Emollients in dermatological creams: Early evaluation for tailoring formulation and therapeutic performance.

The targeted choice of the emollient of a cream determines its physicochemical properties and clinical effectiveness. This work researched the effects of emollient properties on the final characteristics and potential performance of oil-in-water dermatological creams. Seven emollients with different chemical characteristics and structures (alkane, triglyceride, ether, silicone, vegetable oils, and mineral oil) were tested in a model formulation. Early stability, pH, droplet size distribution, rheology, tackiness, adhesivity, spreadability, tribology, and release profile of a lipophilic substance model (in Franz cells, through a synthetic membrane, for six hours) were assessed. The creams had acid epicutaneous pH and a "shear-thinning" "solid-like" viscoelastic behavior. Among the seven emollients' properties, polarity, density, and viscosity were the most influential. Droplet parameters were the most impacted, pH and release were moderately affected, and the textural properties were lowly to moderately impacted. The emollient substitution in the model formulation affected the experimental parameters differently, allowing formulation optimization and tailoring its potential therapeutic performance regarding drug release, coadjutant effects, and dwell time on the skin. By looking at the creams' characteristics, it was possible to select the best-suited emollients for releasing a lipophilic drug, applying on painful skin, and formulation in wash-off products or leave-on protective barrier creams.

Anandamide-loaded nanoparticles: preparation and characterization.

OBJECTIVE: Preparation and characterization of anandamide (N-arachidonoyl-ethanolamine, AEA) loaded polycaprolactone nanoparticles (PCL NP) as a research tool to clarify the presence of an AEA transporter in cell membranes and to avoid AEA plastic adsorption and instability. MATERIALS AND METHODS: High performance liquid chromatography and light scattering were used to determine encapsulation efficiency, particle size, drug release, permeability and stability. RESULTS: A high encapsulation efficiency 96.05 ± 1.77% and a particle size of 83.52 ± 21.38 nm were obtained. Nearly 40% of AEA remained in the NP after a 99.9% dilution and only 50% was released after 24 h at 37 °C with a 99% dilution. PCL NP prevented the adsorption of the drug to polypropylene or polystyrene, but not to acrylic multiwell plates. Drug permeability through artificial membranes was low (10⁻7 to 10⁻8 cm/s) and was affected by the presence of NP. NP increased AEA stability in suspension (drug half-life 431 h vs. 12 h) and freeze-dried with 5% sucrose. CONCLUSION: This article presents the first study where stable AEA-loaded NP with high encapsulation efficiencies have been obtained.

[Epidemiologic survey of acute poisoning in the south area of the Community of Madrid: the VEIA 2004 study]. / Vigilancia epidemiológica de la intoxicación aguda en el área sur de la Comunidad de Madrid: estudio VEIA 2004.

OBJECTIVE: VEIA study is an evolutional registry of acute poisonings (AP) attended in the Emergency Room of the Doce de Octubre Hospital in Madrid (Spain) in a whole year (1979, 1985, 1990, 1994,1997 and 2000). We present the 2004 study and compare the results with the previous years. METHODS AND RESULTS: Methodology has been identical across VEIA STUDY. Of 1508 AP, 610 are suicide attempts (IAVIS), 319 ethylic, (IAVE), and 218 by illicit drugs (IAVD). Of the 2,259 toxics involved, 48% are medications (50% benzodiacepines) alcohol 25% and illicit drugs 13%. CONCLUSIONS: There is an important increase (34%) of cases and the incidence surpasses all published in our country. There are no gender differences nor in the whole neither the Health Area Census, but there are differences in IAVIS, IAVE and IAVD. IAVIS increase in 35%. Benzodiacepines poisoning increases two-fold as well as antidepressive drugs do in women. In men also increase, but in a minor extent. Acetaminophen remains the same in 23%. NSAID's, adjuvants and myorelaxants increase in women as do also alcohol and other poisons that almost equal men's. There are 13 cases of IAVIS in patients with alimentary disorders. Among men, a quarter are illicit drug abusers. In IAVE, the group without alcoholism grows and the total decreases. Illicit drugs duplicate the number of the former year. Cocaine supposes already 2/3 of the cases, MDMA ascends to 22 cases and they appear new substances as glue, without doubt as an effect of immigration and ketamine. Finally 205 household accidents and 57 industrial injuries complete the series.

[The effects of cholestyramine on pancreatic secretion]. / Efectos de la colestiramina sobre la secreción pancreática.

The objective was to evaluate the effect of biliary salt depletion on morphology and function of the exocrine pancreas. Cholestyramine (15 g/day) was given during fifteen days to male Wistar rats in order to evaluate changes in pancreas weight as well as in enzymatic content of pancreatic tissue and duodenal juice (amylase, lipase and trypsinogen); in duodenal juice, bile salt concentration was also measured; Moreover ultrastructure of the exocrine pancreas was studied. Our results show an increase in pancreas weight in rats treated with cholestyramine, with a significant increase of amylase (p < 0.05) and trypsinogen in pancreatic tissue (p < 0.01), and of lipase in duodenal juice (p < 0.05). Ultrastructural changes were absent. It is concluded that cholestyramine, probably through a bile salt depletion, stimulates pancreatic function and growth, as well as lipase secretion.

[Modifications of the enzymatic content and morphology of the exocrine pancreas of rats with experimental hepatic cirrhosis induced by thioacetamide]. / Modificaciones del contenido enzimático y de la morfología del páncreas exocrino de rata con cirrosis hepática experimental inducida por tioacetamida.

In order to assess the experimental level of enzymatic content in exocrine pancreas of cirrhotic rats, cirrhosis was induced with administration of thioacetamide (50 mg/kg) during ten weeks to male Wistar rats with an initial average weight of 350 g. Contents of amylase, lipase and trypsinogen were determined in pancreatic tissues and amylase, lipase and biliary salts in duodenal juice obtained by cannulation and perfusion with physiologic serum. A higher presence of trypsinogen and amylase was detected in pancreatic tissues, and of lipase in the duodenal juice, with a trend, although insignificant, towards a decrease in biliary salts among the cirrhotic group. No changes were observed in the morphologic study. The hypothesis that a deficit of biliary salts in experimental cirrhosis could be responsible of the enzymatic increase in the pancreatic tissue and, in particular, of the selective excretion of lipase, is discussed.

Treatment of extravasation from parenteral nutrition solution.

OBJECTIVE: To report two cases of parenteral nutrition extravasation and their treatment in adult patients. CASE SUMMARIES: Case 1: A 23-year old white woman was admitted to our hospital diagnosed with a gastrointestinal infection by Salmonella paratyphi sv. B. The treatment included peripheral parenteral nutrition (osmolarity 652 mOsm/L). After 4 days an extravasation of parenteral nutrition was detected in the left antecubital fossa. The affected area soon became inflamed. Chondroitinsulfatase 150 turbidity-reducing units (TRUs), diluted in 3 mL of NaCl 0.9% and administered in six subcutaneous applications around the area, was prescribed. The treatment was successful. The patient was discharged several days later with no sequelae of the extravasation. Case 2: A 33-year-old white woman was admitted to the intensive care unit after surgery for a necrohemorrhagic pancreatitis. The treatment included parenteral nutrition via a central catheter (osmolarity 2130 mOsm/L). Two days later the patient presented a parenteral nutrition subcutaneous extravasation in her left hemithorax around the catheter access site. Chondroitinsulfatase 200 TRUs, diluted in 2 mL of NaCl 0.9% and administered in eight subcutaneous applications around the area, was prescribed. No sequelae of the incident remained. The patient was discharged home 2 months later. DISCUSSION: Parenteral nutrition solution can cause tissue harm after extravasation. Both patients presented an intense inflammatory reaction after the accident. Three treatments have been used in extravasation of parenteral nutrition, but in our patients hyaluronidase was the only applicable treatment. As this enzyme is not commercially available in Spain, chondroitinsulfatase, an enzyme very similar to hyaluronidase, was used. CONCLUSIONS: Chondroitinsulfatase was useful in treating extravasation of parenteral nutrition in two adult patients.

Qualitative and quantitative determination of two new antitumor agents from 1-8 naphthalimides in tablets. Validation of a high performance liquid chromatography method.

A high performance liquid chromatography (HPLC) method for the qualitative and quantitative determination of amonafide (CAS 69408-81-7) and mitonafide (CAS 54824-17-8), two new antineoplastic molecules, in finished pharmaceutical dosage forms (tablets) is developed and validated. The results submitted in this work suggest that HPLC method is linear (range 0.54 microgram to 2.70 micrograms for amonafide, and 1.40 micrograms to 5.25 micrograms for mitonafide), sensitive (discriminator capacity 0.1098 microgram for amonafide and 0.1324 microgram for mitonafide), precise (coefficient of variation < or = 2.39% within run, < or = 1.18% between run for tablets with amonafide, and < or = 1.38% within run and < or = 0.96% between run for tablets with mitonafide), accurate (mean recovery 97.55, 98.85, 98.905% for the three different kinds of tablets with amonafide, and 100.73, 101.54% for the two types of tablets with mitonafide) and selective, even when degradation products are present. The volume of extractor liquid must be specially taken into account with regard to the accuracy of the method, because drug extraction can be influenced by the nature of the excipients.