Formulation and Evaluation of Controlled Release Gastro-Retentive In situ Gel for Diltiazem Hydrochloride

Bobade, Nishan Naresh; Pande, Shrikant D.

doi:10.5530/ijper.50.3.36

Cited by 11 publications

(7 citation statements)

References 14 publications

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“…The parameters analyzed include appearance, in-vitro floating, in-vitro gelling capacity, viscosity, drug content and invitro drug release. From the stability study it was confirmed that the optimized formulation is stable at its storage temperature [23][24][25][26][27][28][29] . The prepared formulations were evaluated for visual inspection, surface pH, viscosity, in-vitro floating study, in-vitro gelling capacity, drug content, and in-vitro drug release.…”

Section: Discussionmentioning

confidence: 99%

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2020

IJPSR

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Floating drug delivery system comes with the advantage of sustained release of drugs over a prolonged period of time thereby maximizing the oral absorption of drugs with narrow absorption window, it overcomes the challenges of conventional oral drug delivery system. The aim of the present work was to develop a novel floating in-situ gelling system for sustained drug delivery of Clarithromycin for stomach ulcer. The in-situ gelling system were prepared by dissolving different concentrations of gelling polymers like sodium alginate, gellan gum in deionized water at 70 °C. After cooling to 40 °C fixed amount of drug, CaCO 3 and released retardant polymer xanthan gum were dispersed with continuous stirring. All formulations showed pH in the range of 6.72 to 7.25, drug content was found to be in the range of 86.66% to 96.66%, floating lag time was <2 min, duration of floating was >12 h for all the formulations. It was observed that viscosity of solution increases with an increase in polymer concentration. Invitro drug release was found to be in between 58.88% to 82.50% up to 12 h, and the maximum drug release was shown by formulation F1 (1.0%w/v sodium alginate). Drug release is inversely proportional to polymer concentration. The release kinetics of best formulation F7 (1.0%w/v sodium alginate and 0.25% w/v xanthan gum) followed first order with Higuchi diffusion mechanism. Hence, floating in-situ gelling system of Clarithromycin is a novel approach to increase patient compliance with reduced dosing frequency and increased residence time of drug in the stomach.

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Section: Discussionmentioning

confidence: 99%

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2020

IJPSR

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“…At the free end of the device a lightweight pan (3 g) was attached to which the weights were added. The gel strength was reported in terms of weight required to pass the apparatus through the formed gel mass 17,18 .…”

Section: Gel Strength Determinationmentioning

confidence: 99%

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2019

IJPSR

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The objective of the present study was to formulate and evaluate a gastro-retentive stomach specific novel floating in-situ gelling system of curcumin for potentially treating gastric ulcer, associated with Helicobacter pylori. The in-situ gel of curcumin was prepared by dissolving different concentrations of gelling polymer like sodium alginate in distilled water at 60 ºC. After cooling to 40 ºC, required quantities of sodium citrate and calcium carbonate were dispersed in it with continuous stirring followed by the addition of curcumin and sorbitol. Identification of drug was confirmed by DSC (melting point study), FTIR (functional groups study), and UV spectrophotometric analysis. Compatibility between drug and polymer were confirmed by DSC and FTIR studies. The micromeritic properties of curcumin were done, and all formulations showed pH in the range of 6.6 to 7.4, floating lag time was less than 1 min, duration of floating was more than 24 h for all the prepared formulations. Gelling capacity, gel strength, viscosity, and water uptake by the gel increased with the increase in sodium alginate concentration; the drug content was found to be in the range of 92.5 to 99.1%. Drug release was found to decrease with the increase in polymer concentration of gel. The release kinetics of all the formulations followed zero order mechanism. INTRODUCTION: Floating oral in-situ gel forming system are widely explored for gastro retention purposes and have a bulk density lower than gastric fluids and thus remain buoyant in the stomach without affecting the gastric emptying rate for a prolonged period. While the system is floating on gastric contents, the drug is released slowly at a desired rate from the system.

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“…The viscosity is an essential variable because it affects the gelation of the solution, the flow of the formulation, and time required for gelation [21]. The ease of swallowing FNI liquid primarily depends on the rheological properties of the solutions, and such similar fluid undergoes a rapid sol-gel transition due to ionic interaction with direct contact with stomach contents.…”

Section: Viscosity Measurement Of Fni Gelmentioning

confidence: 99%

Enhance Solubility and Prolong Release of Prochlorperazine Maleate Using Floating Nanoemulsion in Situ Gel

Аlmajidi¹,

Albaderi²,

Fadhel³

2019

Asian J Pharm Clin Res

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Objective: The objective of this study was to prepare floating gastric in situ gel of prochlorperazine maleate (PM) using nanoemulsion technology to improve drug solubility, bioavailability, reduce dosing frequency, and patient compliance.Methods: Eight nanoemulsion formulas (F1–F8) of PM were prepared by ultrasonication method using oil, surfactants: cosurfactants (Smix) with different types, concentrations, and ratios, and deionized distilled water. The nanoemulsion formulas were characterized to select the optimum recipe from which six floating in situ gel formulas (floating nanoemulsion in situ [FNI] 1-FNI 6) were prepared using sodium alginate as gelling agent, hydroxypropyl methylcellulose (HPMCK) 4M as rate retarding polymer, calcium chloride as cross-linking agent, calcium carbonate as floating agent, and sodium citrate as buffering and neutralizing gastric acid. All FNI formulas were subjected for the evaluation to assess the formulations suitability concerning the dosage form and intended therapeutic purpose.Results: Formulation variables such as the concentration of sodium alginate, HPMCK 4M, calcium carbonate, and calcium chloride affected the gelling properties, formulation viscosity, floating behavior, and in vitro drug release. Formulation FNI 6 showed acceptable floating lag time (55±2.3 s) and >12 h floating duration time, and observe prolong release of the drug in in-situ gelling preparation.Conclusion: The prepared FNI formulas of PM could float in the gastric conditions and released the drug in a sustained manner. The present formulation was enhanced drug solubility with good retention properties and better patient compliance.

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Formulation and Evaluation of Controlled Release Gastro-Retentive In situ Gel for Diltiazem Hydrochloride

Cited by 11 publications

References 14 publications

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Enhance Solubility and Prolong Release of Prochlorperazine Maleate Using Floating Nanoemulsion in Situ Gel

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