Effect of Polymers and Permeation Enhancers in the Release of Quetiapine Fumarate Transdermal Patch through the Dialysis Membrane.

Quetiapine Fumarate is potent, and the daily therapeutic dose can be delivered easily across the skin with the help of permeation enhancers. Quetiapine Fumarate-loaded transdermal patches were prepared by solvent evaporation technique. Various formulation parameters, excipients, and their combinations were optimized to get thin, translucent, smooth, stable, and high permeable character patches. A total number of 10 formulations were prepared. All formulations were subjected to various physicochemical evaluations. Three different formulations were prepared and F1, F2, and F3. Various physicochemical studies were carried out and found no significant difference between the three batches. The in vitro release study showed 74.29%, 82.73%, and 77.27%, respectively, up to 24 h. From the results, F2 has been selected as an optimized formulation and evaluated for skin irritation test. The results revealed that there is no irritation produced. The stability study results showed that there is no significant change from its initial nature till the period of three months in both temperatures. Quetiapine Fumarate Transdermal Patch F2 has achieved the goal of extended-release, cost-effectiveness, lowering the dose and frequency of drug administration, and thus may improve patient compliance.

Development and Evaluation of Naproxen Sodium Gel Using Piper cubeba for Enhanced Transdermal Drug Delivery and Therapeutic Facilitation.

BACKGROUND: The absorption of drug through skin avoids many side effects of oral route like gastric irritation, nausea, systemic toxicity etc and thus improves patient compliance. Naproxen sodium (NPRS) is one of the potent NSAID agents. OBJECTIVE: The present study was aimed to develop and evaluate the gel formulation containing NPRS for transdermal drug delivery reducing the side effects and improving patient compliance. The patents on topical delivery of NSAIDS (US 9012402 B1, US 9072659 B2, US 20150258196 A1) and patents indicating use of herbal penetration enhancers (US 20100273746A1, WO 2005009510 A2, US 6004969 A) helped in selecting the drug, excipients. METHOD: Current protocol employs various extracts of Piper cubeba fruit to evaluate its role in absorption of NPRS. Various batches containing 1% NPRS and varying concentrations of synthetic permeation enhancers or the extracts were formulated in carbopol gel. Gel was evaluated for parameters like organoleptic parameters, pH, viscosity and spreadability. An ex-vivo percutaneous absorption of NPRS from gel was investigated and compared with best performing synthetic enhancer, transcutol P (TP). RESULT: The batch containing 2% n-hexane extract (NHE) of Piper cubeba showed higher permeation than TP and Chloroform (CE), Methanolic (ME) and aqueous (AE) extracts as well. It showed improved % cumulative release (85.09%) and flux (278.61µg/cm2.h), as compared to TP and other extracts. Histopathology indicated the formulation safer as compared to that with synthetic enhancer. CONCLUSION: It suggests P. cubeba as effective and safer tool for transdermal delivery and acts as therapeutic facilitator for naproxen. GC-MS analysis indicates lignans & terpenes in NHE to which this permeation enhancement activity may be attributed.

Simultaneous determination of rosuvastatin and amlodipine in human plasma using tandem mass spectrometry: Application to disposition kinetics.

The liquid chromatography-tandem mass spectrometric assay method for the simultaneous determination of rosuvastatin and amlodipine in human plasma using deuterated analogs as internal standards has been developed and validated. The analytes were extracted from 100 µL aliquots of human plasma via liquid-liquid extraction using a mixture of ethyl acetate and n-hexane (80:20, v/v) as an extraction solvent. The optimized mobile phase was composed of 0.1% formic acid in 5 mM ammonium acetate, methanol, and acetonitrile (20:20:60, v/v/v) and delivered at a flow rate of 0.75 mL/min. The calibration curve obtained was linear (R (2) â©¾ 0.999) over the concentration range of 0.52-51.77 ng/mL for rosuvastatin and 0.10-10.07 ng/mL for amlodipine. A sample turnover rate of less than 2.5 min makes it an attractive procedure in high-throughput bioanalysis of rosuvastatin and amlodipine. The present method was found to be applicable to clinical studies and the results were authenticated by incurred sample reanalysis.