RESUMEN

Evaluation of the particle size distribution (PSD) of active pharmaceutical ingredients (APIs) in nasal suspension products is challenging due to the presence of both API and excipients. To characterize these intricate formulations, it is essential to have sophisticated analytical methods that offer high spatial resolution and the ability to chemically pinpoint and map out the presence of API particles. However, such advanced techniques have not been documented for nasal formulations yet. In this proof-of-concept study, we investigated the utility of optical photothermal infrared spectroscopy (O-PTIR) to analyze the PSD of commercially available Nasonex® and its generic Azonaire® nasal mometasone furoate (MM) suspensions. Simultaneous O-PTIR and Raman spectra, as well as IR chemical maps, were collected from the particles in both formulations. Spatially resolved spectra from the particles confirmed the presence of peaks related to MM (1727 cm-1, 1661 cm-1, and 1122 cm-1) and excipient microcrystalline cellulose (MCC) (1061 cm-1). The PSD of MM particles was characterized using chemical maps specific to MM (1661 cm-1) and automated imaging. Results confirmed that the PSD of both formulations were comparable. Spectral analysis also revealed the presence of free MM, free MCC, and particles containing co-localized MM and MCC. For suspension-based nasal products, O-PTIR enables the measurement of API PSD, which is critical for formulators in developing nasal suspension products. This approach holds potential as an innovative complimentary analytical tool that could diminish the need for extensive clinical endpoint bioequivalence studies when evaluating the comparability of generic and brand-name nasal suspension products.

Asunto(s)

Excipientes , Furoato de Mometasona , Rociadores Nasales , Tamaño de la Partícula , Suspensiones , Furoato de Mometasona/química , Furoato de Mometasona/administración & dosificación , Excipientes/química , Celulosa/química , Administración Intranasal , Espectrofotometría Infrarroja/métodos , Espectrometría Raman/métodos , Química Farmacéutica/métodos

RESUMEN

Dupilumab is a novel treatment agent for moderate to severe atopic dermatitis (AD) with few adverse effects. Drug-induced psoriasiform lesions are rare.We report a 4-year-old boy with AD who developed pustular psoriasis during treatment with dupilumab.Pustular psoriasis appeared within 1 week of treatment and worsened in the second week. After stopping dupilumab administration, topical corticosteroids (desonide and mometasone furoate creams) and oral desloratadine without relief. Pustular psoriasis was confirmed by pathological examination, and thiamphenicol was administered. After 2 weeks of treatment, the lesions nearly resolved without recurrence in 1-year follow-up.Dupilumab-induced pustular psoriasis is rare in children.

Asunto(s)

Anticuerpos Monoclonales Humanizados , Dermatitis Atópica , Psoriasis , Humanos , Masculino , Psoriasis/inducido químicamente , Psoriasis/tratamiento farmacológico , Psoriasis/patología , Anticuerpos Monoclonales Humanizados/efectos adversos , Preescolar , Dermatitis Atópica/tratamiento farmacológico , Dermatitis Atópica/inducido químicamente , Dermatitis Atópica/patología , Furoato de Mometasona , Fármacos Dermatológicos/efectos adversos

RESUMEN

INTRODUCTION: Leukotrienes play a significant role in the pathogenesis of adenoid hypertrophy (A.H.). Therefore, we aimed to analyse the role of montelukast, a leukotriene receptor antagonist, alone or in combination with mometasone, a potent local intranasal steroid, for the treatment of A.H. METHODS: Participants were children with A.H. were treated with montelukast alone or montelukast and mometasone furoate. The main outcome measures were effect of montelukast on clinical symptoms of A.H. A literature review was conducted using online search engines, Cochrane Library, PubMed, Web of Science and Scopus, for randomized clinical trials assessing children with A.H. treated with montelukast alone or montelukast and mometasone furoate. Seven randomized clinical trials (RCTs) were included with 742 children. RESULTS: Our study reveals that montelukast alone or in combination with intranasal mometasone furoate significantly improves clinical symptoms of adenoid hypertrophy such as snoring, sleeping disturbance, mouth breathing and A/N ratio. Montelukast was superior to placebo in decreasing snoring (SMD = -1.00, 95% CI [-1.52, -0.49]), sleep discomfort (SMD = -1.26, 95% CI [-1.60, -0.93]), A/N ratio (MD = -0.11, 95% CI [-0.14, -0.09]) and mouth breathing (SMD = -1.36, 95% CI [-1.70, -1.02]). No difference was detected between montelukast and mometasone versus mometasone alone in snoring (SMD = -0.21, 95%CI [-0.69, 0.27]); however, the combination group was superior to the mometasone alone in mouth breathing (SMD = -0.46, 95% CI [-0.73, -0.19]). CONCLUSIONS: The limitation of studies included a small sample size, with an overall low to medium quality. Thus, further larger, higher-quality RCTs are recommended to provide more substantial evidence.

Asunto(s)

Acetatos , Tonsila Faríngea , Ciclopropanos , Hipertrofia , Antagonistas de Leucotrieno , Furoato de Mometasona , Quinolinas , Sulfuros , Humanos , Tonsila Faríngea/patología , Ciclopropanos/uso terapéutico , Quinolinas/uso terapéutico , Acetatos/uso terapéutico , Acetatos/administración & dosificación , Hipertrofia/tratamiento farmacológico , Niño , Furoato de Mometasona/uso terapéutico , Furoato de Mometasona/administración & dosificación , Antagonistas de Leucotrieno/uso terapéutico , Antagonistas de Leucotrieno/administración & dosificación , Administración Intranasal , Quimioterapia Combinada , Resultado del Tratamiento

RESUMEN

The study aimed to create a low loading, high retention, easier to apply O/W mometasone furoate (MF) cream using a chemical enhancer (CE) approach to provide more options for patients with atopic dermatitis (AD) and to investigate molecular mechanisms of its increased release and retention. A Box-Behnken design determined the optimal formulation based on stability and in vitro skin retention. Evaluations included appearance, rheological properties, irritation, in vivo tissue distribution and pharmacodynamics. Molecular mechanisms of enhanced release were studied using high-speed centrifugation, molecular dynamics and rheology. The interaction between the CE, MF and skin was studied by tape stripping, CLSM, ATR-FTIR and SAXS. The formulation was optimized to contain 0.05% MF and used 10% polyglyceryl-3 oleate (POCC) as the CE. There was no significant difference from Elocon® cream in in vivo retention and pharmacodynamics but increased in vivo retention by 3.14-fold and in vitro release by 1.77-fold compared to the basic formulation. POCC reduced oil phase cohesive energy density, enhancing drug mobility and release. It disrupted skin lipid phases, aiding drug entry and formed hydrogen bonds, prolonging retention. This study highlights POCC as a CE in the cream, offering insights for semi-solid formulation development.

Asunto(s)

Liberación de Fármacos , Furoato de Mometasona , Crema para la Piel , Piel , Furoato de Mometasona/administración & dosificación , Furoato de Mometasona/farmacocinética , Furoato de Mometasona/química , Animales , Crema para la Piel/administración & dosificación , Crema para la Piel/química , Piel/metabolismo , Piel/efectos de los fármacos , Administración Cutánea , Masculino , Absorción Cutánea/efectos de los fármacos , Química Farmacéutica/métodos , Glicerol/química , Glicerol/análogos & derivados , Dermatitis Atópica/tratamiento farmacológico , Femenino , Excipientes/química , Antiinflamatorios/administración & dosificación , Antiinflamatorios/química , Antiinflamatorios/farmacología , Antiinflamatorios/farmacocinética , Composición de Medicamentos/métodos , Ácido Oléico/química , Polímeros/química

RESUMEN

Introduction: This work was to explore the efficacy and safety of self-made WenyangJianpi-qushi Decoction plus mometasone furoate cream in atopic dermatitis (AD) of spleen deficiency and dampness accumulation type. Material and method: 120 patients with this kind of atopic dermatitis were grouped: The Observation group (disease health education + basic treatment + mometasone furoate cream + self-made Decoction) and The Control group (disease health education + basic treatment + mometasone furoate cream), 60 cases in each group. The SCORAD score, serum IgE level, peripheral blood eosinophils, adverse events, recurrence rate, and total effective rate after treatment were observed.Result: Through treatment, SCORAD score of the observation group (29.96 ± 2.88) was lower as against controls (36.04 ± 3.12), p < 0.05. Through treatment, the peripheral blood eosinophil count in the observation group was (311.26 ± 50.19) 106/L, which was lower than (582.71 ± 54.75) 106/L in controls; the serum lgE of the observation group was (712.44 ± 93.32) IU/mL, which was lower than the controls (890.12 ± 81.25) IU/mL, p < 0.05. The Observation group (56/60, 93.33%) demonstrated superior total effective rate to the controls (34/60, 56.67%); The recurrence rate of the observation group was 4/60 (6.67%), which was lower than the controls 16/60 (26.67%), p < 0.05.Conclusion: Self-made WenyangJianpi-qushi Decoction plus mometasone furoate cream to treat atopic dermatitis of spleen deficiency and dampness accumulation type has significant efficacy and good safety.

Asunto(s)

Dermatitis Atópica , Medicamentos Herbarios Chinos , Furoato de Mometasona , Dermatitis Atópica/tratamiento farmacológico , Humanos , Furoato de Mometasona/uso terapéutico , Furoato de Mometasona/administración & dosificación , Masculino , Femenino , Medicamentos Herbarios Chinos/uso terapéutico , Medicamentos Herbarios Chinos/efectos adversos , Medicamentos Herbarios Chinos/administración & dosificación , Adulto , Adolescente , Adulto Joven , Eosinófilos/efectos de los fármacos , Bazo/efectos de los fármacos , Bazo/patología , Persona de Mediana Edad , Inmunoglobulina E/sangre , Niño , Quimioterapia Combinada , Resultado del Tratamiento , Crema para la Piel/uso terapéutico

RESUMEN

We report the development and the validation of a sensitive liquid chromatography-mass spectrometry (LC-MS/MS) method for mometasone furoate (MF) analysis in human plasma. Plasma samples were processed through liquid-liquid extraction and analyzed using LC-MS/MS operating in positive mode using multiple reaction monitoring of transitions m/z 520.9 â†’ 355.0 and m/z 525.8 â†’ 355.0 for MF and the internal standard (IS), respectively. Separation was achieved at 1.0 mL/min on a C18 column using a gradient elution of mobile phase of 0.05% ammonia in water (phase A) and acetonitrile (phase B). The assay range was 0.250-100 pg/mL and proved to be accurate and precise MF. Normalized recoveries were consistent and reproducible with a coefficient of variation (CV%) value of 6.0. The CV (%) of the IS normalized matrix factor was not observed in normal, lipemic, and hemolyzed plasmas. Dilutions of 1:10 were accurately quantified. A cycle of three freeze and thaw and stabilities at room temperature and on the autosampler were demonstrated. In addition, MF in the presence of indacaterol and glycopyrronium was proven to be stable at -70°C for at least 157 days. The present method was successfully applied to quantify MF in patients receiving MF, indacaterol, and glycopyrronium as a fixed-dose combination.

Asunto(s)

Furoato de Mometasona , Espectrometría de Masas en Tándem , Humanos , Furoato de Mometasona/sangre , Furoato de Mometasona/farmacocinética , Furoato de Mometasona/química , Espectrometría de Masas en Tándem/métodos , Reproducibilidad de los Resultados , Cromatografía Liquida/métodos , Modelos Lineales , Sensibilidad y Especificidad , Estabilidad de Medicamentos , Extracción Líquido-Líquido/métodos , Límite de Detección , Cromatografía Líquida con Espectrometría de Masas

RESUMEN

BACKGROUND: A single-dose, in-clinic, veterinary professional-administered treatment for canine otitis externa was developed to improve compliance and canine welfare. METHODS: This multicentre, controlled, examiner-masked, randomised field trial was conducted in 316 dogs over 42 days. Dogs were treated once, on day 0, with the investigational product containing gentamicin, posaconazole and mometasone furoate (Mometamax Ultra [MU]) or twice (days 0 and 7) with a control product containing florfenicol, terbinafine and betamethasone acetate (CP). The primary endpoint was a composite otitis index score of 4 or less (of 12) on day 14 and 3 or less (of 12) on day 28. RESULTS: On day 28, treatment success was recorded in 128 of 143 MU-treated dogs (89.5%), significantly non-inferior to 116 of 133 (87.2%) CP-treated dogs (Farrington-Manning test, Z = 4.1351, p < 0.0001). For mixed cultures of Staphylococcus pseudintermedius and Malassezia pachydermatis, there was 100% treatment success in MU-treated dogs (n = 33), significantly non-inferior to 90.2% (37 of 41) in CP-treated dogs (Farrington-Manning test, Z = 3.1954, p = 0.0007). LIMITATIONS: Efficacy in chronic otitis externa cases was not investigated. Cytology was not used to aid in diagnosis or for identification of secondary pathogens. CONCLUSION: This unique combination, single-dose product is safe and effective in dogs with otitis externa. It offers enhanced compliance, canine welfare and quality of life by eliminating the owner burden of treating this painful condition.

Asunto(s)

Enfermedades de los Perros , Gentamicinas , Furoato de Mometasona , Otitis Externa , Triazoles , Animales , Perros , Enfermedades de los Perros/tratamiento farmacológico , Otitis Externa/veterinaria , Otitis Externa/tratamiento farmacológico , Otitis Externa/microbiología , Furoato de Mometasona/uso terapéutico , Furoato de Mometasona/administración & dosificación , Resultado del Tratamiento , Femenino , Masculino , Triazoles/uso terapéutico , Triazoles/administración & dosificación , Gentamicinas/uso terapéutico , Gentamicinas/administración & dosificación , Antibacterianos/uso terapéutico , Antibacterianos/administración & dosificación , Quimioterapia Combinada/veterinaria , Antifúngicos/uso terapéutico , Antifúngicos/administración & dosificación , Suspensiones

RESUMEN

IMPORTANCE: Pediatric obstructive sleep apnea (OSA) is a common disease that can have significant negative impacts on a child's health and development. A comprehensive evaluation of different pharmacologic interventions for the treatment of OSA in children is still lacking. OBJECTIVE: This study aims to conduct a comprehensive systematic review and network meta-analysis of pharmacological interventions for the management of obstructive sleep apnea in pediatric population. DATA SOURCES: PubMed, Web of Science, Embase, The Cochrane Library, and CNKI were searched from 1950 to November 2022 for pediatric OSA. STUDY SELECTION: Multiple reviewers included Randomized controlled trials (RCTs) concerning drugs on OSA in children. DATA EXTRACTION AND SYNTHESIS: Multiple observers followed the guidance of the PRISMA NMA statement for data extraction and evaluation. Bayesian network meta-analyses(fixed-effect model) were performed to compare the weighted mean difference (WMD), logarithmic odds ratios (log OR), and the surface under the cumulative ranking curves (SUCRA) of the included pharmacological interventions. Our protocol was registered in PROSPERO website (CRD42022377839). MAIN OUTCOME(S) AND MEASURE(S): The primary outcomes were improvements in the apnea/hypopnea index (AHI), while secondary outcomes included adverse events and the lowest arterial oxygen saturation (SaO2). RESULTS: 17 RCTs with a total of 1367 children with OSA aged 2-14 years that met the inclusion criteria were eventually included in our systematic review and network meta-analysis. Ten drugs were finally included in the study. The results revealed that Mometasone + Montelukast (WMD-4.74[95%CrIs -7.50 to -2.11], Budesonide (-3.45[-6.86 to -0.15], and Montelukast(-3.41[-5.45 to -1.39] exhibited significantly superior therapeutic effects compared to the placebo concerning apnea hypopnea index (AHI) value with 95%CrIs excluding no effect. Moreover, Mometasone + Montelukast achieved exceptionally high SUCRA values for both AHI (85.0 %) and SaO2 (91.0 %). CONCLUSIONS AND RELEVANCE: The combination of mometasone furoate nasal spray and oral montelukast sodium exhibits the highest probability of being the most effective intervention. Further research is needed to investigate the long-term efficacy and safety profiles of these interventions in pediatric patients with OSA.

Asunto(s)

Ciclopropanos , Metaanálisis en Red , Apnea Obstructiva del Sueño , Sulfuros , Humanos , Apnea Obstructiva del Sueño/tratamiento farmacológico , Niño , Ciclopropanos/uso terapéutico , Ciclopropanos/efectos adversos , Sulfuros/uso terapéutico , Quinolinas/uso terapéutico , Quinolinas/efectos adversos , Ensayos Clínicos Controlados Aleatorios como Asunto , Acetatos/uso terapéutico , Acetatos/efectos adversos , Furoato de Mometasona/uso terapéutico , Furoato de Mometasona/administración & dosificación , Teorema de Bayes

RESUMEN

OBJECTIVE: Endoscopic evaluation becomes difficult when excessive secretion/hypersalivation occurs in the upper airway. Intranasal corticosteroids and antihistamines reduce symptoms of rhinorrhea and nasal congestion. For this reason, in our study, we aimed to examine the effects of mometasone furoate and azelastine on both the amount of secretion and upper airway obstruction in terms of possible benefits during drug-induced sleep endoscopy (DISE). PATIENTS AND METHODS: A total of 92 patients participated in the study [69 (75%) were males and 23 (25%) were females]. Three groups in Group 1 used intranasal mometasone furoate for 30 days, Group 2 used intranasal azelastine for 30 days, and Group 3 did not use any nasal spray for 30 days. Then, DISE was performed on all patients on the 30th day. Upper airway obstructions detected in DISE were interpreted according to the VOTE classification. Furthermore, the amount of secretion and patients' tolerance levels observed during DISE were also assessed. RESULTS: Multilevel obstruction was detected in 94.5% of all patients participating in the study. Tolerance was poor in 18 (19.5%) of the patients participating in the study. Better DISE tolerance was determined in the female gender. DISE tolerance was also better in underweight and normal-weight patients (BMI < 25). CONCLUSIONS: This study first investigated nasal mometasone furoate and azelastine on DISE. This study showed that prior use of nasal mometasone furoate or azelastine before DISE did not affect the amount of secretion, tolerance level, severity, and configuration of obstruction.

Asunto(s)

Endoscopía , Nariz , Ftalazinas , Masculino , Humanos , Femenino , Furoato de Mometasona , Sueño

RESUMEN

Importance: Allergic rhinitis affects an estimated 15% of the US population (approximately 50 million individuals) and is associated with the presence of asthma, eczema, chronic or recurrent sinusitis, cough, and both tension and migraine headaches. Observations: Allergic rhinitis occurs when disruption of the epithelial barrier allows allergens to penetrate the mucosal epithelium of nasal passages, inducing a T-helper type 2 inflammatory response and production of allergen-specific IgE. Allergic rhinitis typically presents with symptoms of nasal congestion, rhinorrhea, postnasal drainage, sneezing, and itching of the eyes, nose, and throat. In an international study, the most common symptoms of allergic rhinitis were rhinorrhea (90.38%) and nasal congestion (94.23%). Patients with nonallergic rhinitis present primarily with nasal congestion and postnasal drainage frequently associated with sinus pressure, ear plugging, muffled sounds and pain, and eustachian tube dysfunction that is less responsive to nasal corticosteroids. Patients with seasonal allergic rhinitis typically have physical examination findings of edematous and pale turbinates. Patients with perennial allergic rhinitis typically have erythematous and inflamed turbinates with serous secretions that appear similar to other forms of chronic rhinitis at physical examination. Patients with nonallergic rhinitis have negative test results for specific IgE aeroallergens. Intermittent allergic rhinitis is defined as symptoms occurring less than 4 consecutive days/week or less than 4 consecutive weeks/year. Persistent allergic rhinitis is defined as symptoms occurring more often than 4 consecutive days/week and for more than 4 consecutive weeks/year. Patients with allergic rhinitis should avoid inciting allergens. In addition, first-line treatment for mild intermittent or mild persistent allergic rhinitis may include a second-generation H1 antihistamine (eg, cetirizine, fexofenadine, desloratadine, loratadine) or an intranasal antihistamine (eg, azelastine, olopatadine), whereas patients with persistent moderate to severe allergic rhinitis should be treated initially with an intranasal corticosteroid (eg, fluticasone, triamcinolone, budesonide, mometasone) either alone or in combination with an intranasal antihistamine. In contrast, first-line therapy for patients with nonallergic rhinitis consists of an intranasal antihistamine as monotherapy or in combination with an intranasal corticosteroid. Conclusions and Relevance: Allergic rhinitis is associated with symptoms of nasal congestion, sneezing, and itching of the eyes, nose, and throat. Patients with allergic rhinitis should be instructed to avoid inciting allergens. Therapies include second-generation H1 antihistamines (eg, cetirizine, fexofenadine, desloratadine, loratadine), intranasal antihistamines (eg, azelastine, olopatadine), and intranasal corticosteroids (eg, fluticasone, triamcinolone, budesonide, mometasone) and should be selected based on the severity and frequency of symptoms and patient preference.

Asunto(s)

Glucocorticoides , Antagonistas de los Receptores Histamínicos , Rinitis Alérgica , Humanos , Budesonida/administración & dosificación , Budesonida/uso terapéutico , Cetirizina/uso terapéutico , Fluticasona/administración & dosificación , Fluticasona/uso terapéutico , Antagonistas de los Receptores Histamínicos H1/administración & dosificación , Antagonistas de los Receptores Histamínicos H1/uso terapéutico , Inmunoglobulina E/inmunología , Furoato de Mometasona/administración & dosificación , Furoato de Mometasona/uso terapéutico , Clorhidrato de Olopatadina/administración & dosificación , Clorhidrato de Olopatadina/uso terapéutico , Prurito/etiología , Rinitis Alérgica/complicaciones , Rinitis Alérgica/diagnóstico , Rinitis Alérgica/inmunología , Rinitis Alérgica/terapia , Rinorrea/etiología , Estornudo , Triamcinolona/administración & dosificación , Triamcinolona/uso terapéutico , Glucocorticoides/administración & dosificación , Glucocorticoides/uso terapéutico , Rinitis/tratamiento farmacológico , Antagonistas de los Receptores Histamínicos/administración & dosificación , Antagonistas de los Receptores Histamínicos/uso terapéutico , Administración Intranasal

RESUMEN

INTRODUCTION: One of the fundamental challenges of managing patients with severe asthma is treatment adherence, particularly with inhaled corticosteroids. Adherence is difficult to measure objectively and poor adherence is associated with worse outcomes. In this study, assess the ability of a 'smart' inhaler to record adherence in severe asthma patients and measure the impact of this on asthma control. METHODS: Consecutive consenting patients meeting criteria for biologics had their existing high-dose ICS/LABA//LAMA combination inhaler/s switched to mometasone/indacaterol/glycopyrronium (114/46/136). Routine clinical data, including blood eosinophils, FeNO, and ACQ-6 scores were collected at baseline and at 4 wk. Adherence was then checked on the Propeller Health app, and good adherence was defined as >80% of prescribed usage. Participants were then followed-up at 12 months to record the proportion of patients who were initiated on biologics. RESULTS: 77 patients (mean [SD] age = 50.4 [15.7] years, 67.5% female [n = 52]) participated. 71 participants were able to use the device and 65% (n = 46) of these attained good asthma control and were not initiated on biologics at 12-month follow-up. Both groups demonstrated a significant reduction in ACQ6 score at follow-up (2.81 vs. 1.92, p < 0.001 and 3.05 vs. 2.60, p < 0.001, respectively), but there was no statistically significant difference in improvement between groups. Patients with optimal adherence also demonstrated a significant reduction in median FeNO at follow-up (47 ppb vs. 40 ppb, p = 0.003). CONCLUSIONS: In severe asthma patients, 'smart' inhalers may represent an effective management tool to improve adherence and asthma control, therefore avoiding the need for patients to commence biological therapies.

Asunto(s)

Antiasmáticos , Asma , Cumplimiento de la Medicación , Humanos , Asma/tratamiento farmacológico , Femenino , Masculino , Persona de Mediana Edad , Adulto , Cumplimiento de la Medicación/estadística & datos numéricos , Administración por Inhalación , Antiasmáticos/administración & dosificación , Antiasmáticos/uso terapéutico , Quinolonas/administración & dosificación , Indanos/administración & dosificación , Glicopirrolato/administración & dosificación , Glicopirrolato/uso terapéutico , Nebulizadores y Vaporizadores , Índice de Severidad de la Enfermedad , Furoato de Mometasona/administración & dosificación , Furoato de Mometasona/uso terapéutico , Anciano , Combinación de Medicamentos , Corticoesteroides/administración & dosificación , Corticoesteroides/uso terapéutico

RESUMEN

BACKGROUND: The presentation of rhinitis has drawn increasing attention in recent years due to the possibility of overlap or confusion between allergic rhinitis symptoms and those of COVID-19. Azelastine hydrochloride (AZH) and mometasone furoate (MOF) are two of the most efficient combinations for enhancing the symptoms of seasonal allergic rhinitis. OBJECTIVE: This work concerns applying and validating different accurate and simple spectrophotometric approaches for simultaneous quantification of the binary mixture of AZH and MOF in raw material, laboratory-prepared mixtures, and pharmaceutical preparation. Moreover, assessment of the environmental impact of the applied approaches on the environment was also a key goal of this study. METHODS: AZH was determined using the direct spectrophotometric (D0) method, while four reliable spectrophotometric approaches namely, induced dual wavelength (IDW), ratio subtraction (RS), ratio difference (RD), and ratio derivative (1DD) were used for MOF determination. RESULTS: The methods were validated in line with the International Conference of Harmonization standards. In the AZH range of (5-56 µg/mL) and MOF range of (2-20 µg/mL), the linearity of the proposed approaches was investigated with high accuracy findings. There were no significant differences between the obtained results and those of the reported method when compared statistically. Furthermore, the applied spectrophotometric methods were deemed to be eco-friendly according to Green Analytical Procedure Index (GAPI) and Analytical Greenness Calculator (AGREE) assessment metrics. CONCLUSIONS: The applied spectrophotometric methods are simpler, more eco-friendly, and take a shorter time to precisely estimate many measurements compared to the only reported chromatographic analysis. HIGHLIGHTS: Neither publications of novel spectrophotometric methods nor reported green ones have been available for simultaneous determination of the binary mixture of AZH and MOF, so this work has a great significance and novelty in the area of pharmaceutical analysis.

Asunto(s)

Furoato de Mometasona , Rociadores Nasales , Ftalazinas , Rinitis Alérgica Estacional , Espectrofotometría , Furoato de Mometasona/análisis , Furoato de Mometasona/administración & dosificación , Espectrofotometría/métodos , Ftalazinas/análisis , Humanos , Tecnología Química Verde/métodos , Combinación de Medicamentos

RESUMEN

OBJECTIVES: To depict the novel use of steroid-eluting stents in the treatment of choanal atresia (CA) restenosis and subglottic stenosis (SGS). METHODS: A retrospective chart review of three pediatric patients, one with CA and two with SGS, treated with mometasone furoate eluting mini stents (PROPEL) was performed. Patients were evaluated for restenosis and adverse events between one to twelve months postoperatively. RESULTS: Postoperatively, patient one with CA showed no signs of restenosis and required no further intervention. Patient two with SGS demonstrated an open subglottic lumen with no signs of restenosis as well as improved phonation following his planned serial procedures. Post-operatively, patient three with SGS exhibited no restenosis of the subglottic lumen, tolerated intermittent tracheostomy capping, and demonstrated improved phonation. CONCLUSION: In this case series, we outline successful treatments for the management of CA restenosis and SGS with mometasone furoate-eluting stents. To our knowledge, this is the first reported application of this treatment in pediatric patients with CA restenosis and the second reported application in pediatric patients with SGS.

Asunto(s)

Atresia de las Coanas , Stents Liberadores de Fármacos , Humanos , Niño , Constricción Patológica , Estudios Retrospectivos , Atresia de las Coanas/cirugía , Stents , Furoato de Mometasona , Resultado del Tratamiento

RESUMEN

Objective: To analyze and summarize the clinical and pathological characteristics, management, and efficacy of patients with vulvar lichen sclerosus (VLS) through a single center large sample study, and preliminarily to explore the frequency of maintenance treatment medication for VLS. Methods: The clinical data of VLS patients in Obstetrics and Gynecology Hospital of Fudan University from 2018 to 2021 were retrospectively collected. The clinicopathological characteristics (patients' age, course of disease, complicated disease history, family history, symptoms, signs and pathology), treatment and effects were retrospectively analyzed. The patients in the maintenance treatment stage were followed up regularly to explore the minimum frequency of individual medication to maintain the stability of the disease. Results: (1) General situation: a total of 345 patients with VLS were included in this study. The average age was (50.4±14.7) years (ranged from 8 to 84 years old), prevalence was highest in the 50-59 years group (30.1%, 104/345). Immune diseases occurred in 18.6% (33/177) of patients, 24.3% (43/177) of patients had allergic skin diseases, and 5.6% (10/177) of the patients' immediate family members had chronic vulvar pruritus or vulvar hypopigmentation. (2) Clinical features: the most common symptom was vulvar pruritus (96.1%, 196/204) among 204 patients with recorded symptoms. The most common sign was hypopigmentation of the vulva (96.3%, 206/214). The most common involved sites were labia minora (70.3%, 142/202), labia majora (67.8%, 137/202), and labial sulcus (59.4%, 120/202). The cumulative number of sites involved in 62 vulvar atrophy patients (2.7±1.1) was significantly higher than that in 152 non-atrophy patients (2.2±1.0; t=3.48, P=0.001). The course of vulvar atrophy was (9.3±8.5) years, which was significantly longer than that of non-atrophy patients [(6.6±5.6) years; t=2.04, P=0.046]. (3) Pathological features: among the 286 patients with electronic pathological sections, the most common pathological feature in the epidermis was epithelial nail process passivation (71.3%, 204/286). The common pathological features in the dermis were interstitial collagenization (84.6%, 242/286), and inflammatory cell infiltration (73.8%, 211/286). (4) Treatment: 177 patients received standardized treatment after diagnosis and were followed up regularly in our hospital. In the initial treatment stage, 26.0% (46/177) of the patients were treated with 0.05% clobetasol propionate cream, and 74.0% (131/177) of the patients were treated with 0.1% mometasone furoate ointment. The complete remission rates of the two methods were respectively 80.4% (37/46) and 74.0% (97/131), and there was no statistically significant difference (χ²=0.76, P=0.385). During maintenance treatment, 27.1% (48/177) of the patients took the medication twice a week, 35.0% (62/177) took the medication once a week, and 37.9% (67/177) took the medication once every 10 days. During follow-up after 6 months of maintenance treatment, there were no patients with recurrence of pruritus or progression of vulvar signs. Conclusions: The majority of VLS patients have itching, hypopigmentation, involvement of labia minora and labia majora, progressive atrophy, and inflammatory infiltration of dermis. Local treatments of mometasone furoate and clobetasol propionate have good initial therapeutic effects. The frequency exploration of individualized maintenance treatment could minimize the occurrence of adverse reactions when ensuring the stability of the patients' condition.

Asunto(s)

Hipopigmentación , Liquen Escleroso Vulvar , Femenino , Humanos , Niño , Adolescente , Adulto Joven , Adulto , Persona de Mediana Edad , Anciano , Anciano de 80 o más Años , Liquen Escleroso Vulvar/tratamiento farmacológico , Liquen Escleroso Vulvar/complicaciones , Liquen Escleroso Vulvar/patología , Clobetasol/efectos adversos , Estudios Retrospectivos , Furoato de Mometasona/uso terapéutico , Prurito/inducido químicamente , Prurito/complicaciones , Prurito/tratamiento farmacológico , Atrofia/inducido químicamente , Atrofia/complicaciones , Atrofia/tratamiento farmacológico , Hipopigmentación/inducido químicamente , Hipopigmentación/complicaciones , Hipopigmentación/tratamiento farmacológico

RESUMEN

PURPOSE: This study aimed to examine the effectiveness of the combined maximal medical treatment for adenoid hypertrophy in preschool children. METHODS: Sixty-four children underwent one-year combined therapy with intranasal mometasone furoate, oral desloratadine, nasal saline irrigation, and bacteriotherapy. Additionally, decongestion drops were applied during scheduled breaks. RESULTS: Of the 64 treated children, 72% showed clinical improvement in adenoid symptoms while 28% did not improve and underwent surgery. These groups differed significantly in terms of the overall reduction in ailments after treatment (p < 0.001), infection rate (p < 0.001), catarrh severity (p < 0.001) and nasal patency (p < 0.001). Endoscopic examination confirmed that responders experienced, on average, a decrease of 8.4% in the adenoid/choana ratio and an improvement in mucosal coverage of the adenoid. These effects were not observed in the group of children whose parents opted for surgery after nine months of conservative treatment. CONCLUSIONS: The proposed new schema of long-term maximal medical treatment with the use of combined intermittent treatment of intranasal mometasone furoate and decongestion drops, oral desloratadine, nasal saline irrigation, and bacteriotherapy can be attempted in patients with adenoid hypertrophy symptoms, and responders may avoid the need for surgery. The applied treatment breaks resulted in a low number of therapeutic side effects.

Asunto(s)

Tonsila Faríngea , Loratadina/análogos & derivados , Humanos , Preescolar , Estudios Prospectivos , Furoato de Mometasona/uso terapéutico , Hipertrofia/tratamiento farmacológico , Adenoidectomía

RESUMEN

OBJECTIVES: The primary objective is to describe a case in which a steroid-eluting implant was utilized to help prevent postoperative granulation and restenosis in a patient who underwent double-stage laryngotracheal reconstruction (dsLTR) for subglottic stenosis. METHODS: This case presents a 3-year-old female who underwent dsLTR with anterior cartilage graft placement and posterior sagittal split for subglottic stenosis. A silicone stent was placed at the time of the dsLTR. After stent removal, direct laryngoscopy and bronchoscopy (DLB) was performed at 4 to 5 week intervals. These visits revealed a significant amount of supraglottic and glottic edema, and granulation tissue at the proximal aspect of the graft contributing to airway obstruction and restenosis. This was treated twice with CO2 laser excision, balloon dilation, and triamcinolone injection. On the third treatment with these modalities, a mometasone furoate implant was inserted as an adjunctive therapy. The implant was inserted to lateralize the vocal folds, prevent webbing, and to extend to the narrowed area within the subglottis to prevent granulation and restenosis. These same treatments were repeated at the fourth visit with another mometasone furoate implant of a smaller size placed in the same location. RESULTS: Findings on DLB since treatment with the steroid-eluting implants have shown persistent granulation tissue limited to the tracheostomy stoma site. Treatments with CO2 laser, balloon dilation, and triamcinolone injection have continued, with occasional use of silver nitrate cautery at the external stoma site. There has not been any significant evidence of edema, granulation, or stenosis in the glottis or subglottis to require another steroid-eluting implant. CONCLUSIONS: Steroid-eluting implants appear to be a safe and effective adjunctive therapy in the routine surveillance of pediatric patients with a tracheostomy who have undergone dsLTR. They may help combat granulation formation and restenosis seen in some dsLTR patients.

Asunto(s)

Dióxido de Carbono , Laringoestenosis , Preescolar , Femenino , Humanos , Constricción Patológica , Edema , Laringoestenosis/cirugía , Furoato de Mometasona , Estudios Retrospectivos , Resultado del Tratamiento , Triamcinolona

RESUMEN

OBJECTIVE: Albumins are protein molecules that account for 50% of total plasma protein. They are imperative in maintaining intravascular colloidal oncotic pressure, act as key scavenger molecules for oxygen free radicals, and perform a major role in transporting numerous substances and in wound healing. Hypoalbuminemia has been reported as the consequence of decreased intake, increased loss, decreased production, and redistribution. While anecdotal evidence of tyrosine kinase inhibitors causing hypoalbuminemia in canine patients exists, to the author's knowledge there is no formal report to this effect to date. This case report aims to bridge the gap between anecdotal evidence and literature. ANIMAL: 3-year-old neutered male hound-mix canine. CLINICAL PRESENTATION, PROGRESSION, AND PROCEDURES: The patient was presented for recurrent otitis externa refractory to treatments with orbifloxacin/mometasone/posaconazole otic suspension, miconazole/polymyxin B/prednisolone otic suspension, ketoconazole/TrizEDTA, and gentamicin/mometasone/clotrimazole, which prompted consideration of oral antifungals. Baseline blood work prior to initiation of fluconazole showed elevated alkaline phosphatase. Treatment was initiated with fluconazole, and blood work was rechecked and revealed hypoalbuminemia. Multiple diagnostic tests failed to reveal a cause of hypoalbuminemia. TREATMENT AND OUTCOME: Discontinuation of oclacitinib that the patient was being administered resulted in normalization of serum albumin. CLINICAL RELEVANCE: It is unclear whether hypoalbuminemia associated with oclacitinib administration is associated with worse outcomes for pathologies in canine patients; however, this seems to be the case in humans according to some reports. This report aims to take a step in the direction of this knowledge.

Asunto(s)

Enfermedades de los Perros , Hipoalbuminemia , Sulfonamidas , Humanos , Masculino , Perros , Animales , Hipoalbuminemia/inducido químicamente , Hipoalbuminemia/tratamiento farmacológico , Hipoalbuminemia/veterinaria , Fluconazol/uso terapéutico , Pirimidinas/efectos adversos , Furoato de Mometasona/uso terapéutico , Enfermedades de los Perros/patología

RESUMEN

Objective: To analyze and summarize the clinical and pathological characteristics, management, and efficacy of patients with vulvar lichen sclerosus (VLS) through a single center large sample study, and preliminarily to explore the frequency of maintenance treatment medication for VLS. Methods: The clinical data of VLS patients in Obstetrics and Gynecology Hospital of Fudan University from 2018 to 2021 were retrospectively collected. The clinicopathological characteristics (patients' age, course of disease, complicated disease history, family history, symptoms, signs and pathology), treatment and effects were retrospectively analyzed. The patients in the maintenance treatment stage were followed up regularly to explore the minimum frequency of individual medication to maintain the stability of the disease. Results: (1) General situation: a total of 345 patients with VLS were included in this study. The average age was (50.4±14.7) years (ranged from 8 to 84 years old), prevalence was highest in the 50-59 years group (30.1%, 104/345). Immune diseases occurred in 18.6% (33/177) of patients, 24.3% (43/177) of patients had allergic skin diseases, and 5.6% (10/177) of the patients' immediate family members had chronic vulvar pruritus or vulvar hypopigmentation. (2) Clinical features: the most common symptom was vulvar pruritus (96.1%, 196/204) among 204 patients with recorded symptoms. The most common sign was hypopigmentation of the vulva (96.3%, 206/214). The most common involved sites were labia minora (70.3%, 142/202), labia majora (67.8%, 137/202), and labial sulcus (59.4%, 120/202). The cumulative number of sites involved in 62 vulvar atrophy patients (2.7±1.1) was significantly higher than that in 152 non-atrophy patients (2.2±1.0; t=3.48, P=0.001). The course of vulvar atrophy was (9.3±8.5) years, which was significantly longer than that of non-atrophy patients [(6.6±5.6) years; t=2.04, P=0.046]. (3) Pathological features: among the 286 patients with electronic pathological sections, the most common pathological feature in the epidermis was epithelial nail process passivation (71.3%, 204/286). The common pathological features in the dermis were interstitial collagenization (84.6%, 242/286), and inflammatory cell infiltration (73.8%, 211/286). (4) Treatment: 177 patients received standardized treatment after diagnosis and were followed up regularly in our hospital. In the initial treatment stage, 26.0% (46/177) of the patients were treated with 0.05% clobetasol propionate cream, and 74.0% (131/177) of the patients were treated with 0.1% mometasone furoate ointment. The complete remission rates of the two methods were respectively 80.4% (37/46) and 74.0% (97/131), and there was no statistically significant difference (χ²=0.76, P=0.385). During maintenance treatment, 27.1% (48/177) of the patients took the medication twice a week, 35.0% (62/177) took the medication once a week, and 37.9% (67/177) took the medication once every 10 days. During follow-up after 6 months of maintenance treatment, there were no patients with recurrence of pruritus or progression of vulvar signs. Conclusions: The majority of VLS patients have itching, hypopigmentation, involvement of labia minora and labia majora, progressive atrophy, and inflammatory infiltration of dermis. Local treatments of mometasone furoate and clobetasol propionate have good initial therapeutic effects. The frequency exploration of individualized maintenance treatment could minimize the occurrence of adverse reactions when ensuring the stability of the patients' condition.

Asunto(s)

Femenino , Humanos , Niño , Adolescente , Adulto Joven , Adulto , Persona de Mediana Edad , Anciano , Anciano de 80 o más Años , Liquen Escleroso Vulvar/patología , Clobetasol/efectos adversos , Estudios Retrospectivos , Furoato de Mometasona/uso terapéutico , Prurito/tratamiento farmacológico , Atrofia/tratamiento farmacológico , Hipopigmentación/tratamiento farmacológico

RESUMEN

Mometasone furoate is a synthetic corticosteroid used in the treatment of skin inflammatory conditions, hay fever and asthma. The industrial manufacturing routes to mometasone furoate are generally accompanied by the formation of numerous process impurities that need to be detected and quantified, as requested by regulatory authorities. The ready availability of such impurities in the required quantity and purity is therefore essential for toxicological studies, analytical method development and process validation. Herein, we report the multi-gram scale preparation of 21'-chloro-(16'α-methyl-3',11',20'-trioxo-pregna-1',4'-dien-17'-yl)-furan-2-carboxylate (mometasone furoate EP impurity C), one of the known impurities of mometasone furoate. This study also includes the systematic investigation of the final acylation step, as well as the characterization of the difuroate enol ether intermediate and its conversion to the target impurity C.

Asunto(s)

Asma , Pregnadienodioles , Humanos , Furoato de Mometasona , Acilación

RESUMEN

BACKGROUND: Mometasone Furoate (MF) is a corticosteroid (glucocorticoid) used to treat eczema, psoriasis, allergies, and rash on the skin; also used to reduce itching, redness, and swelling (inflammation). It has been reported that the bioavailability of MF is less than 11% when given via the nasal route. Encapsulating the drug in niosomes can improve the active pharmaceutical ingredient's bioavailability by enhancing both physical and biological stability. OBJECTIVE: The goal of the study is to develop, a non-ionic surfactant-based vesicular system, by loading mometasone furoate, and introducing it into a gel-based formulation by utilizing an appropriate gelling agent, and performing its evaluation. METHODS: The niosome vesicle was prepared by vacuum rotary evaporation method (Thin film hydration method). Gel was prepared using the dispersion method and in-vitro drug diffusion studies using Franz-diffusion cells. RESULTS: According to the results of the experiments conducted for the study, Mometasone Furoate niosomal gel was prepared utilizing Mometasone Furoate niosomes that were made using the thin film hydration process, Cholesterol, and Span 60, and loaded in various amounts of Carbopol as a geling agent. The niosomes' zeta potential was found to be -24 mV, showing that the formulation is stable. The polydispersity index (PDI) was found to be 0.409 and the average size of niosomes to be 252.7 nm. The performance of the gel of the optimized formulations containing 2% Carbopol showed in vitro diffusion for 7 hours and an increased flux rate as compared to the plain MF. CONCLUSION: The experiments carried out during the study led to the conclusion that the thin-film hydration method was suitable for the formation of the MF-niosomes by using Span 60 and Cholesterol (2:1). The gel formulation containing 2% Carbopol indicated better in vitro diffusion following the Higuchi model across all niosomal gel formulations. Niosomal gel can be regarded as the best vesicular carrier for the efficient distribution of mometasone furoate via the transdermal route.

Asunto(s)

Portadores de Fármacos , Liposomas , Humanos , Absorción Cutánea , Furoato de Mometasona , Vesícula , Colesterol