Fosinopril sodium–hydroxypropyl-β-cyclodextrin inclusion complex

Sbârcea, Laura; Ledeți, Ionuț; Dragan, L.; Kurunczi, Ludovic; Fuliaş, Adriana; Udrescu, Lucreţia

doi:10.1007/s10973-015-4450-2

Cited by 16 publications

(10 citation statements)

References 30 publications

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“…Plotting ln β / T 2 versus 1/ T at the established conversion levels or the ln β against 1/ T , respectively. Activation energy ( E ) can be obtained from the slopes of the plotting straight line 65 …”

Section: Resultsmentioning

confidence: 99%

Comparative study on the effect of two drying methods on the guest encapsulation behavior of osmanthus flavor‐2‐hydroxypropyl‐β‐cyclodextrin inclusion complex

Liu

et al. 2020

Flavour & Fragrance J

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Fragrance and flavor capsules are generally dried into powders due to the convenience of preservation and transportation, while drying has great effect on encapsulation. In this study, osmanthus flavor (OF) and hydroxypropyl‐β‐cyclodextrin (HP‐β‐CD) were used to prepare OF and HP‐β‐CD inclusion complex (OF‐CD). OF‐CD powders were obtained with oven‐drying and freeze‐drying, separately. The effect of drying methods was investigated with the morphology and odor evaluation first. The chemical structure and flavor loading ratio of OF‐CDs were determined by Fourier transform infrared spectroscopy (FTIR) and Gas chromatography‐mass spectrometry (GC‐MS). The flavor was successfully be encapsulated by HP‐β‐CD forming OF‐CD inclusion complex. Oven‐drying led to compact blocky solid, while freeze‐drying resulted in porous morphology. The amount of flavor in OF‐CD with oven‐drying (48.61 μg⁄g) was found lower than that in OF‐CD with freeze‐drying (58.1 μg⁄g). In particular, the content of alcoholics in OF‐CD with oven‐drying (11.8 μg⁄g) was much lower than that in OF‐CD with freeze‐drying (19.04 μg⁄g). Thermogravimetric analysis (TGA) showed that the average activation energy of OF‐CD with oven‐drying (66.3‐135.4 kJ mol−1) was higher than OF‐CD with freeze‐drying (53.0‐100.7 kJ mol−1) by 13.3‐34.7 kJ mol−1. More intermolecular hydrogen bonds in OF‐CD with freeze‐drying led to high encapsulation of partial components; however, they are not thermostable, resulting in fast release at high temperature. The better thermal stability of OF‐CD with oven‐drying makes itself a better candidate for flavor encapsulation for cooking at high temperature.

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Section: Resultsmentioning

confidence: 99%

Comparative study on the effect of two drying methods on the guest encapsulation behavior of osmanthus flavor‐2‐hydroxypropyl‐β‐cyclodextrin inclusion complex

Liu

et al. 2020

Flavour & Fragrance J

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“…The RSP/TM-β-CD PM diffraction pattern exhibits the disappearance of CD peaks at 8.14; 9.73 and 10.84 2θ along with a diminution of the characteristic crystalline reflections of RSP and CD, indicating that the new compound is less crystalline than the drug and TM-β-CD alone. An important reduction in crystallinity is noticed in the diffractometric profile of RSP/TM-β-CD KP together with the appearance of new characteristic reflections (i.e., at 11.99; 12.88; 13.71 and 27.98 2θ) which provides evidence that a new compound is obtained as a result of inclusion complex formation between drug substance and TM-β-CD [34].…”

Section: Thermal Metodsmentioning

confidence: 90%

“…Molecular encapsulation of bioactive compounds in the CDs has achieved pharmaceutical relevance since the physical, chemical and biopharmaceutical characteristics of guest molecules are remarkably improved. CD inclusion complexes can increase the solubility of insoluble drug molecules and the antioxidant properties, can improve the chemical stability, the biological activity and the bioavailability of guest substances, may reduce/eliminate the unpleasant smell and taste, may prevent drug-excipient or drug-drug interactions [6][7][8][9][10][11][12][13][14][15]. β-cyclodextrin (β-CD) is the most frequently used in the pharmaceutical field due to its availability, appropriate internal cavity size for an important number of drug substances and economic advantages.…”

Section: Introductionmentioning

confidence: 99%

Encapsulation of Risperidone by Methylated β-Cyclodextrins: Physicochemical and Molecular Modeling Studies

et al. 2020

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Risperidone (RSP) is an atypical antipsychotic drug which acts as a potent antagonist of serotonin-2 (5TH2) and dopamine-2 (D2) receptors in the brain; it is used to treat schizophrenia, behavioral and psychological symptoms of dementia and irritability associated with autism. It is a poorly water soluble benzoxazole derivative with high lipophilicity. Supramolecular adducts between drug substance and two methylated β-cyclodextrins, namely heptakis(2,6-di-O-methyl)-β-cyclodextrin (DM-β-CD) and heptakis(2,3,6-tri-O-methyl)-β-cyclodextrin (TM-β-CD) were obtained in order to enhance RSP solubility and improve its biopharmaceutical profile. The inclusion complexes were evaluated by means of thermoanalytical methods (TG—thermogravimetry/DTG—derivative thermogravimetry/HF—heat flow), powder X-ray diffractometry (PXRD), universal-attenuated total reflectance Fourier transform infrared (UATR-FTIR), UV spectroscopy and saturation solubility studies. Job’s method was employed for the determination of the stoichiometry of the inclusion complexes, which was found to be 2:1 for both guest–host systems. Molecular modeling studies were carried out for an in-depth characterization of the interaction between drug substance and cyclodextrins (CDs). The physicochemical properties of the supramolecular systems differ from those of RSP, demonstrating the inclusion complex formation between drug and CDs. The RSP solubility was enhanced as a result of drug encapsulation in the CDs cavity, the higher increase being obtained with DM-β-CD as host; the guest–host system RSP/DM-β-CD can thus be a starting point for further research in developing new formulations containing RSP, with enhanced bioavailability.

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“…Angiotensin-converting enzyme inhibitors (ACEIs) are a group of drugs that are effective in controlling high blood pressure and their use in patients has been linked to reduced cardiovascular morbidity and mortality [15].…”

Section: Introductionmentioning

confidence: 99%

Aliskiren, Fosinopril, and Their Outcome on Renin-Angiotensin-Aldosterone System (RAAS) in Rats with Thyroid Dysfunction

Farhadi

Dizaye

2019

International Journal of Endocrinology

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Background and Objectives. Thyroid hormones have an important role in the growth and development of various tissues including the kidney, which is the major site of renin release and the consequent angiotensin and aldosterone formation. Therefore any derangement in thyroid function can result in abnormal functioning in the renin-angiotensin-aldosterone system. The current study was undertaken to find the impact of using a direct renin inhibitor (Aliskiren) and an angiotensin-converting enzyme inhibitor (Fosinopril) on the components of the renin-angiotensin-aldosterone system (RAAS) in rats with thyroid dysfunctions. Method. Forty-two male albino rats were divided into three subgroups. First group (6 rats) served as control. Second group (18 rats) served as hyperthyroid group (6 rats positive control, 6 rats given Aliskiren, and 6 rats given Fosinopril). Third group (18 rats) served as hypothyroid group (6 rats positive control, 6 rats given Aliskiren, and 6 rats given Fosinopril). Induction of hyperthyroidism and hypothyroidism was done through daily oral administration of L-Thyroxine and Propylthiouracil, respectively. On day 40 of the study, the rats were sacrificed and blood was collected for estimation of renin, angiotensin I, angiotensin II, aldosterone, TSH, T3, and T4. The collected blood samples were also used for estimation of levels blood urea, serum creatinine, liver enzymes, and serum electrolytes. Blood pressure and urine collection were done on days 1 and 40. The collected urine was used for estimation of urine flow, sodium excretion, and potassium excretion rates. Results. In hypothyroid induced rats, serum renin level dropped as expected, while the use of Aliskiren and Fosinopril on these hypothyroid rats raised renin level due to the feedback mechanism. Both angiotensin I and II were significantly (P <0.05) lower than normal levels in the hypothyroid rats, unlike the level of aldosterone, which was higher than normal level. There was nonsignificant lowering in BP (systolic, diastolic, and mean BP) in the hypothyroid rats. Treatment of these rats with Aliskiren and Fosinopril did not lower the blood pressure more than normal when compared to the hypothyroid group. The hypothyroid rats also showed a decrease in level of serum creatinine. In hyperthyroid rats, there was a rise in levels of serum renin, angiotensin II, and aldosterone; nevertheless, the increase in angiotensin I level was significant. The use of Aliskiren and Fosinopril increased the level of renin nonsignificantly (decreased angiotensin I significantly). Hyperthyroid rats showed a significant increase in systolic, diastolic, and mean blood pressure. Both Aliskiren and Fosinopril increased urine flow, Na+ excretion, and K+ excretion rates. Aliskiren was better at reducing the high blood pressure. Conclusion. Aliskiren and Fosinopril in hyperthyroid rats decreased serum angiotensin I, angiotensin II, and aldosterone. Blockade of renin and inhibition of angiotensin-converting enzyme both resulted in a rebound increase in level of renin in hypothyroid rats. Aliskiren is better at controlling blood pressure in hyperthyroid rats. Urine flow, sodium excretion, and potassium excretion rates were improved by the use of Aliskiren and Fosinopril in hyperthyroid rats.

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Fosinopril sodium–hydroxypropyl-β-cyclodextrin inclusion complex

Cited by 16 publications

References 30 publications

Comparative study on the effect of two drying methods on the guest encapsulation behavior of osmanthus flavor‐2‐hydroxypropyl‐β‐cyclodextrin inclusion complex

Comparative study on the effect of two drying methods on the guest encapsulation behavior of osmanthus flavor‐2‐hydroxypropyl‐β‐cyclodextrin inclusion complex

Encapsulation of Risperidone by Methylated β-Cyclodextrins: Physicochemical and Molecular Modeling Studies

Aliskiren, Fosinopril, and Their Outcome on Renin-Angiotensin-Aldosterone System (RAAS) in Rats with Thyroid Dysfunction

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