Solid-state characterization and dissolution characteristics of gliclazide-β-cyclodextrin inclusion complexes

Moyano, J. R.; Arias-Blanco, M.J.; Ginés, J. M.; Giordano, F.

doi:10.1016/s0378-5173(96)04848-x

Cited by 51 publications

(31 citation statements)

References 5 publications

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“…Another approach that has been investigated extensively is the complexation of poorly water-soluble drugs with cyclodextrins, which was found to improve the aqueous solubility of such drugs (15)(16)(17)(18)(19). Enhanced GLZ dissolution was also achieved via formulation of ordered mixtures of the hydrophobic drug with water-soluble carriers of larger particle size such as mannitol and lactose (7).…”

Section: Introductionmentioning

confidence: 99%

Improvement of Dissolution Rate of Gliclazide Through Sodium Salt Formation

El-Sabawi¹,

Hamdan²

2014

Dissolution Technol.

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Gliclazide is a hypoglycemic agent exhibiting to some extent inadequate and variable absorption as a consequence of poor aqueous solubility and slow dissolution rates. A sodium salt of gliclazide was prepared and investigated for solubility and dissolution properties in comparison to untreated gliclazide. The salt was formed by adding equimolar amounts of gliclazide and sodium hydroxide in an aqueous-ethanolic phase. To confirm salt formation, sodium gliclazide was fully characterized by spectroscopy, differential scanning calorimetry, and potentiometric titration. Furthermore, solubility and in vitro dissolution studies of formulated tablets were performed at pH values of 1.2, 4.5, and 6.8. Sodium gliclazide demonstrated a significant increase in solubility at pH values of 4.5 and 6.8. The most apparent increase was achieved in unbuffered distilled water with a 235-fold higher solubility. Moreover, sodium gliclazide showed an enhancement in the dissolution rate in all tested media, but most significantly at pH 4.5 and 6.8. The highest difference (60%) in dissolution rate between gliclazide and its sodium salt was obtained at pH 6.8 at 30 min.The sodium salt of gliclazide presents improved solubility and drug dissolution, therefore limiting the possibility of variable absorption and improving the onset of action with potential enhancement in its overall bioavailability.

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Section: Introductionmentioning

confidence: 99%

Improvement of Dissolution Rate of Gliclazide Through Sodium Salt Formation

El-Sabawi¹,

Hamdan²

2014

Dissolution Technol.

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“…For CSDs, a fixed weight of GLZ with the corresponding excipient were co-ground in a mortar for 5 min (Emara et al, 2016;Jayasankar et al, 2006). PMs of GLZ with different excipients were manually mixed in a lowdensity polyethylene bag (Emara et al, 2016;Nama et al, 2008) for 5 min. Content uniformity tests were carried out and the results were found within the acceptable range.…”

Section: Preparation Of Co-ground Solid Dispersions and Physical Mixtmentioning

confidence: 99%

“…Many approaches to enhance the dissolution rate of GLZ have been reported such as complexation with cyclodextrins, salt formation and preparation of different types of solid dispersions (El-Sabawiand Hamdan, 2014;Barzegar-Jalali et al, 2010;Biswal et al, 2008;Sapkal et al, 2007;Moyano et al, 1997b;Moyano et al, 1997a). Among all of these approaches, co-grinding is the simplest and the most environmentally desirable technique because it does not require toxic solvents or complex equipment .…”

Section: Introductionmentioning

confidence: 99%

The Flow-Through Cell as an In Vitro Dissolution Discriminative Tool for Evaluation of Gliclazide Solid Dispersions

2017

J App Pharm Sci

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Gliclazide (GLZ) is used to treat type II diabetes mellitus. It is a poorly soluble drug with variable bioavailability. The aim of this study was to improve GLZ solubility and dissolution rate by mixing or cogrinding with different polymers (PEG 4000, PEG 8000, MCC, HPMC E15 and alginates). Dissolution of two commercial products was carried out for comparison. GLZ solubility in phosphate buffer (pH 7.4) showed that grinding of GLZ considerably increased its solubility while, other polymers did not affect GLZ solubility. Flow-through cell (FTC) dissolution apparatus with two patterns of GLZ powder loading were utilized to achieve sensitive and reproducible dissolution data. Results revealed that distribution of untreated and ground GLZ powder with large volume of glass beads gave the best dissolution profiles in terms of rapid onset of dissolution (Q5min) and dissolution efficiency (DE60min). The best excipient among all was PEG (4000 and 8000), where GLZ physical mixture (PM) enhanced the dissolution rate without co-grinding to form solid dispersion (CSD). The highest dissolution rate and extent were obtained from GLZ:PEG 4000 (1:5) PM, where about 45.88 % was dissolved after 5 min and DE60min was 74.18%.

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“…The system is kept under magnetic agitation with controlled process parameters and protected from the light. The formed precipitate is separated by vacuum filtration and dried at room temperature in order to avoid the loss of the structure water from the inclusion complex 41 . Despite an active research interest, the number of marketed products arising from this approach is disappointing mainly caused by the physical and chemical instability and scale-up problems 46 .…”

Section: Inclusion Complexesmentioning

confidence: 99%

Untitled

2011

IJPSR

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Most of the drugs in the developmental pipeline are emerging from the HighThroughput Screening methodology resulting in increased molecular weights and thus consequential bioavailability problems. The bioavailability issue can be due to insufficient solubility of permeability. Most compounds face the solubility problems. Hence, with the advancement of chemical science, the need of development of pharmaceutical technologies is also increasing. Pharmaceutical approaches to correct the bioavailability are definitely being cost-effective in comparison with chemical approaches which are also timeconsuming. Hence various methods of solubility enhancement are being developed. Each technique is with several merits and demerits. To tackle the disadvantages of conventional approaches, newer techniques are developed by many researchers. In this review, an attempt of comparing the conventional and novel techniques is done.

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Solid-state characterization and dissolution characteristics of gliclazide-β-cyclodextrin inclusion complexes

Cited by 51 publications

References 5 publications

Improvement of Dissolution Rate of Gliclazide Through Sodium Salt Formation

Improvement of Dissolution Rate of Gliclazide Through Sodium Salt Formation

The Flow-Through Cell as an In Vitro Dissolution Discriminative Tool for Evaluation of Gliclazide Solid Dispersions

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