- Diffusion ordered NMR spectroscopy measurements as screening method of potential reactions of API and excipients in drug formulations. [Journal Article]
- JPJ Pharm Biomed Anal 2018 Sep 08; 162:41-46
- In the development of new pharmaceutical formulations it is important to consider the possible interactions between the active pharmaceutical ingredient (API) and excipients which is a well-known pro...
In the development of new pharmaceutical formulations it is important to consider the possible interactions between the active pharmaceutical ingredient (API) and excipients which is a well-known problem. The objective of the work presented here was to investigate such reactions by means of diffusion ordered NMR spectroscopy (DOSY). The known reaction of 5-aminosalicylic acid (5-ASA) and the excipient citric acid was studied. Three reaction products have been verified by DOSY, 1H NMR and HPLC measurements. Despite a poor separation in the DOSY diagram, the reaction products could be assign due to the processing of thoughtful selected parts of the signals. The reaction of 5-ASA with formic acid and benzocaine with dibutyl phthalate was also studied by means of DOSY experiments.
- Association between phosphodiesterase type 5 inhibitors and prostate cancer: A systematic review. [Journal Article]
- PUProg Urol 2018 Sep 07
- CONCLUSIONS: Based on this review, a change in our practice regarding pharmacological reeducation after radical prostatectomy is not justified.
- Contact Dermatitis to Medications and Skin Products. [Review]
- CRClin Rev Allergy Immunol 2018 Aug 25
- Consumer products and topical medications today contain many allergens that can cause a reaction on the skin known as allergic contact dermatitis. This review looks at various allergens in these prod...
Consumer products and topical medications today contain many allergens that can cause a reaction on the skin known as allergic contact dermatitis. This review looks at various allergens in these products and reports current allergic contact dermatitis incidence and trends in North America, Europe, and Asia. First, medication contact allergy to corticosteroids will be discussed along with its five structural classes (A, B, C, D1, D2) and their steroid test compounds (tixocortol-21-pivalate, triamcinolone acetonide, budesonide, clobetasol-17-propionate, hydrocortisone-17-butyrate). Cross-reactivities between the steroid classes will also be examined. Next, estrogen and testosterone transdermal therapeutic systems, local anesthetic (benzocaine, lidocaine, pramoxine, dyclonine) antihistamines (piperazine, ethanolamine, propylamine, phenothiazine, piperidine, and pyrrolidine), topical antibiotics (neomycin, spectinomycin, bacitracin, mupirocin), and sunscreen are evaluated for their potential to cause contact dermatitis and cross-reactivities. Finally, we examine the ingredients in the excipients of these products, such as the formaldehyde releasers (quaternium-15, 2-bromo-2-nitropropane-1,3 diol, diazolidinyl urea, imidazolidinyl urea, DMDM hydantoin), the non-formaldehyde releasers (isothiazolinones, parabens, methyldibromo glutaronitrile, iodopropynyl butylcarbamate, and thimerosal), fragrance mixes, and Myroxylon pereirae (Balsam of Peru) for contact allergy incidence and prevalence. Furthermore, strategies, recommendations, and two online tools (SkinSAFE and the Contact Allergen Management Program) on how to avoid these allergens in commercial skin care products will be discussed at the end.
- Warning For Oral Drugs Containing Benzocaine. [Journal Article]
- AJAm J Nurs 2018; 118(9):23-24
- Evaluation of the aggregation process in a mixture of propofol and benzocaine. [Journal Article]
- PCPhys Chem Chem Phys 2018 Aug 23
- We report on a mass-resolved IR spectrosopic study on propofol-benzocaine aggregates. This is a complex system due to the several conformational isomers that both monomers may adopt and to the combin...
We report on a mass-resolved IR spectrosopic study on propofol-benzocaine aggregates. This is a complex system due to the several conformational isomers that both monomers may adopt and to the combination of functional groups they present, which allow the molecules to interact in many possible ways. However, our results demonstrate that a single conformation is favored for each stoichiometry. In the heterodimer, propofol acts as a proton donor to the ester group of benzocaine, while the whole cluster is stabilized by dispersive forces. These dispersive forces account for an important part of the system's stabilization energy as the calculations suggest. Propofol does not show any affinity for the amino group of benzocaine, even when a second molecule of propofol is introduced. These results demonstrate the difficulty in anticipating the aggregation preferences of even small organic molecules.
- Blocking ion channels induced by antifungal lipopeptide syringomycin E with amide-linked local anesthetics. [Journal Article]
- SRSci Rep 2018 Aug 01; 8(1):11543
- The effects of the amide-linked (lidocaine (LDC), mepivacaine (MPV), prilocaine (PLC)) and ester-bound local anesthetics (benzocaine (BZC), procaine (PRC), and tetracaine (TTC)) on the pore-forming a...
The effects of the amide-linked (lidocaine (LDC), mepivacaine (MPV), prilocaine (PLC)) and ester-bound local anesthetics (benzocaine (BZC), procaine (PRC), and tetracaine (TTC)) on the pore-forming activity of the antifungal lipopeptide syringomycin E (SRE) in lipid bilayers were studied. Independently on electrolyte concentration in the membrane bathing solution the observed changes in conductance of SRE channels agreed with the altered membrane dipole potential under the action of ester-bound local anesthetics. Effects of aminoamides in diluted and concentrated solutions were completely different. At 0.1 M KCl (pH 7.4) the effects of amide-linked anesthetics were in accordance with changes in the membrane surface potential, while at 2 M KCl aminoamides blocked ion passage through the SRE channels, leading to sharp reductions in pore conductance at negative voltages and 100-fold decreases in the channel lifetimes. The effects were not practically influenced by the membrane lipid composition. The interaction cooperativity implied the existence of specific binding sites for amide-bound anesthetics in SRE channels.
- Benzocaine-induced stress in the euryhaline teleost, Centropomus parallelus and its implications for anesthesia protocols. [Journal Article]
- CBComp Biochem Physiol A Mol Integr Physiol 2018 Jul 26; 226:32-37
- The use of anesthetic in fish farming is a traditional practice which aims to reduce the stress caused by transport and handling. However, anesthesia-induction protocols are commonly established and ...
The use of anesthetic in fish farming is a traditional practice which aims to reduce the stress caused by transport and handling. However, anesthesia-induction protocols are commonly established and implemented without proper physiological/behavioral evaluation. Additionally, concentration and time of exposure to the anesthetic are often set without considering species-specific responses. The fat snook (Centropomus parallelus) is a fish with great potential for aquaculture. Given its remarkable euryhalinity, it can grow in fresh- or seawater. Most studies on fat snook anesthesia tested natural compounds (essential oils) instead of traditional anesthetics. However, the use of benzocaine is much more common in the commercial sector, as it is easy to obtain and of relatively low cost. The present study aimed at analyzing the effects benzocaine exposure on glucose and cortisol plasma levels (two traditional stress markers in teleost fish), as well as on plasma osmolality, chloride and magnesium, (indicators of osmo-ionic allostasis) in animals acclimated to different salinities. Results showed that while osmo-ionic allostasis was strictly maintained across the treatments, time of anesthesia had a strong positive relationship to plasma cortisol and glucose, regardless the salinity of exposure and acclimation. The results are discussed as they relate to anesthesia protocols and how stress response generated by time of anesthesia may challenge farming flexibility.
- Ear drops for the removal of ear wax. [Review]
- CDCochrane Database Syst Rev 2018 07 25; 7:CD012171
- CONCLUSIONS: Although a number of studies aimed to evaluate whether or not one type of cerumenolytic is more effective than another, there is no high-quality evidence to allow a firm conclusion to be drawn and the answer remains uncertain.A single study suggests that applying ear drops for five days may result in a greater likelihood of complete wax clearance than no treatment at all. However, we cannot conclude whether one type of active treatment is more effective than another and there was no evidence of a difference in efficacy between oil-based and water-based active treatments.There is no evidence to show that using saline or water alone is better or worse than commercially produced cerumenolytics. Equally, there is also no evidence to show that using saline or water alone is better than no treatment.
- The Analysis of the Physicochemical Properties of Benzocaine Polymorphs. [Journal Article]
- MMolecules 2018 Jul 16; 23(7)
- The study was a pioneering attempt to assess the influence of the structural polymorphism (forms I, II, III) of benzocaine on its solubility, apparent solubility, and chemical stability, which are vi...
The study was a pioneering attempt to assess the influence of the structural polymorphism (forms I, II, III) of benzocaine on its solubility, apparent solubility, and chemical stability, which are vital parameters for preformulation and formulation work. The impact of differences in the solubility of selected polymorphs of benzocaine on their permeability through artificial biological membranes (PAMPA system) was evaluated. The polymorphs of benzocaine were obtained by means of techniques commonly used for the preparation of various pharmaceutical dosage forms: ball milling, micro milling, and cryogenic grinding, which allowed for the appearance or preservation of form III, the initial conformation of benzocaine. Ball milling resulted in the conversion of form III to I, whereas micro milling yielded form II. As a result of cryogenic grinding, form III of benzocaine was preserved. The identification of all polymorphic forms of benzocaine was confirmed via X-ray powder diffraction (PXRD) supported by FT-IR spectroscopy coupled with density functional theory (DFT) calculations. The differences in solubility, dissolution, and permeability through artificial biological membranes resulting from the polymorphic forms of benzocaine were established by using chromatographic determinations. Accelerated stability tests indicated that all polymorphic forms were chemically stable at a required level.
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- Topical Transdermally Delivered Lidocaine and Benzocaine Compared to Compounded Lidocaine/Tetracaine During Microfocused Ultrasound With Visualization Treatment. [Journal Article]
- JDJ Drugs Dermatol 2018 Jul 01; 17(7):729-734
- CONCLUSIONS: Lidocaine 4% and benzocaine 20% formulations utilizing a novel transdermal delivery system perform similarly to compounded lidocaine 23%/tetracaine 7% for discomfort mitigation during MFU-V treatment. More subjects preferred lidocaine 4%/ benzocaine 20% and rated it as "very effective" vs the compounded product. Fewer treatment pauses due to patient discomfort when using the lidocaine 4%/benzocaine 20% may translate to time efficiency. J Drugs Dermatol. 2018;17(7):729-734.