Rapidly dissolving repaglinide powders produced by the ultra-rapid freezing process

Purvis, Troy; Mattucci, Michal E.; Crisp, M. Todd; Johnston, Keith P.; Williams, Robert O.

doi:10.1208/pt0803058

Cited by 60 publications

(33 citation statements)

References 33 publications

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“…After complete drying, the vials were taken out, and the dried products were scraped from the vials. The formulations were powdered and packaged in glass vials (16).…”

Section: Preparation Of Lyophilized Formulationsmentioning

confidence: 99%

Dissolution Enhancement and Physicochemical Characterization of Valsartan in Solid Dispersions with β-CD, HP β-CD, and PVP K-30

Mahapatra¹,

Murthy²,

Biswal³

et al. 2011

Dissolution Technol.

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Solid dispersions (SDs) and physical mixtures (PMs) of valsartan in β-cyclodextrin (β-CD), hydroxypropyl β-cyclodextrin (HP β-CD), and polyvinyl pyrollidone (PVP K-30) were prepared to increase its solubility characteristics. The drug formulations were characterized in the solid state by Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). By these physical determinations, drug-polymer interactions were found. Both the solubility and the dissolution rate of the drug in these formulations were increased. Drug contents were determined by UV spectrophotometry at a λ max of 249.5 nm. The phase solubility behavior of valsartan in various concentrations of β-CD, HP β-CD, and PVP K-30 (0.25-1.0% w/v) in distilled water was obtained at 37 ± 2 °C. The dissolution of valsartan is increased with increasing amounts of the hydrophilic carriers (i.e., β-CD, HP β-CD, and PVP K-30). Gibbs free energy (ΔG o tr ) values were all negative, indicating the spontaneous nature of valsartan solubilization. The SDs of valsartan with β-CD and HP β-CD were prepared at 1:1, 1:3, and 1:5 drug/carrier ratios by a kneading method, and PVP K-30 SDs were prepared at the same ratios (i.e., 1:1, 1:3 and 1:5 drug/carrier) by a lyophilization technique. The FTIR spectroscopic studies show the stability of valsartan and the absence of well-defined drug-polymer interaction. Compared with β-CD, HP β-CD showed better enhancement of dissolution rate; compared with HP β-CD, PVP K-30 showed better solubility and dissolution enhancement.

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“…After complete drying, the vials were taken out, and the dried products were scraped from the vials. The formulations were powdered and packaged in glass vials (16).…”

Section: Preparation Of Lyophilized Formulationsmentioning

confidence: 99%

Dissolution Enhancement and Physicochemical Characterization of Valsartan in Solid Dispersions with β-CD, HP β-CD, and PVP K-30

Mahapatra¹,

Murthy²,

Biswal³

et al. 2011

Dissolution Technol.

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“…17) The in‰uence of pH on Repag at carbon paste and glassy carbon electrodes was studied. Figure 3 shows the plot of peak current (Ip) vs. pH.…”

Section: Resultsmentioning

confidence: 99%

Electrochemical Determination of the Antidiabetic Drug Repaglinide

El-Ries

Attia

2008

YAKUGAKU ZASSHI

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The electrochemical oxidation of repaglinide has been carried out in Britton-Robinson buŠer at carbon paste and glassy carbon electrodes. Repaglinide exhibits a well-deˆned irreversible oxidation peak over the entire pH range (2 11). DiŠerential pulse voltammetry was used to determine repaglinide in pure form. The peak current varied linearly in the following ranges: 8.0×10 -7  3.2×10-6 M and 4.0×10 -7  4.0×10 -6 M in case of carbon paste electrode and glassy carbon electrode, respectively. In case of carbon paste electrode the limits of detection (LOD) and quantiˆcation (LOQ) were 1.348×10 -7 M and 4.494×10 -7 M, respectively. For glassy carbon electrode the LOD and LOQ were 1.062×10 -7 M and 3.54×10 -7 M, respectively. The percentage recoveries were found in the following ranges: 99.09 100.07％ and 99.0 100.50％ for carbon paste electrode and glassy carbon electrode, respectively. The relative standard deviations were found in the following ranges: 0.636 1.395％ and 0.431 1.104％ in case of carbon paste electrode and glassy carbon electrode, respectively. DiŠerential pulse voltammetry was successfully applied for the determination of repaglinide in tablets and human serum.

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“…Tris showed highest solubilizing efficiency and binding affinity followed by PVP-K25 then LM-CH as clarified by the slope and K s values, respectively, of the corresponding linear curves (Table II). Being compratively strong basic, Tris may be expected to form more stabilized complexes with Gmp, hence higher solubility of this drug was observed (5,7,13). The hydrogen bonding of PVP with Gmp as suggested by FTIR results might stabilize the complex with this drug (Fig.…”

Section: Semmentioning

confidence: 92%

“…For example, glibenclamide solubility was enhanced by PVP (11) and Tris (12). That of repaglinide was increased by ultrarapid freezing with Tris (13). The effects of cyclodextrin and chitosan on the solubility of glyburide have been investigated (14).…”

Section: Introductionmentioning

confidence: 99%

Improvement of Dissolution and Hypoglycemic Efficacy of Glimepiride by Different Carriers

et al. 2012

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Abstract. Effects of tromethamine (Tris), polyvinylpyrrolidone (PVP-K25), and low molecular weight chitosan (LM-CH) on dissolution and therapeutic efficacy of glimepiride (Gmp) were investigated using physical mixtures (PMs), coground mixtures, coprecipitates (Coppts) or kneaded mixtures (KMs), and compared with drug alone. Fourier transform infrared spectroscopy, differential scanning colorimetry, and X-ray diffractometry were performed to identify any physicochemical interaction with Gmp. Surface morphology was examined via scanning electron microscopy. The results of Gmp in vitro dissolution revealed that it was greatly enhanced by Coppt with Tris or PVP-K25 and KM with LM-CH at a drug to carrier ratio of 1:8. Gmp amorphization by PVP-K25 and LM-CH was a major factor in increasing Gmp dissolution. Being basic, Tris might increase the pH of the microdiffusion layer around Gmp particles improving its dissolution. Formation of water-soluble complexes suggested by solubility study may also explain the enhanced dissolution. Capsules were prepared from Coppts and KM 1:8 drug to carrier binary systems and also with Tris PMs. In vivo, the hypoglycemic efficacy of Gmp capsules in rabbits increased by 1.63-, 1.50-, and 1.46-fold for 1:8 Coppts with Tris or PVP-K25 and KM with LM-CH respectively, compared with Gmp alone. Surprisingly, the response to Tris PM 1:20 capsules was 1.52-fold revealing statistically insignificant difference to that of Tris Coppt 1:8 (1.63 fold). As a conclusion, dissolution enhancement and hypoglycemic potentiation by 1:20 PM of Gmp/Tris, being simple and easy to prepare, may enable development of a reduced-dose and fast-release oral dosage form of Gmp.

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Rapidly dissolving repaglinide powders produced by the ultra-rapid freezing process

Cited by 60 publications

References 33 publications

Dissolution Enhancement and Physicochemical Characterization of Valsartan in Solid Dispersions with β-CD, HP β-CD, and PVP K-30

Dissolution Enhancement and Physicochemical Characterization of Valsartan in Solid Dispersions with β-CD, HP β-CD, and PVP K-30

Electrochemical Determination of the Antidiabetic Drug Repaglinide

Improvement of Dissolution and Hypoglycemic Efficacy of Glimepiride by Different Carriers

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