Effect of solvent type on retardation properties of diltiazem HCl form liquisolid tablets

Adibkia, Khosro; Shokri, Javad; Barzegar-Jalali, Mohammad; Solduzian, Mohammad; Javadzadeh, Yousef

doi:10.1016/j.colsurfb.2013.08.017

Cited by 28 publications

(11 citation statements)

References 12 publications

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“…Food and drug administration (FDA) guidance proposes that f1 value between 0 and 15 and f2 value between 50-100 indicate equivalence in dissolution profiles [25,26]. In comparison between the dissolution of F2 and the DCT, the results of f1 and f2 were 16.22 and 36.18 respectively gave an indication that the two dissolution profiles are equivalent.…”

Section: In Vitro Dissolution Testmentioning

confidence: 99%

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Formulation and Evaluation of Furosemide Liquisolid Compact

Jassim

2017

Int J App Pharm

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Objective: The purpose of this study was to enhance the dissolution pattern of the practically water-insoluble diuretic drug, furosemide through its formulation into liquisolid tablets.Methods: A mathematical model was used to formulate four liquisolid powder systems using polyethylene glycol 400 as a non-volatile water miscible liquid vehicle. The liquid loading factors of the vehicle were used to calculate the optimum quantities of carrier (Avicel PH 102) and coating materials (Aerosil 200) needed to prepare acceptably flowing and compactible powder mixtures and (R) ratio used was 25. The liquisolid tablets were evaluated for weight variation, percent friability, hardness, content uniformity, disintegration time and in vitro drug release profile. Drug and the prepared systems were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and powder xray diffraction (PXRD) studies. Results:The enhanced dissolution rate due to the increased wetting properties and the large available surface areas for dissolution were obtained in case of the liquisolid tablets. The selected optimal formulation (F2) of 50% drug concentration released 90% of its content during the first 10 min compared to 65% of DCT. FTIR studies revealed that there was no interaction between drug and polymers. DSC and PXRD indicated conversion of crystalline to amorphous form of furosemide. Conclusion:The dissolution rate of furosemide can be enhanced to a great extent by liquisolid technique.

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Section: In Vitro Dissolution Testmentioning

confidence: 99%

“…Where n is the number of time points at which % dissolved was determined, Rt is the % dissolved of one formulation at a given time point, and Tt is the % dissolved of the formulation to be compared at the same time point [26].…”

Section: Dissolution Data Evaluationmentioning

confidence: 99%

Formulation and Evaluation of Furosemide Liquisolid Compact

Jassim

2017

Int J App Pharm

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“…Apart from its antihypertension application, DTH is also a drug of choice in the management of classical and vasospastic angina pectoris, supraventricular tachyarrhythmias and anal fissure [3]. Oral administration of DTH subjected to extensive and complex biotransformation (N-demethylation, O-demethylation and deacetylation) which limits the biological half-life to 3-5 h and bioavailability up to 40% [4]. The drug dosage recommended for DTH is 30 mg or above, usually three to four times a day [5].…”

Section: Introductionmentioning

confidence: 99%

Transdermal delivery of Diltiazem HCl from matrix film: Effect of penetration enhancers and study of antihypertensive activity in rabbit model

Parhi

Suresh²

2016

Journal of Advanced Research

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The present investigation focused on the development of Diltiazem HCl (DTH) matrix film and its characterization by in-vitro, ex-vivo and in-vivo methods. Films were prepared by solvent casting method by taking different ratios of hydroxypropyl methylcellulose K4M (HPMC K4M) and Eudragit RS100. Various parameters of the films were analyzed such as mechanical property using tensile tester, interaction study by Fourier transform infrared spectroscopy (FTIR) and Thermogravimetric analysis (TGA), in-vitro drug release through cellulose acetate membrane, ex-vivo permeation study using abdominal skin of rat employing Franz diffusion cell, and in-vivo antihypertensive activity using rabbit model. The FTIR studies confirmed the absence of interaction between DTH and selected polymers. Thermal analysis showed the shifting of endothermic peak of DTH in film, indicating the dispersion of DTH in molecular form throughout the film. Incorporation of 1,8-cineole showed highest flux (89.7 μg/cm(2)/h) of DTH compared to other penetration enhancers such as capsaicin, dimethyl sulfoxide (DMSO), and N-methyl pyrrolidone (NMP). Photomicrographs of histology study on optimized formulation (DF9) illustrated disruption of stratum corneum (SC) supporting the ex-vivo results. The in-vivo antihypertensive activity results demonstrated that formulation DF9 was effective in reducing arterial blood pressure in normotensive rabbits. SEM analysis of films kept for stability study (40 ± 2 °C/75% ± 5%RH for 3 months) revealed the formation of drug crystals which may be due to higher temperature. The findings of the study provide a better alternative dosage form of DTH for the effective treatment of hypertension with enhanced patient compliance.

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“…It is 100 when the two dissolution profiles are identical and approaches 0 as the dissimilarity increases. An f2 above 50 indicates that the two profiles are similar [25].…”

Section: Comparison Of Dissolution Ratementioning

confidence: 99%

“…Dissolution studies were carried out using 500 ml of purified water with 1% w/v polysorbate 20, at 50 rpm and at temperature of 37±0.5 C˚. 10 ml aliquots were withdrawn at suitable time interval (5,10,15,20,25,30,35, 40 and 45 min), filtered through syringe filter 0.45µm and diluted as per need and replaced with fresh medium.…”

Section: In Vitro Drug Dissolution Testmentioning

confidence: 99%

Preparation and in Vitro Evaluation of Lacidipine Oral Liquid Solid Tablet as an Approach of Solubility and Dissolution Rate Enhancement

Rajab

2018

Int J App Pharm

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Objective: The aim of the present study was to prepare a new liquid-solid tablet to enhance the dissolution and bioavailability of a poor water soluble calcium channel blocker lacidipine.Methods: Firstly, solubility study of lacidipine in different media of water-miscible non-volatile solvents as tween 20, tween 80, propylene glycol, liquid paraffin, PEG200, PEG400, and PEG600 was investigated to select the most suitable solvent. A mathematical model was applied to calculate the appropriate amount of carrier and coating material.Four liquid-solid tablets of 6 mg lacidipine were prepared by dissolving the drug in the previously chosen water miscible non-volatile solvents, then a binary mixture of the carrier (Avicel PH 102) and coating material (Aerosil 200) at a ratio of 45:1 was used in all preparation since it gave the optimal flow property. Croscarmellose and magnesium stearate were incorporated in all prepared formulas as super disintegrant and lubricant respectively. On the other hand, directly compressed lacidipine tablet of the same previous composition without the addition of any non-volatile solvent was prepared for comparism study. Both characterizations of powder mixture and post-compression tablet evaluations were done. Differential scanning calorimetry (DSC) and fourier transform infrared spectroscopy (FTIR) were investigated for the pure drug, physical mixture, and selected liquid-solid tablet to exclude any drug-excipients interaction. Results:The obtained results indicated that PEG 200 was the most suitable solvent with lacidipine solubility of 2.81 mg/ml. Flowability of all the prepared formulas was found to be within the specification limits. The liquid-solid tablet formula with PEG 200 at 10% w/w lacidipine was the most suitable one in the term of disintegration time (21±0.2 second), 100% of drug release within 10 min, and with accepted other tablet properties.DSC thermograms for both physical mixture of selected liquisolid system and its tablets illustrated the formation of lacidipine amorphous solid solution. The absence of chemical interaction between drug and other formula components was confirmed by remaining all characteristic peaks of lacidipine in all investigated FTIR spectra. Conclusion:Liquid-solid tablet was considered as a promising system to enhance solubility and dissolution rate of poor-water soluble lacidipine.

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Effect of solvent type on retardation properties of diltiazem HCl form liquisolid tablets

Cited by 28 publications

References 12 publications

Formulation and Evaluation of Furosemide Liquisolid Compact

Formulation and Evaluation of Furosemide Liquisolid Compact

Transdermal delivery of Diltiazem HCl from matrix film: Effect of penetration enhancers and study of antihypertensive activity in rabbit model

Preparation and in Vitro Evaluation of Lacidipine Oral Liquid Solid Tablet as an Approach of Solubility and Dissolution Rate Enhancement

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