scholarly journals Glucosamine-paracetamol spray-dried solid dispersions with maximized intrinsic dissolution rate, bioavailability and decreased levels of in vivo toxic metabolites

2018 ◽  
Vol Volume 12 ◽  
pp. 3071-3084
Author(s):  
Ahmed Ali ◽  
Ahmed Khames ◽  
Majed Alrobaian ◽  
Mohammad Hamaidi ◽  
Mohammed AS Abourehab
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersions ◽  
Intrinsic Dissolution ◽  
Intrinsic Dissolution Rate ◽  
Toxic Metabolites ◽  
Spray Dried

scholarly journals Crystal-liquid Fugacity Ratio as a Surrogate Parameter for Intestinal Permeability

2016 ◽  
Vol 19 (3) ◽  
pp. 312 ◽  
Author(s):  
Parvin Zakeri-Milani ◽  
Zohreh Fasihi ◽  
Jafar Akbari ◽  
Ensieh Jannatabadi ◽  
Mohammad Barzegar-Jalali ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Intestinal Absorption ◽  
Intestinal Permeability ◽  
Scanning Calorimetry ◽  
Mole Percent ◽  
Intrinsic Dissolution ◽  
Intrinsic Dissolution Rate ◽  
Close Relationship ◽  
Dose Number

Background: We assessed the feasibility of using crystal-liquid fugacity ratio (CLFR) as an alternative parameter for intestinal permeability in the biopharmaceutical classification (BCS) of passively absorbed drugs. Methods: Dose number, fraction of dose absorbed, intestinal permeability, and intrinsic dissolution rate were used as the input parameters. CLFR was determined using thermodynamic parameters i.e., melting point, molar fusion enthalpy, and entropy of drug molecules obtained using differential scanning calorimetry. Results: The CLFR values were in the range of 0.06-41.76 mole percent. There was a close relationship between CLFR and in vivo intestinal permeability (r > 0.8). CLFR values of greater than 2 mole percent corresponded to complete intestinal absorption. Applying CLFR versus dose number or intrinsic dissolution rate, more than 92% of tested drugs were correctly classified with respect to the reported classification system on the basis of human intestinal permeability and solubility. Conclusion: This investigation revealed that the CLFR might be an appropriate parameter for quantitative biopharmaceutical classification. This could be attributed to the fact that CLFR could be a measure of solubility of compounds in lipid bilayer which was found in this study to be directly proportional to the intestinal permeability of compounds. This classification enables researchers to define characteristics for intestinal absorption of all four BCS drug classes using suitable cutoff points for both intrinsic dissolution rate and crystal-liquid fugacity ratio. Therefore, it may be used as a surrogate for permeability studies. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

Spray-dried solid dispersions containing ferulic acid: comparative analysis of three carriers, in vitro dissolution, antioxidant potential and in vivo anti-platelet effect

2016 ◽  
Vol 42 (11) ◽  
pp. 1813-1824 ◽  
Author(s):  
Jessica Mendes Nadal ◽  
Mona Lisa Simionatto Gomes ◽  
Débora Maria Borsato ◽  
Martinha Antunes Almeida ◽  
Fernanda Malaquias Barboza ◽  
...  
Keyword(s):  
Comparative Analysis ◽  
Ferulic Acid ◽  
Solid Dispersions ◽  
Antioxidant Potential ◽  
In Vitro Dissolution ◽  
Spray Dried

scholarly journals Intrinsic Dissolution Rate Profiling of Poorly Water-Soluble Compounds in Biorelevant Dissolution Media

Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 493
Author(s):  
Alexandra Teleki ◽  
Olivia Nylander ◽  
Christel A.S. Bergström
Keyword(s):  
Dissolution Rate ◽  
Water Soluble ◽  
Small Scale ◽  
Intrinsic Dissolution ◽  
Intrinsic Dissolution Rate ◽  
Fed State ◽  
Pharmaceutical Ingredients ◽  
Biorelevant Dissolution ◽  
Intestinal Fluids ◽  
Simulated Intestinal Fluids

The intrinsic dissolution rate (IDR) of active pharmaceutical ingredients (API) is a key property that aids in early drug development, especially selecting formulation strategies to improve dissolution and thereby drug absorption in the intestine. Here, we developed a robust method for rapid, medium throughput screening of IDR and established the largest IDR dataset in open literature to date that can be used for pharmaceutical computational modeling. Eighteen compounds with diverse physicochemical properties were studied in both fasted and fed state simulated intestinal fluids. Dissolution profiles were measured in small-scale experimental assays using compound suspensions or discs. IDR measurements were not solely linked to API solubility in either dissolution media. Multivariate data analysis revealed that IDR strongly depends on compound partitioning into bile salt and phospholipid micelles in the simulated intestinal fluids, a process that in turn is governed by API lipophilicity, hydrophobicity, and ionization.

scholarly journals CHARACTERIZATION AND INTRINSIC DISSOLUTION RATE STUDY OF MICROWAVE ASSISTED CYCLODEXTRIN INCLUSION COMPLEXES OF GEMFIBROZIL

2016 ◽  
Vol 8 (10) ◽  
pp. 160
Author(s):  
S. Ain ◽  
R. Singh ◽  
Q. Ain
Keyword(s):  
Inclusion Complex ◽  
Dissolution Rate ◽  
Inclusion Complexes ◽  
Microwave Drying ◽  
Phase Solubility ◽  
Intrinsic Dissolution ◽  
Intrinsic Dissolution Rate ◽  
Solubility Study ◽  
Microwave Assisted ◽  
Rate Study

<p><strong>Objective: </strong>The aim of the present study was to carry out characterization and intrinsic dissolution rate study of microwave assisted inclusion complex of poorly water soluble, lipid lowering agent gemfibrozil [5-(2,5-dimethylphenoxy)-2,2-dimethylpentanoic acid]<strong> </strong>with naturally occurring β-cyclodextrins (CDs) or cycloheptaamylase.</p><p><strong>Methods: </strong>In this work, the phase solubility study was performed to find the ratio of drug and cyclodextrin complexes. Inclusion complexes were prepared by kneading and the prepared complex was subjected to microwave drying and conventional drying techniques. The prepared complexes were evaluated by intrinsic dissolution rate studies and equilibrium solubility study. Further characterization was done by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and X-ray powder diffractometry (DSC).</p><p><strong>Results: </strong>The phase solubility studies showed a linear A<sub>L</sub>-type diagram indicating the formation of inclusion complexes in 1:1 molar ratio β-CD-gemfibrozil complex with maximum stability constant of 148.88 M<sup>-1</sup>was selected for preparation of inclusion complex. The microwave dried product was identified as the inclusion complex with maximum IDR when compared to the conventional dried product.</p><p><strong>Conclusion: </strong>This study was concluded that the microwave drying is the most suitable of the previously occurring drying techniques. Since it showed the highest solubility and IDR value.</p>

scholarly journals Discovery, Characterization, and Pharmaceutical Applications of Two Loratadine–Oxalic Acid Cocrystals

Crystals ◽  
2020 ◽  
Vol 10 (11) ◽  
pp. 996
Author(s):  
Zhengxuan Liang ◽  
Hongbo Chen ◽  
Chenguang Wang ◽  
Changquan Calvin Sun
Keyword(s):  
Oxalic Acid ◽  
Dissolution Rate ◽  
Physical Stability ◽  
Formulation Development ◽  
Intrinsic Dissolution ◽  
Intrinsic Dissolution Rate ◽  
Conjugate Acid ◽  
Enhanced Solubility ◽  
Antihistamine Drug ◽  
Low Solubility

Loratadine (Lor) is an antihistamine drug commonly used to relieve the symptoms of allergy. It has high permeability but low solubility under physiological conditions. To overcome the problem of low solubility, we synthesized and characterized two Loratadine multi-component crystalline phases with oxalic acid (Oxa), i.e., a 1:1 Lor-Oxa conjugate acid-base (CAB) cocrystal (Lor-Oxa CAB) and a 2:1 Lor-Oxa cocrystal monohydrate (Lor-Oxa hydrate). Both cocrystals exhibited an enhanced solubility and intrinsic dissolution rate (IDR) compared to Lor and adequate physical stability. The intrinsic dissolution rate of Lor-Oxa CAB is 95 times that of Lor, which makes it a promising candidate for tablet formulation development.

scholarly journals An interlaboratory investigation of intrinsic dissolution rate determination using surface dissolution

2020 ◽  
Vol 150 ◽  
pp. 24-32 ◽  
Author(s):  
Kelly Etherson ◽  
Claire Dunn ◽  
Wayne Matthews ◽  
Henrik Pamelund ◽  
Camille Barragat ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Intrinsic Dissolution ◽  
Intrinsic Dissolution Rate

scholarly journals Mechanochemical Formation of Racemic Praziquantel Hemihydrate with Improved Biopharmaceutical Properties

Pharmaceutics ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 289
Author(s):  
Debora Zanolla ◽  
Dritan Hasa ◽  
Mihails Arhangelskis ◽  
Gabriela Schneider-Rauber ◽  
Michele R. Chierotti ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Polymorphic Form ◽  
In Vitro Tests ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Experimental Conditions ◽  
Intrinsic Dissolution ◽  
Intrinsic Dissolution Rate ◽  
X Ray ◽  
Enhanced Solubility

Praziquantel (PZQ) is the first-line drug used against schistosomiasis, one of the most common parasitic diseases in the world. A series of crystalline structures including two new polymorphs of the pure drug and a series of cocrystals of PZQ have been discovered and deposited in the Cambridge Structural Database (CSD). This work adds to the list of multicomponent forms of PZQ a relevant example of a racemic hemihydrate (PZQ-HH), obtainable from commercial PZQ (polymorphic Form A) through mechanochemistry. Noteworthy, the formation of the new hemihydrate strongly depends on the initial polymorphic form of PZQ and on the experimental conditions used. The new PZQ-HH has been fully characterized by means of HPLC, Differential Scanning Calorimetry (DSC), Thermogravimetric Analysis (TGA), Hot-Stage Microscopy (SEM), Powder X-Ray Diffraction (PXRD), Scanning Electron Microscopy (SEM), FT-IR, polarimetry, solid-state NMR (SS-NMR), solubility and intrinsic dissolution rate (IDR), and in vitro tests on Schistosoma mansoni adults. The crystal structure was solved from the powder X-ray diffraction pattern and validated by periodic-DFT calculations. The new bioactive hemihydrate was physically stable for three months and showed peculiar biopharmaceutical features including enhanced solubility and a double intrinsic dissolution rate in water in comparison to the commercially available PZQ Form A.

A thermodynamic based approach on the investigation of a diflunisal pharmaceutical co-crystal with improved intrinsic dissolution rate

2014 ◽  
Vol 466 (1-2) ◽  
pp. 68-75 ◽  
Author(s):  
António O.L. Évora ◽  
Ricardo A.E. Castro ◽  
Teresa M.R. Maria ◽  
M. Ramos Silva ◽  
J.H. ter Horst ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Intrinsic Dissolution ◽  
Intrinsic Dissolution Rate
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