Glibenclamide transdermal patches: Physicochemical, pharmacodynamic, and pharmacokinetic evaluations

Mutalik, Srinivas; Udupa, N.

doi:10.1002/jps.20058

Cited by 132 publications

(85 citation statements)

References 25 publications

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“…This may be due to the bypass of hepatic first-pass effects. These results are in agreement with the findings reported earlier (21,22). Upon statistical evaluation (two-way ANOVA), a significant difference was observed between the test products (p < 0.01) but not within the test products for AUC (0)(1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12) , AUC (0-24) , AUC (0-∞) , t 1/2, K el and MRT values.…”

Section: In Vivo Studies In Rabbitssupporting

confidence: 94%

Development of matrix controlled transdermal delivery systems of pentazocine: In vitro/in vivo performance

Verma

Chandak²

2009

Acta Pharmaceutica

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Transdermal drug delivery system is being extensively investigated as a viable alternative to drug delivery with improved bioavailability. It offers many advantages over conventional administration such as enhanced efficacy, increased safety, and greater convenience and improved patient compliance. Transdermal route permits the use of a relatively potent drug with minimal risk of systemic toxicity and avoids gastrointestinal degradation and hepatic first-pass metabolism (1-3). A number of therapeutic agents, including antihypertensive, antianginal, antihistaminic, anti-inflammatory, analgesic, The present study aimed to develop hydroxypropyl methylcellulose based transdermal delivery of pentazocine.In formulations containing lower proportions of polymer, the drug released followed the Higuchi kinetics while, with an increase in polymer content, it followed the zero-order release kinetics. Release exponent (n) values imply that the release of pentazocine from matrices was non-Fickian. FT-IR, DSC and XRD studies indicated no interaction between drug and polymer. The in vitro dissolution rate constant, dissolution half-life and pharmacokinetic parameters (C max , t max , AUC (s) , t 1/2, K el , and MRT) were evaluated statistically by two-way ANOVA. A significant difference was observed between but not within the tested products. Statistically, a good correlation was found between per cent of drug absorbed from patches vs. C max and AUC (s) . A good correlation was also observed when per cent drug released was correlated with the blood drug concentration obtained at the same time point. The results of this study indicate that the polymeric matrix films of pentazocine hold potential for transdermal drug delivery.Keywords: pentazocine, transdermal drug delivery, Cygnus' sandwich patch holder, in vitro characterization, in vivo evaluation * Correspondence; e-mail: prpverma275730@yahoo.com Unauthenticated Download Date | 8/28/18 7:56 PM and anti-arthritic drugs, are being investigated and developed for the transdermal therapeutic system either for academic research or for commercial purposes (3, 4). The present work is aimed at developing a matrix-dispersion type transdermal drug delivery of pentazocine.Pentazocine (PTZ), a benzomorphan derivative, is an opioid analgesic that has mixed opioid agonist and antagonist actions. It is considered to be a partial agonist or weak antagonist at the m-receptor and a k-receptor agonist. Pentazocine is used for relief of moderate to severe pain. Oral administration of PTZ has the disadvantage of low bioavailability (about 18-22 %) due to extensive first-pass metabolism (5-7). In addition, PTZ has a short half-life of 2-4 h and requires frequent dosing in order to maintain the optimal therapeutic concentration. Repeated injections over long periods may cause fibrotic changes in the skin and muscular tissue. Low molecular mass (285.4), suitable pK a values of 8.5 and 10, log P (octanol/phosphate buffer pH 7.4) of 2.0 and low oral bioavailability provide a rationale for developing a...

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Section: In Vivo Studies In Rabbitssupporting

confidence: 94%

Development of matrix controlled transdermal delivery systems of pentazocine: In vitro/in vivo performance

Verma

Chandak²

2009

Acta Pharmaceutica

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“…Physicochemical properties such as physical appearance, thickness, weight variation [12], folding endurance [14], moisture uptake [15], were determined on developed patches.…”

Section: Evaluation Of Transdermal Patches Of Imipramine Hydrochloridementioning

confidence: 99%

Design, Formulation and in Vitro Drug Release From Transdermal Patches Containing Imipramine Hydrochloride as Model Drug

Hardainiyan

Kumar

Nandy

et al. 2017

Int J Pharm Pharm Sci

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Objective: The aim of the present investigation was to form matrix type transdermal patches containing imipramine hydrochloride were prepared using two polymers by solvent evaporation technique to minimise the dose of the drug for lesser side effect and increase the bioavailability of a drug. Methods:In the present study, drug loaded matrix type transdermal films of imipramine hydrochloride were prepared by the solvent evaporation method with the help of polymers along with polyethene glycol (PEG) 400 was used as plasticizer and dimethyl sulfoxide (DMSO) was used as penetration enhancer. Drug-polymer interactions determine by FTIR and a standard calibration curve of imipramine hydrochloride was determined by using UV estimation. Results:The formulated transdermal patch by using PVP K-30, HPMC K100M showed good physical properties. All prepared formulations indicated good physical stability. The formulation F-1 gave the most suitable transdermal film with all desirable physicochemical properties. The thickness of the patches was varied from 0.263±0.67 mm to 0.301±0.61 mm, uniformity of patches showed that patches prepared by solvent evaporation while low standard deviation values ensued by thickness measurements of the film, and weights ranged between 50.5±0.75 mg and 52.15±2.15 mg, which indicates that different batches patch weights, were comparatively similar. Folding endurance was found to be>200 that is satisfactory for the patches, drug content was found to be 5.33±0.14 mg to 5.57±0.095 mg. In vitro, drug permeation studies of formulations were performed by using K-C diffusion cells using abdomen skin of the albino rat. The results were best in in-vitro skin permeation through rat skin as compared to all other formulations prepared with a hydrophilic polymer containing permeation enhancer. The formulation, F1 is considered as the best formulation, since it shows maximum in vitro drug release as 84.71±3.07 % at 24 h. The drug release kinetics studies showed that the majority of formulations were governed by Higuchi model and mechanism of release was non-Fickian mediated. Conclusion:In conclusion, controlled release transdermal drug delivery system (TDDS) patches of imipramine hydrochloride can be prepared using the polymer combinations, with plasticizer and enhancer. The release rate of drug through patched increased simultaneously as the concentration of hydrophilic polymer was increased. However, the mechanism of drug release of all formulations was non-Fickian. The properties of a film did not change during the period of study.

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“…Low level of moisture absorption can protect the materials from microbial contaminations and bulkiness of the polymer matrices [4,43]. The effects of PVA and PVP concentration on moisture absorption of blank matrices were shown in fig.…”

Section: Moisture Absorptionmentioning

confidence: 99%

Preparation and Characterization of Poly (Vinyl Alcohol)–poly (Vinyl Pyrrolidone) Mucoadhesive Buccal Patches for Delivery of Lidocaine HCL

Jaipakdee

Limpongsa

2018

Int J App Pharm

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Objective: The objectives of this study were to prepare and characterize a buccal mucoadhesive patch using poly (vinyl alcohol) (PVA), poly (vinyl pyrrolidone) (PVP) as a mucoadhesive matrix, Eudragit S100 as a backing layer, and lidocaine HCl as a model drug.Methods: Lidocaine HCl buccal patches were prepared using double casting technique. Molecular interactions in the polymer matrices were studied using attenuated total reflectance-fourier transform infrared spectroscopy (ATR-FTIR), differential scanning calorimetry (DSC) and X-ray diffractometry. Mechanical and mucoadhesive properties were measured using texture analyzer. In vitro permeation of lidocaine HCl from the patch was conducted using Franz diffusion cell.Results: Both of the free and lidocaine HCl patches were smooth and transparent, with good flexibility and strength. ATR-FTIR, DSC and X-ray diffractometry studies confirmed the interaction of PVA and PVP. Mechanical properties of matrices containing 60% PVP were significantly lower than those containing 20% PVP (*P<0.05). Mucoadhesive properties had a tendency to decrease with the concentration of PVP in the patch. The patch containing 60% PVP had significantly lower muco-adhesiveness than those containing 20% PVP (*P<0.05). In vitro permeation revealed that the pattern of lidocaine HCl permeation started with an initial fast permeation, followed by a slower permeation rate. The initial permeation fluxes follow the zero-order model of which rate was not affected by the PVP concentrations in the PVA/PVP matrix. Conclusion:Mucoadhesive buccal patches fabricated with PVA/PVP were successfully prepared. Incorporation of PVP in PVA/PVP matrix affected the strength of polymeric matrix and mucoadhesive property of patches.

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Glibenclamide transdermal patches: Physicochemical, pharmacodynamic, and pharmacokinetic evaluations

Cited by 132 publications

References 25 publications

Development of matrix controlled transdermal delivery systems of pentazocine: In vitro/in vivo performance

Development of matrix controlled transdermal delivery systems of pentazocine: In vitro/in vivo performance

Design, Formulation and in Vitro Drug Release From Transdermal Patches Containing Imipramine Hydrochloride as Model Drug

Preparation and Characterization of Poly (Vinyl Alcohol)–poly (Vinyl Pyrrolidone) Mucoadhesive Buccal Patches for Delivery of Lidocaine HCL

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