scholarly journals Formulation and Evaluation of Floating Oral In Situ Gelling System of Amoxicillin

2011 ◽  
Vol 2011 ◽  
pp. 1-8 ◽  
Author(s):  
Dasharath M. Patel ◽  
Divyesh K. Patel ◽  
Chhagan N. Patel
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
Lag Time ◽  
Solution Viscosity ◽  
High Dose ◽  
In Situ Gelling

Purpose. Effective Helicobacter pylori eradication requires delivery of the antibiotic locally in the stomach. High dose of amoxicillin (750 to 1000 mg) is difficult to incorporate in floating tablets but can easily be given in liquid dosage form. Keeping the above facts in mind, we made an attempt to develop a new floating in situ gelling system of amoxicillin with increased residence time using sodium alginate as gelling polymer to eradicate H. pylori. Methods. Floating in situ gelling formulations were prepared using sodium alginate, calcium chloride, sodium citrate, hydroxypropyl methyl cellulose K100, and sodium bicarbonate. The prepared formulations were evaluated for solution viscosity, floating lag time, total floating time, and in vitro drug release. The formulation was optimized using a 32 full factorial design. Dissolution data were fitted to various models to ascertain kinetic of drug release. Regression analysis and analysis of variance were performed for dependent variables. Results. All formulations (F1–F9) showed floating within 30 s and had total floating time of more than 24 h. All the formulations showed good pourability. It was observed that concentration of sodium alginate and HPMC K100 had significant influence on floating lag time, cumulative percentage drug release in 6 h and 10 h. The batch F8 was considered optimum since it showed more similarity in drug release () to the theoretical release profile. Conclusion. Floating in situ gelling system of amoxicillin can be formulated using sodium alginate as a gelling polymer to sustain the drug release for 10 to 12 h with zero-order release kinetics.

scholarly journals FORMULATION AND EVALUATION OF FLOATING ORAL IN SITU GEL OF DILTIAZEM HYDROCHLORIDE

2016 ◽  
Vol 9 (1) ◽  
pp. 50
Author(s):  
A. Maheswaran ◽  
J. Padmavathy ◽  
V. Nandhini ◽  
D. Saravanan ◽  
P. Angel
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Polymer Concentration ◽  
Methyl Cellulose ◽  
Diltiazem Hydrochloride ◽  
Release Formulation ◽  
Gelling Properties ◽  
In Situ Gelling

Objective: The objective of the present study was to formulate and evaluate the floating in-situ gelling system of diltiazem hydrochloride.Methods: Sodium alginate based diltiazem hydrochloride floating in situ gelling systems were prepared by dissolving hydroxyl propyl methyl cellulose (HPMC) in 25% of water, to which calcium carbonate and diltiazem hydrochloride were added with stirring to form, a proper and a homogenous dispersion of diltiazem hydrochloride. Meanwhile, 30% of water was heated to 60 ˚C on a hot plate to dissolve sodium alginate and cooled to 40 ˚C. The resulting solution was added to HPMC solution and mixed well. To 5% of water at 60 ˚C, sodium methyl paraben was added and dissolved and cooled to 40 ˚C and was added to the above mixture and mixed well. The volume was adjusted finally to 100% with distilled water. Prepared formulae were evaluated for physicochemical properties, drug content, pH, in vitro gelling capacity, in vitro buoyancy, viscosity, water uptake and in vitro drug release.Results: Formulation variables such as type and concentration of viscosity enhancing polymer (sodium alginate) and HPMC affected the formulation viscosity, gelling properties, floating behavior, and in vitro drug release. Formulation F5 and F6 showed the floating time of 5 min and more than 20 h respectively. A significant decrease in the rate and extent of the drug release was observed with the increase in polymer concentration in in-situ gelling preparation. Formulation F4, F5, F6 were shown to have extended drug release until the end of 7 h.Conclusion: The prepared in situ gelling formulations of diltiazem hydrochloride could float in the gastric conditions and released the drug in a sustained manner. The present formulation was non-irritant, easy to administer along with good retention properties, better patient compliant and with greater efficacy of the drug.

DESIGN, CHARACTERIZATION AND EVALUATION OF MUCOADHESIVE NASAL IN SITU GELLING FORMULATIONS OF VENLAFAXINE HYDROCHLORIDE FOR BRAIN TARGETTING

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (01) ◽  
pp. 25-31
Author(s):  
M Priyanka ◽  
◽  
F. S. Dasankoppa ◽  
H. N Sholapur ◽  
NGN Swamy ◽  
...  
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Linear Regression Analysis ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Drug Content ◽  
Venlafaxine Hydrochloride ◽  
In Situ Gelling

The poor bioavailability and the therapeutic effectiveness exhibited by the anti-depressant venlafaxine hydrochloride on oral administration is overcome by the use of ion-activated gel forming systems that are instilled as drops; these undergo gelation in the nasal cavity. The present study describes the design, characterization and evaluation of mucoadhesive nasal in situ gelling drug delivery of venlafaxine hydrochloride using different polymers like sodium alginate, HPMC and pectin in various concentrations. DSC studies revealed compatibility of the drug and excipients used. The in situ gels were characterized for physicochemical parameters, gelling ability, rheological studies, drug content, drug entrapment efficiency, in vitro mucoadhesive strength, water holding capacity, gel expansion coefficient and in vitro drug release studies. The amount of polymer blends was optimized using 23 full factorial design. The influence of experimental factors on percentage cumulative drug release at the end of 2 and 8 hours were investigated to get optimized formulation. The responses were analyzed using ANOVA and polynomial equation was generated for each response using multiple linear regression analysis. Optimized formulation, F9, containing 1.98% w/V sodium alginate, 0.64% w/V hydroxylpropyl methylcellulose, 0.99% w/V pectin showed percentage cumulative drug release of 19.33 and 80.44 at the end of 2 and 8 hours, respectively, which were close to the predicted values. The optimized formulation was subjected to stability study for three months at 300C /75% RH. The stability study revealed no significant change in pH, drug content and viscosity. Thus, venlafaxine hydrochloride nasal mucoadhesive in situ gel could be successfully formulated to improve bioavailability and to target the brain.

scholarly journals DEVELOPMENT AND EVALUATION OF AN IN SITU THERMOGELLING SYSTEM OF OFLOXACIN FOR CONTROLLED OCULAR DELIVERY

2019 ◽  
pp. 567-570 ◽  
Author(s):  
ANANTH PRABHU ◽  
MARINA KOLAND
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Poloxamer 407 ◽  
Temperature Sensitive ◽  
Gelation Temperature ◽  
Mucoadhesive Polymers ◽  
In Situ Gelling

Objective: The purpose of this study was to develop an in situ ocular gel of ofloxacin which aimed to prolong corneal residence time while controlling drug release. Method: In situ gelling solutions were prepared from Poloxamer 407, a temperature-sensitive gelling polymer and to which, mucoadhesive polymers such as hydroxypropyl methyl cellulose 15 cps and polyvinyl alcohol (PVA) were included to provide corneal adhesion. Drug incorporated gels were prepared and evaluated for their appearance, pH, gelation temperature, and in vitro drug release studies. Results: Incorporation of the drug into the formulation increased the gelation temperature while the addition of mucoadhesive polymers decreased the gelation temperature. Increasing the concentration of bio-adhesive polymers retarded the release of ofloxacin from the poloxamer solutions and drug release was sustained over a period of 9 h. PVA had no significant effect on the gelation temperature and could not sustain the drug release for a longer duration. The in vitro release profiles of the drug from all the formulations could be best expressed by Higuchi’s equation which indicated that gels followed matrix diffusion process and drug release from gel formulations followed first-order process. Conclusion: The results showed that the developed system would be promising in the treatment of ocular infections with the combined advantages of ease of administration, the accuracy of dosing, increased bioavailability, and prolonged retention time.

scholarly journals Formulation and characterization of a novel pH-triggered in-situ gelling ocular system containing Gatifloxacin

1970 ◽  
Vol 1 (3) ◽  
pp. 43-49 ◽  
Author(s):  
Jovita Kanoujia ◽  
Kanchan Sonker ◽  
Manisha Pandey ◽  
Koshy M Kymonil ◽  
Shubhini A Saraf
Keyword(s):  
Drug Release ◽  
Research Work ◽  
Gelling Agent ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Carbopol 940 ◽  
In Situ Gelling ◽  
Gel Transition

The present research work deals with the formulation and evaluation of in-situ gelling system based on sol-to-gel transition for ophthalmic delivery of an antibacterial agent gatifloxacin, to overcome the problems of poor bioavailability and therapeutic response exhibited by conventional formulations based a sol-to-gel transition in the cul-de-sac upon instillation. Carbopol 940 was used as the gelling agent in combination with HPMC and HPMC K15M which acted as a viscosity enhancing agent. The prepared formulations were evaluated for pH, clarity, drug content, gelling capacity, bioadhesive strength and in-vitro drug release. In-vitro drug release data of optimized formulation (F12) was treated according to Zero, First, Korsmeyer Peppas and Higuchi kinetics to access the mechanism of drug release. The clarity, pH, viscosity and drug content of the developed formulations were found in range 6.0-6.8, 10-570cps, 82-98% respectively. The gel provided sustained drug release over an 8 hour period. The developed formulation can be used as an in-situ gelling vehicle to enhance ocular bioavailability and the reduction in the frequency of instillation thereby resulting in better patient compliance. Key Words: In-situ gelation; Gatifloxacin; Carbopol 940; HPMC K15M. DOI: http://dx.doi.org/10.3329/icpj.v1i3.9661 International Current Pharmaceutical Journal 2012, 1(3): 43-49

scholarly journals DESIGN AND EVALUATION OF CONTROLLED-RELEASE OCULAR INSERTS OF BRIMONIDINE-TARTRATE AND TIMOLOL MALEATE

2016 ◽  
Vol 9 (1) ◽  
pp. 79 ◽  
Author(s):  
Preethi G. B. ◽  
Prashanth Kunal
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Sodium Alginate ◽  
Calcium Chloride ◽  
Release Kinetics ◽  
Water Soluble ◽  
Moisture Loss ◽  
Timolol Maleate ◽  
Brimonidine Tartrate

<p><strong>Objective: </strong>The current work was attempted to formulate and evaluate a controlled-release matrix-type ocular inserts containing a combination of brimonidine tartrate and timolol maleate, with a view to sustain the drug release in the cul-de-sac of the eye.<strong></strong></p><p><strong>Methods: </strong>Initially, the infrared studies were done to determine the drug–polymer interactions. Sodium alginate-loaded ocuserts were prepared by solvent casting technique. Varying the concentrations of polymer—sodium alginate, plasticizer—glycerine, and cross-linking agent—calcium chloride by keeping the drug concentration constant, made a total of nine formulations. These formulations were evaluated for its appearance, drug content, weight uniformity, thickness uniformity, percentage moisture loss, percentage moisture absorption, and <em>in vitro </em>release profile of the ocuserts. Finally, accelerated stability studies and the release kinetics were performed on the optimised formulation.<strong></strong></p><p><strong>Results: </strong>It was perceived that polymer, plasticizer, and calcium chloride had a significant influence on the drug release. The data obtained from the formulations showed that formulation—F9 was the optimised formulation, which exhibited better drug release. The release data of the optimised formulation tested on the kinetic models revealed that it exhibited first-order release kinetics. <strong></strong></p><p><strong>Conclusion: </strong>It can be concluded that a natural bioadhesive hydrophilic polymer such as sodium alginate can be used as a film former to load water soluble and hydrophilic drugs like brimonidine tartrate and timolol maleate. Among all formulations, F9 with 400 mg sodium alginate, 2% calcium chloride and 60 mg glycerin were found to be the most suitable insert in terms of appearance, ease of handling, thickness, <em>in vitro</em> drug release and stability.</p>

scholarly journals FORMULATION AND EVALUATION OF MUCOADHESIVE MICROSPHERES OF AN ANTI-MIGRAINE DRUG

2018 ◽  
Vol 8 (5) ◽  
pp. 465-474
Author(s):  
S PADMA PRIYA ◽  
AN Rajalakshmi ◽  
P Ilaveni
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Sodium Alginate ◽  
Release Kinetics ◽  
Drug Loading ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Polyvinyl Pyrrolidone ◽  
Anti Migraine Drug

Objective: The objective of this research work is to develop and evaluate mucoadhesive microspheres of an anti-migraine drug for sustained release. Materials and Methods:  Mucoadhesive microspheres were prepared by emulsification method using Sodium alginate (SA), polyvinyl pyrrolidone (PVP) and Chitosan in the various drug-polymer ratios of 1:1, 1:2 and 1:3. Nine  formulations were formulated and  evaluated for  possible drug polymer interactions, percentage yield, micromeritic properties, particle size, drug content, drug entrapment efficiency, drug loading, swelling index, In-vitro wash off test, in vitro  drug release, surface morphology and release kinetics. Results: The results showed that no significant drug polymer interaction in FTIR studies. Among all the formulations SF3 containing sodium alginate showed 77.18% drug release in 6hrs. Conclusion: Amongst the developed mucoadhesive microspheres, SF3 formulation containing sodium alginate exhibited slow and sustained release in a controlled manner and it is a promising formulation for sustained release of Sumatriptan succinate. Keywords: Mucoadhesive microspheres, Sodium alginate, polyvinyl pyrrolidone, Chitosan, sustained release.

scholarly journals DESIGN, DEVELOPMENT, AND EVALUATION OF AN ION-ACTIVATED OPHTHALMIC IN SITU GEL OF MOXIFLOXACIN HYDROCHLORIDE

2019 ◽  
pp. 94-103
Author(s):  
GIRISH KONDALKAR ◽  
ASISH DEV
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Statistical Models ◽  
Bacterial Infections ◽  
Gelling Agent ◽  
Design Development ◽  
Sustained Drug Release ◽  
Exchange Method ◽  
In Situ Gelling

Objective: The objective of this study was to develop an in situ ophthalmic gel of an anti-infective drug, moxifloxacin (MOX) hydrochloride (HCL), for sustained ocular delivery for the treatment of bacterial infections of the eye. Method: In the present work the in situ gelling systems were prepared by ion exchange method with the help of various concentrations of gelling agent gelrite (0.08 g, 0.1 g and 0.12 g) and sodium alginate (0.6 g, 0.8 g and 1 g) as viscosity enhancer were added in the formulation; 9 formulations were prepared according to 32 factorial designs and evaluated. The responses were analyzed for the analysis of variance using Design-Expert version 10 software. Statistical models were generated for each response parameter. Results: Optimized formulation batch F7 (0.12% gelrite and 0.6% sodium alginate) was liquid before addition of simulated tear fluid (STF) and underwent rapid gelation on addition of STF and had given 84.05% cumulative drug release; the formulation was found to be clear, having good in situ gelling capacity, good antibacterial efficacy, having drug content 99.75%; optimized formulation was sterile and showed sustained drug release over 8 h period as compared to marketed eye drop. Conclusions: From the above results, we can concluded that 32 full factorial design and statistical models can be successfully used to optimize the formulations, and it was concluded that the trial batch F7 (0.12% gelrite and 0.6% sodium alginate) is the best formula (percentage cumulative drug release over 84.05%) and it is possible to formulate in situ ophthalmic gels of MOX HCL using gelrite in combination with sodium alginate for the treatment of various bacterial infections of the eyes.

scholarly journals SODIUM ALGINATE/GELATIN MICROBEADS-INTERCALATED WITH KAOLIN NANOCLAY FOR EMERGING DRUG DELIVERY IN WILSON’S DISEASE

2019 ◽  
pp. 71-80 ◽  
Author(s):  
O. SREEKANTH REDDY ◽  
M. C. S. SUBHA ◽  
T. JITHENDRA ◽  
C. MADHAVI ◽  
K. CHOWDOJI RAO ◽  
...  
Keyword(s):  
Electron Microscopy ◽  
Scanning Electron Microscopy ◽  
Drug Release ◽  
Ftir Spectroscopy ◽  
Sodium Alginate ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Vitro Release ◽  
Scanning Electron

Objective: The aim of the present study was to fabricate and evaluate the drug release studies using Sodium Alginate (SA) and Gelatin (GE) microbeads intercalated with Kaolin (KA) nanoclay for sustained release of D-Penicillamine (D-PA). Methods: Sodium alginate/gelatin/Kaolin blend microbeads were prepared by an extrusion method by using glutaraldehyde (GA) as a crosslinker. The obtained microbeads were characterized by Fourier transform infrared (FTIR) spectroscopy, scanning electron microscopy (SEM) and X–ray diffraction (XRD). Drug release kinetics of the microbeads was investigated in simulated intestinal fluid (pH 7.4) at 37 °C. Results: Microbeads formation was confirmed by FTIR spectroscopy. X-RD reveals that the KA should be intercalated with the drug and also it confirms the molecular level dispersion of D-Penicillamine into microbeads. Scanning Electron Microscopy (SEM) studies reveal that the beads were in spherical shape with some wrinkled depressions on the surface. The in vitro release study indicates the D-Penicillamine released in a controlled manner. The in vitro release kinetics was assessed by Korsmeyer-Peppas equation and the ‘n’ value lies in between 0.557-0.693 indicates Non-Fickian diffusion process. Conclusion: The results suggest that the developed KA intercalated microbeads are good potential drug carrier for the controlled release of D-PA.

scholarly journals FORMULATION AND EVALUATION OF FLOATING MICROSPHERES OF CIPROFLOXACIN BY SOLVENT EVAPORATION METHOD USING DIFFERENT POLYMERS

2021 ◽  
pp. 101-108
Author(s):  
KAUSLYA ARUMUGAM ◽  
PAYAL D. BORAWAKE ◽  
JITENDRA V. SHINDE
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
Entrapment Efficiency ◽  
Solvent Evaporation ◽  
Angle Of Repose ◽  
Solvent Evaporation Method ◽  
Evaporation Method

Objective: The main intention of this research was to formulate and evaluate floating microspheres of ciprofloxacin using different polymers to prolong gastric residence time. Methods: The microspheres were formulated by the solvent evaporation method using different ratios of polymers like carbopol 940, ethylcellulose, and Hydroxy Propyl Methyl Cellulose K4M. Further, the floating microspheres were evaluated for micromeritic properties like bulk density, tapped density, angle of repose, etc., percentage yield, particle size, entrapment efficiency, floating capacity, in vitro drug release study, release kinetics, drug content, swelling index, and Fourier Transform Infrared Spectroscopy (FTIR) (Compatibility studies). Results: The ciprofloxacin microspheres showed the good flowing property. The particle size ranged from 258.1±2.21 µm to 278±2.86 µm and entrapment efficiency ranged from 63.17±0.43% to 89.90±1.32%. The IR spectrum revealed that there was no interaction between the drug and polymer. F7 formulation was found to be the best formulation. Drug release was found to be 90.70±0.89% i.e. in a controlled manner at the end of 10 h. Conclusion: The floating microspheres were prepared successfully and the results clearly stated that prepared ciprofloxacin microspheres may be safe and effective controlled drug delivery over an extended period which can increase bioavailability, patient compliance, and decrease dosing frequency.

In vitro and In vivo Characterization of Pectin Based In situ Gelling System of Famotidine

2013 ◽  
Vol 5 (4) ◽  
pp. 1885-1894
Author(s):  
Mohmadmoin K. Modasiya ◽  
A K Patel ◽  
V.M Patel ◽  
G.C Patel
Keyword(s):  
Drug Release ◽  
Calcium Chloride ◽  
Fickian Diffusion ◽  
Similarity Factor ◽  
Drug Content ◽  
Model Drug ◽  
In Situ Gelling

In this study famotidine was used as a model drug to formulate and evaluate pH-induced in situ gelling system for oral sustained release drug delivery in stomach which has shorter biological half-life. To study the effect of independent variables 32 full factorial design was employed, concentration of pectin as pH dependant polymer and concentration of calcium chloride on dependent variables like viscosity, drug content, 50% and 80% drug release and similarity factor. It was found that both the concentration of pectin and concentration of calcium chloride had significant effect on viscosity, drug content, 50% and 80% drug release and similarity factor of the system. In vitro drug release study showed that drug released from the in situ gel followed non-Fickian diffusion. Mathematical modeling was employed for quantitative evaluation of the effect of formulation variables. Rat pylorus legation model was used for in vivo study of the selected formulation. Results shows gel formation in gastric juice and reduction in ulcer index. There were few or no major changes in the formulation during three months stability testing. The in situ gelling systems are useful for delivery of famotidine.

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