Preparation and Characterization of Novel Self Nano Emulsifying Drug Delivery System of Allopurinol

2021 ◽  
pp. 2108-2114
Author(s):  
Priyal Patel ◽  
Shilpa Solanki ◽  
Ashok Mahajan ◽  
Falgun Mehta ◽  
Kautuk Shah
Keyword(s):  
Drug Delivery ◽  
Phase Diagram ◽  
Ternary Phase ◽  
Ternary Phase Diagram ◽  
Stability Study ◽  
Rheological Parameters ◽  
Dissolution Time ◽  
Titration Method ◽  
Uniform Size ◽  
Globule Size

The aim of research was to develop self nanoemulsifying drug delivery technology containing low aqueous soluble drug allopurinol for improving solubility, dissolution and bioavaibility. Preliminary screening were carried on the basis of maximum solubility of allopurinol in oil, surfactant, co-surfactant and pseudo-ternary phase diagram was constructed to identify the ratio of surfactant and co-surfactant for nanoemulsion formulation using water titration method. Based on the solubility study, Labrafil M 1944 CS, Cremophor RH 40, Transcutol used as oil, surfactant, and co-surfactant respectively. Pseudo-ternary phase diagram was constructed to identify the ratio of surfactant and co-surfactant for nanoemulsion formation by water titration method. As per the ternary phase diagram ratio of Smix in 2:1 was identified with maximum emulsification area. SNEDDS composed of 35 % Labrafil M 1944 CS, 43.34% Cremophor RH 40, 21.66% Transcutol. Globule size was found to be 25.42 nm, and zeta potential value was -9.26 mV. Prepared SNEDDS were evaluated for globule size, viscosity, emulsification time, cloud point, dilution test and thermodynamic stability study. Prepared liquid SNEDDS then converted into solid SNEDDS via extrusion/spheronization technique using Aerosil 200, lactose monohydrate and Croscarmellose sodium. The pellets containing SNEDDS possessed good flow properties and mechanical strength and other rheological parameters. Self nanoemulsifying pellet exhibited uniform size and shape. Friability, dissolution time and disintegration of pellets formulation shown promising results. Time required for 80% drug release of self nanoemulsifying pellet was found to be 26 min, which was significantly lower than liquid SNEDDS, plain drug containing pellet and marketed preparation of Allopurinol (ZYRIK).

scholarly journals DESIGN, PREPARATION, AND EVALUATION OF SELF-MICROEMULSIFYING DRUG DELIVERY SYSTEM OF BAMBUTEROL HYDROCHLORIDE

2019 ◽  
pp. 332
Author(s):  
SACHIN SAGGAR ◽  
ASHUTOSH UPADHAYAY ◽  
MANISH GOSWAMI
Keyword(s):  
Drug Delivery ◽  
Phase Diagram ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ternary Phase Diagram ◽  
Ex Vivo ◽  
The Self ◽  
Drug Content ◽  
Intestinal Membrane ◽  
Globule Size

Objective: The self-micro-emulsifying drug delivery system (SMEDDS) of bambuterol hydrochloride was designed, prepared, and evaluated to overcome the problem of poor bioavailability. Methods: The designing of the formulation included the selection of oil phase, surfactant, and cosolvent/cosurfactant based on the saturated solubility studies. Psuedoternary phase diagram was constructed using aqueous titration method, to identify the self-emulsifying region. Different ratios of the selected surfactant and cosolvent/cosurfactant (Smix) were also studied and used to construct the ternary phase diagram. The prepared formulations of the SMEDDS were evaluated for drug content, morphology, globule size, robustness to dilution, emulsification time, optical clarity, and stability. Results: The formulation containing 10 mg bambuterol hydrochloride, triacetin (12.50% w/w), Tween 80 (43.75% w/w), and ethanol (43.75% w/w) was concluded to be optimized. The optimized SMEDDS not only showed optimum globule size, zeta potential, and drug content but was also found to be robust to dilution, formed emulsion spontaneously, and was stable. The optimized SMEDDS showed increased permeability of the drug across the intestinal membrane in ex vivo studies. Conclusion: The results suggest that bambuterol hydrochloride can be formulated as self-microemulsifying drug delivery system, and further, SMEDDS can be used to improve the oral bioavailability of bambuterol hydrochloride.

Resveratrol Loaded Self-Microemulsifying Drug Delivery System (SMEDDS): Development and Optimization

2014 ◽  
Vol 936 ◽  
pp. 763-769
Author(s):  
Guo Qing Liu ◽  
Hua Feng Zhou ◽  
Jing Zhang ◽  
Ze Min Yan ◽  
Ming Xing Duan ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Phase Diagram ◽  
Particle Size ◽  
High Performance Liquid Chromatography ◽  
Oral Delivery ◽  
High Performance ◽  
Ternary Phase ◽  
Ternary Phase Diagram ◽  
Cremophor El ◽  
Central Composite

We developed a SMEDDS to enhance the oral delivery of resveratrol by using high performance liquid chromatography, a pseudo ternary phase diagram and a central composite design (CCD). We found that the optimal formulation of 12.69% greoil gtcc, 62.29% Cremophor EL, and 25.02% Labrasol. We characterized the particle size and zeta potential of the final SMEDDS.

scholarly journals Study of Solubility of Atorvastatin using Ternary Phase Diagram for the Development of Self-Emulsifying Drug Delivery Systems (SEDDS)

2013 ◽  
Vol 11 (2) ◽  
pp. 83-91
Author(s):  
Fariba Khan ◽  
Md Saiful Islam ◽  
Reza-ul Jalil
Keyword(s):  
Drug Delivery ◽  
Phase Diagram ◽  
Oleic Acid ◽  
Oral Bioavailability ◽  
Ternary Phase ◽  
Ternary Phase Diagram ◽  
Tween 80 ◽  
Tween 20 ◽  
Surfactant Mixture ◽  
Cremophor El

Self-emulsifying drug delivery system (SEDDS) is successfully used to improve the aqueous solubility and oral bioavailability of the poorly aqueous soluble drugs. Atorvastatin calcium (ATV), a poorly aqueous soluble drug having low oral bioavailability, was the model drug for this study. The aim of this study was to find out the suitable lipid and surfactant which can be used in formulation of ATV-SEDDS and this was done using ternary phase diagram, an important tool used very essentially in optimizing SEDDS formulations. Ternary phase diagrams of lipid/surfactant/ATV mixture were constructed to generate the solubility data of ATV. Two lipids namely Capmul PG 8, Oleic acid and seven different surfactants namely Tween 20, Tween 80, Cremophor CO 40, Cremophor CO 60, Cremophor EL, Cremophor RH 40 and Cremophor RH 60 were used. For Capmul PG 8/surfactant mixture, solubilizing efficiency order was: Cremophor RH 40 > Tween 80 > Tween 20 > Cremophor CO 60 > Cremophor RH 60 > Cremophor EL > Cremophor CO 40. For Oleic acid/surfactant mixture, solubilizing efficiency order was: Cremophor RH 40 > Tween 80 > Tween 20 > Cremophor RH 60 > Cremophor CO 60 > Cremophor EL > Cremophor CO 40. Considering the solubility phase diagrams of the drug, both Oleic acid and Capmul PG 8 can be used as lipid in combination with any of the surfactants, Cremophor RH40 or Tween 80 or Tween 20 for the development of SEDDS formulations of ATV having enhanced solubility and dissolution property. DOI: http://dx.doi.org/10.3329/dujps.v11i2.14507 Dhaka Univ. J. Pharm. Sci. 11(2): 83-91, 2012 (December)

scholarly journals DESIGN, PREPARATION, AND EVALUATION OF SELF-MICROEMULSIFYING DRUG DELIVERY SYSTEM OF BAMBUTEROL HYDROCHLORIDE

2018 ◽  
Vol 11 (12) ◽  
pp. 389
Author(s):  
Sachin Saggar ◽  
Ashutosh Upadhayay ◽  
Manish Goswami
Keyword(s):  
Drug Delivery ◽  
Phase Diagram ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ternary Phase Diagram ◽  
Ex Vivo ◽  
The Self ◽  
Drug Content ◽  
Intestinal Membrane ◽  
Globule Size

Objective: The self-micro-emulsifying drug delivery system (SMEDDS) of bambuterol hydrochloride was designed, prepared, and evaluated to overcome the problem of poor bioavailability.Methods: The designing of the formulation included the selection of oil phase, surfactant, and cosolvent/cosurfactant based on the saturated solubility studies. Psuedoternary phase diagram was constructed using aqueous titration method, to identify the self-emulsifying region. Different ratios of the selected surfactant and cosolvent/cosurfactant (Smix) were also studied and used to construct the ternary phase diagram. The prepared formulations of the SMEDDS were evaluated for drug content, morphology, globule size, robustness to dilution, emulsification time, optical clarity, and stability.Results: The formulation containing 10 mg bambuterol hydrochloride, triacetin (12.50% w/w), Tween 80 (43.75% w/w), and ethanol (43.75% w/w) was concluded to be optimized. The optimized SMEDDS not only showed optimum globule size, zeta potential, and drug content but was also found to be robust to dilution, formed emulsion spontaneously, and was stable. The optimized SMEDDS showed increased permeability of the drug across the intestinal membrane in ex vivo studies.Conclusion: The results suggest that bambuterol hydrochloride can be formulated as self-microemulsifying drug delivery system, and further, SMEDDS can be used to improve the oral bioavailability of bambuterol hydrochloride.

scholarly journals Design Development and Evaluation of Agomelatine Microemulsion for Intranasal Delivery

2019 ◽  
Vol 9 (1-s) ◽  
pp. 132-138
Author(s):  
B. R. Halde ◽  
A. B. Darekar ◽  
R. B. Saudagar
Keyword(s):  
Ternary Phase ◽  
Ternary Phase Diagram ◽  
Tween 80 ◽  
Intranasal Delivery ◽  
Size Measurement ◽  
Stability Studies ◽  
Titration Method ◽  
Globule Size

The purpose of this study was to develop and optimize microemulsion containing agomelatine for intranasal delivery. Agomelatine, an antidepressant drug, has absolute bioavailability of only 5% due to high first pass metabolism. Agomelatine microemulsion and were prepared by titration method. Ternary phase diagram gave the microemulsion region and the concentration of oil; Smix and water were selected from ternary phase diagram. Based on solubility study, oleic acid, tween 80 and propylene glycol were selected as oil, surfactant and co surfactant respectively. Microemulsions were prepared using water titration method. 1:1% v/v ratio (Tween 80: Propylene glycol) was selected for formulation development. The prepared microemulsions were optimized optical transparency, viscosity measurement, phase separation, determination of pH, measurement of globule size, measurement of zeta potential, drug content, In vitro diffusion study, stability studies. The optimized batch was further characterized for optical transparency, viscosity measurement, phase separation, determination of pH, measurement of globule size, measurement of zeta potential, drug content, In vitro diffusion study, stability studies. Keywords: Depression, Intranasal, Microemulsions, Agomelatine

scholarly journals Formulation and Characterization of Piroxicam as Self-Nano Emulsifying Drug Delivery System

2020 ◽  
Vol 29 (1) ◽  
pp. 174-183
Author(s):  
Fahad F. Salim ◽  
Nawal A. Rajab
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ternary Phase ◽  
Ternary Phase Diagram ◽  
Stability Study ◽  
Drug Dissolution ◽  
Inflammatory Conditions ◽  
Ternary Phase Diagrams

Piroxicam (PIR) is a nonsteroidal anti-inflammatory drug of oxicam category, used in gout, arthritis, as well as other inflammatory conditions (topically and orally). PIR is practically insoluble in water, therefore the aim is prepare and evaluate piroxicam as liquid self-nanoemulsifying drug delivery system to enhance its dispersibility and stability. The Dispersibilty and Stability study have been conducted in Oil, Surfactant and Co-surfactant for choosing the best materials to dissolve piroxicam. The pseudo ternary phase diagrams have been set at 1:1, 2:1, 3:1 as well as 4:1 ratio of surfactants and co-surfactants, also there are 4 formulations were prepared by using various concentrations of transcutol HP, cremophore EL and triacetin oil. All the constructed prepared formulas have been assessed for in vitro drug dissolution, thermodynamic stability, polydispersity index, robustness to dilution, particle size distribution, drug content, and the dispersibility and emulsification time.From the presented research concluded that the self-nanoemulsifying drug delivery system is the convenient method for improving Dispersibilty and Stability of piroxicam.  Keywords: Pseudo-ternary phase diagram, Dissolution rate, SNEDDS, Piroxicam.

scholarly journals Flurbiprofen-Loaded Solid SNEDDS Preconcentrate for the Enhanced Solubility, In-Vitro Dissolution and Bioavailability in Rats

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 247 ◽  
Author(s):  
Rae Kim ◽  
Dong-Jin Jang ◽  
Yu Kim ◽  
Jin-Ha Yoon ◽  
Kyoung Min ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Phase Diagram ◽  
Particle Size ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ternary Phase ◽  
Ternary Phase Diagram ◽  
In Vitro Dissolution ◽  
Enhanced Solubility

The aim of this work was to prepare and optimize a solid self-nanoemulsifying drug delivery system pre-concentrate (SSP) containing water-insoluble flurbiprofen (FL) using a novel pseudo-ternary phase diagram. The pseudo-ternary phase diagram, composed of FL as the drug and dispersion core, Kollisolv MCT 70 as the oil phase, and TPGS (tocopherol polyethylene glycol 1000 succinate) as the surfactant, was constructed for the determination of the SSP region. SSP was investigated in terms of particle size, physical state by differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD), in vitro dissolution and oral pharmacokinetics in rats. The determined SSP (FL/Kollisolv MCT 70/TPGS = 10/10/80, weight %) in the pseudo-ternary phase diagram had the melting point of 32.37 °C and uniform mean particle size of below 30 nm without any precipitation of FL in the dispersion. In the dissolution test, the SSP exhibited 95.70 ± 3.40% of release at 15 min, whereas the raw FL showed poor dissolution (i.e., 6.75 ± 1.30%) at that time point. In addition, the SSP showed the enhanced oral absorption (i.e., 1.93-fold increase in AUCinfinite) as compared to the suspension group of raw FL. Therefore, the developed SSP would be a promising drug delivery system with excellent solubilization, dissolution, and bioavailability for FL.

Using phase boundary mapping to resolve discrepancies in the Mg2Si–Mg2Sn miscibility gap

2021 ◽  
Author(s):  
Rachel Orenstein ◽  
James P. Male ◽  
Michael Toriyama ◽  
Shashwat Anand ◽  
G. Jeffrey Snyder
Keyword(s):  
Phase Diagram ◽  
Phase Boundary ◽  
Ternary Phase ◽  
Ternary Phase Diagram ◽  
Miscibility Gap ◽  
Boundary Mapping

A new understanding of the MgSi–MgSn miscibility gap is reached through phase boundary mapping the Mg–Si–Sn ternary phase diagram.

Calculation of phase diagrams and thermodynamic properties of 14 additive and reciprocal ternary systems containing Li2CO3, Na2CO3, K2CO3, Li2SO4, Na2SO4, K2SO4, LiOH, NaOH, and KOH

1984 ◽  
Vol 62 (3) ◽  
pp. 457-474 ◽  
Author(s):  
A. D. Pelton ◽  
C. W. Bale ◽  
P. L. Lin
Keyword(s):  
Phase Diagram ◽  
Thermodynamic Properties ◽  
Molten Salt ◽  
Phase Diagrams ◽  
Binary Systems ◽  
Ternary Phase ◽  
Ternary Phase Diagram ◽  
Ternary Systems ◽  
Maximum Error ◽  
Critical Assessment

Phase diagrams and thermodynamic properties of five additive molten salt ternary systems and nine reciprocal molten salt ternary systems containing the ions Li+, Na+, [Formula: see text], OH− are calculated from the thermodynamic properties of their binary subsystems which were obtained previously by a critical assessment of the thermodynamic data and the phase diagrams in these binary systems. Thermodynamic properties of ternary liquid phases are estimated from the binary properties by means of the Conformal Ionic Solution Theory. The ternary phase diagrams are then calculated from these thermodynamic properties by means of computer programs designed for the purpose. It is found that a ternary phase diagram can generally be calculated in this way with a maximum error about twice that of the maximum error in the binary phase diagrams upon which the calculations are based. If, in addition, some reliable ternary phase diagram measurements are available, these can be used to obtain small ternary correction terms. In this way, ternary phase diagram measurements can be smoothed and the isotherms drawn in a thermodynamically correct way. The thermodynamic approach permits experimental data to be critically assessed in the light of thermodynamic principles and accepted solution models. A critical assessment of error limits on all the calculated ternary diagrams is made, and suggestions as to which composition regions merit further experimental study are given.

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