Physical characterization and In Vitro evaluation of dissolution rate from Cefpodoxime proxetil loaded Self solidifying Solid SNEDDS

2021 ◽  
Vol 18 ◽  
Author(s):  
Pankaj Kumar Sharma ◽  
Vikesh Kumar Shukla ◽  
Anoop Kumar
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Drug Loading ◽  
Amorphous State ◽  
Tween 80 ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Cefpodoxime Proxetil ◽  
Tract Infections

Background: Cefpodoxime proxetil (CPD) is a broad-spectrum cephalosporin indicated in respiratory and urinary tract infections. CPD is a BCS class IV drug with pH-dependent solubility and has poor bioavailability. This study investigated the challenges of developing ternary components based on solid SNEDDS of CPD for in vitro dissolution rate enhancement and self-solidifying behaviour. Method: Tween 80, Transcutol and PEG6000 were employed as surfactant, solvent & solidifying a base of ternary components to develop self-solidifying solid SNEDDS, respectively. Ternary phase diagrams were used to characterize solidifying behaviour of ternary components in different proportions. S-SNEDDS formulations were drawn on the solidification areas available in the phase diagram and characterized for IR, XRD, DSC and in-vitro drug release in various pH media. Results : Ternary components for the preparation of self solidifying solid SNEDDS were selected based on drug solubility. FTIR and DSC characterization studies ruled out any drug interaction between CPD and components chosen to prepare S-SNEDDS. CPD was transformed from a crystalline into an amorphous state in ternary dispersions as revealed from XRD data. Optimized formulation (S-S 1) demonstrated more than 95% of drug release irrespective of the pH environments of the medium. Calculation of dissolution efficiency and similarity factors indicate that S SNEDDS resulted in a higher drug dissolution rate over binary dispersion (p<0.01). The stability studies showed that the S SNEDDS were stable in performances and CPD assay. Conclusion: Present investigation provides an alternative approach for enhancing the CPD dissolution rate using self-solidifying solid SNEDDS exhibited solidification behaviour at ambient temperature conditions and drug loading. Which could be exploited over conventional dosage form.

scholarly journals Formulation, Development and Evaluation of Ibuprofen Loaded Nano-transferosomal Gel for the Treatment of Psoriasis

2019 ◽  
pp. 1-8
Author(s):  
Marwa H. Abdallah ◽  
Amr S. Abu Lila ◽  
Md. Khalid Anwer ◽  
El-Sayed Khafagy ◽  
Muqtader Mohammad ◽  
...  
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Vesicle Size

The present work was aimed to develop a transferosomal gel of ibuprofen (IBU) for the amelioration of psoriasis like inflammation. Three formulation of IBU loaded transferosomes (TFs1-TFs3) were prepared using different proportions of lipid (phospholipon 90H) and surfactant (tween 80) and further evaluated for vesicle size, zeta potential (ZP), entrapment efficiency and in vitro drug release. The IBU loaded transferosomes (TFs2) was optimized with vesicle size (217±8.4 nm), PDI (0.102), ZP (-31.5±4.3 mV), entrapment efficiency (88.4±6.9%) and drug loading (44.2±2.9%). Further, the optimized IBU loaded transferosomes (TFs2) was incorporated into 1% carbopol 934 gel base and characterized for homogeneity, extrudability, viscosity and drug content. The in vivo pharmacodynamic study of gel exhibited reduction in psoriasis like inflammation in mice. The ibuprofen loaded transferosomal gel was successfully developed and has shown the potential to be a new therapy against psoriasis like inflammation.

scholarly journals Enrichment of aqueous solubility and dissolution profile of mesalamine: In vitro evaluation of solid dispersion

2021 ◽  
Vol 9 (2) ◽  
pp. 127-135
Author(s):  
Anil Raosaheb Pawar ◽  
Pralhad Vitthalrao Mundhe ◽  
Vinayak Kashinath Deshmukh ◽  
Ramdas Bhanudas Pandhare ◽  
Tanaji Dilip Nandgude
Keyword(s):  
Ulcerative Colitis ◽  
Drug Release ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Peg 4000

The aim of the present study was to formulate solid dispersion (SD) of Mesalamine to enrich the aqueous solubility and dissolution rate. Mesalamine is used in the management of acute ulcerative colitis and for the prevention of relapse of active ulcerative colitis. In the present study, Solid dispersion of Mesalamine was prepared by Fusion and Solvent evaporation method with different polymers. SD’s were characterized by % practical yield, drug content, Solubility, FT-IR, PXRD (Powder X- ray diffractometry), SEM (Scanning electron microscopy), in vitro dissolution studies and Stability studies. The percent drug release of prepared solid dispersion of Mesalamine by fusion and solid dispersion method (FM47, FM67, SE47 and SE67) in 1:7 ratio was found 81.36±0.41, 86.29±0.64, 82.45±0.57and 87.25±1.14 respectively. The aqueous solubility and percent drug release of solid dispersion of Mesalamine by both methods was significantly increased. The PXRD demonstrated that there was a significant decrease in crystallinity of pure drug present in the solid dispersions, which resulted in an increased aqueous solubility and dissolution rate of Mesalamine.The significant increase in aqueous solubility and dissolution rate of Mesalamine was observed in solid dispersion as the crystallinity of the drug decreased, absence of aggregation and agglomeration, increased wetability and good dispersibility after addition of PEG 4000 and PEG 6000.

scholarly journals Crushed Tablets: Does the Administration of Food Vehicles and Thickened Fluids to Aid Medication Swallowing Alter Drug Release?

2014 ◽  
Vol 17 (2) ◽  
pp. 207 ◽  
Author(s):  
Yady Juliana Manrique-Torres ◽  
Danielle J Lee ◽  
Faiza Islam ◽  
Lisa M Nissen ◽  
Julie A.Y. Cichero ◽  
...  
Keyword(s):  
Drug Release ◽  
Orange Juice ◽  
Immediate Release ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Simulated Gastric Fluid ◽  
Drug Bioavailability ◽  
Thickening Agents

Purpose. To evaluate the influence of co-administered vehicles on in vitro dissolution in simulated gastric fluid of crushed immediate release tablets as an indicator for potential drug bioavailability compromise. Methods. Release and dissolution of crushed amlodipine, atenolol, carbamazepine and warfarin tablets were tested with six foods and drinks that are frequently used in the clinical setting as mixers for crushed medications (water, orange juice, honey, yoghurt, strawberry jam and water thickened with Easythick powder) in comparison to whole tablets. Five commercial thickening agents (Easythick Advanced, Janbak F, Karicare, Nutilis, Viscaid) at three thickness levels were tested for their effect on the dissolution of crushed atenolol tablets. Results. Atenolol dissolution was unaffected by mixing crushed tablets with thin fluids or food mixers in comparison to whole tablets or crushed tablets in water, but amlodipine was delayed by mixing with jam. Mixing crushed warfarin and carbamazepine tablets with honey, jam or yoghurt caused them to resemble the slow dissolution of whole tablets rather than the faster dissolution of crushed tablets in water or orange juice. Crushing and mixing any of the four medications with thickened water caused a significant delay in dissolution. When tested with atenolol, all types of thickening agents at the greatest thickness significantly restricted dissolution, and products that are primarily based on xanthan gum also delayed dissolution at the intermediate thickness level. Conclusions. Dissolution testing, while simplistic, is a widely used and accepted method for comparing drug release from different formulations as an indicator for in vivo bioavailability. Thickened fluids have the potential to retard drug dissolution when used at the thickest levels. These findings highlight potential clinical implications of the addition of these agents to medications for the purpose of dose delivery and indicate that further investigation of thickened fluids and their potential to influence therapeutic outcomes is warranted. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

scholarly journals Formulation and evaluation of self nano-emulsifying drug delivery system of ezetimibe for dissolution rate enhancement

2020 ◽  
Vol 11 (2) ◽  
pp. 1294-1301
Author(s):  
Geethanjali K ◽  
Vaiyana Rajesh C
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Dissolution Rate ◽  
Delivery System ◽  
Tween 80 ◽  
In Vitro Dissolution ◽  
Cinnamon Oil ◽  
Peg 400 ◽  
Solid Form

The present study was aimed to develop a Self Nano Emulsifying Delivery System of Ezetimibe (EZM) for enhancing its dissolution rate. Ezetimibe is a cholesterol absorption inhibitor, being a lipophilic drug due to its low solubility EZM shows a low dissolution profile. The SNEDDS formulation consisted of excipients Cinnamon oil, Tween 80, PEG 400 as the Oil, Surfactant and Co-surfactant. Twelve formulations with different ratios of Oil, Surfactant and Co-surfactant were prepared. The liquid SNEDDS were then converted into Solid form by adsorption technique using Avicel PH 101 and Aerosil 200 as adsorbents. The liquid SNEDDS was characterised for Particle size, Emulsification time, Dispersibility, percentage transmittance, PCM, Centrifugation, Cloud Point and Freeze thaw cycle. The solid form was characterized for the flow property, SEM, Drug content and in-vitro dissolution. Among the twelve formulations F6 formulation was found to have a particle size of 196 nm and PDI of 0.123. F6 formulation was selected as the best and it was made into solid by adsorption onto solid carriers. The F6 formulation consisted of the 25% Cinnamon oil, 50% tween 80 and 25% PEG 400. The in-vitro dissolution rate of the prepared formulation was compared with the marketed formulation. The in-vitro dissolution data showed that the drug release at the end of 60 mins from marketed formulation was 63.75 % and from SNEDDS formulation was         90.62 %. The dissolution rate of the prepared SNEDDS was increased by 1.42 times than the marketed formulation. The increase in the dissolution rate shows that SNEDDS is a suitable drug delivery system to enhance the rate of dissolution of Ezetimibe.

scholarly journals Formulation of Ramipril Tablets Containing Solid Dispersion Employing Selective Polymers to Enhance Dissolution Rate

2020 ◽  
Vol 10 (3-s) ◽  
pp. 142-149
Author(s):  
Inder Kumar ◽  
Sandeep Verma ◽  
Amit Chaudhary
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Phosphate Buffer ◽  
Flow Property ◽  
In Vitro Dissolution ◽  
Standard Data ◽  
Evaporation Technique ◽  
Good Flow

Objective: The present work based on formulation of Ramipril tablets containing solid dispersion employing selective polymers. The objective of the preparation is to prepare the solid dispersion of the Ramipril, which has more responsive value in terms of the dissolution rate. Method: Solid dispersion complex was prepared with two different carriers PEG 6000 and PVP K30. Nine formulations were developed and each formulation were subjected to pre compression and post compression parameters. Result and Discussion:  Pre-compression and post compression parameters were studied which had shown good flow property and compiled the standard data. In-vitro dissolution studies shows more than 90 % drug release in phosphate buffer pH 6.8 in 30 min. Out of all formulation F4 showed 92.55±0.67 % drug release with in 30min which was the best result rest of the formulation. Conclusion: Ramipril tablets were successfully prepared and evaluated. F4 formulation shows the greater dissolution rate in phosphate buffer pH 6.8 as compared to other formulations. When compared with marketed formulation it also shows better results. Therefore, Ramipril solid dispersion tablets enhanced the dissolution rate and can be more efficacious for improving oral bioavailability of Ramipril. Keywords: Solid dispersion, Ramipril, Solvent Evaporation Technique.

scholarly journals DESIGN AND EVALUATION OF SELF-NANO EMULSIFYING DRUG DELIVERY SYSTEMS OF ALVERINE FOR ENHANCEMENT OF SOLUBILITY

2021 ◽  
Vol 12 (7) ◽  
pp. 25-31
Author(s):  
Pooja . ◽  
Pankaj Kumar Sharma ◽  
Viswanath Agrahari
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Ethyl Oleate ◽  
Spherical Shape ◽  
Tween 80 ◽  
In Vitro Dissolution ◽  
Transmission Electron ◽  
The Stability

Background: The aim of this study is to develop a liquid self-nano emulsifying drug delivery system for alverine (liquid-SNEDDS).Excipients in the alverine SNEDDS include Ethyl oleate as the oil phase, Tween 80 as a surfactant, and PEG600, Propylene glycol as a cosurfactant.The prepared eleven formulations of alverine SNEDDS were performed for emulsification time, percentage transmittance, particle size, drug release, in vitro dissolution and stability studies.The optimised alverine liquid SNEDDS formulation (D1) was studied for drug-excipient compatibility using infrared spectroscopy, as well as particle size, zeta potential, transmission electron microscopy, and stability. Alverine SNEDDS have a spherical shape with uniform particle distribution, according to their morphology. D1's optimised formulation's drug release percentage (96.6). The stability data revealed no discernible changes in drug content, emulsifying properties, drug release, or appearance. As a result, a potential SNEDDS formulation of alverine with improved solubility, dissolution rate, and bioavailability was developed.

Development, Optimization, Characterization and Impact of In vitro Lipolysis on Drug Release of Telmisartan Loaded SMEDDS

2019 ◽  
Vol 9 (4) ◽  
pp. 330-340 ◽  
Author(s):  
Ravinder Verma ◽  
Deepak Kaushik
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Oral Bioavailability ◽  
Research Work ◽  
Mixture Design ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
In Vitro Lipolysis ◽  
Globule Size

Objective: The objective of the current research is systematic optimization and development of microemulsion preconcentrates to get better solubility that results in improvement of oral bioavailability profile of Telmisartan utilizing D-optimal mixture design. Methods: Solubility studies in a variety of lipidic ingredients and optimization of formulations were carried out for the development of liquid SMEDDS. D-optimal mixture design was utilized for assessing the interaction performance of desired responses (such as % cumulative drug release and globule size) and optimized using desirability approach. The optimized batch was evaluated for its % cumulative drug release and globule size performance for determining the dissolution rate and oral bioavailability of drug. Results: The optimized batch (F-8), which contained 10% oil (Capmul MCM EP), 45% surfactant (Labrasol) and 45% co-surfactant (Transcutol HP) resulted in desired qualities of measured responses with 84.6nm globule size and 98.5% drug release within 15 minutes. Optimized SMEDDS showed brilliant goodness of fit between drug release. Stability studies indicated stability of the optimized SMEDDS batch over 3-month storage at 40°C/75% RH and improved dissolution rate in contrast to pure API. The optimized SMEDDS showed no impact of in vitro lipolysis on drug release. Conclusion: Developed and optimized SMEDDS showed improved in vitro dissolution rate and dissolution profile in contrast to pure drug. These investigations further confirm dose reduction in SMEDDS by gaining an equivalent therapeutic profile with non-SMEDDS formulation. This research work successfully shows the potential usage of SMEDDS for delivery of BCS-II class drugs.

DEVELOPMENT AND CHARACTERIZATION OF GASTRO RETENTIVE MUCOADHESIVE MICROBEADS CONTAINING SIMVASTATIN WITH DIFFERENT CROSS LINKING AGENTS

2020 ◽  
pp. 118-126
Author(s):  
VENKATA RAMANA REDDY K. ◽  
NAGABHUSHANAM M. V. ◽  
PAMULA REDDY B. ◽  
RAVINDAR NAIK E.
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Aluminium Chloride ◽  
In Vitro Dissolution ◽  
Cross Linking ◽  
Stability Studies ◽  
Study Results ◽  
Curing Agents

Objective: The aim of the present work was to prepare and examine drug release of the oral controlled release microbeads using different curing agents by emulsification internal ionic gelation technique. Methods: Cross-linked alginate microbeads were prepared with different cross linking agents by using mucoadhesive properties. The formation and compatibility of microbeads were confirmed by compatibility studies. Prepared microbeads evaluated for encapsulated efficiency, micromeritic properties, drug loading, in vitro wash off studies, in vitro dissolution studies, drug release kinetics and stability studies Results: The in vitro drug release was influenced by both type of curing agents and type of polymers and no significant changes in characterization parameters was observed after 3 mo stability studies. The sustained release profile of optimized batch was found to be 99.66±0.18% in comparison to pure drug profile of 28.64±0.02% at 12 h release study. Results of both wash-off and in vitro studies suggests that batch (SF2) prepared with aluminium chloride has shown better mucoadhesive property. Drug release of optimized batch follows zero order with non fickian mechanism according to Korsmeyer-Peppas equation. Conclusion: The data suggest the use of simvastatin mucoadhesive cross linked microbeads to offer the potential for oral controlled drug delivery with improved gastric retention and capable to provide sustained drug release by using cross linking agents.

Formulation and In Vivo Evaluation of Mucoadhesive Buccal Tablets of Carvedilol

2013 ◽  
Vol 6 (3) ◽  
pp. 2164-2171
Author(s):  
S. B. Shirsand ◽  
G V Wadageri ◽  
S A Raju ◽  
Gopikrishna Kolli
Keyword(s):  
Drug Release ◽  
Residence Time ◽  
Hydroxypropyl Methylcellulose ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Stability Studies ◽  
Matrix Layer ◽  
Buccal Tablets ◽  
Carbopol 934P

In present study we studied the feasibility of preparing mucoadhesive buccal delivery systems containing carvedilol to improve drug residence time on buccal mucosa and drug dissolution rate, to circumvent the first-pass metabolism and quick drug entry into the systemic circulation. Bilayer buccal tablets of carvedilol prepared using controlled release and mucoadhesive polymers (hydroxypropyl methylcellulose 15 cps, 50 cps, K4M and Carbopol 934p) along with impermeable backing layer (ethyl cellulose). 15 formulations were developed with varying concentrations of polymers. The designed tablets were evaluated for tablet size, shape, in vitro drug release, stability studies, bioavailability studies and drug-excipients interaction (FTIR). Among the 15 formulations, F151 containing hydroxypropyl methylcellulose 15 cps (48% w/w of matrix layer), Carbopol 934p (2% w/w of matrix layer) and mannitol (channeling agent, 34.5% w/w of matrix layer) was found to be promising. Dissolution tests revealed that 84.73% of carvedilol was dissolved from the formulation F151 in 8 h along with satisfactory bio adhesion strength (5.71 g). Bioavailability studies of the promising formulation were compared with that of the oral solution.  The percentage relative bioavailability of the buccal tablets was found to be 121.27%. Stability studies, on the promising formulation indicated that there are no significant changes in drug content and in vitro dissolution characteristics (p<0.05). FTIR studies show no evidence of interaction between drug and excipients. It was concluded that mucoadhesive buccal tablets of carvedilol with controlled unidirectional drug release along with satisfactory bioadhesion strength and with sufficient residence time can be successfully developed by direct compression method.

Formulation and Evaluation of Directly Compressible Agglomerates of Celecoxib

2011 ◽  
Vol 3 (4) ◽  
pp. 1193-1204
Author(s):  
V. Rama Mohan Gupta ◽  
Srikanth K ◽  
Sree Giri Prasad, B ◽  
G. Naveen Kumar Reddy ◽  
Sudheer B
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Drug Loading ◽  
Hydrophilic Polymers ◽  
Dissolution Rates ◽  
In Vitro Drug Release ◽  
Peg 4000 ◽  
Spherical Crystals

Prepared spherical crystals of Celecoxib to increase the compressible properties, dissolution rate and bioavailability, using hydrophilic polymers such as PEG-4000, sod.CMC, sod.alginate and PVP K-30. All the formulations were characterized for micromeritic properties, Drug loading, solubility, in vitro drug release and mean dissolutiom time (MDT).  New formulations showed higher dissolution rates and less MDT values than the pure celecoxib. Among all, the crystals prepared with 10 % w/v PVP K-30 exhibited maximum dissolution rate (2.95±0.23%) and very less MDT values (18.50 ± 4.01 min). Hence it was considered as optimized formulation. 

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