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Endocrinology and Metabolic Disease

Hormone

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A glimpse into the focused therapeutic areas

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Most used technologies in drug development

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Disease Domain	Count

Endocrinology and Metabolic Disease	1

Top 5 Drug Type	Count

Hormone	1

Top 5 Target	Count

GCGR(Glucagon receptor)	1

Optimum conditions for GABA production utilizing enzyme-treated rice bran by lactic fermentation were investigated.A culture containing 11% enzyme-treated rice bran (nutrient source) and 11.7% monosodium glutamate (additive substrate of GABA) inoculated with Lactobacillus brevis IFO12005 yielded a GABA content of 7.1% (weight/weight) when the pH was maintained at 5.0 throughout the fermentation period.This resulting GABA content is 4-5-fold higher than without pH control.In addition, the fermented product did not have an unfavorable flavor according to sensory testing.Thus, it is possible to add culture broth to food or drink products to enrich GABA content without damaging their original flavor.

01 Jan 2017·European Journal of Pharmaceutical SciencesQ2 · MEDICINE

Self-micellizing solid dispersion of cyclosporine A for pulmonary delivery: Physicochemical, pharmacokinetic and safety assessments

Q2 · MEDICINE

Article

Author: Seto, Yoshiki ; Ueno, Kodai ; Onoue, Satomi ; Suzuki, Hiroki ; Sato, Hideyuki ; Mizumoto, Takahiro

The present study aimed to develop an inhalable self-micellizing solid dispersion of cyclosporine A (SMSD/CsA) for the direct delivery to the respiratory system with improved therapeutic efficacy and minimized systemic exposure. SMSD/CsA was obtained by wet-milling, and then jet-milled SMSD/CsA was blended with lactose carrier, producing a respirable powder of SMSD/CsA (SMSD/CsA-RP). The physicochemical, pharmacological, and pharmacokinetic properties of SMSD/CsA-RP were characterized, and the hepatotoxic and nephrotoxic potentials were investigated by biomarker analysis. Cascade impactor analysis demonstrated that SMSD/CsA-RP had high in vitro inhalation performance, with a fine particle fraction of 36%. In simulated lung fluid, the SMSD/CsA exhibited better dissolution behavior than amorphous CsA. Pretreatment with SMSD/CsA-RP resulted in significant suppression of antigen-evoked inflammatory events in rats. After intratracheal administration of SMSD/CsA-RP at a pharmacologically effective dose (100μg-CsA/rat), the AUC_0-24 value was <1% of that after oral administration of Neoral^® at a toxic dose (10mg-CsA/kg). Compared with oral Neoral^®, insufflated SMSD/CsA-RP showed 99% reductions of CsA concentrations in both liver and kidney. No significant increases of biomarker levels in plasma were observed even after repeated intratracheal administration of SMSD/CsA-RP for 7days. From these findings, SMSD/CsA-RP might be a favorable dosage form for effective and safe inhalation therapy of CsA.

01 Jan 2015·Chemical and Pharmaceutical BulletinQ4 · MEDICINE

Physicochemical Stability Study on Cyclosporine A Loaded Dry-Emulsion Formulation with Enhanced Solubility

Q4 · MEDICINE

Article

Author: Onoue, Satomi ; Sato, Hideyuki ; Kojo, Yoshiki ; Ogawa, Kumiko ; Mizumoto, Takahiro ; Suzuki, Hiroki

The main purpose of the present study was to evaluate the physicochemical stability of cyclosporine A (CsA)-loaded glycerol monooleate-based dry emulsion (DE). DE formulations containing 5-25% CsA (DE5-25) were stored at 25°C/60% relative humidity for 4 weeks, and freeze-dried solid dispersion formulations containing 5-30% CsA (FD5-30) were also prepared as reference formulations. Even after the storage, no significant changes were observed in the appearance of any formulations. In the dissolution study, both DE and FD exhibited marked enhancement of solubility and there was at least 2.0-fold improvement in the initial dissolution rate of DE formulations compared with that of FD formulations. After storage, DE5, DE15 and FD5 maintained relatively high solubility, with 10% reduction compared with the initial state. However, the solubility of DE25 gradually decreased during storage, as evidenced by 76% reduction of the dissolution amount. No significant changes were seen in DE5-25 using powder X-ray diffraction, although thermal analysis revealed moderate changes in crystallinity in DE25 after storage, possibly leading to the decreased dissolution. Furthermore, particle size distributions of micelles in DE5 and DE15 were almost unchanged after storage for 4 weeks. From these findings, it appears that the physicochemical stability of CsA-loaded DE might vary depending on the manufacturing method and that further optimization could improve physical properties and stability.

100 Deals associated with ILS, Inc.

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100 Translational Medicine associated with ILS, Inc.

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Pipeline

Pipeline Snapshot as of 17 Nov 2024

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

Approved

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