Bioavailability Study of Propranolol Patch

Bioavailability is a measure of the rate and amount of drug or active ingredient that is absorbed by a drug product and available at the site of action. By definition, the bioavailability of a drug when administered intravenously is 100%. However, when a drug is given by a different route of administration, its overall bioavailability will decrease (since the drug is not completely absorbed and metabolized first pass effect) or may vary from patient to patient. Bioavailability is very important in pharmacokinetics. One of them is that bioavailability needs to be taken when calculating the doses for administering a drug other than by intravenous route. The aim of this study was to describe the bioavailability of propranolol in patch preparations. Propranolol is made in patch formulations using menthol, PEG, and various combinations of PVP and Eudragit. PVP and Eudragit each dissolved in alcohol and then mixed until homogeneous. Propranolol was dissolved with a menthol solution and then mixed into a solution of PVP and Eudragit. Finally, PEG is added to the solution and stirred until homogeneous and then poured into the patch mold. The patches produced were then measured for each patch and bioavailability assay. The patch formula produced can be used transdermally, but of the three formulas, the F3 formula with a ratio of PVP K30 and Eudragit RS-100 3: 7 gives the best results with a tmax of 2 hours, Cmax 79.33 µg / ml and AUC 49.07 µg hours / ml.

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Clot imaging characteristics predict first pass effect of aspiration—first approach to thrombectomy

Interventional Neuroradiology ◽

10.1177/15910199211019174 ◽

2021 ◽

pp. 159101992110191

Author(s):

Muhammad Waqas ◽

Weizhe Li ◽

Tatsat R Patel ◽

Felix Chin ◽

Vincent M Tutino ◽

...

Keyword(s):

Internal Carotid ◽

Validation Cohort ◽

Area Under The Curve ◽

Large Vessel Occlusion ◽

Vessel Occlusion ◽

First Pass Effect ◽

Imaging Characteristics ◽

First Pass ◽

Sensitivity Specificity ◽

Youden’S Index

Background The value of clot imaging in patients with emergent large vessel occlusion (ELVO) treated with thrombectomy is unknown. Methods We performed retrospective analysis of clot imaging (clot density, perviousness, length, diameter, distance to the internal carotid artery (ICA) terminus and angle of interaction (AOI) between clot and the aspiration catheter) of consecutive cases of middle cerebral artery (MCA) occlusion and its association with first pass effect (FPE, TICI 2c-3 after a first attempt). Results Patients ( n = 90 total) with FPE had shorter clot length (9.9 ± 4.5 mm vs. 11.7 ± 4.6 mm, P = 0.07), shorter distance from ICA terminus (11.0 ± 7.1 mm vs. 14.7 ± 9.8 mm, P = 0.048), higher perviousness (39.39 ± 29.5 vs 25.43 ± 17.6, P = 0.006) and larger AOI (153.6 ± 17.6 vs 140.3 ± 23.5, P = 0.004) compared to no-FPE patients. In multivariate analysis, distance from ICA terminus to clot ≤13.5 mm (odds ratio (OR) 11.05, 95% confidence interval (CI) 2.65–46.15, P = 0.001), clot length ≤9.9 mm (OR 7.34; 95% CI 1.8–29.96, P = 0.005), perviousness ≥ 19.9 (OR 2.54, 95% CI 0.84–7.6, P = 0.09) and AOI ≥ 137°^ (OR 6.8, 95% CI 1.55–29.8, P = 0.011) were independent predictors of FPE. The optimal cut off derived using Youden’s index was 6.5. The area under the curve of a score predictive of FPE success was 0.816 (0.728–0.904, P < 0.001). In a validation cohort ( n = 30), sensitivity, specificity, positive and negative predictive value of a score of 6–10 were 72.7%, 73.6%, 61.5% and 82.3%. Conclusions Clot imaging predicts the likelihood of achieving FPE in patients with MCA ELVO treated with the aspiration-first approach.

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Clinical impact of the first pass effect on clinical outcomes in patients with near or complete recanalization during mechanical thrombectomy for large vessel ischemic stroke

Journal of Neuroimaging ◽

10.1111/jon.12864 ◽

2021 ◽

Author(s):

Muhammad Zeeshan Memon ◽

David Daniel ◽

Mohammad Rauf A. Chaudhry ◽

Manjot Grewal ◽

Vasu Saini ◽

...

Keyword(s):

Ischemic Stroke ◽

Clinical Outcomes ◽

Mechanical Thrombectomy ◽

Clinical Impact ◽

Large Vessel ◽

First Pass Effect ◽

First Pass

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First-Pass Effect in Basilar Artery Occlusions: Insights From the Endovascular Treatment of Ischemic Stroke Registry

Stroke ◽

10.1161/strokeaha.120.030237 ◽

2021 ◽

Author(s):

Mathilde Aubertin ◽

David Weisenburger-Lile ◽

Benjamin Gory ◽

Sébastien Richard ◽

Raphael Blanc ◽

...

Keyword(s):

Basilar Artery ◽

Rescue Therapy ◽

Strong Predictor ◽

Artery Occlusion ◽

Basilar Artery Occlusion ◽

Anterior Circulation ◽

Unique Identifier ◽

First Pass Effect ◽

Improved Outcomes ◽

First Pass

Background and Purpose: In the settings of thrombectomy, the first-pass effect (FPE), defined by a complete recanalization after one pass with no rescue therapy, has been shown to be associated with an improved outcome. As this phenomenon has been predominantly described in anterior circulation strokes, we aimed to study the prevalence, outcomes, and predictors of FPE in patients with a basilar artery occlusion. Methods: From a prospective multicentric registry, we collected the data of all consecutive basilar artery occlusion patients who underwent thrombectomy and compared the outcomes of patients who achieved FPE and those who did not. We also compared FPE patients with those who achieved a complete recanalization with >1 pass. Finally, a multivariate analysis was performed to determine the predictors of FPE. Results: Data from 280 patients were analyzed in our study, including 84 of 280 patients (30%) with an atheromatous etiology. An FPE was achieved in 93 patients (33.2%), with a significantly higher proportion of good outcomes (modified Rankin Scale score 0-2 at 3 months) and lower mortality than non-FPE patients. An FPE was also associated with improved outcomes compared with patients who went on to have full recanalization with >1 pass. Contact aspiration as first-line strategy was a strong predictor of FPE, whereas baseline antiplatelets and atheromatous etiology were negative predictors. Conclusions: In our study, an FPE was achieved in approximately one-third of patients with a basilar artery occlusion and was associated with improved outcomes. More research is needed to improve devices and techniques to increase the incidence of FPE. Registration: URL: https://www.clinicaltrials.gov ; Unique identifier: NCT03776877.

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