Stability of Mixed Preparations Consisting of Commercial Moisturizing Creams with an Ointment Base Investigated by Magnetic Resonance Imaging.

A moisturizing cream mixed with a steroid ointment is frequently prescribed to patients suffering from atopic dermatitis. However, there is a concern that the mixing operation causes destabilization. The present study was performed to investigate the stability of such preparations closely using magnetic resonance imaging (MRI). As sample preparations, five commercial moisturizing creams that are popular in Japan were mixed with an ointment base, a white petrolatum, at a volume ratio of 1 : 1. The mixed preparations were stored at 60°C to accelerate the destabilization processes. Subsequently, the phase separations induced by the storage test were monitored using MRI. Using advanced MR technologies including spin-spin relaxation time (T2) mapping and MR spectroscopy, we successfully characterized the phase-separation behavior of the test samples. For most samples, phase separations developed by the bleeding of liquid oil components. From a sample consisting of an oil-in-water-type cream, Urepearl Cream 10%, a distinct phase-separation mode was observed, which was initiated by the aqueous component separating from the bottom part of the sample. The resultant phase separation was the most distinct among the test samples. To investigate the phase separation quantitatively and objectively, we conducted a histogram analysis on the acquired T2 maps. The water-in-oil type creams were found to be much more stable after mixing with ointment base than those of oil-in-water type creams. This finding strongly supported the validity of the mixing operation traditionally conducted in pharmacies.

Characterization of gamma irradiated petrolatum eye ointment base by headspace-gas chromatography-mass spectrometry.

The effects of gamma irradiation on petrolatum eye ointment base (EOB) and its ingredients (white petrolatum, liquid paraffin, and wool fat) were studied at different irradiation doses. Forty-one volatile radiolysis products were detected and identified by a combined system of headspace-gas chromatography-mass spectrometry (HS-GC-MS). The characteristics of the radiolysis products and the degradation pathway were discussed in each case, respectively. GC method demonstrates that the component distribution patterns of eye ointment as well as its individual ingredients have no differences before and after gamma irradiation. The influence of gamma treatment on EOB was quantitatively determined at 15, 25 and 50 kGy. The concentrations of the radiolysis products increase linearly with increasing doses. Both qualitative and quantitative data show that irradiated eye ointment is safe for human use.

Ingredients and safety of cellulite creams.

There is virtually no knowledge of the ingredients of cellulite creams in the dermatological literature. In the present study, the ingredients of cellulite creams, the frequency of their use and whether the ingredients have been reported to cause allergy were investigated. In the 32 products tested, 263 ingredients were used. On average each product contained 22 ingredients (range 4 to 31). Botanicals and emollients predominated; altogether 44 different botanicals and 39 different emollients were used in the 32 products. Caffeine, present in 14 products was the most common additive, apparently representing an "active" ingredient. In other respects the compositions of the products were similar to those of skin creams. All products contained fragrance. The creams were microbiologically pure. Concentrations of preservatives did not exceed limit values in the regulations. No formaldehyde was present (detection limit 10 ppm). The well-known allergens isothiazolinones or dibromoglutaronitril were declared only in a few products. In spite of the large number of substances used in cellulite creams, their safety seems acceptable for most users. Because, however, one fourth of the substances used have been shown to cause allergy, the risk of adverse effects should be taken into account when using cellulite creams.

Bases dermatológicas utilizadas en preparados magistrales para ácne y rosácea / Dermatological vehicles utilized in masterly preparations for acne and rosacea

Las bases dermatológicas son preparaciones semisólidas que están destinadas a la aplicación de medicamentos en forma externa. La prescripcón de recetas magistrales permite a los dermatológos individulaizar en forma adecuada las terapias de sus pacientes. Las bases pueden ser clasificadas según su composición en: bases oleaginosas, bases de absorción, emulsiones (aceite/agua, agua/aceite), bases hidrosolubles y geles. Por su bajo o nulo contenido en materia grasa, las bases más indicadas en acné o rosácea son las emulsiones de aceite en agua, las bases hidrosolubles, elaboradas con polietilenglicoles, y los geles. Es importante tener presente la posibilidad de interacciones o incompatibilidades entre diversos principios activos y las bases

[Determination of metronidazole in vehicles used externally by titration in a nonaqueous medium]. / Odredivanje metronidazola u vehikulumu za spoljasnju upotrebu titracijom u nevodenoj sredini.

The analytical procedure has been elaborated for determination of metronidazole contents in the formulated preparation for external application in the form of a cream. Ambiphilic and emulsion bases were used as a vehicle. Water is removed from the preparation by drying/1 hour at 105 degrees C/and the amount of dry metronidazole residue is determined by titration in nonaqueous media with, 0.01 mol/l of perchloric acid.

Identificación y cuantificación de benzocaina y eugenol en un ungüento analgésico dental / Identification and quantification of benzocaine and eugenol in a dental analgesic unguent

Se desarrolla un método analítico donde se describen las especificaciones de calidad para el ungüento analgésico dental. Se identifica la benzocaína por espectrofotometría en la zona UV en concentración de 10 y 100 *g/mL, y se determina el valor de la extinción específica en ambos máximos característicos para la benzocaína, utilizándose para la valoración. Se identificó y valoró el grupo amino aromático. Se demostró que los excipientes no interfieren en la valoración , y se obtuvo un recuperado de 100 ñ 2

por los 3 métodos. Se propone un método para la valoración del eugenol, mediante la reacción de los grupos fenólicos presentes en la molécula, por fotometría con p-fenilendiamina sulfato en medio de bicarbonato de sodio y posterior oxidación con ferricianuro de potasio, locual forma un compuesto azul violáceo medible espectrofotométricamente a 596 nm; se comprobó en este máximo de absorción la conformidad con la ley de Beer. Se obtuvieron resultados reproducibles para la cuantificación del eugenol en el ungüento y se observó que ni la benzocaína, ni los excipientes de la formulación interfieren en este método

Identificación y cuantificación de benzocaina y eugenol en un ungüento analgésico dental / Identification and quantification of benzocaine and eugenol in a dental analgesic unguent

Se desarrolla un método analítico donde se describen las especificaciones de calidad para el ungüento analgésico dental. Se identifica la benzocaína por espectrofotometría en la zona UV en concentración de 10 y 100 *g/mL, y se determina el valor de la extinción específica en ambos máximos característicos para la benzocaína, utilizándose para la valoración. Se identificó y valoró el grupo amino aromático. Se demostró que los excipientes no interfieren en la valoración , y se obtuvo un recuperado de 100 ñ 2 % por los 3 métodos. Se propone un método para la valoración del eugenol, mediante la reacción de los grupos fenólicos presentes en la molécula, por fotometría con p-fenilendiamina sulfato en medio de bicarbonato de sodio y posterior oxidación con ferricianuro de potasio, locual forma un compuesto azul violáceo medible espectrofotométricamente a 596 nm; se comprobó en este máximo de absorción la conformidad con la ley de Beer. Se obtuvieron resultados reproducibles para la cuantificación del eugenol en el ungüento y se observó que ni la benzocaína, ni los excipientes de la formulación interfieren en este método

[Development and testing of an ointment base containing a complex emulsifier]. / Entwicklung und Prüfung einer Komplexemulgator enthaltenden Salbengrundlage.

Using a hydrophilic and a lipophilic emulsifier the authors worked out a cream compound (having amphiphilic properties), which can be mixed with oil as well as with water. They convinced themselves that beyond the properties of the emulsifiers their ratio to each other is a crucial element in the development of the composition. They characterized changes in consistency when the composition was modified using rheological methods. In in vitro experiments they determined the influence of the base on the dissolution rate of the agent.

Application of the simple mathematical function for the quantitative description of in vitro release of drug agents from the ointment bases.

An attempt of the quantitative description of the release process by the simple mathematical functions has been made. It was found that the hyperbolic function q = t/(A + Bt) is the best for this application. The values of the parameters 1/A and 1/B are proportional to the released amounts of drug, so they can be useful for the evaluation of the rate of the release process.

[Chromatographic determination of ointment bases and emulsifying agents in European and German pharmacopoeias]. / Chromatographische Bestimmung von Salbengrundlagen und Emulgatoren des Europäischen und Deutschen Arzneibuches.

The ointment bases Lanolinum, Lanae alcoholum unguentum, Zinci unguentum, Polyethylenglycoli unguentum, Unguentum leniens and Unguentum emulsificans, and the emulsifying agents Glyceroli monostearas, Polyethylenglycoli 400 stearas and Polysorbatum 20, 60, 80 were identified by HPTLC and their most important components were determined quantitatively by application of HPLC. The proposed methods of identification are more specific than those described in the monographs of the pharmacopoeias. The obtained results were compared with the nominal values listed in both pharmacopoeias as assays of these bases and emulsifiers are not mentioned, except for glyceroli monostearas.

[Refractometric determination of the fat base content in emulsion ointments (author's transl)]. / Refraktometrische Bestimmung des Fettgrundlagegehaltes von Emulsionssalben.

The Pharmacopoeia of the GDR provides no direct method for the determination of the fat base content in ointments. The indirect determination which is due to in calculating the difference between 100% and the percentages of all the other constituents is tedious and inexact. For this reason, it was tried to find a direct method which was to be reliable, rapid and easy. In principle, the refractometric method divised by Rudischer [2--5, 9] for the determination of fat in meat and meat products, which has been compulsory since 1965, is suitable for this purpose. Consequently, this method was adapted to the requirements of ointment analysis and subjected to modifications which resulted in the variant A for non-ionic ointments, and the variant B for ointments containing ionic fatty alcohol sulphates. The results obtained with the refractometric method from all kinds of ointments tested were in full agreement with the actual fat contents. Parallel determinations differed by 0.5% at the most.

Infrared spectroscopy for tracing of topically applied ointment vehicles and active substances on healthy skin.

Infrared spectroscopy was used to trace active substances and ointment vehicles applied on the skin. Vaseline and lanoline could be traced after 8 hrs but not olive oil. From the active substances, ethyl-4-amino-benzoate (5 per cent), clioquinol (5 per cent), parabenes (15 per cent), 5,7-dichlor-8-hydroxy-2-methyl-chinolin (5 per cent), balsam of Peru (25 per cent) and pyroleum pini (12 per cent) could be traced 1 hr after application but had disappeared after 8 hrs. Ethylenediamine (1 per cent), chlorcresol (1 per cent), pyroleum lithantracis (5 per cent), were not traceable after 1 hr, and curiously neither neomycine sulphate in spite of its high concentration (20 per cent). The reaction of the skin surface lipids, after application of different substances, was deduced from the spectra. Clioquinol and pyroleum lithantracis seem to give rise to hydrolysis of the triglycerides, the free fatty acids being clearly identifiable. It is felt that infrared spectroscopy can be used as an effective method to trace different substances such as potent allergens on healthy or diseased skin.