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Although laurocapram (Azone) significantly enhances the skin permeation of drugs, its development was hindered by its skin irritation. We then developed an Azone-mimic ionic liquid (IL-Azone), composed of less irritating cationic ε -caprolactam and anionic myristic acid. IL-Azone dissociates to the original cation and anion in the presence of water in the formulation. We tried to select a formulation suitable for IL-Azone in the present study. Each formulation contained 5 % of either Azone or IL-Azone along with the model drug antipyrine, and skin permeation experiments of the drug were conducted. The results revealed that IL-Azone did not enhance skin permeation when combined with most formulations tested. However, a notable and rapid enhancement in skin permeation was observed when combined with white petrolatum. This effect could be attributed to the minimal water content in white petrolatum, which prevented IL-Azone degradation. Furthermore, its permeation-enhancing effects from IL-Azone in white petrolatum were more pronounced and rapid than Azone. The rapid onset observed with IL-Azone can be attributed to its degradation into its original components at the interface between the stratum corneum and the living epidermis, which results in a shorter lag time before achieving a steady-state concentration in the SC compared to Azone. [ABSTRACT FROM AUTHOR]

[Display omitted] The present study systematically investigates the impact of active pharmaceutical ingredient (API) variables and oleaginous base characteristics on the in vitro release (IVR) performance of ophthalmic ointments, utilizing dexamethasone as a model drug. The interplay between selected attributes (i.e., particle size distribution, crystallinity, and polymorphic form for API, and rheological factors for compendial-grade white petrolatum) and IVR performance was investigated. APIs from different vendors exhibited variations in crystallinity and polymorphism. Ointments containing amorphous dexamethasone presented higher release amounts/rates compared to crystalline counterparts, emphasizing the role of physical state in release kinetics. Variations in particle size of this lipophilic API (5.4 – 21.2 µm) did not appear to impact IVR performance significantly. In contrast, white petrolatum's rheological attributes, which varied substantially within USP-grade petrolatum, were found to critically affect the drug release rate and extent of the ointment. The study's comprehensive analysis establishes a coherent connection between the quality attributes of both API and petrolatum and IVR, delineating their intricate interdependent effects on ophthalmic ointment performance. These findings provide reference to formulation design, quality control, and regulatory considerations within the pharmaceutical industry, fostering a robust foundational understanding of commonly overlooked quality attributes in ophthalmic ointments. [ABSTRACT FROM AUTHOR]

Objective: To investigate the effect of a novel topical wound-healing agent, low-concentration povidone-iodine ointment (LPIO) with a hydrophobic white petrolatum-rich base on skin-wound models in rats and rabbits. Method: The therapeutic efficacy of topically applied LPIO was compared to that of standard-concentration povidone-iodine ointment (SPIO) and non-treatment control, using a full-thickness skin-wound model in 24 hairless rats and a full-thickness skin-defect model in rabbit earlobes. The animals were kept under standardised conditions at the Central Research Laboratory of Maruishi Pharmaceutical Co. Ltd. (Osaka, Japan). Therapeutic efficacy was evaluated based on macroscopic wound-size reduction, as well as histopathological and immuno-histochemical examinations. Results: LPIO enhanced wound healing in rat full-thickness skin ulcers, reducing wound size and inflammation, when compared with that in SPIO and non-treatment control. LPIO also markedly improved wound healing in rabbit earlobe ulcers by significantly improving re-epithelialisation, compared with that in SPIO. Conclusion: The results of this study suggest that LPIO is a useful topical therapy for ulcerative lesions. [ABSTRACT FROM AUTHOR]

ABSTRACT Petrolatum is widely used in cosmetics, topical pharmaceuticals and also as a vehicle in dermal toxicity studies. New Zealand white rabbits treated with white petrolatum (vehicle control) in a 2-week dermal irritation study exhibited moderate to severe erythema starting on Day 7 that subsided towards the end of the study. Histological examination of abraded and non-abraded petrolatum-treated skin obtained at termination (Day 15) revealed mild acanthosis, hyperkeratosis, dermal edema with mixed inflammatory cells in the dermis. Macroscopic and microscopic features noted in rabbits were consistent with dermal irritation to petrolatum. Wistar-Han rats, CD1 mice, C57/Bl/6J mice and Göttingen minipigs treated topically with white petrolatum did not exhibit clinical or histologic evidence of dermal irritation. Therapeutic agents developed for topical application are generally tested in rabbits during some point in development. Interpretation of skin irritation data from a single species can impact risk assessment for humans and on product labeling. Copyright © 2013 John Wiley & Sons, Ltd. [ABSTRACT FROM AUTHOR]

In the present study, we performed comprehensive pharmaceutical evaluation among an original clobetasone butyrate (CLB) ointment product and three generic products. Although spherocrystal images were observed under a polarizing microscope for only Kindavate®, the original product, distribution of active and inactive ingredients was chemically equivalent between the original and generic medicine by the attenuated total reflection infrared spectroscopy. These results suggest that the spherocrystals observed in Kindavate® are composed of hydrocarbon. On GC/MS, it was revealed that linear alkanes having 25–27 carbon atoms are densely present in Sun White®, the base used in Kindavate®. On the other hand, linear alkanes having 22–31 carbon atoms were broadly distributed in most other white petrolatums. In the CLB ointment products, the distribution equivalent of linear alkane to Sun White® was observed only in Kindavate®. Thus, the GC/MS method is extremely useful for identification of white petrolatum used in the ointment. A similar amount of CLB among the pharmaceutical products was detected in the skin tissue by skin accumulation test, although there were the differences in rheological properties and the quality of white petrolatum. The present results will be very useful for pharmacists in selecting medicine products that match the needs of the patient. Such pharmaceutical information will help spread objective knowledge about products in the future, and will contribute to the appropriate selection of medication. [ABSTRACT FROM AUTHOR]

Background: White petrolatum is broadly used as an ointment vehicle, although hydrophilic drugs cannot be easily dissolved in the vehicle. Method: The aim of this study was to evaluate the release and skin permeation profiles of a model hydrophilic agent, N1-[2-(4-guanidinophenyl)-1(S)-( N-methylcarbamoyl)ethyl]- N4-hydroxy-2(R)-iso-butyl-3(S)-(3-phenylpropyl)succinamide hydrochloride (FYK-1388b), from the ointment. Results: The release rate of FYK-1388b was very low; however, high skin permeation and skin content of the drug were found. We supposed that this was due to endogenous lipids or sebum, because white petrolatum had a high affinity to these lipids. To evaluate the effect of lipids on the enhanced release and skin permeation of FYK-1388b, ‘preapplied white petrolatum’ was made by applying the drug-free white petrolatum on the hairless rat skin for 6 hours. Then the drug ointment was prepared using the ‘preapplied white petrolatum’. The release rate of FYK-1388b was markedly increased from the ‘preapplied ointment’ compared with the ‘original ointment’. In addition, much higher skin permeation was also obtained using the ‘preapplied ointment’. Separately, cholesteryl oleate, cholesterol, and ceramides were found in the ‘preapplied white petrolatum’. Conclusion: Thus, these endogenous lipids on the skin surface may enhance the release and skin permeation of FYK-1388b from white petrolatum ointment. [ABSTRACT FROM AUTHOR]

Sporadic cases of contact allergy to white petrolatum, which is used as a vehicle in patch test preparations, have been reported. The quantitative relevance of the phenomenon remains yet to be elucidated. Methods: Retrospective analysis of patch test data of the Information Network of Departments of Dermatology (IVDK, ) between 1992 and 2004. Results: Analysis of 79 365 patients patch tested with pure petrolatum yielded 27 ‘+’ (0.03%) and 2 ‘+++’ (0.003%) reactions. The majority of non-negative reactions (0.3%) was interpreted as doubtful (235) or mild irritant (32). The negative reaction index (RI) (−0.8), and the high positivity ratio (PR) (93%) especially a lack of concordance with patch test preparations containing ≥99% petrolatum indicate that many of the ‘positive’ (+) reactions have to be considered as irritant. There were 2 ‘+++’ reactions. In 1 case, an ‘angry back reaction’ was confirmed. The other case is probably a reading or documentation error, as the majority of patch test reactions to preparations containing petrolatum remained negative in this case also. Conclusions: True allergic patch test reactions to white petrolatum are extremely rare and probably due to an individually increased susceptibility to allergens and/or irritants. This is in agreement with considering petrolatum as a non-sensitizer. [ABSTRACT FROM AUTHOR]

In the present study, the abilities of major Malassezia species, M. sympodialis, M. globosa and M. furfur, to assimilate topical agents, which have been widely used as a material of ointment for skin diseases, were tested. Obvious growth of M. furfur on GYEP agar plate was noted in the presence of white petrolatum, purified white petrolatum, hydrophilic ointment and heparinoid in hydrophilic ointment, and also M. sympodialis showed similar growth when they were cultured with hydrophilic or heparinoid in hydrophilic ointment. In contrast, M. globosa did not grow on GYEP in the presence of the any topical agents tested. These results suggest that Malassezia species, especially M. furfur and M. sympodialis, assimilate several topical agents and showed the drug-depended cell growth. [Copyright &y& Elsevier]

46 yellow and while petrolatums were screened for their skin sensitizing properties in 3 subjects with known histories of contact sensitivity to yellow petrolatum. Patch testing revealed that all the petrolatums examined contain sensitizing substances in varying amounts. The results were analyzed with regard to origin, color, purification procedures involved in the production of pharmaceutical grade petrolatum, and pharmacopoeial requirements satisfied. Allergenicity correlated positively with these parameters, but only among petrolatums of the same brand. Petrolatum sensitivity may sometimes account for false positive patch test reactions to substances diluted in it. A petrolatum which causes no reaction on healthy skin may cause eczematous reactions on damaged skin. [ABSTRACT FROM AUTHOR]