Development and sedative effect of a new formulation of midazolam in chocolate bars

The aim of this work was to assess the stability and sedative effect of midazolam in chocolate bars. The stability of 5 g chocolate bars containing 6 mg midazolam hydrochloride was evaluated at room temperature (25 ± 2 °C), at 4 and 40 °C, by HPLC. Drug plasma levels were measured and the sedative effect was confirmed in six healthy volunteers according to the Ramsay’s scale. Data regarding chocolate bar administration were compared to those from the apple juice solution. Pharmacokinetic data were processed using the WinNonLin 5.2 software. Midazolam in chocolate bars remained stable for 14 days at room temperature and exposed to light; for 90 days at 4 and 40 °C protected from light, and showed a longer shelf life, better flavour and appearance, inducing the same sedative effect as the apple juice preparation. Raspberry flavour masked midazolam unpleasing taste most favourably.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Development and sedative effect of a new formulation of midazolam in chocolate bars

The aim of this work was to assess the stability and sedative effect of midazolam in chocolate bars. The stability of 5 g chocolate bars containing 6 mg midazolam hydrochloride was evaluated at room temperature (25 ± 2 °C), at 4 and 40 °C, by HPLC. Drug plasma levels were measured and the sedative effect was confirmed in six healthy volunteers according to the Ramsay’s scale. Data regarding chocolate bar administration were compared to those from the apple juice solution. Pharmacokinetic data were processed using the WinNonLin 5.2 software. Midazolam in chocolate bars remained stable for 14 days at room temperature and exposed to light; for 90 days at 4 and 40 °C protected from light, and showed a longer shelf life, better flavour and appearance, inducing the same sedative effect as the apple juice preparation. Raspberry flavour masked midazolam unpleasing taste most favourably.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Clinical evidence of the antiarrhythmic effect of a magistral suspension of propafenone: A case report

Propafenone is an antiarrhythmic that has been used for the treatment of tachiarrytmias in both adults and children. The aim of this study was to analyze the pharmacologic effect of a magistral suspension of propafenone, due to lack of an adequate commercial formulation for use in children. In this study we present, a case of a 2-year-old boy that was diagnosed with Wolff-Parkinson White syndrome and treated with a magistral suspension of propafenone. He has now been one year with no symptoms, no tachycardia and no cyanosis. The clinical status of the patient under treatment with propafenone was improved through constant medical care in the Cardiological Health Care Unit. The use of a magistral formulation of propafenone developed in our laboratory offers a temporal solution due to lack of medicines for children

Sovereignty, security, self-sufficiency or food crisis? Case of Mexico and East Africa region. Basic problem in health and quality of life

Innovación en TICEn este artículo se pretende contribuir a una mejor comprensión sobre el tema de la producción de alimentos. Es por eso que nos basamos en los siguientes enfoques: soberanía, seguridad, autosuficiencia alimentaria y crisis. Para ello, analizamos la situación que presenta México, comparado con lo que se vive en regiones del Este de África, lo que nos lleva a pensar que tenemos que trabajar decididamente en cambiar la forma en como se ha venido apoyando al sector agropecuario en México. De no hacerlo tenemos el riesgo de padecer condiciones cada vez más graves en la producción de alimentos y, por consiguiente, se pondrá en peligro el suministro de alimentos para la población y su calidad de vida, generando una mayor vulnerabilidad y dependencia en el entorno internacional.In this article it is tried to contribute to a better comprehension on the topic of the food production, is because of it that we base on the following approaches: sovereignty, safety, food self-sufficiency and crisis. For it, we analyze the situation that presents Mexico, compared with what one lives in regions of this one Africa, which it leads us to thinking, that we have to work firmly in changing the form in since one has come resting to the agricultural sector on Mexico, since of not doing it we have the risk of suffering conditions increasingly serious in the food production and consequently it will put in danger on the food supply for the population and his quality of life, generating a major vulnerability and dependence in the international environment

Effect of mannitol on the pharmacokinetics of amikacin in wistar rats

The study analyzed the effect of mannitol on the pharmacokinetics (PK) of amikacin. Adult Wistar rats were treated as follows: Group 1 (G1) received mannitol for three days, Group 2 (G2) received mannitol plus 10 mg/kg of amikacin simultaneously, and Group 3 only amikacin. The PK study was conducted on the 4th day. For which, blood samples were drawn at fixed times during 24 h and immunoenzymatically analyzed. Results revealed significant differences (p<0.05) between the groups, e.g. Cmax were 62.26 ± 15.75 µg/ml for G1, 72.63 ± 24.80 µg/ml for G2 and 68.61 ± 27.40 µg/ml for G3. The AUC also differed in the three groups, being largest for G2, 222.52 ± 47.30 µg/ml/h, and smallest for G1, 135.59 ± 39.00 µg/ml/h. Alteration of the PK parameters observed between the groups must be considered when both drugs are prescribed, although human studies are necessary to confirm the results

Development and Validation of a Method to Quantify Midazolam in a New Oral Formulation for Pediatric Use

International audienc

Sex and Age Influence on Association of CYP450 Polymorphism with Midazolam Levels in Critically Ill Children

Midazolam is a drug that is metabolized by cytochrome P450 (CYP450) enzymes, particularly CYP3A4 and CYP3A5. The present study aimed to determine the sex and age influence on association of CYP450 polymorphism with midazolam levels in critically ill children. Seventy-two DNA samples were genotyped by real-time PCR. Children &le; five years of age who carry the rs776746 (T) allele in CYP3A5 gene were associated with lower plasma midazolam levels. The concentration median in patients was 0.0 ng/mL, while in patients with the normal (C) allele, it was 438.17 ng/mL (Q25 135.75&ndash;Q75 580.24), p = 0.005. The midazolam plasmatic concentration in female patients with the minor (T) allele was 0.0 ng/mL (Q250.00&ndash;Q75204.3), while in patients with the normal (C) allele median it was 459.0 ng/mL (Q25296.9&ndash;Q75789.7), p = 0.002. Analysis of the dominant model for the rs2740574 variant in CYP3A4 revealed a median of 0.38 L/kg (Q250.02&ndash;Q751.5) for the volume of distribution parameter in female patients with the normal T allele, while female patients with the minor C allele showed a median of 18.1 L/kg (Q257.5&ndash;Q7528.7) p = 0.02. Our results suggest an altered midazolam metabolism due to the presence the allelic rs2740574 variants of CYP3A4 and rs776746 of CYP3A5, and also the strong influence of age and sex

Influence of Age and Sex on the Pharmacokinetics of Midazolam and the Depth of Sedation in Pediatric Patients Undergoing Minor Surgeries

Whether age and sex influence the depth of sedation and the pharmacokinetics of midazolam is currently unknown. The influence of age and sex was investigated in 117 children (2 to 17 years) who required intravenous sedation for minor surgery (0.05 mg/kg). Plasma concentrations and sedation effects were simultaneously measured. The measured concentrations were analyzed using a two-compartment model with first-order elimination. Among the age ranges, significant differences were found (p < 0.05) between the volume of distribution (Vd) of the first compartment (V1) and that of the second (V2). With respect to sex, differences in V2 were found between age groups. At the administered dose, in patients younger than 6 years, a profound sedative effect (40–60 BIS) was observed for up to 120 min, while in older children, the effect lasted only half as long. The differences found in the Vd and bispectral index (BIS) in patients younger than 6 years compared to older patients may be due to immature CYP3A activity and body fat content; furthermore, the Vd varies with age due to changes in body composition and protein binding. Patients younger than 6 years require intravenous (IV) doses <0.05 mg/kg of midazolam for deep sedation. Dosage adjustments according to age group are suggested

Influence of Age and Sex on the Pharmacokinetics of Midazolam and the Depth of Sedation in Pediatric Patients Undergoing Minor Surgeries

Whether age and sex influence the depth of sedation and the pharmacokinetics of midazolam is currently unknown. The influence of age and sex was investigated in 117 children (2 to 17 years) who required intravenous sedation for minor surgery (0.05 mg/kg). Plasma concentrations and sedation effects were simultaneously measured. The measured concentrations were analyzed using a two-compartment model with first-order elimination. Among the age ranges, significant differences were found (p &lt; 0.05) between the volume of distribution (Vd) of the first compartment (V1) and that of the second (V2). With respect to sex, differences in V2 were found between age groups. At the administered dose, in patients younger than 6 years, a profound sedative effect (40&ndash;60 BIS) was observed for up to 120 min, while in older children, the effect lasted only half as long. The differences found in the Vd and bispectral index (BIS) in patients younger than 6 years compared to older patients may be due to immature CYP3A activity and body fat content; furthermore, the Vd varies with age due to changes in body composition and protein binding. Patients younger than 6 years require intravenous (IV) doses &lt;0.05 mg/kg of midazolam for deep sedation. Dosage adjustments according to age group are suggested