Abstract:The lists of essential medicines of the World Health Organization (WHO) and Brazil include gliclazide as an alternative to the oral antidiabetic drug of first choice, metformin, in the treatment of type 2 diabetes mellitus because of its pharmacokinetic profile and few side effects. Thus, it is also considered by WHO and the International Pharmaceutical Federation (FIP) as a drug candidate to biowaiver, which is the evaluation of how favorable the biopharmaceutics characteristics are in order to obtain waiver … Show more
“…1a are several examples of sulfonamide-containing drugs, including hydrochlorothiazide, 2 macitentan, 3 sulfamethoxazole, 4 pazopanib, 5 and gliclazide. 6 bioactive molecules. 7 It is also established that further synthetic transformations of sulfonamides prepared from ammonia and primary amines can offer new structures and properties.…”
A carbene-catalyzed method for highly enantioselective modification of sulfonamides is disclosed. The reaction proceeds under mild conditions with broad substrate scope, wide functional group tolerance, and good to excellent yields....
“…1a are several examples of sulfonamide-containing drugs, including hydrochlorothiazide, 2 macitentan, 3 sulfamethoxazole, 4 pazopanib, 5 and gliclazide. 6 bioactive molecules. 7 It is also established that further synthetic transformations of sulfonamides prepared from ammonia and primary amines can offer new structures and properties.…”
A carbene-catalyzed method for highly enantioselective modification of sulfonamides is disclosed. The reaction proceeds under mild conditions with broad substrate scope, wide functional group tolerance, and good to excellent yields....
“…The appearance of the characteristic peaks of the drug and polymers in the FTIR spectra of the physical mixtures of GZ with HPC, PVA, and carbopol ( Figure 4B ) exposed the absence of physicochemical interactions between the drug and polymers. 38 , 40 Figure 4 FTIR spectrum of GZ ( A ), and mixture blend of F10 components ( B ). …”
Section: Resultsmentioning
confidence: 99%
“…The appearance of the characteristic peaks of the drug and polymers in the FTIR spectra of the physical mixtures of GZ with HPC, PVA, and carbopol (Figure 4B) exposed the absence of physicochemical interactions between the drug and polymers. 38,40 Table 2 shows the average weight of the films, as well as the standard deviation of the weight measurements. Results reveal that the average weight of all formulated films ranged between 0.047±0.002 and 0.081±0.003.…”
Objective
Development and evaluation of bucco-adhesive films of Gliclazide for pediatric use.
Methods
Sixteen films were formulated using a different combination of Gelatin, Hydroxy propyl methyl cellulose (HPMC), polyvinyl alcohol, Hydroxy propyl cellulose (HPC), chitosan, polyethylene glycol, sodium alginate, and carbopol. Compatibility study for drug and polymers was conducted using differential scanning calorimetry method and Fourier transform infrared spectroscopy. All films were examined for drug content, weight variation, thickness, swelling index, muco-adhesion and folding endurance. In vitro drug release has been completed for two hours. Stability studies were conducted at 4°C, 25°C, and 40°C for selected films. The optimized formulation based on in vitro data was selected for a bioavailability study in rabbits.
Results
The selected film formula (carbopol 2%, HPMC 2%) did not demonstrate interactions between the drug and polymers, while it showed accepted content, muco-adhesion, and mechanical properties. The in vitro release study showed rapid and complete release of drug from films. Stability studies confirmed accepted stability of the selected film at 4°C and 25°C, but the film get hard with few particles at 40°C. The bioavailability studies conducted showed that there was 2.1 fold increase in the AUC
0-24
of selected film compared with oral tablets.
Conclusion
Bucco adhesive films of Gliclazide is a promising dosage form for the treatment of diabetes in children.
“…Various strategies were investigated for the extended-release formulations of antidiabetic drugs such as matrix sustained-release tablets, orodispersable tablets, and depots. 120 - 122 Nevertheless, MDDS had granted great attention to this application. Biodegradable polymeric MPs were used extensively to retard drug release, reduce dosing frequency, and enhance bioavailability and safety.…”
Section: Therapeutic Applications Of Antidiabetic Loaded Microparticlesmentioning
Microparticulate drug delivery system (MDDS) has attained much consideration in the modern era due to its effectiveness in overcoming traditional treatment problems. Microparticles are spherical particles of a diameter ranging from 10 μm to 1000 μm. Microparticles can encapsulate both water-soluble and insoluble compounds. MDDS proved their efficacy in improving drugs bioavailability, stability, targeting, and controlling their release patterns. Microparticles also offer comfort, easy administration, and improvement in patient compliance by reducing drugs toxicity and dosage frequency. This review elucidates the fabrication techniques, drug release, and therapeutic application of MDDS. Further details concerning the therapeutic applications of antidiabetic drugs-loaded microparticles were also reviewed, including controlling drugs release by gastroretention, improving drugs dissolution, reducing side effects, localizing drugs to the site of disease, improving insulin stability, natural products loaded with microparticles, sustained drug release, mucosal delivery, and administration routes. Additionally, the current situation and future prospects in developing microparticles loaded with antidiabetic drugs were discussed.
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