scholarly journals EXPLORING THE POTENTIAL OF EUDRAGIT FOR DEVELOPMENT OF MICROPARTICLES OF WATER SOLUBLE DRUG USING QUALITY BY DESIGN APPROACH

2019 ◽  
pp. 110-116
Author(s):  
SHAILESH SHARMA ◽  
NIMRATA SETH
Keyword(s):  
Drug Release ◽  
Optimization Design ◽  
Optimization Technique ◽  
Entrapment Efficiency ◽  
Water Soluble ◽  
Statistical Interpretation ◽  
Independent Variables ◽  
Water Soluble Drug ◽  
Response Variables

Objective: In the present protocol, employability of polymethacrylate polymer Eudragit RS100 for development of microparticles of water soluble drug with desired values of response variables was investigated by central composite optimization design through application of Design Expert® software (Series DX10). Methods: The microparticles were developed by emulsion solvent evaporation process employing Eudragit RS100. Two effective independent variables drug: polymer ratio and stirring speed were selected to assess performance prospective of Eudragit on mean particle size, entrapment efficiency, percent yield and drug release in 12 h of microparticles. Thirteen batches generated by software were prepared and subjected to different characterization test parameters obligatory for the evaluation of formulation. Validation of optimization model and Statistical interpretation of results was done using Analysis of Variance (ANOVA) Results: ANOVA indicated that the independent variables had significant effect on response variables. Optimized formulation demonstrated close agreement amongst experimental and predicted responses with high desirability factor. In vitro drug liberation study for optimized formulation proposed a sustained release of drug from microparticles. Conclusion: In conclusion, optimization technique was imperative in indicating the efficient applicability of Eudragit RS100 polymer in controlling the drug release of hydrophilic drugs.

Formulation and Evaluation of Solid Self-Nanoemulsifying Drug Delivery System for Enhancing the Solubility and Dissolution Rate of Budesonide

2021 ◽  
pp. 5755-5763
Author(s):  
Kanuri Lakshmi Prasad ◽  
Kuralla Hari
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Dissolution Rate ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ternary Phase Diagram ◽  
Water Soluble ◽  
Drug Release Profile ◽  
Water Soluble Drug

Objective: To enhance solubility and dissolution rate of budesonide through development of solid self-nanoemulsifying drug delivery system (S-SNEDDS). Methods: Liquid self-nanoemulsifying drug delivery systems (L-SNEDDS) were prepared and ternary phase diagram was constructed using Origin pro 8. Liquid self-nanoemulsifying formulation LF2 having 20% oil and 80% of surfactant/co-surfactant was optimized from the three formulations (LF1-LF3) to convert in to solid, through various characterization techniques like self-emulsification, in vitro drug release profile and drug content estimation. The prepared L-SNEDDS converted into S-SNEDDS, SF1-SF6 by adsorption technique using Aerosil 200, Neusilin US2, and Neusilin UFL2 to improve flowability, compressibility and stability. Results: Formulation LF2 exhibited globule size of 82.4 nm, PDI 0.349 and Zeta potential -28.6 mV with drug indicating the stability and homogeneity of particles. The optimized formulation SF4 containing Neusilin UFL2 was characterized by DSC, FTIR, X-Ray diffraction studies and found no incompatibility and no major shifts were noticed. Formulation SF4 released 100 % drug in 20 min against pure drug release of 47 % in 60 min. Regardless of the form (i.e. liquid or solid) similar performance of emulsification efficiency is observed. Conclusion: The results demonstrated that the technique of novel solid self-nanoemulsifying drug delivery system can be employed to enhance the solubility and dissolution rate of poorly water-soluble drug budesonide.

scholarly journals FORMULATION AND CHARACTERIZATION OF GASTRORETENTIVE FLOATING MICROBALLOONS OF POORLY WATER-SOLUBLE DRUG DIACEREIN

2021 ◽  
Vol 15 (5) ◽  
pp. 8-12
Author(s):  
Kajal Tomer ◽  
Dilip Kumar Gupta
Keyword(s):  
Particle Size ◽  
Entrapment Efficiency ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Diffusion Method ◽  
Acrylic Polymer ◽  
Water Soluble Drug ◽  
Technological Advances ◽  
S 100

The drug can be released in a controlled manner using a gastro retentive dosage type. The main focus on the novel technological advances in the floating drug delivery method for gastric retention. The preparation of diacerein micro balloon is done by solvent diffusion method, using acrylic polymer like Eudragit S 100 and HPMC K4 M. The various evaluation of the prepared floating microsphere like its % yield, drug entrapment efficiency, particle size in-vitro dissolution, buoyancy, was studied. The floating microsphere was found to be spherical and range from 85 μm - 192 μm. Whereas the buoyancy in gastric mucosa between the range 30.5% -49.5%. The % yield and % entrapment efficiency were found under the range 61% - 82% and 45.1–84.1% respectively. The microsphere showed favorable in-vitro dissolution 76.8 to 94.45. The optimized formulation was found based on evaluation of floating micro-balloons, Formulation (M3E3) showed the best result as particle size 192 μm, DDE 84.1%, in vitro drug release 94.5%, and in vitro buoyancy 49.5%. all the formulations showed controlled release up to 24 hours.

scholarly journals Method Development Technologies for Clopidogrel Bisulphate by Improving Solubility and Bioavailability

2021 ◽  
Vol 6 (02) ◽  
pp. 15-21
Author(s):  
Deevan Paul A. ◽  
Avilala Neelima ◽  
Chitra Prasanthi ◽  
Navyaja Kota
Keyword(s):  
Drug Release ◽  
Method Development ◽  
Physical Nature ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Adenosine Diphosphate ◽  
Water Soluble ◽  
Irreversible Inhibitor ◽  
Water Soluble Drug ◽  
Drug Entrapment Efficiency

Clopidogrel bisulphate (CB) is a crystalline, poorly water-soluble drug of bioavailability less than 50%. The drug is an irreversible inhibitor of the P2Y12 adenosine diphosphate receptor found on the membranes of platelet cells. The present work was performed using different polymers such as Polyvinylpyrrolidone (PVP) K-30 and polyvinyl alcohol with varied surfactants such as Tween 80 in comparison by using superdisintegrants like Sodium Starch Glycolate (SSG) and Microcrystalline Cellulose (MCC). By performing the particle size distribution, the size ranges from 232.6 nm to 995.6 nm and the polydispersity index ranges from 0.11 to 0.96, these ranges indicating the good physical nature of nanoparticles. The drug entrapment efficiency (DEE) of clopidogrel bisulphate nanoparticles was found to be in the range of 30.10% to 94.4%. From the study, it was found that F2 formulation containing PVP K-30 and L-arginine has given the best release in 80mins and the maximum cumulative drug release was 96.8% in comparison with other formulation, and the dissolution studies were performed for the seven formulations of prepared clopidogrel bisulphate granules among which F5 formulation containing crospovidone has given maximum drug release of 91.6% within 80mins. Here we state that the method development technologies improve the solubility and bioavailability studies by producing the nanoparticles.

Formulation Development of Metoprolol Succinate Controlled Release Tablets using Ethyl-cellulose-polyvinyl-pyrrolidone Coating

2015 ◽  
Vol 8 (2) ◽  
pp. 2851-2857
Author(s):  
Kiran Kumar Vangara ◽  
Kishore K. Konda ◽  
Shiva K. Ravula ◽  
Pradeep K Vuppala ◽  
Vijay K. Sripuram ◽  
...  
Keyword(s):  
Weight Gain ◽  
Controlled Release ◽  
Drug Release ◽  
Ethyl Cellulose ◽  
Film Coating ◽  
Release Profile ◽  
Water Soluble ◽  
Metoprolol Succinate ◽  
Water Soluble Drug

It is challenging to develop a controlled release (CR) formulation for a freely water soluble drug molecule without using rate controlling polymers in the core matrix. This study is aimed to develop and evaluate cost-effective ethyl cellulose (EC)-polyvinyl pyrrolidone (PVP) film coating that can effectively control the release of freely water soluble drug, metoprolol succinate (MS) and to match that of release profile with its marketed tablet. Simple core tables of MS were compressed and coated with a solution composed of hydrophobic rate controlling polymer, EC and water soluble pore forming polymer, PVP. The effect of formulation parameters such as the ratio of EC to PVP and tablet coating weight gain on the in-vitro drug release were evaluated. Release profile of the optimized formulation at different pH conditions was determined and the similarity factor (f2) with marketed release profile was calculated.It was observed that drug release rate increased with a decrease in the ratio of ethyl cellulose to PVP and decreased with increased weight gain of the coating membrane. Among all the formulations, the formulation with EC and PVP at a ratio of 60:40 %w/w and 9% weight gain showed matching release profile to marketed tablet with f2 value of 72.25. The optimized formulation showed pH independent in-vitro release. This study successfully demonstrated that EC-PVP film coating can effectively control the release rate of freely soluble drugs. Once a day CR formulation of metoprolol succinate pharmaceutically equivalent to marketed tablet was developed.  

scholarly journals Improved Bioavailability of Poorly Water-Soluble Drug by Targeting Increased Absorption through Solubility Enhancement and Precipitation Inhibition

2021 ◽  
Vol 14 (12) ◽  
pp. 1255
Author(s):  
Ju-Hyun Lee ◽  
Chulhun Park ◽  
Kwon-Yeon Weon ◽  
Chin-Yang Kang ◽  
Beom-Jin Lee ◽  
...  
Keyword(s):  
Drug Release ◽  
Amorphous State ◽  
Water Soluble ◽  
Pharmacokinetic Data ◽  
In Vivo Test ◽  
Water Soluble Drug ◽  
Absorption Area ◽  
Poorly Water Soluble

Itraconazole (ITZ) is a class II drug according to the biopharmaceutical classification system. Its solubility is pH 3-dependent, and it is poorly water-soluble. Its pKa is 3.7, which makes it a weak base drug. The aim of this study was to prepare solid dispersion (SD) pellets to enhance the release of ITZ into the gastrointestinal environment using hot-melt extrusion (HME) technology and a pelletizer. The pellets were then filled into capsules and evaluated in vitro and in vivo. The ITZ changed from a crystalline state to an amorphous state during the HME process, as determined using DSC and PXRD. In addition, its release into the gastrointestinal tract was enhanced, as was the level of ITZ recrystallization, which was lower than the marketed drug (Sporanox®), as assessed using an in vitro method. In the in vivo study that was carried out in rats, the AUC0–48h of the commercial formulation, Sporanox®, was 1073.9 ± 314.7 ng·h·mL−1, and the bioavailability of the SD pellet (2969.7 ± 720.6 ng·h·mL−1) was three-fold higher than that of Sporanox® (*** p < 0.001). The results of the in vivo test in beagle dogs revealed that the AUC0–24h of the SD-1 pellet (which was designed to enhance drug release into gastric fluids) was 3.37 ± 3.28 μg·h·mL−1 and that of the SD-2 pellet (which was designed to enhance drug release in intestinal fluids) was 7.50 ± 4.50 μg·h·mL−1. The AUC of the SD-2 pellet was 2.2 times higher than that of the SD-1 pellet. Based on pharmacokinetic data, ITZ would exist in a supersaturated state in the area of drug absorption. These results indicated that the absorption area is critical for improving the bioavailability of ITZ. Consequently, the bioavailability of ITZ could be improved by inhibiting precipitation in the absorption area.

scholarly journals Formulation and Optimization of Sustained Release Stavudine Microspheres Using Response Surface Methodology

2011 ◽  
Vol 2011 ◽  
pp. 1-7 ◽  
Author(s):  
Sanjay Dey ◽  
Soumen Pramanik ◽  
Ananya Malgope
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Entrapment Efficiency ◽  
Sustained Drug Release ◽  
Independent Variables ◽  
Optimum Formulation ◽  
Dependent Variables ◽  
High Entrapment Efficiency ◽  
Full Factorial

The aim of the current study was to formulate and optimize the formulation on the basis of in vitro performance of microsphere. A full factorial design was employed to study the effect of independent variables, polymer-to-drug ratio () and stirring speed (), on dependent variables, encapsulation efficiency, particle size, and time to 80% drug release. The best batch exhibited a high entrapment efficiency of 70% and mean particle size 290 μm. The drug release was also sustained for more than 12 hours. The study helped in finding the optimum formulation with excellent sustained drug release.

scholarly journals Development and in vitro evaluation of sustained release multiparticulate tablet of freely water soluble drug

2010 ◽  
Vol 46 (3) ◽  
pp. 463-471 ◽  
Author(s):  
Ashlesha Pravin Pandit ◽  
Rajendra Dattatray Shinde
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
Aqueous Dispersion ◽  
Water Soluble ◽  
Coating Materials ◽  
Metoprolol Succinate ◽  
Water Soluble Drug ◽  
Zero Order Release

Blends of aqueous dispersion of a hydrophobic and hydrophilic polymer, namely Surelease®: hydroxypropyl methylcellulose (Surelease®: HPMC E15) were used as coating materials to control the drug release from coated pellets of the highly water soluble drug metoprolol succinate. Varying the polymer blends, ranges of drug release patterns were obtained at pH 6.8. The present study dealt with diffusion of drug through plasticized Surelease®/ hydroxypropyl methylcellulose (HPMC E15) films prepared by coating of drug and polymers onto non-pareil seeds using the solution layering technique. The release of metoprolol succinate from coated pellets was decreased with increased coating load of polymer. The optimized formulation was obtained by 3² full factorial design. The release profile revealed that the optimized formulation follows zero order release kinetics. The stability data showed no interaction for storage at 25ºC and 60% relative humidity.

scholarly journals COMPARISON AND CHARACTERIZATION OF INCLUSION COMPLEXES AND SOLID DISPERSIONS IN ENHANCEMENT OF DISSOLUTION RATE OF POORLY WATER SOLUBLE DRUG

2018 ◽  
Vol 10 (5) ◽  
pp. 173
Author(s):  
Radha Rani Earle ◽  
Rambabu Jammu ◽  
Lakshmi Usha ◽  
Ratna Kanth Lingam
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Inclusion Complexes ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Peg 6000 ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Objective: The purpose of the present study was to enhance solubility and dissolution characteristics of indomethacin by preparing inclusion complexes with hydroxypropyl β-cyclodextrin (HP β-CD) and solid dispersions with PEG 6000 to enhance its in vitro drug release and to further formulate it as a tabletMethods: Solid dispersions (SDs) and inclusion complexes (ICs) of Indomethacin with PEG 6000 and HP β-CD respectively were prepared to enhance the dissolution rate of this poorly water-soluble drug belonging to BCS class II. A comparison was made between two systems: solid dispersions with PEG 6000 obtained using melting and solvent evaporation technique, inclusion complexes with HP β-CD prepared by kneading technique. SDs were prepared in 1:1, 1:2, 1:3 and ICs in 1:0.25, 1:0.5, 1:1 w/w ratios of drug: polymer. Both the systems were characterized by FTIR, SEM, DSC, X-RD.Results: The dissolution of indomethacin increased with the increase in the concentration of the polymers. F4 and F9 formulations showed complete drug release in less than 30 min. Dissolution studies indicated that cyclodextrin complexes showed a better enhancement of dissolution rate when compared to solid dispersions. CDs were found to be more effective than PEGs at lower concentrations. These formulations were further compressed as tablets.Conclusion: The FTIR and DSC studies showed that no interactions existed between the drug and the polymer.

NANO-SIZED SOLID DISPERSION OF A POORLY WATER-SOLUBLE DRUG

2012 ◽  
pp. 31-35
Author(s):  
Truong Dinh Thao Tran ◽  
Ha Lien Phuong Tran ◽  
Nghia Khanh Tran ◽  
Van Toi Vo
Keyword(s):  
Drug Release ◽  
Droplet Size ◽  
Solid Dispersion ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Dissolution Enhancement ◽  
Particle Size Reduction ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Purposes: Aims of this study are dissolution enhancement of a poorly water-soluble drug by nano-sized solid dispersion and investigation of machenism of drug release from the solid dispersion. A drug for osteoporosis treatment was used as the model drug in the study. Methods: melting method was used to prepare the solid dispersion. Drug dissolution rate was investigated at pH 1.2 and pH 6.8. Drug crystallinity was studied using differential scanning calorimetric and powder X-ray diffraction. In addition, droplet size and contact angle of drug were determined to elucidate mechanism of drug release. Results: Drug dissolution from the solid dispersion was significantly increased at pH 1.2 and pH 6.8 as compared to pure drug. Drug crystallinity was changed to partially amorphous. Also dissolution enhancement of drug was due to the improved wettability. The droplet size of drug was in the scale of nano-size when solid dispersion was dispersed in dissolution media. Conclusions: nano-sized solid dispersion in this research was a successful preparation to enhance bioavailability of a poorly water-soluble drug by mechanisms of crystal changes, particle size reduction and increase of wet property.

Formulation and In Vivo Evaluation of Mucoadhesive Micro-spheres of Rebamipide, a Mucoprotective Drug for GIT Disorders

2018 ◽  
Vol 11 (3) ◽  
pp. 4089-4097
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Kanteepan P
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
In Vivo Studies ◽  
Amino Acid Derivative ◽  
Release Mechanism ◽  
In Vivo Evaluation ◽  
In Vitro Drug Release ◽  
Percentage Yield

Rebamipide, an amino acid derivative of 2-(1H)-quinolinone, is used for mucosal protection, healing of gastroduodenal ulcers, and treatment of gastritis. The current research study aimed to develop novel gastro-retentive mucoadhesive microspheres of rebamipide using ionotropic gelation technique. Studies of micromeritic properties confirmed that microspheres were free flowing with good packability. The in vitro drug release showed the sustained release of rebamipide up to 99.23 ± 0.13% within 12 h whereas marketed product displayed the drug release of 95.15 ± 0.23% within 1 h. The release mechanism from microspheres followed the zero-order and Korsmeyer-Peppas (R2 = 0.915, 0.969), respectively. The optimized M12 formulation displayed optimum features, such as entrapment efficiency 97%, particle size 61.94 ± 0.11 µm, percentage yield 98%, swelling index 95% and mucoadhesiveness was 97%. FTIR studies revealed no major incompatibility between drug and excipients. SEM confirmed the particles were of spherical in shape. Optimized formulation (M12) were stable at 40°C ± 2°C/75% RH ± 5% RH for 6 months. In vivo studies were performed and kinetic parameters like Cmax, Tmax, AUC0-t, AUC0-∞, t1/2, and Kel  were calculated. The marketed product Cmax (3.15 ± 0.05 ng/mL) was higher than optimized formulation (2.58 ± 0.03 ng/mL). The optimized formulation AUC0-t (15.25 ± 1.14 ng.hr/mL), AUC0-∞ (19.42 ± 1.24 ng.hr/mL) was significantly higher than that of marketed product AUC0-t (10.21 ± 1.26 ng.hr/mL) and AUC0-∞ (13.15 ± 0.05 ng.hr/mL). These results indicate an optimized formulation bioavailability of 2.5-fold greater than marketed product.  

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