Dissolution Enhancement of Clarithromycin Using Ternary Cyclodextrin Complexation

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.

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Influence of β-Cyclodextrin and Hydroxypropyl-β-Cyclodextrin on Enhancement of Solubility and Dissolution of Isradipine

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2017.10.3.8 ◽

2017 ◽

Vol 10 (3) ◽

pp. 3752-3757

Author(s):

Narendar D ◽

Ettireddy S

Keyword(s):

Inclusion Complex ◽

Dissolution Rate ◽

Solid Dispersions ◽

Physical Stability ◽

Molecular Complexes ◽

In Vitro Dissolution ◽

Molar Ratio ◽

Phase Solubility ◽

Cyclodextrin Complexation

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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Formulation and Characterization of Glimepiride Nanoparticles for Dissolution Enhancement

Nanoscience &Nanotechnology-Asia ◽

10.2174/2210681209666190422160115 ◽

2020 ◽

Vol 10 (5) ◽

pp. 649-663

Author(s):

Reena Siwach ◽

Parijat Pandey ◽

Harish Dureja

Keyword(s):

Drug Release ◽

Dissolution Rate ◽

Oral Absorption ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Class Ii ◽

Dissolution Enhancement ◽

In Vitro Drug Release ◽

Bcs Class Ii

Background: The rate-limiting step in the oral absorption of BCS class II drugs is dissolution. Their low solubility is one of the major obstacles in the process of drug development. Dissolution rate can be increased by decreasing the particle size to the nano range, eventually leading to increased bioavailability. Objective: : In the present study, glimepiride loaded nanoparticles were prepared to enhance the dissolution rate. The aim of the work was to examine the effect of polymer-drug ratio, solvent-antisolvent ratio and speed of mixing on in vitro release of glimepiride. Methods: Glimepiride is an antidiabetic drug belonging to the BCS class II drugs. The polymeric nanoparticles were formulated according to Box-Behnken Design (BBD) using nanoprecipitation technique. The prepared nanoparticles were evaluated for in vitro drug release, loading capacity, entrapment efficiency, and percentage yield. Result: It was found that NP-8 has maximum in vitro drug release and was selected as an optimized batch. Analysis of Variance (ANOVA) was applied to the in vitro drug release to study the fitness and significance of the model. The batch NP-8 showed 70.34 ± 1.09% in vitro drug release in 0.1 N methanolic HCl and 92.02 ± 1.87% drug release in phosphate buffer pH 7.8. The release data revealed that the nanoparticles followed zero order kinetics. Conclusion: The study revealed that the incorporation of glimepiride into gelucire 50/13 resulted in enhanced dissolution rate.

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Synthesis and Characterization of Nano-Sized 4-Aminosalicylic Acid–Sulfamethazine Cocrystals

Pharmaceutics ◽

10.3390/pharmaceutics13020277 ◽

2021 ◽

Vol 13 (2) ◽

pp. 277 ◽

Cited By ~ 1

Author(s):

Ala’ Salem ◽

Anna Takácsi-Nagy ◽

Sándor Nagy ◽

Alexandra Hagymási ◽

Fruzsina Gősi ◽

...

Keyword(s):

High Power ◽

Active Pharmaceutical Ingredient ◽

Polymorphic Form ◽

Degree Of Crystallinity ◽

Dissolution Enhancement ◽

Aminosalicylic Acid ◽

Nano Technology ◽

Power Ultrasound ◽

High Power Ultrasound ◽

High Degree

Drug–drug cocrystals are formulated to produce combined medication, not just to modulate active pharmaceutical ingredient (API) properties. Nano-crystals adjust the pharmacokinetic properties and enhance the dissolution of APIs. Nano-cocrystals seem to enhance API properties by combining the benefits of both technologies. Despite the promising opportunities of nano-sized cocrystals, the research at the interface of nano-technology and cocrystals has, however, been described to be in its infancy. In this study, high-pressure homogenization (HPH) and high-power ultrasound were used to prepare nano-sized cocrystals of 4-aminosalysilic acid and sulfamethazine in order to establish differences between the two methods in terms of cocrystal size, morphology, polymorphic form, and dissolution rate enhancement. It was found that both methods resulted in the formation of form I cocrystals with a high degree of crystallinity. HPH yielded nano-sized cocrystals, while those prepared by high-power ultrasound were in the micro-size range. Furthermore, HPH produced smaller-size cocrystals with a narrow size distribution when a higher pressure was used. Cocrystals appeared to be needle-like when prepared by HPH compared to those prepared by high-power ultrasound, which had a different morphology. The highest dissolution enhancement was observed in cocrystals prepared by HPH; however, both micro- and nano-sized cocrystals enhanced the dissolution of sulfamethazine.

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Supercritical Carbon Dioxide as a Green Alternative to Achieve Drug Complexation with Cyclodextrins

Pharmaceuticals ◽

10.3390/ph14060562 ◽

2021 ◽

Vol 14 (6) ◽

pp. 562

Author(s):

Mauro Banchero

Keyword(s):

Release Kinetics ◽

Drug Bioavailability ◽

Residual Content ◽

Supercritical Solvent ◽

Cyclodextrin Complexation ◽

Supercritical Fluid Technology ◽

Conventional Drug ◽

Size And Morphology ◽

Solvent Residue ◽

Complexation Mechanism

Cyclodextrins are widely used in pharmaceutics to enhance the bioavailability of many drugs. Conventional drug/cyclodextrin complexation techniques suffer from many drawbacks, such as a high residual content of toxic solvents in the formulations, the degradation of heat labile drugs and the difficulty in controlling the size and morphology of the product particles. These can be overcome by supercritical fluid technology thanks to the outstanding properties of supercritical CO2 (scCO2) such as its mild critical point, its tunable solvent power, and the absence of solvent residue after depressurization. In this work the use of scCO2 as an unconventional medium to achieve the complexation with native and substituted cyclodextrins of over 50 drugs, which belong to different classes, are reviewed. This can be achieved with different approaches such as the “supercritical solvent impregnation” and “particle-formation” techniques. The different techniques are discussed to point out how they affect the complexation mechanism and efficiency, the physical state of the drug as well as the particle size distribution and morphology, which finally condition the release kinetics and drug bioavailability. When applicable, the results obtained for the same drug with various cyclodextrins, or different complexation techniques are compared with those obtained with conventional approaches.

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