Preparation and evaluation of diltiazem hydrochloride-gelucire 43/01 floating granules prepared by melt granulation

Shimpi, Shyam; Chauhan, Bhaskar; Mahadik, Kakasaheb R.; Paradkar, Anant

doi:10.1208/pt050343

Cited by 53 publications

(30 citation statements)

References 24 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…In vitro percent buoyancy studies reveal that, in spite of stirring the dissolution medium for more than 12 h, 80-90% of minitablets of formulation F2-F4 still continued to float (Table 5). The surface hydrophobicity imparted to the drug particle by the hydrophobic lipid coat was responsible for floating behavior (Shimpi et al, 2004). But all low HLB excipient did not ensure floating, as similar granules prepared using Compritol and glyceryl monosterate separately did not show floating property (Chauhan et al, 2005).…”

Section: In Vitro Buoyancy and Percent Buoyancymentioning

confidence: 99%

Design and characterization of cefuroxime axetil biphasic floating minitablets

et al. 2014

View full text Add to dashboard Cite

Biphasic floating minitablets of cefuroxime axetil were prepared by melt granulation technique using two different grades of gelucire namely 50/13 and 43/01 to maintain constant plasma drug concentration. Loading dose of cefuroxime axetil was formulated as immediate release (IR) minitablets by using hydrophilic grade of gelucire 50/13. Maintenance dose was formulated as floating sustained release (SR) minitablets by using hydrophobic grade of gelucire 43/01. The prepared IR and SR granules were subjected to micromeritic studies and scanning electron microscopy. Fourier transform infrared spectroscopy (FT-IR) study revealed that drug and selected carriers were compatible. In vitro dissolution study of optimized IR minitablets showed more than 85% of loading dose dissolved within 30 min. Optimized SR minitablets showed zero lag time with floating duration more than 12 h. The drug release from SR minitablets was linear with square root of time with non-Fickian diffusion-controlled release. The optimized batch of minitablets was filled into 0 size hard gelatin capsule. In vitro dissolution study for capsule showed an immediate burst release followed by SR up to 12 h. There is no significant change in dissolution data after storage at 40 C and 75% RH for three months. Microbiological assay of dissolution samples of optimized minitablets filled in capsules showed proportionate increase in inhibition of growth against Escherichia coli up to 12 h samples. In vivo bioavailability study in albino rabbits showed three times improvement in oral bioavailability.

show abstract

Section: In Vitro Buoyancy and Percent Buoyancymentioning

confidence: 99%

Design and characterization of cefuroxime axetil biphasic floating minitablets

et al. 2014

View full text Add to dashboard Cite

show abstract

“…1. Gelucire 43/01 was selected as a release-retarding agent, which minimized the variation in the release profile of highly water soluble drugs (15). HPMC K4M was selected as a matrixing agent because of its excellent gelling and sustained-release properties.…”

Section: Resultsmentioning

confidence: 99%

“…The failure of therapy can be avoided by providing the effective concentration of antibiotics at the site of action (13). In this study, an attempt was made to formulate Levo floating tablets with the use of low density polymer hydroxypropyl methylcellulose (HPMC K4M) and the release-retarding hydrophobic polymer Gelucire 43/01 (14,15). Gelucire, a mixtures of mono-, di-, and triglycerides with polyethylene glycol (PEG) esters of fatty acids, was used in combination with the hydrophilic polymer (HPMC K4M) to minimize the hydration rate of the floating tablet and variability in the release profiles of the highly water soluble drug (Levo).…”

Section: N a Relatively Short Time Helicobacter Pylori (H Pylori)mentioning

confidence: 99%

Goodness-of-Fit Model-Dependent Approach for Release Kinetics of Levofloxacin Hemihydrates Floating Tablet

Thakkar¹,

Shah²,

Soni³

et al. 2009

Dissolution Technol.

View full text Add to dashboard Cite

The objective of this work was to develop floating levofloxacin tablets and to understand the kinetics of drug release by applying mathematical and model-dependent approaches. Nine formulations of floating tablets were prepared by the direct compression method using Gelucire 43/01 (hydrophobic) and hydroxypropyl methylcellulose (hydrophilic) as matrix-forming excipients. The in vitro drug release was studied in pH 1.2 HCl using USP dissolution Apparatus 2 at 50 rpm. Zero-order, first-order, Higuchi, Hixson-Crowell, and Korsmeyer et al. models were used to estimate the kinetics of drug release. The criteria for selecting the most appropriate model were based on the goodness-of-fit test and lowest sum of squares residual. Drug release from the optimal batch was explained by the Higuchi model. A simple mathematical approach was applied to determine the deviation in area under the curve (AUC) between predicated and observed dissolution data. The difference in percent deviation of AUC at each point was lowest for the optimum batch. Drug release was a function of the ratio of hydrophobic to hydrophilic matrixing agent.

show abstract

“…There are some reports on the use of gelucires in the development of SR products. [8] Multi-unit forms are developed by initially preparing calcium alginate microspheres of captopril, which are subsequently used as a core to prepare the microcapsules employing ethyl cellulose as the coat material. This novel technique of microencapsulating the alginate microspheres is not reported earlier.…”

Section: Introductionmentioning

confidence: 99%

Untitled

Ramesh

2017

AJP

View full text Add to dashboard Cite

Background: Multi-unit dosage forms such as microcapsules and microspheres offer the advantage of better control over the release and lesser chances of dose dumping. This is critical for drugs with high dose, and no comparative study between single and multi-unit forms for controlled release was done previously. Objectives: To explore the utility of using a combination of almond gum and gelucire for preparing sustained-release (SR) matrix tablets. To employ a novel technique of microencapsulating the alginate beads of captopril for SR. Materials and Methods: Almond gum, gelucire (43/01), and ethyl cellulose were the major polymers used. Direct compression and emulsion solvent evaporation methods were employed to prepare the matrix tablets and microcapsules. The prepared products were evaluated for drug release and characterized by scanning electron microscopy, differential scanning calorimetry (DSC), and infrared spectroscopic studies. Accelerated stability study was performed, and drug release was studied before and after stability test. Results and Discussion: Drug release from the matrix tablets could be modified by changing the proportion of gelucire or almond gum in the formulation. The combined use of almond gum and gelucire is found to be more effective in giving a slow, and complete release spread over 12 h. Infrared spectroscopic and DSC studies revealed that there are no interactions of captopril with the various polymers. The microcapsules of alginate beads prepared employing ethyl cellulose are found to be free flowing and had an average size in the range of 750-850 µ. The matrix tablets of captopril are found to be giving more controlled release for a longer period of 12 h compared to the microcapsules. Conclusion: Entrapping the drug in a lipophilic material such as gelucire or beeswax and preparing the calcium alginate microspheres which are subsequently microencapsulated is a promising new approach to obtain the SR of highly water soluble drugs such as captopril.

show abstract

Preparation and evaluation of diltiazem hydrochloride-gelucire 43/01 floating granules prepared by melt granulation

Cited by 53 publications

References 24 publications

Design and characterization of cefuroxime axetil biphasic floating minitablets

Design and characterization of cefuroxime axetil biphasic floating minitablets

Goodness-of-Fit Model-Dependent Approach for Release Kinetics of Levofloxacin Hemihydrates Floating Tablet

Untitled

Contact Info

Product

Resources

About