The nasal route for RS-93522 (I) appears to be as effective as the i.v. route.The onset of absorption was rapid and the drug plasma levels after nasal administration were similar to those following i.v. administration.Excellent nasal bioavailability and rapid absorption were observedTherefore, therapeutic treatment with this compound via nasal administration is a viable approach and offers an alternative to oral administration where ineffective and variable absorption is a problem.

01 Dec 1988·Journal of Molecular and Cellular CardiologyQ2 · MEDICINE

A dihydropyridine calcium channel blocker with phosphodiesterase inhibitory activity: Effects on cultured vascular smooth muscle and cultured heart cells

Q2 · MEDICINE

Article

Author: Mary Chiu ; Thomas W. Smith ; Mary Ann M. Dionne ; James D. Marsh

To define the cellular mechanism of action of a dihydropyridine Ca channel antagonist in an experimental model system devoid of neural influences and reflex effects, we studied the actions of RS93522 on cultured vascular smooth muscle cells and on cultured chick embryo ventricular cells. 45Ca uptake by monolayer cultures of vascular smooth muscle cells was inhibited in a concentration-dependent manner. The IC50 for this effect was 10 nM, similar to that for nifedipine (7 nM) in the same system. 10(-6) M RS93522 inhibited 45Ca uptake more fully than 10(-6) M nifedipine (P less than 0.05). Using an optical-video system, the effect of RS93522 on amplitude of contraction of spontaneously beating cultured ventricular cells was studied. Amplitude of contraction was inhibited with IC50 = 7.9 x 10(-8)M. 45Ca uptake in myocytes was depressed by 15% at 5 min. RS93522 had the additional property of inhibiting phosphodiesterase activity in myocardial homogenates with IC50 = 1.6 x 10(-5)M; the potency and efficacy of phosphodiesterase inhibition was similar to that for milrinone in the same system. As expected of Ca channel antagonists, it has a negative inotropic effect on cultured myocardial cells. The compound also has phosphodiesterase inhibitory activity that possibly may potentiate vasodilatation and ameliorate, in part, negative inotropic effects. Thus, RS93522 has two distinct pharmacodynamic effects in myocytes and is a potent calcium channel blocker.

01 Jan 1988·Pharmaceutical ResearchQ3 · MEDICINE

In vitro and in vivo studies evaluating a liposome system for drug solubilization.

Q3 · MEDICINE

Article

Author: Philip L. Feigner ; John Whatley ; Roger Cherng-Chi Fu ; Jeffrey S. Fleitman ; Deborah M. Lidgate

A liposome system was developed which demonstrates suitability as an intravenous drug carrier for a lipophilic drug compound (RS-93522, a dihydropyridine CA2+ channel blocker). An aqueous phospholipid suspension was employed as a nontoxic solubilizing vehicle for this drug. The liposome formulation, composed of a 3% mixture of dioleoylphosphatidylcholine and dioleoylphosphatidylglycerol, produced a physically and chemically stable preparation which solubilized the lipophilic drug compound at a concentration 500 times above its intrinsic aqueous solubility. Characterizing the liposome-drug system by gel filtration chromatography showed that the drug comigrated with the lipid constituents of the liposome. Further in vitro studies established that the liposome-RS-93522 formulation allowed for rapid and complete transfer of the drug from the liposome to bind with albumin when added to human serum. In vivo studies with rats were performed in which the pharmacokinetics of the liposomal-RS-93522 system were compared to those of a cosolvent-solubilized RS-93522 solution. This study showed that the pharmacokinetic profiles of the two solutions were identical. All the evidence indicates that a liposome formulation of this type does not alter the distribution of the drug in serum and is, therefore, not likely to affect the intrinsic pharmacological or toxicological parameters of the drug relative to the conventional solvent/excipient-containing formulation. This liposome system demonstrates utility as a biocompatible, nontoxic drug delivery vehicle.

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Indication	Highest Phase	Country/Location	Organization	Date
Hypertension	Phase 1	-	F. Hoffmann-La Roche Ltd.	-

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