Doxylamine Succinate/Pyridoxine Hydrochloride

Cada, Dennis J.; Demaris, K M; Levien, Terri; Baker, Danial E.

doi:10.1310/hpj4809-762

Cited by 4 publications

(3 citation statements)

References 8 publications

(11 reference statements)

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“…Doxylamine and pyridoxine are both reported as being absorbed along the gastrointestinal tract, mainly in the jejunum [ 36 ]. To reproduce the potential gastrointestinal transit experience of Cariban ® in vitro, a 7-h dissolution profile at different pH conditions was performed.…”

Section: Resultsmentioning

confidence: 99%

“…There is barely probability of degradation in the acid environment of the stomach, as the stability of doxylamine and pyridoxine in acidic pH has been well established and reported [ 38 – 41 ]; furthermore, no significant degradation was observed in the Cariban ® dissolution profile since the actives are fully recovered at the end of the assay. Both doxylamine and pyridoxine are absorbed along the gastrointestinal tract, mainly in the jejunum [ 16 , 36 ]; therefore, early dissolution of doxylamine and pyridoxine opens the possibility to some absorption of the actives at the stomach and duodenal level [ 42 ], as described for similar prolonged-release formulations [ 43 ], as well as to speed up the absorption in the jejunum, as the actives reach the site already dissolved. The concept of a fast absorption derived from a fast release of the formulation is proven by the correlation between the in vitro dissolution and in vivo data that show appearance of the actives in plasma at early timepoints.…”

Section: Discussionmentioning

confidence: 99%

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Bioavailability of Cariban® Capsules: A Modified-Release Fixed-Dose Combination of Doxylamine and Pyridoxine to Relieve Nausea and Vomiting During Pregnancy

Saz-Leal,

Zamorano-Domínguez,

Frías

et al. 2023

Drugs R D

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Background Nausea and vomiting is a very prevalent condition during pregnancy. Combination of doxylamine and pyridoxine is placed as first-line pharmacological option for its treatment in most clinical guidelines. Among different release forms available, Cariban ® is a fixed-dose combination of doxylamine/pyridoxine 10/10 mg, formulated as modified-release capsules. Objectives In the present study, we aimed to characterize the bioavailability performance of Cariban ® in vitro and in vivo. Methods An in vitro dissolution test was performed to evaluate the release profile of Cariban ® , together with immediate- and delayed-release formulations available on the market. A single-center, single-dose, open-label bioavailability study following Cariban ® administration in 12 healthy adult female patients was carried out to explore the drug behavior in vivo (protocol NBR-002-13; EUDRA-CT 2013-005422-35). These data were additionally used to perform a computational pharmacokinetic simulation of the posology approved for this drug. Results Cariban ® capsules demonstrate a prolonged-release performance, with an early, gradual, and progressive release of both actives until reaching a complete dissolution after 4–5 h in solution. The pharmacokinetic features of these capsules show that doxylamine and pyridoxine metabolites are early absorbed, being all detectable in plasma within 1 h following oral administration. Computational pharmacokinetic simulation predicts that different posology provides distinct profiles of metabolites in plasma, with 1–1–2 (morning–midafternoon–night) being the one that concentrates higher plasma levels but lower dose dumping for 24 h. Conclusion Cariban ® behaves as a prolonged-release formulation, which correlates with rapid absorption and arising of the actives in the plasma, but also long-lasting and sustained bioavailability, especially when administered following the complete posology. These results would underlie its demonstrated efficacy to relieve nausea and vomiting of pregnancy (NVP) under clinical settings.

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Section: Resultsmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Bioavailability of Cariban® Capsules: A Modified-Release Fixed-Dose Combination of Doxylamine and Pyridoxine to Relieve Nausea and Vomiting During Pregnancy

Saz-Leal,

Zamorano-Domínguez,

Frías

et al. 2023

Drugs R D

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“…Однако, согласно недавнему анализу соответствующих клинических исследований, ингибирование лактации пиридоксином носит противоречивый и необоснованный характер и требует дальнейших изысканий [58]. Тем не менее, в ряде стран в качестве лекарственного средства при терапии тошноты и рвоты у беременных используют сочетание доксиламина и пиридоксин гидрохлорида [59][60][61].…”

Section: возможности терапевтического применения витамина вunclassified

Molecular Mechanisms Underlying Therapeutic Action of Vitamin B6

Zagubnaya

Nartsissov

2023

Farm. farmakol. (Pâtigorsk)

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The aim of the study was to analyze the molecular mechanisms that determine the possibility of using vitamin B6 in clinical practice for the correction of various pathological conditions.Materials and methods. Information retrieval (Scopus, PubMed) and library (eLibrary) databases were used as research tools. In some cases, the ResearchGate application was used for a semantic search. The analysis and generalization of the scientific literature on the topic of research, covering the period from 1989 to the present, has been carried out in the work.Results. It has been shown that all chemical forms of vitamin B6 are able to penetrate the membranes of most cells by free diffusion, while forming phosphorylated forms inside. Pyridoxal phosphate is a biologically important metabolite that is directly involved as a cofactor in a variety of intracellular reactions. Requirements for this cofactor depend on the age, sex and condition of the patient. Pregnancy and lactation play a special role in the consumption of vitamin B6. In most cases, a balanced diet will provide an acceptable level of this vitamin. At the same time, its deficiency leads to the development of a number of pathological conditions, including neurodegenerative diseases, inflammations and diabetes. Negative manifestations from the central nervous system are also possible with an excessive consumption of B6.Conclusion. Replenishment of the vitamin B6 level in case of its identified deficiency is a necessary condition for the successful treatment of the central nervous system diseases, diabetes and correction of patients’ immune status. At the same time, it is necessary to observe a balanced intake of this cofactor in order to avoid negative effects on metabolism in case of its excess.

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