scholarly journals DESIGN, OPTIMIZATION & IN-VITRO EVALUATION OF SODIUM ALGINATE BASED IN-SITU GEL OF RANITIDINE HYDROCHLORIDE IN ULCER TREATMENT

2021 ◽  
Vol 9 (1) ◽  
Author(s):  
Sanket Kumar ◽  
Mahesh Singh ◽  
Babulal Patel
Keyword(s):  
Peptic Ulcer ◽  
Drug Release ◽  
Sodium Alginate ◽  
Gelling Agent ◽  
Cross Linking ◽  
Physical Interaction ◽  
In Situ Gel ◽  
Ranitidine Hydrochloride ◽  
Ulcer Treatment

Peptic ulcer, it is the most common type of stomach disease, according to the American Gastroenterology Association. “We know that ulcers occur because there has been a disruption in the balance of factors that injure the digestive tract and those factors that protect it from injury,” The present investigation deal with the formulation, optimization and evaluation of sodium alginate based in situ gel of ranitidine hydrochloride (R-HCl) in ulcer treatment. The in-situ formulation are homogenous liquid when administration orally and become gel at the contact site. The evaluation of the formulation is dependent upon accurate results obtained by analytical method used during the study. Accurate results require the use of standard and a calibration procedure. Hence, standard plots of Ranitidine hydrochloride were prepared in (0.1N HCL, pH 1.2) solutions. Two, sodium alginate and calcium carbonate used as a polymer and cross-linking agent respectively in the formulation of in-situ gel. From the IR studies it may be concluded that the drug and carriers used undergo physical interaction there is no chemical change, and thus the gelling agent, cross-linking agent and other excipient is suitable for formulation of in-situ gel of ranitidine hydrochloride. Indicate that the formulation, DKF9 which was prepared by the Sodium alginate (2 gm) with Ranitidine Hydrochloride showed minimum drug release (sustained drug release) after 8 hrs. It can be concluded that the In-situ gel was beneficial for delivering the drug which needs sustained release to achieve the slow action. Keywords: In-situ gel, Peptic Ulcer, Ranitidine Hydrochloride (R-HCl), Sodium alginate.

scholarly journals FORMULATION AND EVALUATION OF FLOATING IN SITU GEL OF CIPROFLOXACIN

2019 ◽  
Vol 11 (1) ◽  
pp. 198
Author(s):  
Shailaja Pashikanti ◽  
Jyothsna B.
Keyword(s):  
Calcium Carbonate ◽  
Drug Release ◽  
Sodium Alginate ◽  
Gelling Agent ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Degradable Polymer ◽  
Gel Formulations

Objective: The objective of the study was to develop floating in situ gel formulations of Ciprofloxacin that has a narrow absorption window and mainly absorbed in the proximal areas of GIT. These formulations increases the targeted action on bacteria for a longer time that can be used in the treatment of Helicobacter pylori (H. pylori) infections and urinary tract infections.Methods: In situ gel formulations were prepared by varying concentrations of sodium alginate as in situ gel forming bio-degradable polymer and calcium carbonate as a cross-linking agent. The formulations were evaluated for Physical appearance, pH, in vitro drug release, viscosity, in vitro floating behaviour, in vitro gelling capacity and drug content. FTIR was conducted for Ciprofloxacin, excipients used and optimized formulation.Results: All the formulations showed an optimum viscosity that will allow ease of administration and swallowing. Floating lag time of all formulations was between 32-70 seconds and floated for>12 h. The in vitro gelling capacity increased with increasing the polymer and gelling agent concentrations. Increase in polymer concentration decreased the rate and extent of the drug release. Among all the formulations, F4 containing 4% w/v of sodium alginate and 4% w/v of calcium carbonate showed sustained in vitro drug release (95.6%) over an extended period of 12 h. FTIR studies revealed no interaction between drug and excipients used. Drug release from the formulations followed First order kinetics with Fickian diffusion.Conclusion: Ciprofloxacin was successfully formulated as a pH-triggered floating in situ gelling system using sodium alginate.

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.

Floating In Situ Gel based on Alginate as Carrier for Stomach-Specific Drug Delivery of Famotidine

2010 ◽  
Vol 3 (3) ◽  
pp. 1092-1104 ◽  
Author(s):  
Jayvadan K. Patel Patel ◽  
Jayant R. Chavda ◽  
Moin K Modasiya
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Calcium Chloride ◽  
Sodium Citrate ◽  
Sustained Drug Release ◽  
In Situ Gel ◽  
In Vivo Testing ◽  
In Situ Gelling

Alginate based floating in situ gelling systems of famotidine (FIGF) were prepared by dissolving varying concentrations of alginate in deionized water containing sodium citrate, to which varying concentrations of drug and calcium chloride was added and dissolved by stirring. Results of preliminary trials indicate that concentrations of sodium alginate, calcium chloride and sodium citrate affected the characteristics of in situ gel. A 32 full factorial design was employed to study the effect of independent variables, concentration of sodium alginate (X1) and concentration of calcium chloride (X2) on dependent variables, i.e. viscosity, drug content, drug release at 4 hrs (Q50) and drug release at 8 hrs (Q80). A sustained drug release was obtained for more than 8 hrs. In vivo testing of FIGF to albino Wistar rats demonstrated significant anti-ulcer effect of famotidine.

scholarly journals DEVELOPMENT AND CHARACTERIZATION OF DICLOFENAC SODIUM LOADED EUDRAGIT RS100 POLYMERIC MICROSPONGE INCORPORATED INTO IN SITU GEL FOR OPHTHALMIC DRUG DELIVERY SYSTEM

2021 ◽  
pp. 63-69
Author(s):  
RAJASHRI B. AMBIKAR ◽  
ASHOK V. BHOSALE
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Diclofenac Sodium ◽  
Entrapment Efficiency ◽  
Gelling Agent ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Drug Content

Objective: Purpose of the study to design and formulate Diclofenac sodium (DIC) microsponges. Methods: With varied polymer: drug ratio DIC loaded microsponges were prepared with Eudragit RS100 polymer by quasi solvent diffusion method. Microsponges evaluated for particle size, entrapment efficiency, drug content, in vitro drug release, Fourier Transform Infrared Spectroscopy (FTIR), Differential scanning calorimetry (DSC) and Scanning electron microscopy (SEM). DIC loaded microsponges incorporated into ocular in situ gel to attained controlled release by microsponge and improved residence time by gelling system. Ocular in situ gel evaluated for pH, drug content determination, gelling capacity, in vitro drug release and sterility study. Results: DSER4 microsponge formulation having polymer to drug ratio 1:7 showed satisfactory production yield (68.13%), entrapment efficiency (62.86%), drug content (80.73%), requisite particle size (less than 10 µm) (7.52 µm) and in vitro release 87.94% after 6 h. Selected DSER4 formulation was incorporate into in situ gel. Carbopol 940 forms stiff gel at higher pH so used as a gelling agent, whereas Hydroxypropyl Methylcellulose E4M was used as a viscosity-enhancing agent for the formulation of in situ gel in varied compositions. In situ gel formulation IG4 showed sustained release of 76.92% till the end of 8 h and satisfactory gelling capacity so IG4 further evaluated for sterility test. Rheological studies reveal the sol-gel transition of in situ gel occur at the physiological condition to form stiff gel. Conclusion: Prepared in situ gel formulations showed sustained drug release for a period of 8 h, which is satisfactory for management of ocular pain.

scholarly journals Micro spect in vivo bio-distribution study of azithromycin ophthalmic in situ gel

2020 ◽  
Vol 11 (3) ◽  
pp. 4546-4554
Author(s):  
Manish Wani ◽  
Swati Jagdale ◽  
Vishal Bhujbal ◽  
Akshay Baheti ◽  
Ashwin Kuchekar
Keyword(s):  
Drug Release ◽  
Residence Time ◽  
Polymer Concentration ◽  
Experimental Studies ◽  
Poloxamer 407 ◽  
Gelling Agent ◽  
In Situ Gel ◽  
Biodistribution Studies

Azithromycin (AZT) is a broad-spectrum antibiotic and is found in ocular tissues when administered systemically. AZT inhibits RNA-dependent protein synthesis and hence has effective bactericidal capability against Staphylococcus aureus, Pseudomonas aeruginosa, which are the primary causative organisms for bacterial infection. In situ ophthalmic gels are systems which undergo a sol-to-gel transformation when instilled in eyes. In situ gels overcome the shortcoming of ophthalmic drops as they get washed out and diluted due to tear fluid. The aim and objective of present study was to formulate in situ ophthalmic gelling systems of Azt and determine in vivo ocular residence time in rat eyes of Tc99 labelled Azt by Micro SPECT. The in situ gel was formulated using Poloxamer 407, which is a temperature-induced gelling agent and HPMC K4M, which is known to increases mucosal adhesivity and enhance viscosity to facilitate sustained release of drug. The formulations developed were evaluated for pH, clarity, viscosity, gelling capacity and % drug release. The selected formulation was subjected to isotonicity and In Vivo Bio-distribution studies. Experimental studies on compatibility showed no interaction between polymers and AZT. AZT was found soluble in PB6.8. All formulations were found clear immediately after preparation and after sterilization & pH after gelation was satisfactorily in the range of 6 to 7. Viscosity and Gelation capacity of in situ gel increased with increase in polymer concentration. Formulations F2 showed desired results w.r.t viscosity, gelation capacity, drug release. In Vivo Biodistribution studies of Tc99 labelled AZT by Micro SPECT showed there was a significant increase in ocular residence time of in situ gel when compared with Tc99 labelled marketed solutions.

scholarly journals ENHANCE SOLUBILITY AND PROLONG RELEASE OF PROCHLORPERAZINE MALEATE USING FLOATING NANOEMULSION IN SITU GEL

2019 ◽  
Vol 12 (1) ◽  
pp. 537
Author(s):  
Yasser Q Almajidi ◽  
Ahmed A Albaderi ◽  
Hasan Fadhel
Keyword(s):  
Calcium Carbonate ◽  
Sodium Alginate ◽  
Calcium Chloride ◽  
Hydroxypropyl Methylcellulose ◽  
Gelling Agent ◽  
Drug Solubility ◽  
Release Formulation ◽  
In Situ Gel

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.

scholarly journals ENHANCE SOLUBILITY AND PROLONG RELEASE OF PROCHLORPERAZINE MALEATE USING FLOATING NANOEMULSION IN SITU GEL

2019 ◽  
Vol 12 (1) ◽  
pp. 537
Author(s):  
Yasser Q Almajidi ◽  
Ahmed A Albaderi ◽  
Hasan Fadhel
Keyword(s):  
Calcium Carbonate ◽  
Sodium Alginate ◽  
Calcium Chloride ◽  
Hydroxypropyl Methylcellulose ◽  
Gelling Agent ◽  
Drug Solubility ◽  
Release Formulation ◽  
In Situ Gel

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.

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

2018 ◽  
Vol 11 (7) ◽  
pp. 277 ◽  
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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