scholarly journals Preparation and characterization of Efavirenz nanosuspension with the application of enhanced solubility and dissolution rate

2016 ◽  
Vol 15 (4) ◽  
pp. 170-176 ◽  
Author(s):  
Pavan Kommavarapu ◽  
Arthanareeswari Maruthapillai ◽  
Kamaraj Palanisamy
Keyword(s):  
Dissolution Rate ◽  
Enhanced Solubility

scholarly journals Synthesis and Characterization of a New Norfloxacin/Resorcinol Cocrystal with Enhanced Solubility and Dissolution Profile

Pharmaceutics ◽  
2021 ◽  
Vol 14 (1) ◽  
pp. 49
Author(s):  
Hanan Fael ◽  
Rafael Barbas ◽  
Rafel Prohens ◽  
Clara Ràfols ◽  
Elisabet Fuguet
Keyword(s):  
Dissolution Rate ◽  
Shake Flask ◽  
Ph Value ◽  
Dissolution Profile ◽  
Ph Values ◽  
Enhanced Solubility ◽  
Poorly Soluble ◽  
Transformation Experiment ◽  
Solvent Mediated Transformation

A new cocrystal of Norfloxacin, a poorly soluble fluoroquinolone antibiotic, has been synthetized by a solvent-mediated transformation experiment in toluene, using resorcinol as a coformer. The new cocrystal exists in both anhydrous and monohydrate forms with the same (1:1) Norfloxacin/resorcinol stoichiometry. The solubility of Norfloxacin and the hydrated cocrystal were determined by the shake-flask method. While Norfloxacin has a solubility of 0.32 ± 0.02 mg/mL, the cocrystal has a solubility of 2.64 ± 0.39 mg/mL, approximately 10-fold higher. The dissolution rate was tested at four biorelevant pH levels of the gastrointestinal tract: 2.0, 4.0, 5.5, and 7.4. In a first set of comparative tests, the dissolution rate of Norfloxacin and the cocrystal was determined separately at each pH value. Both solid forms showed the highest dissolution rate at pH 2.0, where Norfloxacin is totally protonated. Then, the dissolution rate decreases as pH increases. In a second set of experiments, the dissolution of the cocrystal was evaluated by a unique dissolution test, in which the pH dynamically changed from 2.0 to 7.4, stepping 30 min at each of the four biorelevant pH values. Results were quite different in this case, since dissolution at pH 2 affects the behavior of Norfloxacin at the rest of the pH values.

Studies on the Preparation, Characterization and Solubility of -Cyclodextrin-Roxythromycin Inclusion Complexes

2009 ◽  
Vol 2 (2) ◽  
pp. 523-530
Author(s):  
D. Nagasamy Venkatesh ◽  
S. Karthick ◽  
M. Umesh ◽  
G. Vivek ◽  
R.M. Valliappan ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Inclusion Complexes ◽  
Phase Solubility ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Ir Studies ◽  
Poorly Soluble ◽  
Poorly Soluble Drug

Roxythromycin/ β-cyclodextrin (Roxy/ β-CD) dispersions were prepared with a view to study the influence of β-CD on the solubility and dissolution rate of this poorly soluble drug. Phase-solubility profile indicated that the solubility of roxythromycin was significantly increased in the presence of β-cyclodextrin and was classified as AL-type, indicating the 1:1 stoichiometric inclusion complexes. Physical characterization of the prepared systems was carried out by differential scanning calorimetry (DSC), X-ray diffraction studies (XRD) and IR studies. Solid state characterization of the drug β-CD binary system using XRD, FTIR and DSC revealed distinct loss of drug crystallinity in the formulation, ostensibly accounting for enhancement of dissolution rate.

scholarly journals Assessment of dissolution profile of Pantoprazole tablets available in Bangladesh

2012 ◽  
Vol 4 (2) ◽  
pp. 58-62
Author(s):  
Aparajita Malakar ◽  
Bishwajit Bokshi ◽  
Utpal Kumar Karmakar
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Water Soluble ◽  
Dissolution Profile ◽  
Coating Materials ◽  
Volatile Solvents ◽  
Kneading Method ◽  
Enhanced Solubility ◽  
Materials Used ◽  
Liquisolid Compacts

The aim of the present study was to increase the solubility of a poorly water soluble BCS class II drug, valsartan. Liquisolid technology and solid dispersion by kneading method were techniques used to improve the solubility of the drug by using non-volatile solvents and some hydrophilic carriers. Liquisolid compacts were prepared by dissolving the drug in suitable non volatile solvents. The various non volatile solvents used were PG, PEG, and glycerine. The carrier coating materials play an important role in improving the solubility of the drug. The dissolution rate of the drug was increased by using propylene glycol as non-volatile solvent at 20:1 ratio of carrier to coating material. Solid dispersion by kneading method were another attempt to improve solubility the various carrier materials used were PVP K 30, PEG 6000 and mannitol, these carriers are used in various ratios to improve its solubility. The dissolution rate of drug using solid dispersion kneading method with mannitol was increased at 1:3 ratio. The DSC and FTIR studies revealed no drug excipients interactions, whereas XRD revealed the reduced crystalinity of drug, which showed enhanced solubility. From the results it was concluded that the liquisolid compacts enhanced the solubility of valsartan in comparison to traditional solid dispersion method.DOI: http://dx.doi.org/10.3329/sjps.v4i2.10441  S. J. Pharm. Sci. 4(2) 2011: 58-62

scholarly journals PREPARATION AND CHARACTERIZATION OF NANOCRYSTALS FOR SOLUBILITY AND DISSOLUTION RATE ENHANCEMENT OF PALIPERIDONE USING DIFFERENT HYDROPHILIC CARRIERS: IN VITRO-IN VIVO STUDY

2018 ◽  
Vol 11 (4) ◽  
pp. 393
Author(s):  
Moon Rajkumar ◽  
Gattani Surendra
Keyword(s):  
Dissolution Rate ◽  
Antipsychotic Agent ◽  
Aqueous Solubility ◽  
In Vivo Study ◽  
Scanning Calorimetry ◽  
Antisolvent Precipitation ◽  
Enhanced Solubility ◽  
Pure Drug

 Objective: The objective of this study was to increase the solubility and dissolution rate of paliperidone (PAL) by preparing its nanocrystals using different hydrophilic carriers by antisolvent precipitation technique.Methods: The nanoparticles (NP) were characterized for aqueous solubility, drug content, Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction, scanning electron microscopy, particle size, and in vitro-in vivo analysis.Results: The results showed improved solubility and dissolution rate of NPs when compared to pure drug and physical mixture (PM). Solubility data showed a linear graph giving an indication that there is a gradual increase in the solubility profile of the drug with an increase in concentration of the carriers. At highest concentration, the solubility of NPs with Plasdone S630, Povidone K-25, and PVP K-30 found to be increased by 12 folds, 9 folds and 6 folds, respectively, as compared to pure drug. The release profile of NPs with Plasdone S630 in terms of dissolution efficiency at 60 min (DE60), initial dissolution rate (IDR), amount release in 15 min (Q15 min), and time for 75% release (t75%) shows better results when compared to pure drug, PM, and also NPs with povidone 25 and povidone 30. In vivo study reveals that optimized NPs elicited significant induction of cataleptic behavior which is the indication of antipsychotic agent(s) effect.Conclusion: The process antisolvent precipitation under constant stirring may be a promising method to produce stable PAL NPs with markedly enhanced solubility and dissolution rate due to nanonization with the increased surface area, improved wettability, and reduced diffusion pathway.

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