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 Formulation and Evaluation of Meloxicam In-Situ Gel Designed for Sustained Drug Release to Reduce Dosing Frequency in the Management of Arthritis

2021 ◽  
Vol 69 (2) ◽  
Author(s):  
Meesala. Srinivasa Rao ◽  
M. S Chandra Goud ◽  
C. V. Reddy
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Dosing Frequency ◽  
Gel Formulations

Meloxicam has short biological half-life and is rapidly eliminated, frequent oral administration is necessary to maintain its therapeutic concentration, but this can increase chances of missing dose. This makes Meloxicam a good applicant for oral sustained release formulation. The objective of study was to develop in-situ gel formulations of Meloxicam for sustained release to reduce the dosing frequency in the treatment of rheumatoid arthritis. Method of Ion sensitive in-situ gelation was used in this study. Meloxicam In-situ gel formulations were prepared by varying concentrations of sodium alginate as a bio-degradable gel forming polymer, CaCl2 as a cross-linking agent and Chitosan/ HPMCK4/HPMCK15/Guar gum/Gellan gum/ Xantha gum/pectin were used as drug release rate controlling polymers. The formulations F11-F18 were assessed for Physical appearance, pH, in-vitro drug release, viscosity, in-vitro gelling capacity and drug content. FTIR, DSC and in-vivo drug kinetics studies was conducted for Meloxicam, excipients used and optimized formulation. Formulations showed an optimum viscosity that will allow ease of administration and swallowing. All formulations are shown pH between4.7-4.9, floating lag time was 2-3sec and floated for >12 hrs. In vitro drug release studies reporting that commercially available product Meloxicam SR has showed 99.92% drug release in 8 hrs and out of eight formulations F11 showing in-vitro drug release of 99.52% over a 12hrs extended period. FTIR studies revealed no interaction between drug and excipients used. The results of In-vivo kinetic studies are approving the better performance of the optimized formulation in comparison to marketed formulation, The Cmax, Tmax, half-life AUC values are confirming the same thing. In conclusion, Formulation (F11) was selected as optimized formulations could be offered as shows optimum sustained drug release compared to commercial formulation. Hence Meloxicam containing Chitosan as drug release controll

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 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.

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, 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, Development and Evaluation of Chewable Bi-layered Tablets for Treating Gastro Esophageal Reflux Disease

2020 ◽  
Vol 10 (4-s) ◽  
pp. 92-99
Author(s):  
Ankur Vasoya ◽  
Sunil Kumar Shah ◽  
C K Tyagi ◽  
Prabhakar Budholiya ◽  
Harish Pandey
Keyword(s):  
Calcium Carbonate ◽  
Drug Release ◽  
Sodium Bicarbonate ◽  
Sodium Alginate ◽  
Acid Neutralization ◽  
In Vitro Drug Release ◽  
Neutralization Capacity ◽  
Acid Neutralization Capacity ◽  
Bilayer Tablets

The purpose of this research work was to formulate raft-forming chewable bilayer tablets of sodium alginate using a raft-forming agent along with gas-generating agents. Tablets were prepared by wet granulation and evaluated for raft strength, acid neutralization capacity, weight variation, % drug content, thickness, hardness, friability and in vitro drug release. Various raft-forming agents were used in preliminary screening. The amount of sodium alginate, amount of calcium carbonate and amount sodium bicarbonate were selected as variables. Raft strength, acid neutralization capacity and drug release at 30 min were selected as responses.Tablets containing sodium alginate were having maximum raft strength as compared with other raft-forming agents. Acid neutralization capacity and in vitro drug release of all factorial batches were found to be satisfactory. Prepared tablets were found to be pharmaceutically equivalent to the marketed product. It was concluded that raft-forming chewable bilayer tablets prepared using an optimum amount of sodium alginate, calcium carbonate and sodium bicarbonate could be an efficient dosage form in the treatment of gastro oesophageal reflux diseases. Keywords: Chewable bilayer tablet, Sodium alginate, Raft forming agent, Acid Neutralizing capacity

Fabrication and Characterization of Ocular Phase Transition Systems for Blepharitis: A Novel Approach

2020 ◽  
Vol 10 (1) ◽  
pp. 24-37
Author(s):  
Deepali Verma ◽  
Shreya Kaul ◽  
Neha Jain ◽  
Upendra Nagaich
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Eye Drops ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Drug Content ◽  
Erythromycin Estolate

Introduction: In the present research, erythromycin estolate loaded in-situ gel was formulated and evaluated for blepharitis in order to improve its therapeutic efficacy, precorneal residence time of the system and to enhance the ocular bioavailability. Material and Methods: The developed formulation was characterized by several parameters viz. FTIR, clarity, pH, gelation temperature, rheological studies, drug content, in vitro drug release studies, transcorneal permeation studies, bioadhesion studies, isotonicity and stability studies. Results: The optimized formulation exhibited non-fickian release diffusion with a sustained release of drug 82.76 ± 0.94% up to 8h and drug content 93.64%. Isotonicity revealed that the formulation was isotonic in nature and there was no shrinkage and busting of cells. Bioadhesion study was performed to check the adherence of the prepared in situ gel to the corneal surface for 4h. Ex vivo transcorneal permeation was observed to be significantly higher when compared with market eye drops. Histopathological studies were conducted to confirm the presence of normal ocular surface tissues by maintaining their morphological structures without causing damage to the tissues. The formulation was nonirritant as confirmed by the HET-CAM test. Stability studies and accelerated stability studies were conducted for 13 weeks and 26 weeks respectively and formulations were analyzed for the visual appearance, pH, viscosity, gelling capacity, drug content and in vitro drug release and results showed no change in the formulations. Conclusion: The formulation was therapeutically efficacious, sterile, stable and provided controlled release over a period of time. The developed system could be a viable alternative to conventional eye drops for treatment of various ocular diseases.

scholarly journals FORMULATION AND EVALUATION OF NOVEL IN SITU GEL OF LAFUTIDINE FOR GASTRO RETENTIVE DRUG DELIVERY

2018 ◽  
Vol 11 (8) ◽  
pp. 88
Author(s):  
Sindhoor S M ◽  
Sneh Priya ◽  
Amala Maxwell
Keyword(s):  
Drug Release ◽  
Imaging Study ◽  
Lag Time ◽  
In Vivo Studies ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Drug Content

Objective: The aim of the present study was to formulate and evaluate the novel in situ gel of lafutidine for gastroretentive drug deliveryMethods: A gastroretentive in situ gel of lafutidine was formulated by pH-triggered ionic gelation method using different concentrations of gelling polymer such as sodium alginate, gellan gum, and xanthum gum. Prepared formulations were evaluated for viscosity, density, buoyancy lag time and buoyancy duration, and drug content. In vitro drug release studies of all formulations were also performed. In vivo fluorescence imaging study was conducted for optimized formulation and compared with control.Results: The concentration of gelling agents and release retardant polymers significantly affected viscosity, floating behavior, and in vitro drug release of the formulations. The pH and drug content were found in the range of 6.72–7.20 and 88.74–95.33%, respectively. Floating lag time was <2 min; duration of floating was more than 12 h. Minimum and maximum in vitro drug release were found to be for formulation F9 (51.74%) and F1 (82.76%), respectively, at the end of 12 h. The drug was released from the all the formulations in a sustained manner. In vivo studies confirmed the gastroretention of the formulation in mice stomach for 8 h. Stability studies indicated that the there was no significant change in the visual appearance, floating behavior, and drug content.Conclusion: The gastroretentive in situ gel system, prolonged the gastric residence time, thereby targeting site-specific drug release in the upper gastrointestinal tract.

scholarly journals Evaluation of in situ gel forming system loaded with etoricoxib and herbal adjuvant nanoparticles against human colon cancer cell lines (HT-29)

2020 ◽  
Vol 9 (1) ◽  
pp. 789-795
Keyword(s):  
Drug Release ◽  
Human Colon ◽  
Human Colon Cancer ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Drug Content ◽  
Tamarind Seed ◽  
Ht 29

The aim of the research work was to fabricate the nanosuspension of etoricoxib with polyherbal components (extract of ginger root and basil leaf) to enhance the solubility of API; furthermorein situ gel forming system for stomach specific drug delivery was prepared utilizing formulated nanosuspension as base. The objective of the present research is to enhance the solubility of poorly aqueous soluble drug by fabricating nanoparticles and improve their residence time within stomach by formulating in situ gel forming system. Tamarind seed polysaccharide as polymer, etoricoxib as drug, ethanolic extract of ginger (GE) and basil (BE), was used for preparation of nanoparticles.Solvent antisolvent precipitation method was used to prepare nanoparticles. The fabricated nanoparticles were evaluated for various parameters such as physical appearance, Scanning electron microscope, drug content, in-vitro drug release. For preparation of in-situ gel containing nanoparticles, tamarind seed polysaccharides, calcium carbonate and sodium alginate were used. The prepared formulations were evaluated for different characterization parameters such as,- pH, viscosity, floating behaviour, drug content, in-vitro drug release and in-vitro cytotoxic study. The in-situ gel containing nanoparticles were successfully prepared and evaluated. Firstly, the nanoparticles were evaluated for physical appearance, Scanning electron microscope, drug content, in-vitro drug release and found that the formulations were clear as well as homogenous, size of nanoparticles was evaluated in the range of 498nm to 587nm, the drug content of etoricoxib was found in the range of 71.38±0.01 (F5) to 79.45±0.01 (F6), the drug content of GE was found in the range of 69.25±0.05 (F4) to 74.25±0.02 (F1) and the drug content of BE was 69.48±0.09 (F1) to 75.59±0.08 (F6). The drug release was taken up to 12 h and found to be 99%. In-situ gel containing nanoparticles were also evaluated for different parameters such as pH, viscosity, floating behaviour, drug content, and in-vitro drug release. The pH of the prepared formulation was found to be in the range of 7.1±0.04 to 7.5±0.02. The viscosity of the prepared formulation was found in the range of 11.25±0.023 to 12.78 ±0.025. The lag time was found in the range of 11 to 20 sec and floating time was upto 24 h. The drug release was taken up to 8 h and found to be 99±0.2%. It can be concluded that etoricoxib with phytoconstituents (GE and BE) improved its potential to control the growth of human colon cancer cell line (HT-29) in in-vitro conditions. It was concluded from the findings that the in-situ gel containing nanoparticles of etoricoxib from solvent antisolvent method was successfully prepared and found that it has improved the solubility of the poorly soluble drug etoricoxib and dissolution rates.

Sign in / Sign up

Export Citation Format

Share Document