Urea co-inclusion compounds of glipizide for the improvement of dissolution profile

Thakral, Seema; Мадан, А. К.

doi:10.1007/s10847-007-9368-2

Cited by 13 publications

(9 citation statements)

References 24 publications

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“…Therefore, the attribution of the glipizide DSC peak to a simple melting process is not correct [ 10 , 11 , 12 ]. The calorimetric peak is undoubtedly triggered by a decomposition process, which involves a gaseous product evolution and then a mass loss under the peak.…”

Section: Resultsmentioning

confidence: 99%

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The Physico-Chemical Properties of Glipizide: New Findings

et al. 2021

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The present work is a concrete example of how physico-chemical studies, if performed in depth, are crucial to understand the behavior of pharmaceutical solids and constitute a solid basis for the control of the reproducibility of the industrial batches. In particular, a deep study of the thermal behavior of glipizide, a hypoglycemic drug, was carried out with the aim of clarifying whether the recognition of its polymorphic forms can really be done on the basis of the endothermic peak that the literature studies attribute to the melting of the compound. A number of analytical techniques were used: thermal techniques (DSC, TGA), X-ray powder diffraction (XRPD), FT-IR spectroscopy and scanning electron microscopy (SEM). Great attention was paid to the experimental design and to the interpretation of the combined results obtained by all these techniques. We proved that the attribution of the endothermic peak shown by glipizide to its melting was actually wrong. The DSC peak is no doubt triggered by a decomposition process that involves gas evolution (cyclohexanamine and carbon dioxide) and formation of 5-methyl-N-[2-(4-sulphamoylphenyl) ethyl] pyrazine-2-carboxamide, which remains as decomposition residue. Thermal treatments properly designed and the combined use of DSC with FT-IR and XRPD led to identifying a new polymorphic form of 5-methyl-N-[2-(4-sulphamoylphenyl) ethyl] pyrazine-2-carboxamide, which is obtained by crystallization from the melt. Hence, our results put into evidence that the check of the polymorphic form of glipizide cannot be based on the temperature values of the DSC peak, since such a peak is due to a decomposition process whose Tonset value is strongly affected by the particle size. Kinetic studies of the decomposition process show the high stability of solid glipizide at room temperature.

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Section: Resultsmentioning

confidence: 99%

“…According to the studies published in the scientific literature, GPZ melts at a temperature higher than 200 °C, and different melting temperatures have been reported [ 10 , 11 , 12 ]. The crystal structure of glipizide has been recently addressed by single-crystal X-ray diffraction data [ 13 ].…”

Section: Introductionmentioning

confidence: 99%

The Physico-Chemical Properties of Glipizide: New Findings

et al. 2021

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“…The drug, being insoluble in water, belongs to BCS class II and its dissolution is considered to be a rate-determining step in its absorption from gastrointestinal fluids. [26] Thus improvement of solubility and dissolution of glipizide from its dosage form is an important issue for its in-vivo bioavailability and therapeutic efficacy.…”

Section: Introductionmentioning

confidence: 99%

Microwave-generated bionanocomposites for solubility and dissolution enhancement of poorly water-soluble drug glipizide: in-vitro and in-vivo studies

Kushare¹,

Gattani

2013

Journal of Pharmacy and Pharmacology

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The novelty of this work is the green and cost-effective way of forming drug nanocomposites with the help of microwave, which can be scaled up to an industrial level. The method gives an immaculate means of solubilisation by generating drug dispersion at the micro and nanoscale level in natural biodegradable stabilising media. Hence, this study demonstrates the use of BNCs in solubility and dissolution enhancement.

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“…NNCG drugs for oral use as inclusion complexes have been reported. These NNCG drugs included enalapril maleate, glipizide, amiloride hydrochloride, lafutidine, simvastatin and ezetimbe [25][26][27][28][29][30] . Co-inclusion of NNCG drugs in urea has also been reported for reduction in moisture sensitivity of nicorandil and improvement of safe handling and photostability characteristics of cis-retinoic acid [31,32] .…”

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confidence: 99%

Preparation, Characterization and Evaluation of Human Guarded Chlorpyrifos Urea Co-inclusion Complexes

Manish¹

2017

ijps

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Dhall and Madan: Human Guarded Chlorpyrifos Urea Co-inclusion ComplexesPresent study pertains to preparation, characterization and evaluation of human guarded chlorpyrifos urea co-inclusion complexes for agricultural use. Chlorpyrifos a widely used organophosphate insecticide was coincluded along with long linear chain rapidly complexing agent in urea lattice. A three component powder form comprising of urea as host cum fertilizer, oleic acid as an insect pheromone and an insecticide for killing/ disabling the insects was prepared. Resulting insecticide fertilizer amalgamation offered improvement in safe handling and formulation characteristics. Insecticide was engulfed in tunnels of hexagonal urea and is accordingly not accessible for either contact with skin or for inhalation/odour. Hence, personnel engaged in handling of chlorpyrifos will not be exposed to its toxic effects after co-inclusion in hexagonal urea. Insecticide will be activated/released only after chlorpyrifos urea co-inclusion complex comes in contact with water following switching on of automated water sprinkling system in agricultural fields. Steep reduction in mercaptan like odour of chlorpyrifos was observed following engulfment of chlorpyrifos in hexagonal urea lattice. Minimum proportion of long linear chain rapidly complexing agent required for co-inclusion of insecticide in urea lattice was determined calorimetrically. Chlorpyrifos urea co-inclusion complexes were characterized by Fourier transform infrared spectroscopy, X-ray powder diffraction, differential scanning calorimetry and 1 H-nuclear magnetic resonance spectroscopy studies. Regression analysis depicted gradual increase in heat of decomposition with corresponding increase in molar fraction of rapidly complexing agent. Increased heat of decomposition simply indicates better physical stability of complexes. These complexes chlorpyrifos urea co-inclusion complex revealed uniform formulation composition and improved dissolution profile of chlorpyrifos. Studies reveal insecticide fertilizer amalgamation to be a promising approach for formulation of poorly soluble hazardous insecticide into an effective rapidly soluble human guarded insecticide product with improved handling/formulation characteristics at minimal cost.

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Urea co-inclusion compounds of glipizide for the improvement of dissolution profile

Cited by 13 publications

References 24 publications

The Physico-Chemical Properties of Glipizide: New Findings

The Physico-Chemical Properties of Glipizide: New Findings

Microwave-generated bionanocomposites for solubility and dissolution enhancement of poorly water-soluble drug glipizide: in-vitro and in-vivo studies

Preparation, Characterization and Evaluation of Human Guarded Chlorpyrifos Urea Co-inclusion Complexes

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