β1-adrenergic receptor antagonists(Beta-1 adrenergic receptor antagonists), β2-adrenergic receptor antagonists(Beta-2 adrenergic receptor antagonists), β3-adrenergic receptor antagonists(Beta-3 adrenergic receptor antagonists)

Therapeutic Areas

Nervous System DiseasesCardiovascular DiseasesOther Diseases

Active Indication-

Inactive Indication

Angina PectorisAnxietyArrhythmias, Cardiac+ [1]

Originator Organization

Novartis Pharmaceuticals Corp.

Active Organization-

Inactive Organization

Novartis Pharmaceuticals Corp.

Drug Highest PhaseWithdrawn

First Approval Date

US (28 Dec 1983),

Angina PectorisAnxietyArrhythmias, Cardiac+ [1]

Regulation-

Structure

Molecular FormulaC15H24ClNO3

InChIKeyCOAJXCLTPGGDAJ-UHFFFAOYSA-N

CAS Registry6452-73-9

100 Clinical Results associated with Oxprenolol Hydrochloride

100 Translational Medicine associated with Oxprenolol Hydrochloride

100 Patents (Medical) associated with Oxprenolol Hydrochloride

116

Literatures (Medical) associated with Oxprenolol Hydrochloride

01 Jan 2003·Journal of microencapsulationQ4 · MEDICINE

Oxprenolol-loaded bioadhesive microspheres: preparation and in vitro / in vivo characterization

Q4 · MEDICINE

Article

Author: S. E. Leucuta ; M. Preda

Biologically adhesive delivery systems offer important advantages over conventional drug-delivery systems. In this paper, microspheres intended as a sustained release carrier for oral or nasal administration have been prepared by associating a known bioadhesive polymer, poly(acrylic acid), in gelatin microspheres. A model drug oxprenolol hydrochloride was chosen. It was found that some of the formulation variables can influence the characteristics of the beads in a controlled manner. The internal structure of the microspheres studied by X-ray diffraction, thermal analysis and optical microscopy showed the absence of drug crystals in microspheres and a lowering in the glass transition temperature. The dynamic swelling of the beads obeyed the square root of time and a shift from the diffusional to the relaxational process dependent on the content of poly(acrylic acid) in gelatin microspheres was observed. As expected, drug release from gelatin/poly(acrylic acid) microspheres was influenced by the poly(acrylic acid) content in beads, by the particle size of microspheres and by the pH of the medium. The mechanism of release was analysed by applying the empirical exponential equation and by calculation of the approximate contribution of the diffusional and relaxational mechanisms to the anomalous release process by fitting the data to the coupled Fickian/Case II equation. In vitro and in vivo experiments in rats showed good adhesive characteristics of the gelatin/poly(acrylic acid) microspheres, which were greater if the poly(acrylic acid) content was greater. A significant retardation in gastric and intestinal emptying time of the beads was observed. This was also suggested by the bioavailability of the model drug after intragastric and intranasal administration of the microspheres. The pharmacokinetic parameters after microsphere administration were more appropriate to a slow release drug-delivery system. The work suggests the potential of this pharmaceutical delivery system as an alternative controlled-release dosage form, either for oral or nasal administration.

01 Jan 1999·Journal of biomaterials science. Polymer editionQ3 · ENGINEERING & TECHNOLOGY

FTIR spectroscopic investigation and modeling of solute / polymer interactions in the hydrated state

Q3 · ENGINEERING & TECHNOLOGY

Article

Author: Mary T. Am Ende ; Nikolaos A. Peppas

Attenuated total reflectance infrared spectroscopy was used to investigate possible interactions during transport of oxprenolol x HCl, bovine serum albumin, alpha-chymotrypsin, and fibrinogen through poly(acrylic acid) and its random copolymeric gels. Carbonyl and carboxylate ion peak shifts were used to identify drug/gel binding due to electrostatic and hydrogen bond interactions between the polymer carrier and the drugs tested. These findings were used to interpret the decrease in calculated diffusion coefficients of drugs diffusing through these gels and the associated hindering of drug transport. A model was developed to analyze this transport process as a function of the binding heat of the drug with the polymer.

01 Jan 1999·Pharmaceutical researchQ3 · MEDICINE

Gastropods as an evaluation tool for screening the irritating potency of absorption enhancers and drugs.

Q3 · MEDICINE

Article

Author: Els Adriaens ; Jean Paul Remon

PURPOSE:

The objective of this study was to develop a simple alternative test using naked snails (slugs) for screening the irritating potency of chemicals on mucosal surfaces.

METHODS:

The effect of various absorption enhancers and two beta-blocking agents on the mucosal tissue was determined from the total protein and lactate dehydrogenase released from the foot mucosa after treatment. Additionally, mucus production and reduction in body weight of the slugs caused by the treatment were measured.

RESULTS:

According to the effects on the mucosal epithelium of the slugs the following rank order of increasing toxicity was established: PBS, HP-beta-CD (5%), beta-CD (1.8%) and oxprenolol hydrochloride (1%) < DDPC (1%) < STDHF (1%) < BAC (1%), SDC (1%) and propranolol hydrochloride (1%). The results of the present study are in agreement with other studies using the same compounds on other models.

CONCLUSIONS:

The results of this study indicated the mucosa of slugs can serve as a primary screening tool for the evaluation of chemicals on mucosal surfaces. By simply measuring mucus production and weight loss reliable toxicity information can be obtained. This demonstrates rapid screening tests can be carried out using simple toxicity endpoints.

100 Deals associated with Oxprenolol Hydrochloride

External Link

KEGG	Wiki	ATC	Drug Bank
D01806	Oxprenolol Hydrochloride	C07AA02	DBSALT001070

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Angina Pectoris	US	Novartis Pharmaceuticals Corp.	28 Dec 1983
Anxiety	US	Novartis Pharmaceuticals Corp.	28 Dec 1983
Arrhythmias, Cardiac	US	Novartis Pharmaceuticals Corp.	28 Dec 1983
Hypertension	US	Novartis Pharmaceuticals Corp.	28 Dec 1983

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