Formulation and Evaluation of Sustained ReleaseMatrix Tablets of Glimepiride Based on Combinationof Hydrophilic and Hydrophobic Polymers

Hadi,

doi:10.7324/japs.2012.2613

Cited by 18 publications

(18 citation statements)

References 3 publications

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“…GMP is a weak acid (pK a =6.2) and practically insoluble in water. 21) These results demonstrate that GMP would be more soluble in an aqueous solution at a neutral or basic pH, which is consistent with our results.…”

Section: Discussionsupporting

confidence: 82%

Effect of Piperazine Dithioctate on the Oral Pharmacokinetics of Glimepiride in Rats

Kim

Choi

et al. 2015

Biological & Pharmaceutical Bulletin

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The objective of the present work was to investigate the potential for pharmacokinetic drug-drug interactions between glimepiride (GMP) and piperazine dithioctate (PDT) in rats to support the development of an orally combined product of the two drugs. An LC-MS/MS bioanalytical method was developed for simultaneous quantification of GMP and thioctic acid (TA) in rat plasma. The accuracy, precision, linearity, selectivity, and recovery were all within an acceptable range. The oral plasma exposure of the GMP solution was more than 14-times greater than that of the GMP suspension at a dose of 0.5 mg/kg, suggesting a dissolutionlimited absorption of the GMP suspension. Oral co-administration of PDT (72 mg/kg) with GMP suspension (0.5 mg/kg) reduced the plasma GMP exposure by approximately 80% without a significant change in t 1/2 and t max . Oral co-administration of PDT with GMP solution had no significant effect on the plasma pharmacokinetics of GMP. PDT lowered the pH (from ca. 7 to 5.6) and the dissolved GMP concentration in the GMP suspension. It was also shown that GMP was more soluble at pH 7 than at 5.7 in an aqueous solution, and the oral plasma exposure of a GMP suspension at pH 7.0 was substantially higher than that of a suspension at pH 5.7. These results suggest that the pH-dependent solubility of GMP was likely responsible for PDT's effect on the oral absorption of GMP. In conclusion, the current work suggests a possibility of drug-drug interaction between GMP and PDT upon oral co-administration.Key words glimepiride; piperazine dithioctate; pharmacokinetics; thioctic acid; drug-drug interaction Glimepiride (GMP) (Fig. 1) is a medium-to long-acting oral sulfonylurea widely prescribed to treat type 2 diabetes. 1)GMP lowers blood glucose by stimulating the release of insulin and by enhancing the activity of intracellular insulin receptors.2,3) GMP is rapidly and completely absorbed following oral administration, with a bioavailability close to 100% and a t max of 2-3 h in humans. 4) GMP is eliminated mainly by metabolism by CYP2C9, and the mean plasma elimination half-life (t 1/2 ) is 5-8 h in humans. 5)Thioctic acid (TA) (Fig. 1) is an antioxidant present in prokaryotic and eukaryotic cells. It has been administered for the treatment of various oxidative stress-related diseases, including alcoholic liver disease, diabetes, glaucoma, and neurodegenerative disorders.6,7) TA can also decrease neuropathy symptoms, therefore, it has been approved as a prescription drug for the treatment of diabetic polyneuropathy, and has been frequently co-prescribed with GMP. [8][9][10][11] TA also is widely available as a nutritional supplement in the United States. TA was shown to be absorbed rapidly with a t max of 0.8 h following a single oral dose of 200 mg in humans, and its mean oral bioavailability is 29.1%, with a mean t 1/2 of 0.5 h. 12)Piperadine dithioctate (PDT) (Fig. 1) is a piperazine salt of TA with physicochemical properties more suitable for formulations than TA itself. The melting points of PDT and TA are...

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Section: Discussionsupporting

confidence: 82%

Effect of Piperazine Dithioctate on the Oral Pharmacokinetics of Glimepiride in Rats

Kim

Choi

et al. 2015

Biological & Pharmaceutical Bulletin

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“…Before compression, the flow properties of prepared granules were characterized in terms of angle of repose, Carr's index and Hausner's ratio [15], and results were represented as mean ± SD.…”

Section: Evaluation Of the Pre-compression Parameters Of Powder Mixturesmentioning

confidence: 99%

Development of Multiple-Unit Floating Drug Delivery System of Clarithromycin: Formulation, in vitro Dissolution by Modified Dissolution Apparatus, in vivo Radiographic Studies in Human Volunteers

Reddy¹,

Reddy²

2017

Drug Res (Stuttg)

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Clarithromycin (CM), a broad spectrum macrolide antibiotic used to eradicate H. pylori in peptic ulcer. Clarithromycin (CM) is well absorbed from the gastrointestinal tract, but has a bioavailability of 50% due to rapid biodegradation. The aim of this investigation was to increase the gastric residence time, and to control the drug release of clarithromycin by formulating into multiple unit floating mini-tablets. Floating tablets were prepared by using direct compression method with HPMC KM and Polyox WSR 1105 as release retarded polymers and sodium bicarbonate as gas generating agent. The prepared mini-tablets were evaluated for thickness, weight variation, friability, hardness, drug content, in vitro buoyancy, swelling studies, in vitro dissolution studies by using modified Rossett-Rice test and in vivo radiographic studies in healthy human volunteers in fasting conditions. DSC analysis revealed that no interaction between drug and excipients. All the physical parameters of the tablets were within the acceptable limits. The optimized formulation (F6) had showed controlled drug release of 99.16±3.22% in 12 h, by zero-order release kinetics, along with floating lag time of 9.5±1.28 s and total floating time of 12±0.14 h. X-ray imaging studies revealed that in vivo gastric residence time of clarithromycin floating mini-tablet in the stomach was about 3.5 h. The results demonstrated that the developed floating mini-tablets of clarithromycin caused significant enhancement in gastric retention time along with sustained effect and increased oral bioavailability.

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“…Various properties of granules such as bulk density, tapped density, Carr's index, Hausner's ratio and angle of repose were determined [14] and the results are shown in the ▶Table 3. The angle of repose for all the formulations was found to be < 30 indicating free flowing of the material and Carr's index values were found to be in the range of 12-16 indicating good flow properties .…”

Section: Determination Of Flow Properties Of Core Tablet Granulesmentioning

confidence: 99%

Design and Evaluation of Chronomodulated Drug Delivery of Tramadol Hydrochloride

et al. 2017

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Rheumatoid arthritis is an auto immune disease which requires chronotherapy as it occurs during early morning. Tramadol hydrochloride (TH) is an analgesic drug, used to treat rheumatoid arthritis. The aim of the present investigation was to develop chronomodulated drug delivery system of tramadol hydrochloride such that it releases the drug early in the morning, during which the symptoms of rheumatoid arthritis worsen. To develop chronomodulated drug delivery system of TH, initially core tablets of TH were prepared using three different supradisintegrants followed by coating with pH dependent polymer of Eudragit S100. The prepared core tablets are evaluated for physical parameters and an optimal system was identified. Further, coating composition of Eudragit S100 was optimized and coating tablets of TH was prepared. The prepared coated tablets were evaluated for weight variation, hardness, drug content and in vitro release studies in 0.1N HCl, pH 6.8 phosphate buffer and pH 7.4 phosphate buffer. Formulation with 7.5% of coating solution (ES2) had shown a significant drug release after a lag time of 3 h (in pH 6.8 medium), 6 h (in pH 6.8 medium) and 8 h (in pH 7.4 medium), respectively. DSC studies revealed that no interaction between core and coated materials with drug was observed. Thus, chronomodulated drug delivery system of TH was formulated and assuming that if a tablet is administered around 9 pm to 10 pm, the drug release starts after a lag time of 6 h i. e., around 3am to 4 am.

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Formulation and Evaluation of Sustained ReleaseMatrix Tablets of Glimepiride Based on Combinationof Hydrophilic and Hydrophobic Polymers

Cited by 18 publications

References 3 publications

Effect of Piperazine Dithioctate on the Oral Pharmacokinetics of Glimepiride in Rats

Effect of Piperazine Dithioctate on the Oral Pharmacokinetics of Glimepiride in Rats

Development of Multiple-Unit Floating Drug Delivery System of Clarithromycin: Formulation, in vitro Dissolution by Modified Dissolution Apparatus, in vivo Radiographic Studies in Human Volunteers

Design and Evaluation of Chronomodulated Drug Delivery of Tramadol Hydrochloride

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