CHARACTERIZATION OF DRUG ANTIRETROVIRAL EFAVIRENZ FROM THE METHOD OF INTRINSIC DISSOLUTION

2013 ◽  
Vol 10 (19) ◽  
pp. 81-86
Author(s):  
Ana Cristina Sousa Gramoza VILARINHO ◽  
José Lamartine SOARES SOBRINHO ◽  
Monica Felts de La Roca OARES ◽  
Livio Cesar Cunha NUNES
Keyword(s):  
Dissolution Rate ◽  
Calibration Curve ◽  
Classification System ◽  
Water Solubility ◽  
Sodium Lauryl Sulphate ◽  
Intrinsic Dissolution ◽  
Intrinsic Dissolution Rate ◽  
Antiretroviral Drug ◽  
Biopharmaceutical Classification System

The intrinsic dissolution is a test which has been used for many years for the characterization of solid drug. This study aimed to characterize the antiretroviral drug efavirenz from the intrinsic dissolution and compared to the biopharmaceutical classification system (BCS). Initially, was prepared a calibration curve with 5 points read at wavelength of 247 nm in order to analyze the concentration of the samples. For the formation of the tablet was used 20 mg of the drug under pressure of 2 tons for 1 minute. Then, the test was carried out intrinsic dissolution in the middle sodium lauryl sulphate 0.5% at 37 ° C under agitation of 50 rpm. By analyzing the data obtained, it was observed that the calibration curve was linear with r = 0.9998. Regarding the intrinsic dissolution rate (VDI), this was equal to 0.0058 mg/ml/min corroborating the SBC is a drug of low water solubility. Thus, by having more controlled conditions the intrinsic dissolution has become evidence for the purpose of being employed in the SBC and is used for characterization of pharmaceuticals.

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

scholarly journals Solubility Enhancement of Clozapine Through Co-Crystal Formation with Isonicotinamide

2019 ◽  
Vol 2 (1) ◽  
Author(s):  
Fikri Alatas ◽  
Hestiary Ratih ◽  
Hesti Kurnia ◽  
Sundani Nurono Soewandhi
Keyword(s):  
Dissolution Rate ◽  
Phosphate Buffer Solution ◽  
Crystal Formation ◽  
X Ray Diffraction ◽  
High Permeability ◽  
Buffer Solution ◽  
Pxrd Pattern ◽  
Low Solubility ◽  
Biopharmaceutical Classification System

Clozapine (CLO) is an effective atypical antipsychotic to control the symptoms of psychosis and schizophrenia. Clozapine has low solubility and high permeability, so it is classified as a class II in the biopharmaceutical classification system. The aim of this study was to improve the solubility and dissolution rate of clozapine by clozapine-isonicotinamide (CLO-INA) co-crystal formation. CLO-INA co-crystal was prepared by solvent-drop grinding (SDG) method using water as a solvent. Characterization of SDG result was conducted by powder X-ray diffraction (PXRD) and Fourier transform infrared (FTIR).  Solubility test was performed in water at room temperature. The dissolution test was performed in 900 mL of pH 6.8 phosphate buffer solution, 50 rotation per minute of paddle rotation, and at 37±0.5 °C. The PXRD pattern of  SDG result of CLO-INA has many different peaks from its parent components, and this may indicate the co-crystal formation. The solubility of the co-crystal clozapine was fifteen folds higher than pure clozapine. The dissolution rate of CLO-INA co-crystal increased in the first 10 minutes compared to pure clozapine. Percentage of clozapine dissolved after 10 minutes from CLO-INA co-crystal and pure CLO were 10.2 and 2.4%, respectively. CLO and INA can form co-crystal by SDG method that can improve the solubility and dissolution rate of clozapine.Keywords: Clozapine, Isonicotinamide, Co-crystal, Solubility, Dissolution

scholarly journals The effect of dissolution medium, rotation speed and compaction pressure on the intrinsic dissolution rate of amlodipine besylate, using the rotating disk method

2014 ◽  
Vol 50 (3) ◽  
pp. 513-520 ◽  
Author(s):  
Leandro Giorgetti ◽  
Michele Georges Issa ◽  
Humberto Gomes Ferraz
Keyword(s):  
Dissolution Rate ◽  
Rotation Speed ◽  
Compaction Pressure ◽  
Rotating Disk ◽  
Fractional Factorial ◽  
Amlodipine Besylate ◽  
Dissolution Medium ◽  
Intrinsic Dissolution ◽  
Intrinsic Dissolution Rate ◽  
Disk Method

The aim of this study was to evaluate the effect of dissolution medium, rotation speed and compaction pressure on the intrinsic dissolution rate (IDR) of the antihypertensive drug amlodipine besylate, using the rotating disk method. Accordingly, a fractional factorial design (33-1) was used, employing dissolution media (water, phosphate buffer pH 6.8 and HCl 0.1 M), rotation speed (50, 75 and 100 rpm), and compaction pressure (1000, 1500 and 2000 psi) as independent variables. The assays were randomized and statistically compared using the Statistica(r) 11 software program. Significance testing (ANOVA) indicated that the dissolution medium had a considerable impact on the IDR of amlodipine besylate. Analysis of the linear and quadratic components of the variables led to the proposition of a mathematical model that describes the IDR as a function of the parameters studied. Conversely, the levels of compaction pressure and rotation speed employed during experimental planning were less relevant, especially when the assay was conducted in the HCl 0.1 M medium.

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