Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 7

Dissolution Related Publications

7 Solid Dispersions of Cefixime Using β-Cyclodextrin: Characterization and in vitro Evaluation

Authors: Nagasamy Venkatesh Dhandapani, Amged Awad El-Gied

Abstract:

Cefixime, a BCS class II drug, is insoluble in water but freely soluble in acetone and in alcohol. The aqueous solubility of cefixime in water is poor and exhibits exceptionally slow and intrinsic dissolution rate. In the present study, cefixime and β-Cyclodextrin (β-CD) solid dispersions were prepared with a view to study the effect and influence of β-CD on the solubility and dissolution rate of this poorly aqueous soluble drug. Phase solubility profile revealed that the solubility of cefixime was increased in the presence of β-CD and was classified as AL-type. Effect of variable, such as drug:carrier ratio, was studied. Physical characterization of the solid dispersion was characterized by Fourier transform infrared spectroscopy (FT-IR) and Differential scanning calorimetry (DSC). These studies revealed that a distinct loss of drug crystallinity in the solid molecular dispersions is ostensibly accounting for enhancement of dissolution rate in distilled water. The drug release from the prepared solid dispersion exhibited a first order kinetics. Solid dispersions of cefixime showed a 6.77 times fold increase in dissolution rate over the pure drug.

Keywords: Dissolution, release kinetics, solid dispersions, β-cyclodextrin, cefixime, Kneading method

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6 Investigation of Dissolution in Diammonium Hydrogen Phosphate Solutions of Gypsum

Authors: Turan Çalban, Soner Kuşlu, Nursel Keskin, Sabri Çolak

Abstract:

Gypsum (CaSO4.2H2O) is a mineral that is found in large quantities in the Turkey and in the World. In this study, the dissolution of this mineral in the diammonium hydrogen phosphate solutions has been studied. The dissolution and dissolution kinetics of gypsum in diammonium hydrogen phosphate solutions will be useful for evaluating of solid wastes containing gypsum. Parameters such as diammonium hydrogen phosphate concentration, temperature and stirring speed affecting on the dissolution rate of the gypsum in diammonium hydrogen phosphate solutions were investigated. In experimental studies have researched effectiveness of the selected parameters. The dissolution of gypsum were examined in two parts at low and high temperatures. The experimental results were successfully correlated by linear regression using Statistica program. Dissolution curves were evaluated shrinking core models for solidfluid systems. The activation energy was found to be 34.58 kJ/mol and 44.45 kJ/mol for the low and the high temperatures. The dissolution of gypsum was controlled by chemical reaction both low temperatures and high temperatures.

Keywords: Kinetics, gypsum, Dissolution, diammonium hydrogen phosphate

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5 Comparative Evaluation of the Biopharmaceutical and Chemical Equivalence of the Some Commercial Brands of Paracetamol Tablets

Authors: Raniah Al-Shalabi, Omaima Al- Gohary, Samar Afify, Eram Eltahir

Abstract:

Acetaminophen (Paracetamol) tablets are popular OTC products among patients as analgesics and antipyretics. Paracetamol is marketed by a lot of suppliers around the world. The aim of the present investigation was to compare between many types of paracetamol tablets obtained from different suppliers (six brands produced by different pharmaceutical companies in middle east countries, and Panadol® manufactured in Ireland), by different quality control tests according to USP pharmacopeia.Using Non official tests-hardness and friability; official tests- disintegration, dissolution, and drug content. Additionally, evaluate the influence of temperatures 4°C, 25°C and 40°C at 75% relative humidity on the stability of the same brands in their original packaging has been conducted for two months. The results revealed that all paracetamol tablet brands complied with the official USP specifications. In conclusion, paracetamol tablets preferred to be stored at 25°C. All the tested brands being biopharmaceutically and chemically equivalent.

Keywords: Dissolution, Non official tests-hardness and friability, official tests –disintegration, and drug content

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4 Salbutamol Sulphate-Ethylcellulose Tabletted Microcapsules: Pharmacokinetic Study using Convolution Approach

Authors: Ghulam Murtaza, Kalsoom Farzana

Abstract:

The aim of this article is to narrate the utility of novel simulation approach i.e. convolution method to predict blood concentration of drug utilizing dissolution data of salbutamol sulphate microparticulate formulations with different release patterns (1:1, 1:2 and 1:3, drug:polymer). Dissolution apparatus II USP 2007 and 900 ml double distilled water stirrd at 50 rpm was employed for dissolution analysis. From dissolution data, blood drug concentration was determined, and in return predicted blood drug concentration data was used to calculate the pharmacokinetic parameters i.e. Cmax, Tmax, and AUC. Convolution is a good biwaiver technique; however its better utility needs it application in the conditions where biorelevant dissolution media are used.

Keywords: Pharmacokinetics, Dissolution, convolution, Salbutamol sulphate

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3 Electrolytic Dissolutions of UO2 and SIMFUEL in Carbonate Solutions at Several pHs

Authors: Geun-Il Park, Kwang-Wook Kim, Kee-Chan Song, Eil-Hee Lee, Kune-Woo Lee

Abstract:

Electrolytic dissolution characteristics of UO2 and SIMFUEL electrodes were studied at several potentials in carbonate solutions of a high concentration at several pHs. The electrolytic uranium dissolution was much affected by a corrosion product of UO2CO3 generated at the electrode during the dissolution in carbonate solution. The corrosion product distorted the voltammogram at UO2 and SIMFUEL electrodes in the potential region of oxygen evolution and increased the overpotential of oxygen evolution at the electrode. The effective dissolution in a carbonate solution could be obtained at an applied potential such as +4 V (vs SSE) or more which had an overpotential of oxygen evolution high enough to rupture the corrosion product on the electrode surface.

Keywords: Dissolution, electrolytic, carbonate, Anodic, SIMFUEL, Uranium dioxide

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2 Metoprolol Tartrate-Ethylcellulose Tabletted Microparticles: Development of a Validated Invitro In-vivo Correlation

Authors: Ghulam Murtaza, Fatima Rasool, Mahmood Ahmad, Haji M. S. Khan, Shujaat A. Khan, Sonia Khiljee, Muhammad Qamar-Uz-Zaman

Abstract:

This study describes the methodology for the development of a validated in-vitro in-vivo correlation (IVIVC) for metoprolol tartrate modified release dosage forms with distinctive release rate characteristics. Modified release dosage forms were formulated by microencapsulation of metoprolol tartrate into different amounts of ethylcellulose by non-solvent addition technique. Then in-vitro and in-vivo studies were conducted to develop and validate level A IVIVC for metoprolol tartrate. The values of regression co-efficient (R2-values) for IVIVC of T2 and T3 formulations were not significantly (p<0.05) different from 1 while the values of R2 for IVIVC of T1 and Mepressor® were significantly (p<0.05) different from 1. Internal prediction errors of IVIVC, calculated from observed Area under Curve (AUC) and predicted AUC, were less than 10%. This study successfully presents a valid level A IVIVC for metoprolol tartrate modified dosage forms.

Keywords: Bioavailability, Dissolution, Metoprolol tartrate, Validated in-vitro in-vivo correlation

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1 Increased Solubility, Dissolution and Physicochemical Studies of Curcumin- Polyvinylpyrrolidone K-30 Solid Dispersions

Authors: Nattha Kaewnopparat, Sanae Kaewnopparat, Amaravadee Jangwang, Daungkhae Maneenaun, Thitima Chuchome, Pharkphoom Panichayupakaranant

Abstract:

Solid dispersions (SD) of curcuminpolyvinylpyrrolidone in the ratio of 1:2, 1:4, 1:5, 1:6, and 1:8 were prepared in an attempt to increase the solubility and dissolution. Solubility, dissolution, powder X-ray diffraction (XRD), differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR) of solid dispersions, physical mixtures (PM) and curcumin were evaluated. Both solubility and dissolution of curcumin solid dispersions were significantly greater than those observed for physical mixtures and intact curcumin. The powder X-ray diffractograms indicated that the amorphous curcumin was obtained from all solid dispersions. It was found that the optimum weight ratio for curcumin:PVP K-30 is 1:6. The 1:6 solid dispersion still in the amorphous from after storage at ambient temperature for 2 years and the dissolution profile did not significantly different from freshly prepared.

Keywords: Curcumin, Dissolution, physicochemical, polyvinylpyrrolidone K-30, solid dispersion

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