Characterization and Physical Stability of Tolfenamic Acid-PVP K30 Solid Dispersions

The content of this investigation was to study the influence of β-cyclodextrin and hydroxy propyl-β-cyclodextrin complexation on enhancement of solubility and dissolution rate of isradipine. Based on preliminary phase solubility studies, solid complexes prepared by freeze drying method in 1:1 molar ratio were selected and characterized by DSC for confirmation of complex formation. Prepared solid dispersions were evaluated for drug content, solubility and in vitro dissolution. The physical stability of optimized formulation was studied at refrigerated and room temperature for 2 months. Solid state characterization of optimized complex performed by DSC and XRD studies. Dissolution rate of isradipine was increased compared with pure drug and more with HP-β-CD inclusion complex than β-CD. DSC and XRD analyzes that drug was in amorphous form, when the drug was incorporated as isradipine β-CD and HP-β-CD inclusion complex. Stability studies resulted in low or no variations in the percentage of complexation efficiency suggesting good stability of molecular complexes. The results conclusively demonstrated that the enhancement of solubility and dissolution rate of isradipine by drug-cyclodextrin complexation was achieved.

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Influence of Solvent Composition on the Miscibility and Physical Stability of Naproxen/PVP K 25 Solid Dispersions Prepared by Cosolvent Spray-Drying

Pharmaceutical Research ◽

10.1007/s11095-011-0539-x ◽

2011 ◽

Vol 29 (1) ◽

pp. 251-270 ◽

Cited By ~ 64

Author(s):

Amrit Paudel ◽

Guy Van den Mooter

Keyword(s):

Spray Drying ◽

Solid Dispersions ◽

Physical Stability ◽

Solvent Composition ◽

Influence Of Solvent

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Investigations on noval method for the formulation of solid dispersions part- I Formulation, characterization and selection

International Journal of Drug Delivery ◽

10.5138/09750215.2173 ◽

2017 ◽

Vol 9 (3) ◽

pp. 71

Author(s):

Rakesh Kumar Sharma ◽

Anil Kumar Middha

Keyword(s):

Ir Spectroscopy ◽

Solid Dispersions ◽

Hydrophilic Polymers ◽

Modulated Dsc ◽

Dissolution Test ◽

Stability Testing ◽

Sustained Drug Release ◽

Ft Ir ◽

Pvp K30 ◽

Ft Ir Spectroscopy

<p>The solid dispersions of indomethacin with hydrophilic polymers were prepared by lyophilization. The polymers used in the investigation were HPMC, PVP K30, CBR and PLF 127. The solubility and dissolution of indomethacin from prepared lyophilized solid dispersions were investigated in 0.1 N HCl, purified water and USP-NF dissolution media. Out of fifteen lyophilized formulations from F1 to F15, five formulations F2, F5, F8, F12 and F14 showed highest solubility in purified water. Formulation F2, F8 failed to comply with the USP-NF dissolution test for indomethacin capsules. Formulation F14 showed maximum dissolution in the respective dissolution media within 60 min. Sustained drug release was observed for 6 h with formulations F2 and F8 in USP-NF media. The formulations F2, F5, F8, F12 and F14 were characterized by modulated DSC and FT-IR spectroscopy. Some Formulations on stability testing were found physico-chemically stable at accelerated temperature conditions.</p>

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SOLID DISPERSION FOR INCREASING DISSOLUTION RATE OF SODIUM DICLOFENAC WITH VARIATIONS OF POLYVINYL PYRROLIDONE K30

Journal of Pharmaceutical Care Anwar Medika ◽

10.36932/jpcam.v3i2.46 ◽

2021 ◽

Vol 3 (2) ◽

pp. 86-98

Author(s):

Noval Noval ◽

◽

Rosyifa Rosyifa ◽

Keyword(s):

Dissolution Rate ◽

Solid Dispersion ◽

Solid Dispersions ◽

Diclofenac Sodium ◽

Sodium Diclofenac ◽

Significant Difference ◽

Moisture Percentage ◽

Inert Carrier ◽

Low Solubility ◽

Pvp K30

Diclofenac sodium is included in class II category based on biopharmaceutics classification system (BCS), sodium diclofenac has low solubility and high permeability. Low solubility will affect absorption of drugs in body because rate of dissolution will decrease. PVP K30 is inert carrier that dissolves easily in water and can affect solubility of an active drug substance. To know solid dispersion system increasing dissolution rate of sodium diclofenac by adding variations concentration of PVP K30. Solid dispersion uses solvent method with variations concentration of PVP K30 1:3, 1:5, 1:7 and 1:9. Test physical properties of solid dispersions using a moisture test and compressibility. Solid dispersion dissolution test using type 2 dissolutions test and determination of concentration using UV-VIS spectrophotometry. Test results were analyzed using One Way ANOVA and continued test. Solid dispersion has a good physical whit moisture percentage not >5% and compressibility not >20%. Solid dispersion of sodium diclofenac with addition of PVP K30 can increase dissolution rate compared to pure sodium diclofenac (p<0,05) with highest at ratio 1:7. Each comparison has significant difference (p<0,05) expect in ratio 1:9. Solid dispersion of sodium diclofenac with PVP K30 can increase dissolution rate of pure sodium diclofenac.

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Application of Solid Dispersion Technique to Improve Solubility and Sustain Release of Emamectin Benzoate

Molecules ◽

10.3390/molecules24234315 ◽

2019 ◽

Vol 24 (23) ◽

pp. 4315

Author(s):

Bin Bin Huang ◽

Dong Xu Liu ◽

De Kun Liu ◽

Gang Wu

Keyword(s):

Solid Dispersion ◽

Rotational Speed ◽

Mixing Time ◽

Solid Dispersions ◽

Aqueous Solubility ◽

Feed Ratio ◽

Emamectin Benzoate ◽

Wettable Powder ◽

Dispersion Technique ◽

Pvp K30

The solid dispersion technique, which is widely used in the medical field, was applied to prepare a pesticide dosage form of emamectin benzoate (EM). The preparation, physicochemical characterization, aqueous solubility, release dynamics, photolytic degradation, bioactivity, and sustained-release effects of the prepared EM solid dispersions were studied by a solvent method, using polymer materials as the carriers. Water-soluble polyvinyl pyrrolidone (PVP) K30 and water-insoluble polyacrylic resin (PR)III were used as the carriers. The influence of various parameters, such as different EM:PVP-K30 and EM:PRIII feed ratios, solvent and container choices, rotational speed and mixing time effects on pesticide loading, and the entrapment rate of the solid dispersions were investigated. The optimal conditions for the preparation of EM-PVP-K30 solid dispersions required the use of methanol and a feed ratio between 1:1 and 1:50, along with a rotational speed and mixing time of 600 rpm and 60 min, respectively. For the preparation of EM-PRIII solid dispersions, the use of methanol and a feed ratio between 1:4 and 1:50 were required, in addition to the use of a porcelain mortar for carrying out the process. Under optimized conditions, the prepared EM-PVP-K30 solid dispersions resembled potato-like, round, and irregular structures with a jagged surface. In contrast, the EM-PRIII solid dispersions were irregular solids with a microporous surface structure. The results of X-ray powder diffraction (XRD), differential scanning calorimetry (DSC), ultraviolet (UV) spectrometry, and infrared (IR) spectrometry showed that the solid dispersions were formed by intermolecular hydrogen bonding. The solid dispersion preparation in PVP-K30 significantly improved the solubility and dissolution rate of EM, particularly the aqueous solubility, which reached a maximum of 37.5-times the EM technical solubility, when the feed ratio of 1:10 was employed to prepare the dispersion. Importantly, the wettable powder of EM-PVP-K30 solid dispersion enhanced the insecticidal activity of EM against the Plutella xylostella larvae. Furthermore, the solid dispersion preparation in PRIII afforded a significant advantage by prolonging the EM technical release in water at a pH below 7.0, especially when the PRIII content in solid dispersions was high. While the amplified toxicity of the wettable powder of EM-PRIII solid dispersions against the P. xylostella larvae showed no significant differences from that of the EM technical, the long-term toxicity under the field condition was much better than that of the commercially available EM 1.5% emulsifiable concentrate. Notably, solid dispersions with both the PVP-K30 and PRIII carriers reduced the effect of UV photolysis.

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Effect of Drug–Polymer Interactions through Hypromellose Acetate Succinate Substituents on the Physical Stability on Solid Dispersions Studied by Fourier-Transform Infrared and Solid-State Nuclear Magnetic Resonance

Molecular Pharmaceutics ◽

10.1021/acs.molpharmaceut.9b00301 ◽

2019 ◽

Vol 16 (6) ◽

pp. 2785-2794 ◽

Cited By ~ 9

Author(s):

Yuya Ishizuka ◽

Keisuke Ueda ◽

Hitomi Okada ◽

Junpei Takeda ◽

Masatoshi Karashima ◽

...

Keyword(s):

Nuclear Magnetic Resonance ◽

Fourier Transform ◽

Solid State ◽

Magnetic Resonance ◽

Solid Dispersions ◽

Physical Stability ◽

Fourier Transform Infrared ◽

Polymer Interactions ◽

Hypromellose Acetate Succinate ◽

Nuclear Magnetic

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The Effect of PVP Molecular Weight on Dissolution Behavior and Physicochemical Characterization of Glycyrrhetinic Acid Solid Dispersions

Advances in Polymer Technology ◽

10.1155/2020/8859658 ◽

2020 ◽

Vol 2020 ◽

pp. 1-13

Author(s):

Xiaoyu Sui ◽

Yan Chu ◽

Jie Zhang ◽

Honglian Zhang ◽

Huiyu Wang ◽

...

Keyword(s):

Molecular Weight ◽

Dissolution Rate ◽

Solid Dispersions ◽

Physicochemical Characterization ◽

Dissolution Behavior ◽

Enhancement Effect ◽

Glycyrrhetic Acid ◽

Equilibrium Solubility ◽

Drug Molecules ◽

Pvp K30

The effect of polyvinylpyrrolidone (PVP) as glycyrrhetic acid (GA) solid dispersions carrier at different molecular weights on the dissolution behavior and physicochemical properties was investigated. PVP-GA-SDs prepared with all four molecular weight PVPs displayed good enhancement of dissolution rate and equilibrium solubility compared with pure drug and corresponding physical mixtures. The results showed that the enhancement effect of molecular weight on dissolution rate and equilibrium solubility follows PVP K 30 > PVP K 60 > PVP K 17 > PVP K 15 . In addition, the dissolution rate and solubility of the SDs with a carrier-drug ratio of 8 : 1 were better than the samples of 4 : 1. The DSC and XRD patterns showed that the crystallization of GA in SDs prepared by PVP K30 and PVP K60 was significantly inhibited, and both were transformed to amorphous. Based on FTIR and Raman detection, a hydrogen-bond between PVP and drug molecules is formed. SEM results showed that there were no significant differences in the appearance of SDs prepared with four PVPs, and no crystalline morphology of GA was seen. In conclusion, the findings of this study demonstrated that the dissolution performance of the PVP-GA-SDs prepared by the solvent method is related to the molecular weight of PVP, and the change in the molecular weight of PVP does not cause a monotonic change in dissolution of GA. The samples with PVP K30 as the carrier have the best dissolution performance.

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