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  1. Substantial Effect of Fenugreek Seeds Aqueous Extract on Serum Estradiol Level in Ovarian Hyperstimulation Syndrome Rat Model
    Ben Hameid AS, Al-Sindi TA, Allow AK, Nafie EM, Alahmad BE, Faisal GG
    Oman Med J, 2019 May;34(3):238-243.
    PMID: 31110632 DOI: 10.5001/omj.2019.45
    Objectives: Estradiol (E2) plays an important role in the pathophysiology of ovarian hyperstimulation syndrome (OHSS). This study aimed to evaluate the effect of fenugreek seed aqueous (FSA) extract on serum E2 levels in a rat model of OHSS.

    Methods: A total of 34 female Sprague Dawley rats, aged 18 days old, weighing 40 to 45 g, were randomly divided into negative control, positive control, and treatment groups. A daily dose of 1500 mg/kg per body weight of FSA extract was administrated orally to rats in the treatment group for 13 days. On day eight of the study, OHSS was induced in both positive control and treated groups by subcutaneous injection of pregnant mare's serum gonadotropin 50 IU for four consecutive days, followed by human chorionic gonadotropin 25 IU on the fifth day. The effect of FSA extract was evaluated by measuring the concentration of serum E2 using the enzyme-linked immunosorbent assay.

    Results: FSA extract reduced serum E2 level significantly in the treated OHSS model (p-value < 0.050) compared to the positive control group.

    Conclusions: The finding has important implications on the development of female infertility adjuvant drugs for safe assisted reproduction technology cycles in terms of OHSS prevention.

  2. Fulltext Lyophilized Amorphous Dispersion of Telmisartan in a Combined Carrier-Alkalizer System: Formulation Development and In Vivo Study
    Al-Japairai KAS, Alkhalidi HM, Mahmood S, Almurisi SH, Doolaanea AA, Al-Sindi TA, et al.
    ACS Omega, 2020 Dec 22;5(50):32466-32480.
    PMID: 33376884 DOI: 10.1021/acsomega.0c04588
    Telmisartan suffers from low oral bioavailability due to its poor water solubility. The research work presents a formulation of solid dispersed (SD) telmisartan formulation as a ternary mixture of a drug, a polymeric carrier (poly(vinylpyrrolidone) (PVP) K30), and an alkalizer (Na2CO3). The preparation method, which was lyophilization of an aqueous solution containing the ingredients, was free from any organic solvent. The developed SD formulations resulted in a significant improvement in in vitro dissolution (>90% drug dissolution in 15 min) compared to pure telmisartan. Solid-state characterization by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffraction (XRD) studies indicated the conversion of crystalline telmisartan into an amorphous form. Fourier transform infrared (FTIR) spectroscopy revealed the drug-polymer interaction that was responsible for reducing the chances of recrystallization. A short-term stability study showed that selected SD formulations were stable in terms of in vitro dissolution and retained their amorphous structure in ambient and accelerated conditions over 2 months. Selected formulations (drug/PVP K30/Na2CO3 as 1:1:2 or 1:2:2 weight ratio) resulted in >2.48 times relative oral bioavailability compared to marketed formulations. It was considered that the incorporation of an alkalizer and a hydrophilic polymer, and amorphization of telmisartan by lyophilization, could enhance in vitro dissolution and improve oral bioavailability.
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