HPLC Estimation, Ex vivo Everted Sac Permeability and In Vivo Pharmacokinetic Studies of Darunavir

Suvarna, Vasanti; Sangave, Preeti C.

doi:10.1093/chromsci/bmx113

Cited by 9 publications

(2 citation statements)

References 29 publications

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“…The interactions described for the animal studies in most cases also resulted in increased bioavailability (increased serum/plasma C max and/or increased AUC values) of the investigated drugs. However, interactions in animal studies were observed with several additional drugs, such as ibuprofen, nimesulide, oxyphenylbutazone (non-steroidal anti-inflammatory drugs); amoxycillin, ampicillin, norfloxacin, marbofloxacin, metronidazole (antibiotic drugs); glimepiride, nateglinide (antidiabetic drugs); simvastatin, rosuvastatin (lipid-lowering drugs); verapamil, diltiazeme (calcium channel blockers); sodium valproate (antiepileptic drug); darunavir ethanolate (HIV protease inhibitor); losartan (angiotensin II receptor type 1 antagonist); domperidone (antiemetic drug); almotriptan (anti-migraine drug); and fexofenadine (antihistaminic drug) [126][127][128][129][130][131][132][133][134][135][136][137][138][139][140][141][142][143][144].…”

Section: Interactions Of Piperine With Medicinal Products and Other Substancesmentioning

confidence: 99%

Safety Aspects of the Use of Isolated Piperine Ingested as a Bolus

Ziegenhagen

Heimberg

Lampen

et al. 2021

Foods

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Piperine is a natural ingredient of Piper nigrum (black pepper) and some other Piper species. Compared to the use of pepper for food seasoning, piperine is used in food supplements in an isolated, concentrated form and ingested as a bolus. The present review focuses on the assessment of the possible critical health effects regarding the use of isolated piperine as a single ingredient in food supplements. In human and animal studies with single or short-term bolus application of isolated piperine, interactions with several drugs, in most cases resulting in increased drug bioavailability, were observed. Depending on the drug and extent of the interaction, such interactions may carry the risk of unintended deleteriously increased or adverse drug effects. Animal studies with higher daily piperine bolus doses than in human interaction studies provide indications of disturbance of spermatogenesis and of maternal reproductive and embryotoxic effects. Although the available human studies rarely reported effects that were regarded as being adverse, their suitability for detailed risk assessment is limited due to an insufficient focus on safety parameters apart from drug interactions, as well as due to the lack of investigation of the potentially adverse effects observed in animal studies and/or combined administration of piperine with other substances. Taken together, it appears advisable to consider the potential health risks related to intake of isolated piperine in bolus form, e.g., when using certain food supplements.

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Section: Interactions Of Piperine With Medicinal Products and Other Substancesmentioning

confidence: 99%

Safety Aspects of the Use of Isolated Piperine Ingested as a Bolus

Ziegenhagen

Heimberg

Lampen

et al. 2021

Foods

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“…The protease enzyme is responsible for the breaking of HIV encoded Gag-Pol protein in a host cell infected with a virus and leads to the formation of the mature infectious viral particles. [8][9][10] For the effective management of HIV-1 infection, darunavir is administered with other PIs. The co-administration of cytochrome P450 enzyme inhibitor (ritonavir) with darunavir, there is a significant decrease in the viral load and enhanced Analytical method development is a crucial step in product development and the validation of the developed methods as per the guidelines ensures the suitability of the method for intended purpose.…”

Section: Crasmentioning

confidence: 99%

Untitled

Kavitha¹

2020

AJP

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Objective: Darunavir ethanolate is the last United States Food and Drug Administration approved protease inhibitor (PI). The drug is used along with other PIs (ritonavir/cobicistat) for the effective management of human immunodeficiency virus (HIV) HIV-1 infection. Darunavir ethanolate exerts its action by binding noncompetitively to HIV protease enzyme. The main objective of the present research work was to develop a new profound and novel reverse-phase high-performance liquid chromatography (RP-HPLC) for the estimation of darunavir ethanolate. Methods: As per the guidelines of the Food and Drug Administration and International Council for harmonization, the method was validated. The HPLC analysis was performed on the waters 2695 equipped with symmetry C 18 column 3.5 µm, 150 mm × 4.6 mm, with a mixture of acetonitrile:0.1% phosphate buffer (50:50 V/V) as the mobile phase, at the flow rate of 1 ml/min. The total run time was 5 min and the detection was performed at the wavelength (λ) of 262 nm. Results: The retention time for darunavir ethanolate was found to be 2.269 min. The standard curves were obtained with R 2 0.9997 and linear at the concentration range of 8-120 µg/ml. The limit of quantitation and limit of detection for darunavir ethanolate were found to be 0.08 µg/ml and 0.8 µg/ml, respectively. The method's accuracy was tested by percentage recovery tests and found to be 100.3%. The results obtained were within the accepted standards for linearity, accuracy, precision, specificity, and robustness. Conclusion: The proposed RP-HPLC method can be applied for the routine analytical estimation of darunavir ethanolate in bulk and tablet formulations.

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