scholarly journals Characterization of Ketoprofen/Methyl-β-Cyclodextrin Complexes Prepared Using Supercritical Carbon Dioxide

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Mauro Banchero ◽  
Silvia Ronchetti ◽  
Luigi Manna
Keyword(s):  
Dissolution Rate ◽  
Water Solubility ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Pharmaceutical Formulations ◽  
Drug Dissolution ◽  
Scanning Calorimetry ◽  
Supercritical Treatment ◽  
The Fourier Transform

Complexes of methyl-β-cyclodextrin and ketoprofen, a crystalline anti-inflammatory drug with poor water solubility, have been prepared for the first time in the presence of supercritical CO2at 40°C and 20 MPa. The supercritical treatment allows these pharmaceutical formulations to be prepared without the use of any auxiliary agents or organic solvents. The treated samples were characterized through differential scanning calorimetry, X-ray diffractometry, and the Fourier transform infrared spectroscopy to exclude the presence of crystalline drug and check the formation of the complexes. The increase of the drug dissolution rate was investigated performing in vitro release tests in aqueous solutions. The results showed that the supercritical treatment can be an efficient method to obtain inclusion complexes with enhanced release kinetics. The operating methods of the release tests, that is, the “tablet method” or the “dispersed amount method,” affected both the dissolution rate and its dependence on the drug amount in the samples. On the contrary, the variation of the pH of the dissolution medium did not show any effect on the release rate of the supercritical complexes.

scholarly journals Formulation and development of metformin-loaded microspheres using Khaya senegalensis (Meliaceae) gum as co-polymer

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Chukwuebuka H. Ozoude ◽  
Chukwuemeka P. Azubuike ◽  
Modupe O. Ologunagba ◽  
Sejoro S. Tonuewa ◽  
Cecilia I. Igwilo
Keyword(s):  
Controlled Release ◽  
Sodium Alginate ◽  
Release Kinetics ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Metformin Hydrochloride ◽  
Scanning Calorimetry ◽  
Khaya Senegalensis

Abstract Background Khaya gum is a bark exudate from Khaya senegalensis (Maliaecae) that has drug carrier potential. This study aimed to formulate and comparatively evaluate metformin-loaded microspheres using blends of khaya gum and sodium alginate. Khaya gum was extracted and subjected to preformulation studies using established protocols while three formulations (FA; FB and FC) of metformin (1% w/v)-loaded microspheres were prepared by the ionic gelation method using 5% zinc chloride solution as the cross-linker. The formulations contained 2% w/v blends of khaya gum and sodium alginate in the ratios of 2:3, 9:11, and 1:1, respectively. The microspheres were evaluated by scanning electron microscopy, Fourier transform-infrared spectroscopy, differential scanning calorimetry, entrapment efficiency, swelling index, and in vitro release studies. Results Yield of 28.48%, pH of 4.00 ± 0.05, moisture content (14.59% ± 0.50), and fair flow properties (Carr’s index 23.68 ± 1.91 and Hausner’s ratio 1.31 ± 0.03) of the khaya gum were obtained. FTIR analyses showed no significant interaction between pure metformin hydrochloride with excipients. Discrete spherical microspheres with sizes ranging from 1200 to 1420 μm were obtained. Drug entrapment efficiency of the microspheres ranged from 65.6 to 81.5%. The release of the drug from microspheres was sustained for the 9 h of the study as the cumulative release was 62% (FA), 73% (FB), and 80% (FC). The release kinetics followed Korsmeyer-Peppas model with super case-II transport mechanism. Conclusion Blends of Khaya senegalensis gum and sodium alginate are promising polymer combination for the preparation of controlled-release formulations. The blend of the khaya gum and sodium alginate produced microspheres with controlled release properties. However, the formulation containing 2:3 ratio of khaya gum and sodium alginate respectively produced microspheres with comparable controlled release profiles to the commercial brand metformin tablet.

COMPLEX OF ELUXADOLINE WITH SODIUM CAPRYLATE FOR IMPROVED SOLUBILITY AND DISSOLUTION RATE

INDIAN DRUGS ◽  
2021 ◽  
Vol 57 (11) ◽  
pp. 22-26
Author(s):  
Manisha Dhere ◽  
◽  
Arti Majumdar ◽  
Neelesh Malviya
Keyword(s):  
Dissolution Rate ◽  
Solvent Evaporation ◽  
Drug Dissolution ◽  
Dissolution Enhancement ◽  
Solvent Evaporation Method ◽  
Scanning Calorimetry ◽  
Evaporation Method ◽  
Solubility Study ◽  
Sodium Caprylate

In the present research, newly developed complex with sodium caprylate was investigated for solubility and dissolution enhancement of eluxadoline. Complexes were prepared in different ratios by solvent evaporation method and characterised solubility study, Infrared spectroscopy (IR), Diffrential scanning calorimetry (DSC), X-Ray Diffraction (XRD), drug content analysis and in vitro Drug release. The solubility and dissolution rate revealed most suitable ratio of eluxadoline and sodium caprylate (1:4). The IR, DSC and X-RD data also confirmed the results. It was concluded that complex prepared with (1:4 drug:sodium caprylate ratio) using solvent evaporation method showed significant improvement in solubility and drug dissolution.

Formulation and Evaluation of Fast Dissolving Gliclazide Tablets by Complexation with Hydroxypropyl-β-Cyclodextrin

2014 ◽  
Vol 7 (1) ◽  
pp. 2399-2405
Author(s):  
Adel M Aly ◽  
Khaled M. Al-Akhali ◽  
Hesham Alrefaey ◽  
Mahmoud A. Shaker
Keyword(s):  
Dissolution Rate ◽  
Spray Drying ◽  
Inclusion Complexes ◽  
In Vitro Release ◽  
Hypoglycemic Effect ◽  
Scanning Calorimetry ◽  
Molar Ratios ◽  
Market Product

Gliclazide (GZ) is practically insoluble in water and its bioavailability is limited by dissolution rate. The aim of the present study was to enhance the dissolution rate and bioavailability of GZ by complexation with hydroxypropyl (HP)-β-cyclodextrin (CD) applying three different methods; physical mixing, kneading technique and spray drying technique.  Also, to evaluate the dissolution rate and the hypoglycemic effect of the prepared complexes, in comparison with the GZ market product (Glizide tablets) in Saudi market. The produced complexes were characterized and evaluated using Differential Scanning Calorimetry (DSC), X-ray Diffractometry (XRD), Scanning Electron Microscope (SEM) and the in vitro release studies. All the methods of preparation of complexes were found to be effective in improving the solubility of gliclazide in comparison with the commercial product (Glizide tablets). The formation of inclusion complexes was evident in these formulations as shown by DSC and XRD studies. The inclusion complexes prepared by spray drying method in 1:1 molar ratios were the most effective method for improving the solubility of GZ. The in-vivo hypoglycemic effect of the complexed GZ-HP-β-CD prepared by spray drying significantly improved the biological performance and therapeutic efficacy of the drug compared to Glizide market product.  

Formulation and Characterization of Nateglinide Nanosuspension by Precipitation Method

2014 ◽  
Vol 7 (4) ◽  
pp. 2685-2691
Author(s):  
Amruta Papdiwal ◽  
Kishor Sagar ◽  
Vishal Pande
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
Water Solubility ◽  
Average Particle Size ◽  
Biologically Active ◽  
In Vitro Dissolution ◽  
Precipitation Method ◽  
Average Particle ◽  
Scanning Calorimetry

Poor water solubility and slow dissolution rate are major issues for the majority of upcoming and existing biologically active pharmaceutical compounds. Nateglinide is Biopharmaceutical Classification System Class-II drug that has low solubility and high permeability. The purpose of the present study was to improve the solubility and dissolution rate of Nateglinide by the preparation of nanosuspension by the nanoprecipitation technique. Nateglinide nanosuspension was evaluated for its particle size, in vitro dissolution study, and characterized by differential scanning calorimetry and scanning electron microscopy. The optimized formulation showed an average particle size of 207 nm and zeta potential of -25.8 mV. The rate of dissolution of the optimized nanosuspension was enhanced by 83% in 50 min relative to micronized suspension of nateglinide (37% in 50 min). This improvement was mainly due to the formulation of nanosized particles of Nateglinide. Stability study revealed that nanosuspension was more stable at room temperature and refrigerator condition with no significant change in particle size distribution. These results indicate that the nateglinide loaded nanosuspension may significantly improve in vitro dissolution rate and thereby possibly enhance the onset of therapeutic effect.

Validation of RP-HPLC Method for Determination of Omeprazole in Dissolution Media and Application to Study in-vitro Release from Solid-SNEDDS

2021 ◽  
Vol 17 ◽  
Author(s):  
Suhair S. Al-Nimry ◽  
Khouloud A. Alkhamis ◽  
Bashar M. Altaani
Keyword(s):  
Dissolution Rate ◽  
Phosphate Buffer ◽  
Water Solubility ◽  
In Vitro Release ◽  
Hplc Method ◽  
In Vitro Dissolution ◽  
Limit Of Quantification ◽  
Rp Hplc

Background: Omeprazole has poor water solubility, is unstable in acidic solutions, and undergoes first pass metabolism which results in lowering its bioavailability. A solid Self-Nano Emulsifying Drug Delivery System (SNEDDS) was previously prepared to enhance its dissolution. Objective: Development and validation of a RP-HPLC method with UV detection for the determination of omeprazole in 0.1N HCl and in 0.01 M phosphate buffer (pH 7.4). Methods: Validation was according to the ICH Q2 (R1) guidelines in terms of linearity, accuracy and precision, lower limit of quantification, sensitivity, specificity, and robustness. The developed and validated method was used to study the in-vitro dissolution of the drug from the solid-SNEDDS, commercial products and of the unprocessed drug. The dissolution was studied in 500 ml of 0.1N HCl during the first 2 hours, and 900 mL of 0.01 M phosphate buffer (pH 7.4) during the last hour (37 ± 0.5 oC and 100 rpm). Results: The method was linear in the range 1-50 μg/ml, accurate and precise as indicated by the ANOVA test. It was specific to the drug and the pharmaceutical excipients did not affect the determination of its concentration. The method was robust to small changes in pH, composition, and flow rate of the mobile phase. The dissolution rate of omeprazole from the Solid-SNEDDS was faster than that from two commercial dosage forms and than the dissolution rate of the unprocessed drug. Conclusion: The method met the acceptance criteria and was applied successfully in studying the rate of dissolution of the drug.

scholarly journals DESIGN, OPTIMIZATION AND IN VITRO EVALUATION OF ANTIFUNGAL ACTIVITY OF NANOSTRUCTURED LIPID CARRIERS OF TOLNAFTATE

2019 ◽  
pp. 109-115
Author(s):  
AHMED GARDOUH ◽  
Samar H. Faheim ◽  
Samar M. Solyman
Keyword(s):  
Zeta Potential ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Homogenization Method ◽  
Nanostructured Lipid Carriers ◽  
Scanning Calorimetry ◽  
Release Study ◽  
Vitro Release

Objective: The main purpose of this work was to prepare tolnaftate (TOL) loaded nanostructured lipid carriers (NLCs), Evaluate its characteristics and in vitro release study. Methods: Tolnaftate loaded Nanostructured lipid carriers were prepared by the high shear homogenization method using different liquid lipids types (DERMAROL DCO® and DERMAROL CCT®) and concentrations, different concentration ratios of tween80® to span20® and different homogenization speeds. All the formulated nanoparticles were subjected to particle size (PS), zeta potential (ZP), polydispersity index (PI), drug entrapment efficiency (EE), Differential Scanning Calorimetry (DSC), Transmission Electron microscopy (TEM), release kinetics and in vitro release study was determined. Results: The results revealed that NLC dispersions had spherical shapes with an average size between 154.966±1.85 nm and 1078.4±103.02 nm. High entrapment efficiency was obtained with negatively charged zeta potential with PDI value ranging from 0.291±0.02 to 0.985±0.02. The release profiles of all formulations were characterized by a sustained release behavior over 24 h and the release rates increased as the amount of surfactant decreased. The release rate of TOL is expressed following the theoretical model by Higuchi. Conclusion: From this study, It can be concluded that NLCs are a good carrier for tolnaftate delivery

scholarly journals ENHANCING DISSOLUTION RATE OF INDOMETHACIN BY IN SITU CRYSTALIZATION; DEVELOPMENT OF ORALLY DISINTEGRATING TABLETS

2018 ◽  
Vol 10 (5) ◽  
pp. 18
Author(s):  
Nadia H. Naiem ◽  
Ebtessam A. Essa ◽  
Gamal M. Elmaghraby
Keyword(s):  
Dissolution Rate ◽  
In Vitro Release ◽  
Alkaline Media ◽  
Drug Dissolution ◽  
Precipitation Process ◽  
Acid Media ◽  
Enhanced Dissolution ◽  
In Situ Crystallization

Objective: The main objective of this study was to investigate the potential of in situ crystallization of indomethacin, in presence or absence of hydrophilic materials, to improve drug dissolution with the goal of developing fast disintegrating tablets.Methods: Indomethacin crystals were prepared by bottom up approach. Water containing hydrophilic additive (polymer or/and surfactant) was added to ethanolic solution of indomethacin while stirring. The selected polymers were hydroxylpropylmethyl cellulose E5 (HPMC E5), polyethylene glycol 6000 (PEG6000) and polyvinylpyrrolidone K40 (PVP K40). The surfactants used were Tween80 and Glucire 44/14. The precipitated particles were collected and air dried. Solid state characterization were performed in addition to in vitro release studies in both acidic (0.1 N HCL) and alkaline medium (phosphate buffer pH 6.8). Optimized formulation was selected to develop fast disintegrating tablets.Results: Thermal behavior suggested modulation in crystalline nature with reduction in particle size that was confirmed by X-ray diffraction results. Infrared spectroscopy excluded any interaction between drug and hydrophilic excipients. Drug dissolution in acid media showed slight improve in drug release, while marked increase was observed in the alkaline media. Combination between Tween80 and HPMC (F7) showed the best dissolution parameters with 5-folds enhancement in release efficiency (RE) compared to pure drug. Formula F7 was successively used to formulate fast disintegrating tablets with prompted release of 58% of the loaded dose and RE of 83%.Conclusion: In situ crystallization of indomethacin is a good approach for enhanced dissolution rate with the presence of hydrophilic additives during precipitation process improving the efficiency.

scholarly journals FORMULATION AND EVALUATION OF LIQUISOLID COMPACTS OF LORNOXICAM

2019 ◽  
pp. 33-37
Author(s):  
Asma Azaruddin Mokashi ◽  
SNEHALATA L. GAIKWAD
Keyword(s):  
Dissolution Rate ◽  
Drug Concentration ◽  
In Vitro Release ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Spectra Analysis ◽  
X Ray ◽  
Liquisolid Compacts

Objective: Objective of the present investigation was to enhance the solubility and dissolution rate of poorly water-soluble drug lornoxicam using liquisolid technique with comparative determination of in vitro release profile of liquisolid compacts and conventional formulation of lornoxicam. Methods: Formulation was prepared by a liquisolid technique using different drug concentration in a liquid vehicle and different carrier/coating ratio. Prepared liquisolid compact was evaluated for Fourier transform infrared (FTIR) spectra analysis, differential scanning calorimetry (DSC), X-ray diffraction (P-XRD), scanning electron microscopy (SEM) and in vitro dissolution study. Results: The result showed that liquisolid compacts of lornoxicam displayed significantly higher drug release rate as compared to pure drug and conventional tablet prepared. The results of both DSC and X-ray crystallography indicated loss of crystallinity of the drug upon formulated into the liquisolid compact. Conclusion: Dissolution rate of the drug from liquisolid compacts was affected by changing the drug concentration and excipient ratio. The liquisolid technique appeared to be a promising approach for improving the dissolution of poorly soluble drug lornoxicam.

scholarly journals Preparation, Characterization and Dissolution Behaviour of Freeze Dried Complexes of Curcumin-Gamma Cyclodextrin

2021 ◽  
pp. 17-26
Author(s):  
M. J. Ansari ◽  
K. Kohli ◽  
J. Ali
Keyword(s):  
Inclusion Complexes ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Stoichiometric Ratio ◽  
Scanning Calorimetry ◽  
First Order ◽  
Rate Of Dissolution ◽  
Freeze Dried ◽  
Gamma Cyclodextrin

The aim of the current research was to develop and characterize curcumin-gamma cyclodextrin inclusion complexes in order to enhance solubility and rate of dissolution of poorly soluble curcumin. Based on the stoichiometric ratio of 1:1, the inclusion complexes of curcumin with γ-cyclodextrin were prepared by freeze drying method. The prepared dried and solidified inclusion complexes were characterized with the help of infrared spectroscopy, differential scanning calorimetry, and X-ray diffractometry. The comparative evaluation of solubility and rate of dissolution were investigated and compared with pure curcumin. Dissolution study demonstrated only 10% release from pure curcumin at 1 hour as opposed of approximately 72% release form freeze dried curcumin complexes. The freeze dried complexes exhibited almost complete release after 5 hours while only 34% release was observed from the pure curcumin during the same time period. Therefore, the freeze dried complex provided approximately 3 to 7-fold enhancement in the dissolution and release of curcumin over a period of 6 hours of dissolution testing.  The kinetics of the in vitro release behaviors of the curcumin and curcumin complexes were investigated by applying various models such as zero order, first order, Higuchi and Peppas models. The release of the curcumin was observed to follow the first order release kinetics, since the correlation coefficient (R2) for the first order was the highest in comparison to other kinetic models.

scholarly journals INVESTIGATION OF KONDAGOGU GUM TO DEVELOP TRANSDERMAL FILM OF REPAGLINIDE

2018 ◽  
Vol 11 (4) ◽  
pp. 440
Author(s):  
Poreddy Srikanth Reddy ◽  
Penjuri Subhash Chandra Bose ◽  
Vuppula Sruthi ◽  
Damineni Saritha
Keyword(s):  
Chemical Interaction ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Study Data ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release ◽  
Pure Drug ◽  
The Fourier Transform ◽  
Transdermal Film

 Objective: In the present study, an attempt was made to develop polymeric blend transdermal patch of repaglinide using hydroxypropyl methyl cellulose (HPMC) K4M and kondagogu gum.Methods: A series of repaglinide drug-incorporated HPMC K4M-kondagogu gum matrix films were prepared by solvent casting method. The prepared transdermal films were evaluated for various parameters such as thickness, tensile strength, folding endurance, % elongation, % moisture content, % moisture uptake, % drug content, in vitro drug release, and drug excipient compatibility.Results: The Fourier-transform infrared spectra of the pure drug as well as drug-incorporated formulation indicated that no chemical interaction occurred between the drug and the polymers used. Differential scanning calorimetry thermograms of the pure drug and prepared formulation indicated that the drug has dispersed in micron level in the prepared films. In vitro release study data of prepared formulations were fitted into various mathematical models, and the best-fit model was found to be Higuchi model.Conclusion: Among all the formulations studied, the formulation F4 was found to be an optimized composition for efficient transdermal delivery of repaglinide for 24 h study period. Stability studies of the drug formulations concluded that the drug was stable in the optimized formulation for the study period.

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