Nateglinide Controlled Release Tablet Containing Compressionable Enteric Coated Granules

Makino, Chisato; Sakai, Hidetoshi; Yabuki, Akira

doi:10.1248/cpb.58.1136

Cited by 12 publications

(3 citation statements)

References 3 publications

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“…According to the Biopharmaceutical Classification System, NTG with low water solubility and high permeability is classified as a class II drug. [1,2] Its efficacy is significantly shorter than sulphonylureas and may reduce the risk of hypoglycemic episodes caused by sulphonylureas. [3] From a chemical structural point of view, NTG is a derivative of alanine which exhibits four polymorphic structures, namely, A, B, H, and S forms.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and dissolution behaviour of nateglinide‐nicotinamide cocrystals by simple slurry crystallization

et al. 2022

Can J Chem Eng

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Pharmaceutical cocrystals have received increasing attention in improving drug physicochemical properties. Here, we successfully synthesized a cocrystal of nateglinide (a non-sulphonylurea hypoglycemic agent) and nicotinamide by slurry crystallization. The cocrystal formation was confirmed by powder X-ray diffraction, differential scanning calorimetry, and Fourier-transform infrared spectroscopy. The density functional theory calculation at the theoretical level of B3LYP/6-31 + G (d, p) revealed that the hydrogen bonding site of the cocrystal was formed between the carboxyl group of nateglinide and the amide bond of nicotinamide. Moreover, the cocrystal showed improved dissolution capacity in 3 pH buffers, which provides an opportunity for rapid absorption of the active ingredient.

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Section: Introductionmentioning

confidence: 99%

Synthesis and dissolution behaviour of nateglinide‐nicotinamide cocrystals by simple slurry crystallization

et al. 2022

Can J Chem Eng

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“…Controlled‐release particles include microcapsules, microspheres, coated granules, embedded granules, and other sustained‐release agents. Among them, microsphere CR technology has been widely applied in applications relating to pharmaceuticals, disease diagnosis, biological and chemical materials, electronics, environmental monitoring, and food security .…”

Section: Introductionmentioning

confidence: 99%

Preparation and characterization of a novel controlled‐release nano‐delivery system loaded with pyraclostrobin via high‐pressure homogenization

Wang

Cui

Wang

et al. 2020

Pest Management Science

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BACKGROUNDThe development of efficient and safe green pesticides is a scientific strategy to alleviate current pesticide residues, environmental pollution, and threats to non‐target organisms. Pesticide controlled‐release formulations (CRFs) have attracted wide attention because they can control the rate of release of active ingredients and prolong the effective duration. In particular, nanoscale pesticide sustained‐release systems have excellent biological activity and distribution performance because of their small particle size. Some technical difficulties remain in obtaining nanoscale CRFs.RESULTSWe successfully fabricated pyraclostrobin nanosphere CRF by combining high‐pressure homogenization technology and emulsion–solvent evaporation methods. The pyraclostrobin nanospheres had a uniform spherical shape with a mean particle size of 450 nm and polydispersity index of less than 0.3. The pyraclostrobin loading capacity reached 53.6%, with excellent storage stability. The contact angle of nanospheres on cucumber leaf surfaces demonstrated that it had good wettability. Compared with pyraclostrobin technical and commercial formulations, the nanosphere systems showed a significantly sustained release of pyraclostrobin for longer (up to 250 h). A preliminary bioassay against Penicillium ochrochloron showed that the bioactivity and long‐term efficiency of pyraclostrobin nanospheres were superior to those of the commercial formulation.CONCLUSIONThis research introduced a simple, fast, expandable method for preparing pyraclostrobin nanospheres. The results showed that pyraclostrobin nanospheres could prolong the duration of pesticide efficacy and enhance bioactivity. Furthermore, this technology provides a platform for scale‐up production of nano‐scale pesticide CRFs. © 2020 Society of Chemical Industry

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“…[15] Moreover, it is reported that it is expected to enable control of both PBG (Post-Prandial Blood Glucose) and FBG (Fasting Blood Glucose) for moderate and severe diabetes patients with a controlled release formulation containing a short-acting type oral blood glucose regulator (repaglinide, meglitinide, etc.). [16,17] The physicochemical properties of repaglinide, its half life of 1 hour, and its low dose (2-16 mg), make it suitable candidate for administration by the buccal route. [18] The present study examined mucoadhesive bilayer buccal tablets of repaglinide using Hydroxy Propyl Methyl Cellulose K15M (HPMC K15M) as a sustained release polymer, Chitosan as a bioadhesive polymer, and Ethyl Cellulose (EC) as an impermeable backing layer.…”

Section: Introductionmentioning

confidence: 99%

Formulation and evaluation of bioadhesive buccal drug delivery of repaglinide tablets

Patel¹,

Patel²,

Shah³

2012

Asian J Pharm

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T he purpose of this research was to formulate and evaluate bioadhesive buccal tablets of repaglinide using HPMC K15M as a sustained release polymer, chitosan as a bioadhesive polymer and ethyl cellulose as an impermeable backing layer. The tablets were evaluated for weight variation, thickness, hardness, friability, surface pH, mucoadhesive strength, swelling index, in vitro drug release, ex vivo mucoadhesion time and ex vivo drug permeation. A 3 2 full factorial design was used in present study for optimization. Tablets containing HPMC K15M and chitosan in the ratio of 1:1 and lactose as a filler (F2) had the maximum percentage of in vitro drug release. The swelling index, friability and in vitro drug release was affected by type of filler as dicalcium phosphate (DCP) had good binding ability compared to lactose. The surface pH of all tablets was found to be satisfactory (between 6.26 and 7.01), close to neutral pH; hence buccal cavity irritation should not occur with these tablets. F2 batch was considered optimum based on good bioadhesive strength (17.83±0.51 gm) and maximum similarity factor (64.43). The drug release from optimum batch followed zero order kinetics with non-Fickian diffusion. Drugexcipients compatibility study showed no interaction between drug and excipients. Stability study of optimized formulation showed that tablets were stable at accelerated environment condition. Thus, buccal adhesive tablet of repaglinide could be an alternative route to bypass hepatic first pass metabolism and to improve bioavailability of repaglinide.

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Nateglinide Controlled Release Tablet Containing Compressionable Enteric Coated Granules

Cited by 12 publications

References 3 publications

Synthesis and dissolution behaviour of nateglinide‐nicotinamide cocrystals by simple slurry crystallization

Synthesis and dissolution behaviour of nateglinide‐nicotinamide cocrystals by simple slurry crystallization

Preparation and characterization of a novel controlled‐release nano‐delivery system loaded with pyraclostrobin via high‐pressure homogenization

Formulation and evaluation of bioadhesive buccal drug delivery of repaglinide tablets

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