FOOD CHEMISTRY
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2025
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IF 9.8
Hongfei Yang,Hao Wen,Yu Si,Mingyue Ding,Yiting Liu,Ziyan Yu,Linwei Zhang,Jiacan Wang,Xiaoming Pan,Shiyun Han,Yiting Wang,Shixiang Wu,Jixiang Liang,Jiaxu Xiao,Rui Fang,Dapeng Peng
Altrenogest is one of the most commonly used steroid hormones; however, there are currently no relevant reports on monospecific molecular recognition elements and immunoassay methods for altrenogest. Herein, a computer-aided precise hapten design strategy was proposed for monospecific monoclonal antibodies (mAb) preparation. Based on this strategy, a monospecific and sensitive mAb-D7 was prepared for the first time. The mAb-D7 has the 50 % inhibitory concentration (IC 50 ) of 0.12 ng/mL for altrenogest and does not cross-react with other common steroid hormones. Additionally, a single-chain variable fragment (scFv) for altrenogest was constructed for the first time, which exhibits an IC 50 of 1.7 ng/mL for altrenogest. The molecular recognition mechanism studies showed the monospecific mAb-D7 to altrenogest originated from the amino acids PHE-94 and LEU-237, demonstrating the reliability of this strategy. Finally, two monospecific, rapid, and sensitive immunoassays were established for altrenogest in pork and pork liver for the first time.
研究领域:
生物化学
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免疫学
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兽医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Frontiers in Veterinary Science
·
2024
·
IF 2.6
Xu Jinxia,Ling Lifang,Lan Yanhua,Yuan Ye,Ran Long,Jiang Jiaxin,Huang Xianhui
Introduction: Altrenogest (ALT) is widely used to regulate the estrous cycle of sows and mares; however, currently used oral solutions of ALT are deficient in terms of dose accuracy and stability during use. To resolve these problems, we aimed to prepare softgel capsules of ALT with a unit dose equal to the clinically administered dose.Method: The shell of the softgel capsule was mainly composed of gelatin and glycerol, with titanium dioxide and red iron oxide as masking agents. Using the shake flask method, the contents were screened for ethyl acetate as a lipophilic solubilizing carrier based on soya bean oil. The contents were automatically filled and compressed into softgel capsules by a softgel capsule machine. The quality of the prepared softgel capsules was evaluated through a drug content test, an in vitro release test, and stability studies. Furthermore, bioequivalence studies were conducted with atrenogest oral solution.Results: The content is an ALT concentration of 2% oil solution and the specification of the softgel is 20 mg/capsule. In in vitro dissolution experiments, the softgel capsules were rapidly disintegrated and released in three different pH buffers, with a cumulative release rate of nearly 100% at 1 h. The softgel capsules were stable at high temperature and under strong light for 10 days, and the concentration of ALT was >99% in the 6-month accelerated and long-term tests. In the bioequivalence study, Tmax of the softgel capsules was 2.20 ± 0.77 h, t1/2 was 6.36 ± 1.74 h, and Cmax was 64.65 ± 20.69 ng/ml. The main pharmacokinetic parameters Tmax, Cmax, AUC0−t, and AUC0−∞, did not differ significantly between the softgel capsules and the commercially available ALT oral solution (P > 0.05), and bioequivalence was demonstrated within the 90% confidence interval.Conclusion: The prepared softgel capsules have the advantages of higher content, ease of use with accurate dosing, good stability, and equivalence to ALT oral solution, implying that our softgels are ready for clinical use.
研究领域:
兽医学
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药剂学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
·
2024
·
IF 4.3
Wojun Chen,Xianwen Zheng,Wenxuan Lao,Hongxin Wang,Shengfeng Chen,Canying Liu,Zhisheng Chen,Yinshan Bai,Hui Zhang,Xiaoshu Zhan,Bingyun Wang
Altrenogest (ALT), a synthetic progestogen, serves a critical role in estrus synchronization among animals like gilts and mares. However, its practical application in animal husbandry is hampered due to its poor solubility and limited oral bioavailability. To address this challenge, a solvent evaporation method was employed to create an inclusion complex of ALT with hydroxypropyl-β-cyclodextrin (ALT/HP-β-CD). The formation of this inclusion complex was confirmed by scanning electron microscopy, power X-ray diffraction, differential scanning calorimetry, Fourier transform infrared spectroscopy, nuclear magnetic resonance spectroscopy, and docking calculations. In addition, we further conducted pharmacokinetic investigation involving gilts, comparing ALT/HP-β-CD inclusion complex to an ALT oral solution. The physicochemical characterization results unveiled a transformation of ALT's crystal morphology into an amorphous state, with ALT effectively entering the cavity of HP-β-CD. Compared with ALT, the solubility of ALT/HP-β-CD inclusion complex increased by 1026.51-fold, and its dissolution rate demonstrated significant improvement. Pharmacokinetic assessments further revealed that the oral bioavailability of ALT/HP-β-CD inclusion complex surpassed that of the ALT oral solution, with a relative bioavailability of 114.08 %. In conclusion, complexation with HP-β-CD represents a highly effective approach to improve both the solubility and oral bioavailability of ALT.
研究领域:
兽医学
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药学
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畜牧业
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）