Formulation, evaluation and optimization of stomach specific in situ gel of clarithromycin and metronidazole benzoate.

Patel, Rakesh P.; Dadhani, B.; Ladani, R.; Baria, Ashok; Patel, Jigar P.

doi:10.5138/ijdd.2010.0975.0215.02023

Cited by 26 publications

(18 citation statements)

References 9 publications

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“…The gelation involves formation of double helical junction zone followed by aggregation of the double helical segments to form a three dimensional network by complexation with Ca +2 ions and hydrogen bonding with water. 27 It was observed that all formulations showed immediate gelation on contact with acidic environment and retained gel structure for more than 12 h. The rigidity of the gel confers controlled release property to the formulation as the drug molecules have to traverse through the complex network of polymer chains to reach the physiological environment.…”

Section: In Vitro Gelling Capacitymentioning

confidence: 96%

Controlled Release Ion Sensitive Floating Oral in situ Gel of a Prokinetic Drug using Gellan Gum.

Rao¹,

Shelar²

2015

IJPER

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There are various approaches commonly used for gastric retention, one of which is raft forming system. Floating oral in situ gel is a type of raft forming system. The present work concerns with the formulation, evaluation and optimization of floating oral in situ gel of Itopride Hydrochloride for controlled release. Gellan gum has been used as a gel forming polymer and calcium carbonate as cross linking agent and Ca 2+ ion source, and HPMC K100M as release retardant. The floating oral in situ gel undergoes gelation by ion sensitive mechanism. In this formulation 3 2 factorial designs was performed and the effect of variation in concentration of gellan gum and HPMC K100M on drug release at 1 h, 6 h, and viscosity was evaluated. The gel was evaluated for other parameters like floating lag time, floating duration, gel strength, density, pH, in vitro drug release, drug content, and in vitro gelling capacity. The results of 3 2 full factorial design revealed that the concentration of gellan gum and of HPMC K100M significantly affected the dependent variables i.e. drug release at 1 h, at 6 h, and viscosity. A controlled release profile was observed for these formulations. The drug release mechanism was found to follow Korsmeyer-Peppas model. In vivo studies revealed higher T max of gel compared to plain drug which is suggestive of slower absorption. However the AUC 0-12 h was found to be nearly 90% higher than plain drug.

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Section: In Vitro Gelling Capacitymentioning

confidence: 96%

Controlled Release Ion Sensitive Floating Oral in situ Gel of a Prokinetic Drug using Gellan Gum.

Rao¹,

Shelar²

2015

IJPER

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“…Accurately weighed solids were used to make the formulations as per the method described elsewhere 8,14 . Accordingly, in about 30 ml of deionized water, HPMC K4M was allowed to hydrate overnight.…”

Section: Methods: Preparation Of In Situ Gelling Formulationsmentioning

confidence: 99%

“…These systems can sustain drug release, improve bioavailability, reduce dosing frequency and improve patient acceptability 4,5 . These systems have been investigated for the gastric delivery of amoxicillin 6 , clarithromycin 7 , metronidazole 8 , acetohydroxamic acid 9 , and levofloxacin hemihydrates 10 for eradication of Helicobacter pylori (H. pylori) and showed significant anti-H.pylori effect than the conventional dosage forms.…”

mentioning

confidence: 99%

Untitled

2016

IJPSR

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Salbutamol is a selective β2-adreno-receptor stimulant and is given four times daily in a dose of 2.4 mg orally to maintain therapeutic blood level. It is known to be absorbed in proximal parts of the small intestine. Prolonging gastric residence time is, therefore, beneficial to improve its bioavailability. Hence, seven in situ gelling liquid formulations were prepared using sodium alginate (SA) as gel forming agent and HPMC as viscosity enhancer. CaCO 3 was incorporated as crosslinker and floating agent. Gelling capacity was evaluated based on a graded response which indicates rapidity of gelation and time taken by the gel to dissolve. All the formulations showed instant gelation but with regard to integrity, all formulations except the one with lowest SA level formed stiff gels maintaining integrity for at least 12 hr. With respect to floating behavior, all formulations except the one with the lowest SA level floated for more than 12 hr irrespective of their composition. Most of the formulations took less than 1 min to float but those with the lowest SA and CaCO 3 levels floated after about 2 min. Drug release study revealed release retarding behavior of the formulations and noticeable burst release. This effect was reduced at higher concentration of SA and CaCO 3 . Release retarding effect of SA was only marginal at higher concentrations. CaCO 3 showed a similar effect but at higher levels insignificant change in release was observed. The drug release process, in all cases, best fits first order kinetics (R2 ranged between 0.932 and 0.991) and in most cases it seemed to occur by non-Fickian mechanisms (0.43 < n < 0.85). In formulations with lowest levels of SA and CaCO 3 , quasi-Fickian diffusion (n < 0.43) process prevailed. The study demonstrated that the in situ gelling formulations can be used as novel formulations with sustained drug release, improved bioavailability and thereby improve patient compliance.

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“…In vitro Floating Study 28 The in vitro floating study was carried out using USP dissolution apparatus II having 500 ml of 0.1N HCl (pH 1.2) .The medium temperature was kept at 37 o C. Accurately weighed 10 mL of the prepared in situ gel formulations were drawn up using disposable syringe and placed into the Petridis (4.5 mm internal diameter) and finally the Petridis containing the formulation was kept in the dissolution vessel containing medium without much disturbance. The time the formulation took to emerge on to the medium surface (Floating Lag Time) and the time over which the formulation constantly floated on the dissolution medium surface Duration of Floating) were noted.…”

Section: 27mentioning

confidence: 99%

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

Bobade¹,

Pande²

2016

IJPER

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In present study is to develop Gastro-Retentive controlled release in situ gel using natural and synthetic polymers. Gastro-retentive controlled release in situ gels were prepared to controlled drug delivery, to improve bioavailability, stability, reducing side effects. For the present work 3 2 factorial designs was selected. The two independent variables were selected sodium alginate (X 1 ) and ratio of polymers HPMC K4M: Gellum Gum (X 2 ) combined concentration of HPMC K4M and Gellum Gum was kept constant i.e. 2% and nine formulations were formulated as per experimental design, From evaluation of in situ gel formulation for factorial batches, formulation HPGG7 has show good gel strength, lag time (98 ± 0.57) sec, pH value (7.4 ± 0.20), drug contain (99.92 ± 0.04)%, viscosity before and after gel (32715 ± 1.15) and (39850 ± 1.73)cp respectively, total floating time more than 24 hours and also have good controlled release behaviour as it retard drug release up to (79.2 ± 0.50) % . Formulated in situ gel were stable at the selected temperature and humidity in storage for 3 month. Hence, from above it was concluded that formulation, in situ gel formulation HPPGG7 was containing sodium alginate (1.5%)w/v, HPMC K4M (0.5%)w/v, Gellum gum (1.5%)w/v, which could be most promising gastro-retentive in situ gel formulation. It was concluded that the prepared controlled release in situ gel of Diltiazem Hydrochloride may prove to be potential candidate for safe and effective controlled drug delivery for extended period of time.

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Formulation, evaluation and optimization of stomach specific in situ gel of clarithromycin and metronidazole benzoate.

Cited by 26 publications

References 9 publications

Controlled Release Ion Sensitive Floating Oral in situ Gel of a Prokinetic Drug using Gellan Gum.

Controlled Release Ion Sensitive Floating Oral in situ Gel of a Prokinetic Drug using Gellan Gum.

Untitled

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

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