Solid-State Characterization of Candesartan Cilexetil (TCV-116): Crystal Structure and Molecular Mobility.

Matsunaga, Hirokazu; Eguchi, Taro; Nishijima, Kiyoto; Enomoto, Toshio; Sasaoki, Kazumichi; Nakamura, Nobuo

doi:10.1248/cpb.47.182

Cited by 25 publications

(11 citation statements)

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“…The FTIR spectrum of CC, PVPK30, SC, PM, and F1 was compared (Figure 7C). The CC spectra revealed prominent peaks bands characteristic of the polymeric form I of CC [47]; the aromatic and aliphatic CH stretching in 3070-2855 cm −1 range with peaks at 3068, 3000, 2940, and 2860 cm −1 ; the C=O group stretching from the asymmetric organic carbonate -OC(=O)O-moiety with an intense band at 1753 cm −1 ; an ester carbonyl group at 1713 cm −1 ; the -NH bending at 1622 cm −1 ; and the aromatic C-N stretching at 1348 cm −1 and C-O ether stretch at 1032 cm −1 . PVPK-30 showed distinct -C=O stretching at 1651 cm −1 and broad absorption bands at 3434 cm −1 from -OH stretching vibrations, correlating to the broad endotherm peak in the DSC The powder X-ray diffraction (PXRD) of CC, PVPK30, SC, PM and F1 were performed (Figure 7B).…”

Section: Physiochemical Characterizationmentioning

confidence: 99%

Developing pH-Modulated Spray Dried Amorphous Solid Dispersion of Candesartan Cilexetil with Enhanced In Vitro and In Vivo Performance

Surendra

Kim

2021

Pharmaceutics

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Candesartan cilexetil (CC), a prodrug and highly effective antihypertensive agent, is a poorly soluble (BCS Class II) drug with limited bioavailability. Here, we attempted to improve CC’s bioavailability by formulating several CC-loaded amorphous solid dispersions with a hydrophilic carrier (PVPK30) and pH modifier (sodium carbonate) using the spray drying technique. Solubility, in vitro dissolution, and moisture content tests were used for screening the optimized formulation. We identified an optimized formulation of CC/PVPK30/SC, which at the ratio of 1:0.5:1 (w/w/w) exhibited a 30,000-fold increase in solubility and a more than 9-fold enhancement in dissolution compared to pure CC. Solid-state characterization revealed that in pH-modulated CC amorphous solid dispersion (CCSDpM), CC’s crystallinity was altered to an amorphous state with the absence of undesirable interactions. Stability studies also showed that the optimized formulation was stable with good drug content and drug release under accelerated conditions of up to 4 weeks and real-time stability conditions of up to 12 weeks. Furthermore, pharmacokinetic parameters, such as AUC and Cmax of candesartan, had a 4.45-fold and 7.42-fold improvement, respectively, in CCSDpM-treated rats compared to those in the CC-treated rats. Thus, these results suggest that CCSDpM is highly effective for increasing oral absorption. The application of these techniques can be a viable strategy to improve a drug’s bioavailability.

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Section: Physiochemical Characterizationmentioning

confidence: 99%

Developing pH-Modulated Spray Dried Amorphous Solid Dispersion of Candesartan Cilexetil with Enhanced In Vitro and In Vivo Performance

Surendra

Kim

2021

Pharmaceutics

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“…4 Selected examples include, among others, indomethacin, 5 foconazole, 6 lomeridine 7 and candesartan cilexetil. 8 Dehydrocholic acid (3,7,12-triketo-5b-cholan-24-oic acid, 1, hereafter called DHA and shown in Chart 1) is an unnatural bile acid having the cholanoic acid structure. This derivative, usually obtained from cholic acid via oxidation of the C3, C7 and C12 hydroxyl groups, possesses important therapeutic and chemical applications.…”

Section: Introductionmentioning

confidence: 99%

Polymorphism of dehydrocholic acid: crystal structure of the β-phase and guest-mediated solid phase conversion

Fantin¹,

Fogagnolo²,

Bortolini³

et al. 2003

New J. Chem.

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“…The DSC thermogram of CC bulk powder, physical mixture and poloxamer 407 are shown in Figure 5a and b. The DSC thermogram of CC bulk powder showed a sharp endothermic peak at 169°C followed by an exothermal peak which is due to decomposition of drug (Matsunaga et al, 1999). Poloxamer thermogram showed endothermic peak at 55°C.…”

Section: Differential Scanning Calorimetry (Dsc)mentioning

confidence: 99%

Formulation, optimization and characterization of candesartan cilexetil nanosuspension for in vitro dissolution enhancement

Mahesh¹,

Umang²,

Dhaval³

et al. 2015

Afr. J. Pharm. Pharmacol.

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According to Biopharmaceutical classification system (BSC), candesartan cilexetil (CC) is a class-II drug which has limited bioavailability mainly due to its low solubility. In order to enhance its solubility, a universal approach of making nanosuspension is been used in the present investigation. High pressure homogenization, controlled precipitation, media milling and high speed homogenization are the various approaches which are most widely used to produce the nanosuspension. Here, nanosuspension is formulated by combination of two approaches; high speed homogenization and media milling to expedite and ease the process. The polymers used to stabilized the nanoparticles were polyvinylpyrrolidone K-30 (PVP K-30), poloxamer 407, HPMC E 50. To optimize the concentration of the polymer and surfactant the simplex lattice design is used. Various process parameters like homogenization speed, time, media milling cycle, drug to bead ration are optimized by changing one parameter at a time. The nanoparticles produced were of particle size less than 500 nm and were also found to be stable. The saturation solubility was enhaced more than 20 times than the bulk drug. The nanonization of the particles by combination of high speed homogenization and media milling is an effective method of enhancing in vitro dissolution of Candesartan cilexetil.

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Solid-State Characterization of Candesartan Cilexetil (TCV-116): Crystal Structure and Molecular Mobility.

Cited by 25 publications

References 0 publications

Developing pH-Modulated Spray Dried Amorphous Solid Dispersion of Candesartan Cilexetil with Enhanced In Vitro and In Vivo Performance

Developing pH-Modulated Spray Dried Amorphous Solid Dispersion of Candesartan Cilexetil with Enhanced In Vitro and In Vivo Performance

Polymorphism of dehydrocholic acid: crystal structure of the β-phase and guest-mediated solid phase conversion

Formulation, optimization and characterization of candesartan cilexetil nanosuspension for in vitro dissolution enhancement

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