China
Africa
Explore chapters and articles related to this topic
Granulation of Poorly Water-Soluble Drugs
Published in Dilip M. Parikh, Handbook of Pharmaceutical Granulation Technology, 2021
Albert W. Brzeczko, Firas El Saleh, Hibreniguss Terefe
Both HPC and HPMC exhibit good solubility in a range of solvents including cold water. The average MW of the HPCs ranges from 37,000 to 1,150,000. Studies with flurbiprofen showed that the dissolution rate was improved as low MW HPC was used in the solid dispersion [114]. HPMCs have an average MW in a range from 10,000 to 1,500,000, and their glass transition temperatures are as high as 170°C to 180°C. Studies with tacrolimus compared the dissolution profiles of solid dispersions having HPMC, PVP, and PEG as a carriers [115]. Significant increases in dissolution rates were confirmed for the solid dispersions formulated with all these polymers. However, severe precipitation was observed for PVP- and PEG-based solid dispersions due to supersaturation. Though all three polymers were shown equally effective in dissolution rate improvement, their capabilities for maintaining supersaturation were significantly different and the rank order was HPMC > PVP > PEG. Studies with albendazole, a poorly water-soluble compound, showed that the release rate and bioavailability could be improved through the preparation of solid dispersion in HPMC [116]. Other drugs that exhibit faster release from solid dispersion in HPMC include poorly soluble weak acids nilvadipine and benidipine [117,118].
Hypertension and the kidney
Published in H. Gavras, The Year in Hypertension 2004, 2004
BACKGROUND. Although calcium antagonists are used as first-line antihypertensive agents, controversy abounds regarding their renal microvascular effects. Since calcium antagonists elicit a predominant vasodilatation of the afferent arteriole, they might ostensibly aggravate glomerular hypertension. Recently, novel types of calcium antagonists have been developed, some of which are reported to dilate efferent as well as afferent arterioles. This review attempted to characterize the renal microvascular action of calcium antagonists, and evaluated the consequences of renal injury following the treatment with these antagonists. In contrast to the predominant action on afferent arterioles of conventional calcium antagonists (e.g. nifedipine, nicardipine, amlodipine, and diltiazem), novel antagonists (e.g. manidipine, nilvadipine, benidipine, and efonidipine) potently dilated both afferent and efferent arterioles. The vasodilator action on efferent arterioles appears to be mediated in part by the blockade of T-type calcium channels, particularly through the inhibition of the intracellular calcium release mechanism. The comparison of the anti-proteinuric action of calcium antagonists in subtotally nephrectomized rats showed that efonidipine and enalapril, both possessing vasodilator action on efferent arterioles, exerted more prominent action than other calcium antagonists. Finally, in patients with chronic renal disease, a 48-week treatment with efonidipine reduced proteinuria, and this effect was seen even when the mean arterial blood pressure failed to fall below 100 mmHg. In conclusion, although calcium antagonists potently inhibit afferent arteriolar constriction, efferent arteriolar responses to these agents vary, depending on the types of calcium antagonists used. The divergent actions of these agents on the efferent arteriole may alter glomerular haemodynamics differently, and could affect the final outcome of underlying renal diseases.
An antihypertensive agent benidipine is an effective neuroprotective and antiepileptic agent: an experimental rat study
Published in Neurological Research, 2021
Mehmet Nuri Koçak, Remzi Arslan, Abdulmecit Albayrak, Erdal Tekin, Mustafa Bayraktar, Muhammet Çelik, Zülküf Kaya, Hüseyin Bekmez, Taha Tavaci
Although calcium channel blockers are used in the treatment of epilepsy, the antiepileptic effectiveness of benidipine, which is effective on all calcium channels, has not been investigated before. Benidipine has been used for years for anti-hypertensive purposes in humans and is a safe agent with a low incidence of side effects. In addition to seizure control in epilepsy treatment, neuroprotective activity should be included in treatment planning. In this study, the antiepileptic and neuroprotective efficacy of benidipine was investigated for the first time in the literature. As a result of our study, it was determined that benidipine had antiepileptic and neuroprotective activity. It seems possible that bendipine will enter medical use as a new drug in the treatment of epilepsy because of its low incidence of side effects and its cost-effectiveness.
Development and optimization of drug-loaded nanoemulsion system by phase inversion temperature (PIT) method using Box–Behnken design
Published in Drug Development and Industrial Pharmacy, 2021
Manish Kumar, Ram Singh Bishnoi, Ajay Kumar Shukla, Chandra Prakash Jain
In this study, we have used the PIT method to produce a stable and optimized drug-loaded nanoemulsion system. As per our literature search, no previous research has been reported to use the PIT method to developed a drug-loaded nanoemulsion system. For the development of an optimized nanoemulsion system and to study the effects of formulation variables on the characteristics of the developed nanoemulsion system, we have used response surface methodology (Box–Behnken design). The benidipine was used as a modal drug for the formulation of the drug-loaded nanoemulsion system. Benidipine is used as an anti-anginal and antihypertensive agent. It belongs to the calcium channel blockers category of an anti-hypertensive agent. Benidipine is a highly lipophilic drug. In the literature partition coefficient (log PO/W) of benidipine was reported as 3.79 (by shake flask method) and 4.61(measured with liquid chromatography). The high log p value indicating the extreme lipophilic nature of the drug. Its bioavailability is also strongly affected by the pH of gastric fluid [18–20].
Edaravone and benidipine protect myocardial damage by regulating mitochondrial stress, apoptosis signalling and cardiac biomarkers against doxorubicin-induced cardiotoxicity
Published in Clinical and Experimental Hypertension, 2020
Md Quamrul Hassan, Md Sayeed Akhtar, Obaid Afzal, Ibraheem Hussain, Mohd Akhtar, Syed Ehtaishamul Haque, Abul Kalam Najmi
Table 4 demonstrates the TGF-β level in serum of different experimental groups. In DOX-treated rats (toxic control), increased in serum level of TGF-β (P < 0.01) was observed in comparison to normal control group. Pre-treatment with edaravone (10 mg/kg/day), and combination of edaravone (3 mg/kg/day) with benidipine (3 µg/kg/day) showed significant (P < 0.01) decreased level of TGF-β in comparison to the toxic control group. Whereas, less pronounced effect (P < 0.05) was observed with benidipine (10 mg/kg/day) in comparison to the toxic control group. Non-significant change in TGF-β was observed in rats treated with edaravone and benidipine (per se groups) as compared to the normal control group.