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<title>European Journal of Pharmaceutical Sciences 1 March 2024</title>
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<dateIssued>2024</dateIssued>
<issuance>monographic</issuance>
<edition>1 March 2024</edition>
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<languageTerm type="text">Indonesia</languageTerm>
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<note>ABSTRACT
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-&beta;-cyclodextrin (ALT/HP-&beta;-CD). The formation of this inclusion

complex was confirmed by scanning electron microscopy, power X-ray diffraction, differential scanning calo-
rimetry, Fourier transform infrared spectroscopy, nuclear magnetic resonance spectroscopy, and docking cal-
culations. In addition, we further conducted pharmacokinetic investigation involving gilts, comparing ALT/HP-
&beta;-CD inclusion complex to an ALT oral solution. The physicochemical characterization results unveiled a

transformation of ALT&rsquo;s crystal morphology into an amorphous state, with ALT effectively entering the cavity of
HP-&beta;-CD. Compared with ALT, the solubility of ALT/HP-&beta;-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-&beta;-CD inclusion complex surpassed that of the ALT oral solution, with a relative
bioavailability of 114.08 %. In conclusion, complexation with HP-&beta;-CD represents a highly effective approach to improve both the solubility and oral bioavailability of ALT.</note>
<subject authority=""><topic>Inclusion complex</topic></subject>
<subject authority=""><topic>Hydroxypropyl-β-cyclodextrin</topic></subject>
<subject authority=""><topic>Altrenogest</topic></subject>
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