Physicochemical Properties, Formulation, and Drug Delivery

Barich, Dewey H.; Munson, Eric J.; Zell, Mark T.

doi:10.1002/9781118833322.ch3

Cited by 7 publications

(3 citation statements)

References 31 publications

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“…Obviously, not all marketed drugs achieve all of these parameters, and, for this reason, there is a vast scientific work toward finding new solid forms of APIs, in particular, for those exhibiting aqueous solubility issues. Drugs presenting low water solubility will pose low therapeutic effectiveness when orally administered. , In this sense, over the years, different techniques have been developed to enhance the final clinical/dosage efficiency of APIs in their solid-state form, such as formulation approaches; particle size reduction; nanocrystal approach; amorphization; synthesis of an API salt or cocrystal; and use of different polymorphs …”

Section: Introductionmentioning

confidence: 99%

Fluconazole: Synthesis and Structural Characterization of Four New Pharmaceutical Cocrystal Forms

Owoyemi

Silva

Souza

et al. 2019

Crystal Growth & Design

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Pharmaceutical cocrystals have emerged over the past several decades as an alternative path for synthesizing stable and/or improved crystalline forms of active pharmaceutical ingredients. In this contribution, we developed a reproducible cocrystallization path for the supramolecular synthesis of four new pharmaceutical cocrystal forms of fluconazole (FLZ), an antifungal multifunctional drug: fluconazole–fumaric acid monohydrate (1:1:1), fluconazole–malic acid (1:1), fluconazole–dipicolinic acid (1:1), and fluconazole–adipic acid (1:1). All the new cocrystals were characterized by powder/single-crystal X-ray diffraction, Raman, Fourier transform infrared spectroscopy, differential scanning calorimetry/thermogravimetric analysis, and hot-stage polarized optical microscopy, and their water solubility was determined. Structurally, although the coformers were different, the same strong O–H···N hydrogen bond between the FLZ molecule and the coformers was observed. The aqueous solubility studies revealed that all the cocrystals were found to exhibit improved aqueous solubility when compared to the commercialized FLZ polymorph.

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Section: Introductionmentioning

confidence: 99%

Fluconazole: Synthesis and Structural Characterization of Four New Pharmaceutical Cocrystal Forms

Owoyemi

Silva

Souza

et al. 2019

Crystal Growth & Design

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“…Localized administration of microdosed antibiotics within local anesthetic has a number of advantages. These include immediate and targeted delivery to the operative site, no additional punctures or injection volume requirements, guaranteed compliance with therapy, substantial reduction in systemic antibiotic selection pressure (particularly within gut flora), minimized risk of drug interactions, low cost, and a feasible and scalable applicability to high-volume skin cancer treatment centers …”

Section: Introductionmentioning

confidence: 99%

“…These include immediate and targeted delivery to the operative site, no additional punctures or injection volume requirements, guaranteed compliance with therapy, substantial reduction in systemic antibiotic selection pressure (particularly within gut flora), minimized risk of drug interactions, low cost, and a feasible and scalable applicability to high-volume skin cancer treatment centers. 19 The aim of the current Prophylactic Incisional Antibiotics in Skin Cancer Surgery (PICASSo) trial was to evaluate the safety and efficacy of a single preoperative microdose of locally infiltrated flucloxacillin or clindamycin for reducing SSIs in cutaneous surgery for skin cancer. We hypothesized that a significant reduction in SSI could be demonstrated with a single microdose of locally applied antibiotic relative to controls without adverse effects.…”

mentioning

confidence: 99%

Effect of Microdoses of Incisional Antibiotics on the Rate of Surgical Site Infections in Skin Cancer Surgery

et al. 2023

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ImportanceSurgical site infections (SSIs) represent a costly and preventable complication of cutaneous surgery. However, there is a paucity of randomized clinical trials investigating antibiotic prophylaxis for reducing SSIs in skin cancer surgery, and evidence-based guidelines are lacking. Incisional antibiotics have been shown to reduce the rate of SSIs before Mohs micrographic surgery, but this represents a small subset of skin cancer surgery.ObjectiveTo determine whether microdosed incisional antibiotics reduce the rate of SSIs before skin cancer surgery.Design, Setting, and ParticipantsIn this double-blind, controlled, parallel-design randomized clinical trial, adult patients presenting to a high-volume skin cancer treatment center in Auckland, New Zealand, for any form of skin cancer surgery over 6 months from February to July 2019 were included. Patient presentations were randomized to one of 3 treatment arms. Data were analyzed from October 2021 to February 2022.InterventionsPatients received an incision site injection of buffered local anesthetic alone (control), buffered local anesthetic with microdosed flucloxacillin (500 µg/mL), or buffered local anesthetic with microdosed clindamycin (500 µg/mL).Main Outcomes and MeasuresThe primary end point was the rate of postoperative SSI (calculated as number of lesions with SSI per total number of lesions in the group), defined as a standardized postoperative wound infection score of 5 or more.ResultsA total of 681 patients (721 total presentations; 1133 total lesions) returned for postoperative assessments and were analyzed. Of these, 413 (60.6%) were male, and the mean (SD) age was 70.4 (14.8) years. Based on treatment received, the proportion of lesions exhibiting a postoperative wound infection score of 5 or greater was 5.7% (22 of 388) in the control arm, 5.3% (17 of 323) in the flucloxacillin arm, and 2.1% (9 of 422) in the clindamycin arm (P = .01 for clindamycin vs control). Findings were similar after adjusting for baseline differences among arms. Compared with lesions in the control arm (31 of 388 [8.0%]), significantly fewer lesions in the clindamycin arm (9 of 422 [2.1%]; P &lt; .001) and flucloxacillin (13 of 323 [4.0%]; P = .03) arms required postoperative systemic antibiotics.Conclusions and RelevanceThis study evaluated the use of incisional antibiotics for SSI prophylaxis in general skin cancer surgery and compared the efficacy of flucloxacillin vs clindamycin relative to control in cutaneous surgery. The significant reduction in SSI with locally applied microdosed incisional clindamycin provides robust evidence to inform treatment guidelines in this area, which are currently lacking.Trial Registrationanzctr.org.au Identifier: ACTRN12616000364471

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Baicalein: Advances on Resources, Biosynthesis Pathway, Bioavailability, Bioactivity, and Pharmacology

Hritcu,

Edmond,

Eldahshan

2023

Handbook of Dietary Flavonoids

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Physicochemical Properties, Formulation, and Drug Delivery

Cited by 7 publications

References 31 publications

Fluconazole: Synthesis and Structural Characterization of Four New Pharmaceutical Cocrystal Forms

Fluconazole: Synthesis and Structural Characterization of Four New Pharmaceutical Cocrystal Forms

Effect of Microdoses of Incisional Antibiotics on the Rate of Surgical Site Infections in Skin Cancer Surgery

Baicalein: Advances on Resources, Biosynthesis Pathway, Bioavailability, Bioactivity, and Pharmacology

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