Intranasal Microemulgel as Surrogate Carrier to Enhance Low Oral Bioavailability of Sulpiride

Ayoub, Abdallah Mohamed; Ibrahim, Mohammed; Abdallah, Marwa H.; Mahdy, Mahmoud A.

doi:10.22159/ijpps.2016v8i10.13776

Cited by 12 publications

(4 citation statements)

References 30 publications

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“…Modern researchers involved in topical semi-solid dosage forms quality assessment use a limited set of techniques to test the spreadability (various modifications of the parallel-plate method or the "slip and drag" method are most often used) [5][6][7][8][9][10][11][12][13][14][15]. In each same study, the conditions of the experiment are often subjected to significant or minor changes (parameters such as the exposure time of the load, the mass of the load, the mass of the dosage form, and the size of the glass plates).…”

Section: Discussionmentioning

confidence: 99%

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Dermatologic Gels Spreadability Measuring Methods Comparative Study

et al. 2022

Int J App Pharm

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Objective: The main objective of our study is the comprehensive analysis and characterization of the existing spreadability evaluation strategies, the comparison of the obtained results reproducibility and convergence through the example of the 9 most widely used dermatological gels. Methods: Dolobene®, Flucinar®, Ketorol®, Contractubex®, Dr. Theiss Venen gel®, Solcoseryl®, Deep Relief®, Hepatrombin® pharmacopoeia gel samples were analyzed using parallel-plate, “slip and drag”, and viscometry methods. Analysis was performed in flow mode at 32±0.2 °C, over shear rates ranging from 0 to 350 s−1, increasing over a period of 120 s, and was maintained at the superior limit for 10 s and then decreased during the same period. At least 5 replicates of each sample were evaluated, and the upward flow curves were fitted using the Casson mathematical model. Results: Solcoseryl® and Dolobene® showed the best spreadability in the parallel-plate method (3115.66±50.00 and 3316.63±50.00, respectively); Contractubex® and Dolobene showed the best spreadability in the “slip and drag” test (73.46±0.5 and 18.32±0.5, respectively); Solcoseryl® and Contractubex® showed the best spreadability in the viscometry test (43.86±0.5 and 76.92±0.5, respectively). Conclusion: This study analyzed the existing methods for determining the spreadability using commercially available samples of the dermatological gels as examples. The viscometric and the "Slip and drag" methods use different characteristics of spreadability, giving a complex evaluation of the measured parameter in vitro. Therefore, the combination of these two methods has the greatest prospects for reliable determination of this indicator.

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Section: Discussionmentioning

confidence: 99%

“…A weight (50-500 g) of 125 g is placed on top for 1 minute. Then the diameter of the sample between the plates is measured [7][8][9][10][11].…”

Section: Parallel-plate Methodsmentioning

confidence: 99%

Dermatologic Gels Spreadability Measuring Methods Comparative Study

et al. 2022

Int J App Pharm

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“…Then the beaker should be placed over the magnetic stirrer for 24hrs after 24 hrs. The samples were then filtered, suitably diluted and determined at 287 using a double beam spectrophotometer 15,16 .…”

Section: Saturation Solubilitymentioning

confidence: 99%

Untitled

2023

IJPSR

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Background: Solubility is an important boundary to obtaining the needed drug concentrations in systemic circulation for pharmacological response to be shown. In today"s time, poor water solubility is the crucial issue faced with developing new chemical entities. Objective: Cefixime trihydrate (CT) is an oral third-generation cephalosporin antibiotic used to treat bacterial diseases. It has an oral bioavailability of 40-50% and belongs to the BCS class-IV. This study aims to boost the solubility of poorly aqueous soluble anti-bacterial drug cefixime trihydrate (CT) by the hydrotropic solubilization technique. Methods: Hydrotropy is one of the solubility improvement techniques that enhance the solubility to many folds with hydrotropes. Sodium benzoate (SB) and piperazine (PP) are the hydrotropes that were selected for the preparation of solid dispersion to improve the solubility of cefixime trihydrate. Thus, prepared solid dispersions were evaluated for percentage yield, drug content, saturation solubility and in-vitro dissolution studies. Results: The result showed increased solubility and in-vitro drug release of CT compared to the pure drug. The solubility of cefixime trihydrate was enhanced 6 times by using two hydrotropes. Conclusion: In this work, it was concluded that the use of two hydrotropes gave an effective and safe approach to the solubility enhancement of CT. Hence, we can say that hydrotropic techniques can be used to improve the solubility of cefixime trihydrate. INTRODUCTION:Improving the solubility of the poorly aqueous soluble drug is one of the major current difficulties in the pharmaceutical sciences. The bioavailability of the drug depends on the dissolution rate and solubility, which can affect the drug's therapeutic activity. Various factors affect the solubility of a drug i.e temperature, molecular size, pressure, polymorph form, pH of solvent, nature of solute and solvent, porosity, etc.

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“…The co-surfactant's function in the pseudoternary system was able to reduce interfacial tension and boost the fluidity of the interface. Moreover, it makes the hydrocarbon tail more mobile, allowing more oil to penetrate the NE zone [43,48]. The optimum formula (F15) produces 100% release in 15 minutes, as seen in Figure 3, which depicts the release profile of NE formulations.…”

Section: Estimate Of Drug Contentmentioning

confidence: 99%

Lasmiditan Nanoemulsion Based in Situ Gel Intranasal Dosage Form: Formulation, Characterization and in Vivo Study

JABER

2023

FARMACIA

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This study aimed to formulate lasmiditan (LAS) as a nanoemulsion in situ gel (NEIG) by utilising nanotechnology in order to escape the problems associated with the poor oral bioavailability of the drug. A study regarding the LAS solubility in different oils, surfactants and co-surfactants, was determined. Different nanoemulsion (NE) formulations were prepared depending on the pseudo-ternary phase diagrams, which were first constructed. Visual characterization, thermodynamic stability study and droplet size were determined for the prepared NEs. Muco-ciliary clearance can be overcome with the in situ gelling agent carbopol 934, a pH-sensitive polymer that was selected to increase the residence time on the nasal mucosa. The gel strength, pH, gelation time and viscosity were predicted for the prepared NEIG. In vitro release and ex vivo nasal permeation were measured for both NE and NEIG formulations. Formula coded-15 (F15) with a droplet size of 58.4 nm provided a maximum in vitro as well as ex vivo permeation to be considered as a selected one, to which 0.5% carbopol 934 was added for the preparation of NEIG2 that exerts comparable release and permeation values as F15 with more residence time in order to overcome the normal nasal physiological clearance. Finally, LAS as NEIG2 was subjected to an in vivo study as a promising intranasal novel formula that exerts rapid onset of action (Tmax 0.75 hours) accompanied by higher bioavailability (2.5 folds) and tissue permeation (4 folds) relative to the oral dosage form (8% aqueous LAS suspension) was considered. RezumatStudiul a avut ca scop formularea lasmiditanului (LAS) sub forma unui gel de tip nanoemulsie in situ (NEIG) prin utilizarea nanotehnologiei, pentru a evita problemele asociate cu biodisponibilitatea orală scăzută a substanței. S-au preparat diferite nanoemulsii (NE) în funcție de diagramele de fază pseudoternare. Caracterizarea vizuală, studiul stabilității termodinamice și dimensiunea picăturilor au fost determinate pentru NE-urile preparate. Clearance-ul mucociliar poate fi redus cu ajutorul agentului de gelificare in situ carbopol 934, un polimer sensibil la pH care a fost selectat pentru a crește timpul de rezidență pe mucoasa nazală. Rezistența gelului, pH-ul, timpul de gelifiere și vâscozitatea au fost estimate pentru NEIG preparate. Cedarea in vitro și permeabilitatea nazală ex vivo au fost măsurate pentru ambele formulări NE și NEIG. Formula F15, cu o dimensiune a picăturilor de 58,4 nm, a prezentat o permeabilitate maximă in vitro, precum și ex vivo; la aceasta s-a adăugat 0,5% carbopol 934, rezultând NEIG2, care prezintă valori de cedare și permeabilitate comparabile cu F15, cu un timp de rezidență mai mare, ce depășește clearance-ul fiziologic nazal normal. În cele din urmă, LAS sub formă de NEIG2 a fost supus unui studiu in vivo, fiind considerat o formulă nouă intranazală promițătoare, care exercită un debut rapid al acțiunii (Tmax de 0,75 ore) însoțit de o biodisponibilitate mai mare (de 2,5 ori) și o permeabilitate tisulară (de 4 ori) în compa...

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Intranasal Microemulgel as Surrogate Carrier to Enhance Low Oral Bioavailability of Sulpiride

Cited by 12 publications

References 30 publications

Dermatologic Gels Spreadability Measuring Methods Comparative Study

Dermatologic Gels Spreadability Measuring Methods Comparative Study

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Lasmiditan Nanoemulsion Based in Situ Gel Intranasal Dosage Form: Formulation, Characterization and in Vivo Study

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