scholarly journals Formulation development and characterization of eplerenone insitu oralgels

2021 ◽  
pp. 69-78
Author(s):  
M.Parthy ◽  
T.Malyadri ◽  
Ch.Saibabu
Keyword(s):  
Drug Release ◽  
Oral Dosage ◽  
Gelling Agent ◽  
In Vitro Dissolution ◽  
Compatibility Study ◽  
Gastric Retention ◽  
Formulation Development ◽  
Sustained Drug Release

Gastro retentive drug delivery systems have been widely used to prolong the retention of dosage forms in the stomach. Among the various approaches, the floating in-situ gelling formulation offers sustained drug release as well as prolonged gastric retention, along with the added advantage of the liquid oral dosage form. The present study was an attempt to formulate and evaluate floating in situ gel of Eplerenone by using various polymers like Xanthan gum, Carbopol, HPMC K100M, and Karaya gum which undergoes pH dependant sol-gel transition at gastric pH, thereby prolonging the retention of the system in the stomach. Sodium alginate a natural polymer was employed as a gelling agent where Gelation is triggered by the source of calcium ions in the form of calcium carbonate. Drug and polymers were subjected for compatibility study using FTIR studies, which revealed that there was no interaction between drugs and polymers. The evaluation was carried out for invitro parameters such as gelling nature, Total floating time, drug content, viscosity, & in vitro dissolution studies. Among all the formulations, the F12 formulation containing HPMC K100M was chosen as an optimized formulation that shows maximum drug release by the end of 12hrs and has excellent floating characteristics and gastric retention. From kinetic studies, the optimized formulation shows zero-order release with super case II transport mechanism.

scholarly journals Formulation Development and Evaluation of Sustained Release Microsphere of Levetiracetam

2021 ◽  
Vol 71 (2) ◽  
Author(s):  
Dinesh V. Panpaliya ◽  
Atish Y. Sahare ◽  
Priyanka Lanje ◽  
Pooja Dhoke
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
Solvent Evaporation ◽  
In Vitro Dissolution ◽  
Compatibility Study ◽  
Solvent Evaporation Method ◽  
Formulation Development ◽  
Sustained Drug Release ◽  
Evaporation Method

The aim of the present work was to develop and evaluate of oral microsphere of Levetiracetam to reduce the frequency of dosing by achieving 12 hours sustained drug release. The microsphere formed will also mask the bitter taste of the drug and thus increase the compatibility of the drug with the patients. Levetiracetam is a second-generation anti-epileptic agent useful in the treatment of partial onset and monoclinic seizures. It has a short half life of 7 hours and its recommended dose is 500 mg twice a daily. Microspheres are suitable drug delivery system for such drug candidate. For these reasons it is must to formulate a suitable dosage form by which it will be easier to administer the dose and also to get a sustained drug release hence microsphere was prepared using solvent evaporation method. Preformulation studies were carried out to rule out any drug polymer interaction by FTIR technique. In this study formulation was done solvent evaporation method using different percentage of HPMC– K 100, HPMC- K 15 and coated with Eudragit S100. Drug, polymer and physical mixture were evaluated for in compatibility study by Fourier transforms infrared spectroscopy. All the batches of microsphere (F1 to F5) were subjected for in vitro dissolution. Microsphere was evaluated for surface morphology, micromeritics properties, entrapment efficiency and in vitro drug release. The entrapment efficiency of microsphere ranged from 71.16%-73.66%. The size of the prepared microsphere ranges between 42.8 µm to 55.64 µm which was found to increase with increase in RPM at same polymer ratio. Micromeritics studies showed good flow properties. Among the microsphere batches, F5 was observed as an optimized batch as its formulation with polymer i.e. Eudragit-S 100 and HPMC-K 100 was found to be release in sustained manner. The F-5 batch shows is 79.45% drug release at the end of 7 hrs and its stability study indicate that these microspheres were stable at selected temperature and humidity

Formulation development and in vitro Evaluation of sustained release matrix tablets of Cefpodoxime proxetil

2021 ◽  
pp. 273-278
Author(s):  
A. Bhavani ◽  
B. Hemalatha ◽  
K. Padmalatha
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Sustained Release ◽  
Matrix Tablets ◽  
Oral Dosage ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Formulation Development ◽  
Cefpodoxime Proxetil

The present focus is on the development of sustained release formulations due to its inherent boons. There are several advantages of sustained release drug delivery over conventional dosage forms like improved patient compliance, reduction in fluctuation and increased safety margin of potent drug. The present study was aimed to prepare a sustained drug delivery system to design a controlled release oral dosage form of Cefpodoxime proxetil. The sustained release matrix tablets of Cefpodoxime proxetil were prepared by wet granulation and evaluated for different parameters such as weight variation, drug content, thickness, hardness, friability and In vitro release studies. The in vitro dissolution study was carried out for 12 hours using USP (Type- II) paddle apparatus in hydrochloride (0.1N) as dissolution media for first 2 hours and phosphate buffer (pH 6.8) for next 10 hours. Based on the in vitro dissolution data, formulation F8 was selected as the best formulation from Cefpodoxime proxetil formulations (F1 – F9) as the drug release was retarded up to 12 hours with 96.29 % and followed zero order release kinetics & drug release mechanism was diffusion.

scholarly journals FORMULATION DEVELOPMENT AND EVALUATION OF pH TRIGGERED IN SITU OPHTHALMIC GEL OF BESIFLOXACIN HYDROCHLORIDE

2018 ◽  
Vol 8 (5) ◽  
pp. 313-321 ◽  
Author(s):  
Vishakha Waghulde ◽  
Ravindranath Saudagar
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Drug Release ◽  
Stability Study ◽  
Gelling Agent ◽  
Formulation Development ◽  
Drug Content ◽  
Wide Range

The aim of the present work was to formulation and evaluation of pH Triggered in-situ Ophthalmic Gel of Besifloxacin Hydrochloride to overcome the drawbacks obtained by conventional eye drop. There are two independent variables were used i.e. Carbopol 934 and HPMC K100. Carbopol 934 were used as gelling agent and HPMC K100 were used as bioadhesive polymer. Besifloxacin Hydrochloride shows activity against a wide range of Gram-positive and negative ocular pathogens: examples are  Corynebacterium pseudodiphtheriticum, Moraxella lacunata, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae and Streptococcus salivarius. The in situ gelling system involves sol-to-gel transition in the cul-de-sac upon instillation to avoid pre corneal elimination. The formulations were prepared by 32 factorial design. The prepared formulations were evaluated for clarity, pH, viscosity, Bioadhesive strength of gel, gel strength gel, Drug Content, In-vitro Drug Release Study, Antibacterial Activity, Isotonicity Evaluation, HET-CAM Test and stability studies. The drug content was in the range of 97-99.57 %. Formulation F5 selected as optimized on the basis of evaluation. It shows highest drug release upto 8hrs. It shows good antibiotic activity against Staphylococcus aureus. The optimized formulation was isotonic with blood cells. It passes sterility test. The optimized formulation passes the ocular irritancy test i.e. HET-CAM Test. The formulation kept for the stability study for 3 months. Short term stability study indicates that room temperature 400±20 was appropriate storage condition for formulations. Keywords: pH Triggered, bioadhesive polymer, Carbopol 934, HPMC K100, HET-CAM Test, Antibacterial Activity.

Formulation development of folic acid conjugated PLGA nanoparticles for improved cytotoxicity of Caffeic acid phenethyl ester

2021 ◽  
Vol 09 ◽  
Author(s):  
Harshad S Kapare ◽  
Sathiyanarayanan L ◽  
Arulmozhi S ◽  
Kakasaheb Mahadik
Keyword(s):  
Folic Acid ◽  
Drug Release ◽  
Caffeic Acid ◽  
Caffeic Acid Phenethyl Ester ◽  
Therapeutic Effects ◽  
Formulation Development ◽  
Sustained Drug Release ◽  
Active Constituent

Background: Honey bee propolis is one of the natural product reported in various traditional systems of medicines including Ayurveda. Caffeic acid phenethyl ester (CAPE) is an active constituent of propolis which is well known for its anticancer potential. The therapeutic effects of CAPE are restricted owing to its less aqueous solubility and low bioavailability. Objective: In this study CAPE loaded folic acid conjugated nanoparticle system (CLFPN) was investigated to enhance solubility, achieve sustained drug release and improved cytotoxicity of CAPE. Methods: Formulation development, characterization and optimization were carried out by design of experiment approach. In vitro and in vivo cytotoxicity study was carried out for optimized formulations. Results: Developed nanoparticles showed particle size and encapsulation efficiency of 170 ± 2 - 195 ± 3 nm and 75.66 ± 1.52 - 78.80 ± 1.25 % respectively. Optimized formulation CLFPN showed sustained drug release over a period of 42 h. GI50 concentration was decreased by 46.09% for formulation as compared to CAPE in MCF-7 cells indicating targeting effect of CLFPN. An improved in vitro cytotoxic effect was reflected in in-vivo Daltons Ascites Lymphoma model by reducing tumor cells count. Conclusion: The desired nanoparticle characteristic with improved in vivo and in vitro cytotoxicity was shown by developed formulation. Thus it can be further investigated for biomedical applications.

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, 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 Fixed Dose Oral Dispersible Tablet of Bitter Drug Using Okra Mucilage: Formulation and Evaluation

2020 ◽  
Vol 10 (5) ◽  
pp. 149-158
Author(s):  
Pintu Dhar ◽  
Himangshu Sarma ◽  
Hemanta Kumar Sharma
Keyword(s):  
Drug Release ◽  
Bitter Taste ◽  
Oral Dosage ◽  
Taste Masking ◽  
Fixed Dose ◽  
Wet Granulation ◽  
Formulation Development ◽  
Dispersible Tablet ◽  
Promethazine Hydrochloride

Background: The solid oral dosage forms containing bitter drugs need improved palatability for administration. Formulation scientists have given attention to the improvement of taste masking technologies and utilised various strategies. Objective: The present work aimed to mask the bitter taste of Promethazine Hydrochloride by formulating Oral Dispersible Tablets using Okra mucilage as a taste-masking agent.  Methods: The Okra mucilage was extracted from Okra by the aqueous extraction process. An emulsion solvent diffusion technique was used for masking the bitter taste of Promethazine Hydrochloride by using Okra mucilage. The Oral Dispersible Tablet was prepared by the wet granulation method. The mucilage and the formulation were characterized and evaluated by standard methods and protocols. Results: Taste masking of the bitter drug was successfully achieved by Okra mucilage. The DSC and FTIR study revealed that the drug molecule was compatible with okra mucilage and drug entrapment efficacy was found to be 94.76%. The palatability test asserted that masking of the bitter taste of the drug.  The In vitro drug release study showed that the F7 tablet batch has a better drug release rate and followed non- fickian mechanism of drug release. Conclusion: Thus, taste masking with Okra mucilage was successful and this opens opportunities for application of common edible substances in formulation development. Keywords: Fast disintegrating tablet; Natural polymer; Mouth dissolving tablet; Promethazine Hydrochloride; Taste masking

scholarly journals Oleic Acid Based Emulgel for Topical Delivery of Ofloxacin

2019 ◽  
Vol 9 (4-A) ◽  
pp. 183-190
Author(s):  
A. Manaswitha ◽  
P. V. L. D. Sai Swetha ◽  
N.K.D. Devi ◽  
K. Naveen Babu ◽  
K. Ravi Shankar
Keyword(s):  
Oleic Acid ◽  
Drug Release ◽  
Ph Value ◽  
Liquid Paraffin ◽  
Tween 80 ◽  
Gelling Agent ◽  
Compatibility Study ◽  
Zero Order Kinetics ◽  
Carbopol 940

The objective of the present study is to formulate and evaluate ofloxacin emulgel. Emulgel formulations of ofloxacin were prepared using different concentrations of gelling agent’s Carbopol-940 and Xanthum gum. Tween-80 and span-80 were used as emulsifiers and propylene glycol as a humectant in the preparation of emulgel. The effect of the concentration of gelling agent on the drug release from the prepared emulgel was investigated. The compatibility study was conducted using Fourier-transform infrared (FTIR). The formulated emulgel was characterized by their physical appearance, pH determination, viscosity, spreadability, drug content, microbial test and in vitro diffusion study. FTIR indicated that the drug and excipients used in the study are compatible with each other. All the prepared formulations showed acceptable physical properties, homogeneity, consistency, spreadability, viscosity, and pH value. Drug release from all the formulations depended upon the concentration of the polymer used. As the concentration of Carbopol 940 increased the spreadability and drug release was found to be decreased. Emulgels formulated with oleic acid gave a much higher release rate of ofloxacin than emulgels formulated with liquid paraffin. The release of drug from all the emulgels prepared followed Zero-order kinetics. The linear Higuchi plots indicated that the drug release from all the emulgels prepared followed diffusion kinetics. Emulgel formulated with oleic acid exhibited greater flux when compared with those formulated with liquid paraffin. The formulations were found to be stable during stability testing. It can be concluded that Carbopol 940 and oleic acid are recommended for the formulation and preparation of Ofloxacin emulgels for topical drug delivery. Key words: Ofloxacin, Emulgel, Spreadibility, Zone of inhibition.

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 DESIGN EXPERT SUPPORTED FORMULATION DEVELOPMENT, MATHEMATICAL OPTIMIZATION AND PREDICTABILITY STUDY OF FLOATING TABLETS OF BISOPROLOL FUMARATE

2021 ◽  
pp. 242-248
Author(s):  
SHAIKH SHAOOR AHMAD ◽  
SHAIKH SIRAJ N. ◽  
PATEL M. SIDDIK ◽  
KHALIFA MAHMADASIF YUNUS ◽  
MAKRANI SHAHARUKH I. ◽  
...  
Keyword(s):  
Drug Release ◽  
Scale Up ◽  
Mathematical Optimization ◽  
Lag Time ◽  
Stability Study ◽  
In Vitro Dissolution ◽  
Formulation Development ◽  
Floating Tablets ◽  
Design Expert

Objective: Focus of the study was to formulate Design expert Software assisted floating tablet of Bisoprolol Fumarate. Bisoprolol Fumarate is a Beta adrenergic blocking agent, used to treat cardiac diseases favorable characters to be formulated as sustained release Gastro retentive floating tablets. Methods: Floating Tablets of Bisoprolol Fumarate were prepared by using polymers such as Polyox N 12 K and Carbapol 940 P. Formulations were prepared by using direct compression method and evaluated for various parameters like Hradness, thickness, weight variations, Floating lag time Total floating time,% drug release and Stability Study etc. Results: FTIR spectroscopic study indicates no drug-excipients interaction in the prepared formulations. Hardness or crushing strength of the tablets of all the formulation was found between 5.8 and 6.5 kg/cm2. Floating lag time of all batches is in range of 1.18±2.0 to 2.43±1.6 (minutes). All other parameters of all batches are within an acceptable range. The polymer Carbopol 940 P had the significant negative effect of on the floating lag times. The In vitro dissolution profiles of optimized A3 Floating formulation of Bisoprolol Fumarate were found to sustain drug release 99.25 % up to 12 h with floating lag time of 1.45 min; Designed formulation was stable after Stability study. Optimization study was carried out by using 32 factorial designs to fabricate formulations. Conclusion: It can be conclude that reproducible results of various parameters in this developed formulation can easily scale up. Furthermore designed formulation will be very effective for controlling blood pressure.

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