At the hospital, the pharmacist is constantly challenged to prepare extemporaneous solutions from tablets, capsules or drug powder for patients unable to swallow, such as pediatric, elderly and patients that use nasoenteric and nasogastric tubes. The preparation of extemporaneous solutions from capsules, tablets and drug powder requires stability studies analysis. This article is a bibliographic review of preparation of extemporaneous oral liquid from solid oral dosage forms used in clinical practice. The selected articles contain all the information regarding manipulation techniques, pharmaceutical excipients, packaging, storage conditions and results of stability studies above 90% performed by HPLC analysis. In addition, a situational analysis of the strategies for the preparation of the extemporaneous solution was described to help the manipulator in the decision. The preparation of extemporaneous solution from solid oral dosage forms is based on information from official compendium or scientific literature, to ensure safe and effective manipulated medicine.
In the present study, an inclusion complex composed of hydrocortisone acetate (HA) and 2-hydroxypropyl-β-cyclodextrin (HPβCD) was prepared according phases solubility diagram of Higuchi & Connors and by a method described by with minor modifications to improve the HA water solubility. This new method improved percentage of inclusion reaching the maximum percentage of inclusion (91.52±0.92%) using 5.75mM HA and 135mM HPβCD. This percentage of inclusion was higher than that found by Filipović-Grcić J et al.[1] which was 25%. The complex HA/HPβCD was characterized by 1 H-NMR through chemical shifts in 1 H NMR spectra after the inclusion of HA into the HPβCD cavity, especially H-3, H-5 and H-6 protons was observed to the formation of molecular inclusion complex. Other technique used to characterize the inclusion complex was FT-IR, which showed in the FT-IR spectra of inclusion complex no features bands similar to pure HA molecule; the spectrum is very similar to the HPβCD. The molecular modeling studies results are in agreement with the experimental data that estimates a HA/HPβCD molar ratio of 1:1. The calculated apparent stability constant (K S ) was 484 M -1. The results indicate that the HA/HPβCD inclusion complex is more water soluble than HA crystalline powder (pure), the AH solubility was increased on the order of 64 times.
Background:
Severe Acute Respiratory Syndrome Coronavirus 2, initially first appeared in China and spread
rapidly around the world, causing a pandemic. Due to the absence of an effective vaccine, many drugs have been
extensively studied for the treatment of SARS-CoV-2.
Objective:
The aim of this work is to provide a current trend of potential drugs for the treatment of SARS-CoV-2, through
literature research over drug repositioning.
Methods:
A literature review was performed on databases such as PubMed, ScienceDirect, Scielo, Lilacs, World Health
Organization and Clinical Trials to identify relevant articles of drugs used for the treatment of SARS-CoV-2 since 2003 up
to 2020.
Results and Discussion :
Nelfinavir presented favorable results in molecular modelling and in vitro studies.
Hydroxychloroquine and Chloroquine showed positive results, nevertheless, the World Health Organization discontinued
the clinical trials because these drugs might increase the frequency of ventricular arrhythmias. Darunavir and Ribavirin
presented one positive and negative result for molecular modelling and in vitro studies, respectively. The combination of
Lopinavir/Ritonavir and Umifenovir alone demonstrated negative results in the clinical trials performed. Remdesivir was the
major drug tested which presented more positive results.
Conclusion:
The data do not support the use of Lopinavir/Ritonavir and Umifenovir with the potential for treatment against
SARS-CoV-2. Nelfinavir has potential to be explored against SARS-CoV-2. Due to the union of several positive results
obtained from studies against SARS-CoV-2, the Remdesivir should be explored as the most effective drug for the potential
treatment against this virus.
DEET is considered the gold standard for insect repellent products. However, it behaves as a strong skin permeant. DEET was encapsulated in Solid Lipid Microparticles (SLM) and characterized in terms of morphology, particle size, cytotoxicity and ex vivo permeation. The particles exhibited micrometric size with a spherical shape. In addition, we developed and validated an analytical method for DEET quantifi cation by high performance liquid chromatography (HPLC), which was selective, linear, precise, accurate and robust. The toxicity test in cell culture of keratinocytes, fi broblasts and macrophages showed that the formulation did not present cytotoxicity. The SLM were able to decrease the skin permeation of DEET in relation to the free active in ethanol with gain in the safe.Microparticles were able to increase the skin retention of DEET, which can contribute to extend the time of repellent action. The results showed that Solid Lipid Microparticles are safe and promising topical formulation to insect bite prevention.
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