Interactions and incompatibilities of pharmaceutical excipients with active pharmaceutical ingredients: a comprehensive review

Studies of active drug/excipient compatibility represent an important phase in the preformulation stage of the development of all dosage forms. The potential physical and chemical interactions between drugs and excipients can affect the chemical nature, the stability and bioavailability of drugs and, consequently, their therapeutic efficacy and safety. The present review covers the literature reports of interaction and incompatibilities of commonly used pharmaceutical excipients with different active pharmaceutical ingredients in solid dosage forms. Examples of active drug/excipient interactions, such as transacylation, the Maillard browning reaction, acid base reactions and physical changes are discussed for different active pharmaceutical ingredients belonging to different therapeutic categories viz antiviral, anti-inflammatory, antidiabetic, antihypertensive, anti-convulsant, antibiotic, bronchodialator, antimalarial, antiemetic, antiamoebic, antipsychotic, antidepressant, anticancer, anticoagulant and sedative/hypnotic drugs and vitamins. Once the solid-state reactions of a pharmaceutical system are understood, the necessary steps can be taken to avoid reactivity and improve the stability of drug substances and products

Man against machine reloaded : performance of a market-approved convolutional neural network in classifying a broad spectrum of skin lesions in comparison with 96 dermatologists working under less artificial conditions

Copyright © 2019 European Society for Medical Oncology. Published by Elsevier Ltd. All rights reserved.Background: Convolutional neural networks (CNNs) efficiently differentiate skin lesions by image analysis. Studies comparing a market-approved CNN in a broad range of diagnoses to dermatologists working under less artificial conditions are lacking. Materials and methods: One hundred cases of pigmented/non-pigmented skin cancers and benign lesions were used for a two-level reader study in 96 dermatologists (level I: dermoscopy only; level II: clinical close-up images, dermoscopy, and textual information). Additionally, dermoscopic images were classified by a CNN approved for the European market as a medical device (Moleanalyzer Pro, FotoFinder Systems, Bad Birnbach, Germany). Primary endpoints were the sensitivity and specificity of the CNN's dichotomous classification in comparison with the dermatologists’ management decisions. Secondary endpoints included the dermatologists’ diagnostic decisions, their performance according to their level of experience, and the CNN's area under the curve (AUC) of receiver operating characteristics (ROC). Results: The CNN revealed a sensitivity, specificity, and ROC AUC with corresponding 95% confidence intervals (CI) of 95.0% (95% CI 83.5% to 98.6%), 76.7% (95% CI 64.6% to 85.6%), and 0.918 (95% CI 0.866–0.970), respectively. In level I, the dermatologists’ management decisions showed a mean sensitivity and specificity of 89.0% (95% CI 87.4% to 90.6%) and 80.7% (95% CI 78.8% to 82.6%). With level II information, the sensitivity significantly improved to 94.1% (95% CI 93.1% to 95.1%; P < 0.001), while the specificity remained unchanged at 80.4% (95% CI 78.4% to 82.4%; P = 0.97). When fixing the CNN's specificity at the mean specificity of the dermatologists’ management decision in level II (80.4%), the CNN's sensitivity was almost equal to that of human raters, at 95% (95% CI 83.5% to 98.6%) versus 94.1% (95% CI 93.1% to 95.1%); P = 0.1. In contrast, dermatologists were outperformed by the CNN in their level I management decisions and level I and II diagnostic decisions. More experienced dermatologists frequently surpassed the CNN's performance. Conclusions: Under less artificial conditions and in a broader spectrum of diagnoses, the CNN and most dermatologists performed on the same level. Dermatologists are trained to integrate information from a range of sources rendering comparative studies that are solely based on one single case image inadequate.publishersversionPeer reviewe

Preparation and In Vitro Evaluation of Budesonide Spray Dried Microparticles for Pulmonary Delivery

The present study describes development and in vitro evaluation of budesonide microparticles prepared by spray drying for delivering drug directly to lungs via dry powder inhaler. This paper introduces new formulations for pharmaceutical applications which includes conventional formulations and novel spray dried microparticles viz., pulmosols, microspheres and porous particles. Optimized spray drying parameters for generation of microparticles were: inlet temperature, 130 °C; outlet temperature, 80 °C; aspirator rate, 240 mWc (60%); solution feed rate, 2 ml/min; spraying air flow pressure, 2 bar. Microparticles appeared to be spherical, low-density particles characterized by smooth surface. MMAD and GSD ranged from 2.5–4.6 μm and 1.5–2.7 respectively. Effective index of microspheres (54.48) and porous particle formulations (64.22) was higher than the conventional formulation (49.21) indicating more effective deposition of microparticles to the lungs. Carr’s Index (20–30%) and Hausner ratio (1.2–1.7) for all formulations indicated good powder flow properties. Formulations emitted a fine particle fraction of 25–47%. Microparticles showed extended in vitro drug release upto 4 hours with high respirable fractions, thus use of microparticles potentially offers sustained release profile along with improved delivery of drug to the pulmonary tract

ACCEPTANCE OF OTT VIDEO STREAMING PLATFORMS IN INDIA DURING COVID -19: EXTENDING UTAUT2 WITH CONTENT AVAILABILITY

The paper aims at identifying factors that stimulates the customers to adopt and use OTT video streaming platforms in India by applying unified theory of acceptance and use of technology 2 (UTAUT2) model. The study has also attempted to check the moderation effect of age, gender, experience. The study uses a questionnaire to gather the primary data of 277 users of OTT video streaming platforms of India as respondents. The data was examined using SmartPLS 3.3.2 software. The key drivers of adopting and using OTT video streaming platforms are performance expectancy, price value, habit and content availability. The study approves the relevance of UTAUT2 model in the present context. The study also explains the moderating effect of gender, experience and age in UTAUT2 model constructs with respect to OTT video streaming platforms. The market of OTT platforms in India is growing tremendously and is projected to gain the momentum in coming years. Thus, it is imperious to comprehend the behavioral intention of consumers. The outcomes of the study will help the managers in comprehending and devising different strategies for consumers of OTT video streaming platforms. The study is first ever attempt to the best understanding of research to observe the acceptance of OTT video streaming apps using UTAUT2 model.</jats:p

Incompatibilities of Pharmaceutical Excipients with Active Pharmaceutical Ingredients: A Comprehensive Review

Studies of drug-excipient compatibility represent an important phase in the pre-formulation stage for the development of all dosage forms. The potential physical and chemical interactions between drugs and excipients can affect the chemical nature, the stability and bioavailability of drugs and, consequently, their therapeutic efficacy and safety. The present review covers the literature reports of incompatibilities of commonly used pharmaceutical excipients with different active pharmaceutical ingredients. Examples of drug-excipient interactions, such as transacylation, the Maillard browning reaction, acid base reactions and physical changes are discussed for different active pharmaceutical ingredients belonging to different therapeutic areas viz. antiviral, anti-inflammatory, antidiabetic, antihypertensives, CNS drugs, anti-convulsants, antibiotics, bronchodialators, antimalarial, amtiemetic, vitamins, antiamoebics, antipsychotics, antidepressants, anticancer, anticoagulants and sedatives/ hypnotics. Once solid-state reactions are understood in a pharmaceutical system, the necessary steps can be taken to prevent reactivity and improve the stability of drug substances and products