In vitro dissolution method for evaluation of buprenorphine in situ gel formulation: A technical note

Objective: The objective of this study was to find the best base mixture composition (poloxamer 407 and HPMC) of chloramphenicol in situ gel formula based on in vitro property (Cumulative amount of drug release). Methods: The in vitro diffusion of chloramphenicol in situ gel study was carried out using franz diffusion cells to know the effect of the Critical Process Parameters (CPPs) as independent variables (poloxamer 407 and hydroxypropyl methylcellulose (HPMC)) on the Critical Quality Attribute (CQA) as dependent variable (cumulative amount of drug release) with 22 factorial design. Results: 22 factorial design of chloramphenicol in situ gel yielded 4 variations of poloxamer 407 and HPMC bases component in %w/v as follows, F1 (5:0.45), F2 (10:0.45) F3 (5:1) and F4 (10:1). The amount of drug release results from in vitro dissolution assay were 30.60% (F1), 45.64% (F2), 58.30% (F3), and 22.50%) (F4). Conclusion: Formula 3 (F3) was considered as the best formula component in terms of in vitro assay of chloramphenicol in situ gel with a desirability value of 0.58.

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Design and optimization of novel in situ gel of mercaptopurine for sustained drug delivery

Brazilian Journal of Pharmaceutical Sciences ◽

10.1590/s1984-82502011000100011 ◽

2014 ◽

Vol 50 (1) ◽

pp. 107-119 ◽

Cited By ~ 7

Author(s):

R. Nagendra ◽

Roopa S. Pai ◽

Gurinder Singh

Keyword(s):

Sodium Chloride ◽

Xanthan Gum ◽

Oral Absorption ◽

In Vitro Dissolution ◽

Disintegration Time ◽

In Situ Gel ◽

Weight Variation ◽

Swelling Studies

Mercaptopurine is a purine antagonist, belonging to the class of antimetabolites. Its oral absorption is erratic and variable throughout GIT, with bioavailability of 5-37% and belongs to Biopharmaceutical Classification System (BCS) class IV. The focus of the present study was to improve solubility of mercaptopurine and to release the drug uniformly throughout the GIT by formulating into a novel in situ gel tablet. By in vitro swelling studies, xanthan gum was selected as the best gelling polymer and the tablets were prepared by direct compression. Sodium chloride was used as a release modifier to improve the release of drug from the tablet. A 32 full factorial design was applied to optimize the percentage of xanthan gum and sodium chloride to get desired swelling index and release profile. Tablets were evaluated for weight variation, hardness, friability, disintegration time, drug content, in vitro swelling studies and in vitro dissolution studies. The best optimized formulation showed good swelling index and extended the release up to 12 h, where as conventional tablet released the drug within 45 min. The results indicate that mercaptopurine loaded in situ gel tablet could be effective in sustaining drug release for a prolonged period of time throughout the GIT, which can possibly improve the oral bioavailability.

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In vitro dissolution method fitted to in vivo absorption profile of rivaroxaban immediate-release tablets applying in silico data

Drug Development and Industrial Pharmacy ◽

10.1080/03639045.2017.1411939 ◽

2017 ◽

Vol 44 (5) ◽

pp. 723-728 ◽

Cited By ~ 1

Author(s):

Nathalie R. Wingert ◽

Natália O. dos Santos ◽

Sarah C. Campanharo ◽

Elisa S. Simon ◽

Nadia M. Volpato ◽

...

Keyword(s):

In Silico ◽

Immediate Release ◽

In Vitro Dissolution ◽

Absorption Profile ◽

Dissolution Method ◽

In Vivo Absorption

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In Vitro Dissolution Testing with Flow-Through Method: A Technical Note

AAPS PharmSciTech ◽

10.1208/s12249-009-9339-6 ◽

2009 ◽

Vol 10 (4) ◽

Cited By ~ 16

Author(s):

Zongming Gao

Keyword(s):

Technical Note ◽

In Vitro Dissolution ◽

Dissolution Testing ◽

Flow Through

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Facile one pot microbe-mediated in situ synthesis and antibacterial activity of reduced graphene oxide-silver nanocomposite

Nanotechnology ◽

10.1088/1361-6528/ac4521 ◽

2021 ◽

Author(s):

Ashwini Patil

Keyword(s):

Antibacterial Activity ◽

Graphene Oxide ◽

Zeta Potential ◽

Reduced Graphene Oxide ◽

In Vitro Dissolution ◽

Size Analysis ◽

X Ray ◽

Reduced Graphene

Abstract The present research deals with the development of a novel bioinspired in situ fabrication of reduced graphene oxide (rGO)-silver nanoparticle (AgNPs) nanocomposite (rGO@AgNCs) using microbes namely Pseudomonas aeruginosa (PA) and Staphylococcus aureus (SA). The fabricated rGO@AgNCs were characterized using Ultraviolet-visible (UV) spectroscopy, Fourier-transform infrared spectroscopy (FTIR), particle size analysis, polydispersity index (PDI), zeta potential analysis, energy dispersive X-ray analysis (EDAX), Raman spectroscopy, powder X-ray diffraction (PXRD), high-resolution transmission electron microscopy (HR-TEM) analysis, etc. Furthermore, the rGO@AgNCs-PA and rGO@AgNCs-SA interaction with serum protein, pH stability study, and in vitro dissolution of AgNPs were also performed. The research findings of the proposed study demonstrated the simultaneous reduction of graphene oxide (GO) and AgNPs and the formation of rGO@AgNCs in the presence of microbes. The in vitro dissolution studies of rGO@AgNCs composites showed better AgNPs dissolution with controlled release and offered remarkable matrix integrity throughout the dissolution period. The size and stability of rGO@AgNCs-PA and rGO@AgNCs-SA had no significant changes at physiological pH 7.4. A minimal decrease in the zeta potential of rGO@AgNCs was observed, which may be due to the weak interaction of nanocomposites and albumin. The antibacterial application of the synthesized nanocomposite was evaluated against a pathogenic mastitis-forming bacterium. The obtained results suggested an admirable antibacterial activity of synthesized nanocomposites against the tested microbes. This knowledge will assist the scientific fraternity in designing novel antibacterial agents with enhanced antibacterial activity against various veterinary pathogens in near future.

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DEVELOPMENT AND CHARACTERIZATION OF IN SITU GEL OF XANTHAN GUM FOR OPHTHALMIC FORMULATION CONTAINING BRIMONIDINE TARTRATE

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i7.25221 ◽

2018 ◽

Vol 11 (7) ◽

pp. 277 ◽

Cited By ~ 3

Author(s):

Vazir Ashfaq Ahmed ◽

Divakar Goli

Keyword(s):

Drug Release ◽

Xanthan Gum ◽

Gelation Time ◽

Gel Strength ◽

Eye Drops ◽

In Situ Gel ◽

23 Factorial Design ◽

Brimonidine Tartrate

Objective: The goal of this study was to develop and characterize an ion-activated in situ gel-forming brimonidine tartrate, solution eye drops containing xanthan gum as a mucoadhesive polymer.Method: Sol-gel formulation was prepared using gellan gum as an ion-activated gel-forming polymer, xanthan gum as mucoadhesive agent, and hydroxypropyl methyl cellulose (HPMC E50LV) as release retardant polymer. Phenylethyl alcohol is used as preservatives in borate buffer. The 23 factorial design was employed to optimize the formulation considering the concentration of gelrite, xanthan gum and HPMC as independent variables, gelation time, gel strength, and mucoadhesive force (N). Gelation time , gel strength, mucoadhesive force (N), viscosity (cP) and in vitro percentage drug release were chosen as dependent variables. The formulation was characteristics for pH, clarity, isotonicity, sterility, rheological behavior, and in vitro drug release, ocular irritation, and ocular visualization.Result: Based on desirability index of responses, the formulation containing a concentration of gelrite (0.4%), xanthan gum (0.21%), and HPMC (HPMC E50 (0.24%) was found to be the optimized formulation concentration developed by 23 factorial design. The solution eye drops resulted in an in situ phase change to gel-state when mixed with simulated tear fluid. The gel formation was also confirmed by viscoelastic measurements. Drug release from the gel followed non-fickian mechanism with 88% of drug released in 10 h, thus increased the residence time of the drug.Conclusion: An in situ gelling system is a valuable alternative to the conventional system with added benefits of sustained drug release which may ultimately result in improved patient compliance.

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IN SITU GEL AS PLATFORM FOR KETOCONAZOLE SLOW RELEASE DOSAGE FORM

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2018v10i5.27849 ◽

2018 ◽

Vol 10 (5) ◽

pp. 76

Author(s):

Methaq Hamad Sabar ◽

Iman Sabah Jaafar ◽

Masar Basim Mohsin Mohamed

Keyword(s):

Drug Release ◽

Guar Gum ◽

Polymer Concentration ◽

Hydroxypropyl Methylcellulose ◽

In Vitro Release ◽

High Viscosity ◽

In Situ Gel ◽

Alginate Concentration

Objective: The aim of this study was to formulate ketoconazole (keto) as oral floating in situ gel to slow the release of keto in the stomach.Methods: Sodium alginate (Na alginate) was used as a primary polymer in the preparation of the in situ gel and was supported by the following polymers: guar gum (GG), hydroxypropyl methylcellulose (HPMC) K4M, K15M and carbapol 940 as viscosity enhancing agents. As a consequence, and to complete the gelation process of above formulations was by adding the calcium carbonate (CaCO3). The in situ gels were investigated by the following tests: floating lag time, floating duration, viscosity, drug content, in vitro gelling studies and in vitro release study.Results: The study showed that the faster release was obtained with F1 which contained Na alginate alone. Additionally, reduction in Na alginate concentration resulted in significant increase in drug release. It was also noted that the increase in GG (viscosity enhancing polymer) concentration resulted in non-significant decrease in percent drug release and the reduction in CaCO3 concentration led to significant increase in drug release. Moreover, the release of drug was also affected by grade of viscosity enhancing polymer, the faster release was observed with the formula which contained a polymer of low viscosity (HPMC K4M) and an opposite result was with the high viscosity polymer (HPMCK15M).Conclusion: This study showed the formulation of Na alginate with GG and CaCO3, led to gain floating in situ gel and a sustained release of keto.

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