Solubility of Nifedipine by Shake Flask UV-Spectrometry; Review of Safety Concerns in Pregnancy

Nifedipine is chemically dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, a dihydropyridine derivative used frequently as anti-hypertensive. It is a L- type calcium channel blocker (CCB). Few analogical discrepancies were found between Nifedipine’s clinical output report and chemical analysis of solubility. The ambition of this research is to conduct a re-check and proper quantification of partition co-efficient (logP) of Nifedipine and clarify the discrepancy and rectify if any mistake has been done in recent past. The method used is the “gold standard” shake-flask method followed by analysis through UV-scpectrophotmetry.

Application of Hantzsch reaction for sensitive determination of eflornithine in cream, plasma and urine samples

Eflornithine (EFN) is an anti- Trypanosoma brucei agent for the medication of sleeping sickness and widely distributed for the treatment of hirsutism (unwanted facial hair in women). The presented work demonstrates a comprehensive analytical approach for the spectrofluorometric determination of EFN in commercial cream samples and various biological samples. The proposed method is based on the formation of a highly yellow–green fluorescence dihydropyridine derivative after the interaction between EFN and acetylacetone/formaldehyde reagent in a slightly acidic medium. Furthermore, the optimal variables such as reagent volumes, pH of the medium, heating time, buffer volume, heating temperature and diluting solvent were carefully selected to achieve the maximum fluorescence activity. The fluorescence activity for the formed derivative was measured at λ emission = 477 nm after λ excitation = 418 nm. Concerning linearity, accuracy, sensitivity, precision and robustness, the presented method was validated and verified according to ICH guidelines. Moreover, the proposed work offered a selective determination for EFN in various brands of pharmaceutical cream without any interference from excipients. Eventually, the current approach was assured to be successful in the estimation of EFN in urine and plasma samples with acceptable recovery results.

SEARCH FOR NOVEL ANTI-FERTILITY AGENT BY MONITORING IN VITRO METABOLIC INHIBITION, CELL MOTILITY AND CELLULAR INTERACTIONS OF NIFEDIPINE ANALOGUES

Current family planning measures predominantly target a female clientele, with relatively few significant developments in male fertility regulation. At present, only effective methods for contraception in men are those that prevent sperm transport, such as condoms and vasectomy. Thus, in an attempt to synthesize non-hormonal, safe, reversible and oral male contraceptive, we have used nifedipine as a prototype molecule. Nifedipine is a calcium channel blocker and popular anti-hypertensive drug. Its reversible anti-fertility effect is a well-known side effect. In order to develop male oral contraceptive, we have synthesized four analogues; m-hydroxy (D5), m-chloro (D6), p-nitro (D7), p-methoxy (D8) aryl 1, 4-dihydropyridine derivative of nifedipine and monitored their effect on sperm motility and metabolic activity. To highlight their mechanism of action on sperm function through membrane interaction, we have studied their molecular level interactions with model membrane using NMR and DSC technique. One of the synthesized analogues (D5) showed promising results.

A New Generation of Dihydropyridine Calcium Channel Blockers: Photostabilization of Liquid Formulations Using Nonionic Surfactants

: The stability profile of a new 1,4-dihydropyridine derivative (DHP), representative of a series with a hexahydroquinoline ring, was studied to design light-stable liquid formulations. This molecule, named M3, has been shown among the analogs to have a high capacity to block both L- and T-type calcium channels. The ethanol solution of the drug was subjected to a photodegradation test, in accordance with standard rules. The concentrations of the drug and its byproducts were estimated using multivariate curve resolution, applied to the spectral data collected during the test. The improvement of both the photostability and water solubility of M3 was investigated by adding the surfactant polysorbate 20 in a 1:5 ratio to aqueous solutions of the drug. These formulations were exposed to stressing light in containers of bleu polyethylene terephthalate (PET), amber PET, and covered amber PET. The best results were obtained when using the covered amber PET container, reaching a degradation percentage of the drug less than 5% after 12 h under an irradiance power of 450 W/m2. The stability of the compound was compared to that of nimodipine (NIM) under the same conditions.