < 0.001). CONCLUSION: This study demonstrates that little information concerning QoL is elicited during dermatology outpatient consultations.

Attitude toward women's societal roles moderates the effect of gender cues on target individuation.

In 4 studies, participants read trait descriptions and formed impressions of 2 male and 2 female targets. They then attempted to recall which traits had described each target. As predicted, participants with a "progressive" attitude toward women's rights and roles (J. T. Spence, R. L. Helmreich, & J. Stapp, 1973) made fewer within-group recall errors for female targets than for male targets, indicating greater individuation of the female targets, whereas participants with a "traditional" attitude made fewer errors for male targets. The findings of a 5th study suggested that progressive participants were motivated to individuate women by their belief that it is important to improve the status of women and other groups low in power and by their identification with women and feminism. Traditional participants' greater individuation of men was believed to stem from their perception of men's higher status (as confirmed by pretests) and their acceptance of the status quo.