Pharmaceutical development for transdermal dosage forms of nifedipine: justification of the choice and specificity of the action

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Abstract

Background. Present day in medicine can be assessed as an active period of the fight against cardiovascular diseases. This group of diseases cannot be considered obsolete in any way, and even taking into account the emerging new pathology – coronavirus infection – cardiovascular diseases have consolidated their dominant position. Among the drugs used for appropriate pharmacotherapy, stands out nifedipine (1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridindicarboxylic acid dimethyl ether) – a drug that can inhibit the flow of calcium into the cardiomyocytes of vascular smooth muscle cells. The drug has been on the domestic pharmaceutical market for quite a long time, but it is still in demand. However, nifedipine has quite pronounced side effects, including those associated with its oral administration – nausea caused by irritation of the gastrointestinal tract, rarely gum hyperplasia. And at the same time, the main modern dosage form of nifedipine is tablets. Therefore, expanding the range of its dosage forms is an urgent issue. Moreover, well-chosen dosage forms reduce the side effect of the drug. This is especially true for extended versions. So pharmaceutical development in relation to the creation of original dosage forms of nifedipine is quite appropriate.

Aim. Determination of the possibility of absorption of nifedipine from the proposed dosage forms – transdermal patch and transdermal gel.

Materials and methods. To determine nifedipine in rat blood plasma samples, high-performance liquid chromatography was used (chromatograph “Millichrome A-02” (Institute of Chromatography “EcoNova”, LLC, Russia).

Results. Chromatograms of blood plasma samples of all animals on whose skin a transdermal gel or patch was applied revealed a peak coinciding in retention time with the peak of the standard sample of nifedipine.

Conclusion. The possibility of penetration of nifedipine from the patch and transdermal gel through intact animal skin has been confirmed.

About the authors

V. V. Tokaev

Pyatigorsk Medical and Pharmaceutical Institute – Branch of the Volga State Medical University of the Ministry of Health of Russia

ORCID iD: 0000-0002-7133-8258

11 Kalinina Ave., 357532 Pyatigorsk, Russia

Russian Federation

E. F. Stepanova

Pyatigorsk Medical and Pharmaceutical Institute – Branch of the Volga State Medical University of the Ministry of Health of Russia

Author for correspondence.
Email: efstepanova@yandex.ru
ORCID iD: 0000-0002-4082-3330

Eleonora Fedorovna Stepanova

11 Kalinina Ave., 357532 Pyatigorsk, Russia

Russian Federation

M. S. Makieva

K.L. Khetagurov North Ossetian State University

ORCID iD: 0000-0002-2232-5549

44–46 Vatutina St., Vladikavkaz 362025, Republic of North Ossetia – Alania, Russia

Russian Federation

Yu. A. Morozov

K.L. Khetagurov North Ossetian State University

ORCID iD: 0000-0002-6260-1341

44–46 Vatutina St., Vladikavkaz 362025, Republic of North Ossetia – Alania, Russia

Russian Federation

D. I. Pozdnyakov

Pyatigorsk Medical and Pharmaceutical Institute – Branch of the Volga State Medical University of the Ministry of Health of Russia

ORCID iD: 0000-0002-5595-8182

11 Kalinina Ave., 357532 Pyatigorsk, Russia

Russian Federation

D. I. Gagloeva

K.L. Khetagurov North Ossetian State University

ORCID iD: 0000-0002-7106-7582

44–46 Vatutina St., Vladikavkaz 362025, Republic of North Ossetia – Alania, Russia

Russian Federation

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