Development of a Prolonged-Release Pramipexole Transdermal Patch: In Vitro and In Vivo Evaluation.

Abstract:

:The current study aimed to develop a prolonged-release pramipexole (PPX) transdermal patch for the treatment of Parkinson's disease. Permeation parameters of PPX were investigated using human cadaver skin. Pramipexole patches were prepared using DURO-TAK® pressure-sensitive-adhesive (PSA) and evaluated for drug stability, drug loading, in vitro drug release, and in vitro permeation through mouse skin. The results indicated that blends of DURO-TAK® 87-2852 and DURO-TAK® 87-2510 were suitable for creating a prolonged-release PPX patch due to their advantages in drug release, drug loading, and stability. The final formulation consisted of 87-2852/87-2510 (70:30), 10% PG, and 15% PPX and showed a cumulative permeation amount of 1497.19 ± 102.90 μg/cm2 with a continuous flux over 6.0 μg/(cm2·h) across human cadaver skin for 7 days. In vivo studies in rats indicated that PPX patch produced a significantly longer (p < 0.001) half-life (t 1/2, 75.16 ± 17.37 h) and mean residence time (MRT, 135.89 ± 24.12 h) relative to oral tablets (Sifrol®) and had a relative bioavailability of 51.64 ± 21.32%. Therefore, this study demonstrated the feasibility of developing a prolonged-release PPX patch, which proposed the potential to serve as an alternate to conventional oral tablets and may therefore improve patient compliance.

journal_name

AAPS PharmSciTech

journal_title

AAPS PharmSciTech

authors

Pu T,Li X,Sun Y,Ding X,Pan Y,Wang Q

doi

10.1208/s12249-016-0555-6

subject

Has Abstract

pub_date

2017-04-01 00:00:00

pages

738-748

issue

3

issn

1530-9932

pii

10.1208/s12249-016-0555-6

journal_volume

18

pub_type

杂志文章
  • Evaluation of the performance characteristics of bilayer tablets: Part II. Impact of environmental conditions on the strength of bilayer tablets.

    abstract::Ambient air humidity and temperature are known to influence the mechanical strength of tablets. The objective of this work is to understand the influence of processing parameters and environmental conditions (humidity and temperature) on the strength of bilayer tablets. As part of this study, bilayer tablets were comp...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-012-9846-8

    authors: Kottala N,Abebe A,Sprockel O,Bergum J,Nikfar F,Cuitiño AM

    更新日期:2012-12-01 00:00:00

  • Influence of Polyvinyl Alcohol (PVA) on PVA-Poly-N-hydroxyethyl-aspartamide (PVA-PHEA) Microcrystalline Solid Dispersion Films.

    abstract::This study was conducted to formulate buccal films consisting of polyvinyl alcohol (PVA) and poly-N-hydroxyethyl-aspartamide (PHEA), to improve the dissolution of the drug through the oral mucosa. Ibuprofen sodium salt was used as a model drug, and the buccal film was expected to enhance its dissolution rate. Two diff...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-020-01811-z

    authors: Al-Sahaf Z,Raimi-Abraham B,Licciardi M,de Mohac LM

    更新日期:2020-10-02 00:00:00

  • A novel nanoparticle formulation for sustained paclitaxel delivery.

    abstract:PURPOSE:To develop a novel nanoparticle drug delivery system consisting of chitosan and glyceryl monooleate (GMO) for the delivery of a wide variety of therapeutics including paclitaxel. METHODS:Chitosan/GMO nanoparticles were prepared by multiple emulsion (o/w/o) solvent evaporation methods. Particle size and surface...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-008-9063-7

    authors: Trickler WJ,Nagvekar AA,Dash AK

    更新日期:2008-01-01 00:00:00

  • Characterization and In Vitro Evaluation of the Complexes of Posaconazole with β- and 2,6-di-O-methyl-β-cyclodextrin.

    abstract::Posaconazole is a triazole antifungal drug that with extremely poor aqueous solubility. Up to now, this drug can be administered via intravenous injection and oral suspension. However, its oral bioavailability is greatly limited by the dissolution rate of the drug. This study aimed to improve water solubility and diss...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-016-0497-z

    authors: Tang P,Wang L,Ma X,Xu K,Xiong X,Liao X,Li H

    更新日期:2017-01-01 00:00:00

  • Supercritical assisted atomization: a novel technology for microparticles preparation of an asthma-controlling drug.

    abstract::The objective of this study was to produce microparticles of a new asthma-controlling drug by supercritical assisted atomization (SAA), proposed as an alternative to conventional jet-milling process. SAA is based on the solubilization of supercritical carbon dioxide in a liquid solution containing the drug; the ternar...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt060352

    authors: Della Porta G,De Vittori C,Reverchon E

    更新日期:2005-10-22 00:00:00

  • Physicochemical and Preclinical Evaluation of a Novel Buccal Measles Vaccine.

    abstract::The aim of this study is to develop an orally disintegrating film (ODF) containing a microparticulate measles vaccine formulation for buccal delivery. The measles vaccine microparticles were made with biocompatible and biodegradable bovine serum albumin (BSA) and processed by spray drying. These vaccine microparticles...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-016-0566-3

    authors: Gala RP,Popescu C,Knipp GT,McCain RR,Ubale RV,Addo R,Bhowmik T,Kulczar CD,D'Souza MJ

    更新日期:2017-02-01 00:00:00

  • Effect of Carbopol and polyvinylpyrrolidone on the mechanical, rheological, and release properties of bioadhesive polyethylene glycol gels.

    abstract::This study examined the mechanical (hardness, compressibility, adhesiveness, and cohesiveness) and rheological (zero-rate viscosity and thixotropy) properties of polyethylene glycol (PEG) gels that contain different ratios of Carbopol 934P (CP) and polyvinylpyrrolidone K90 (PVP). Mechanical properties were examined us...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt010324

    authors: Tan YT,Peh KK,Al-Hanbali O

    更新日期:2000-08-17 00:00:00

  • In vitro dissolution of generic immediate-release solid oral dosage forms containing BCS class I drugs: comparative assessment of metronidazole, zidovudine, and amoxicillin versus relevant comparator pharmaceutical products in South Africa and India.

    abstract::Biowaivers are recommended for immediate-release solid oral dosage forms using dissolution testing as a surrogate for in vivo bioequivalence studies. Several guidance are currently available (the World Health Organization (WHO), the US FDA, and the EMEA) where the conditions are described. In this study, definitions, ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-014-0135-6

    authors: Reddy NH,Patnala S,Löbenberg R,Kanfer I

    更新日期:2014-10-01 00:00:00

  • Triamterene-beta-cyclodextrin systems: preparation, characterization and in vivo evaluation.

    abstract::The purpose of this research was to improve the solubility and therefore dissolution and bioavailability of triamterene, a poorly water soluble diuretic, by complexation with beta-cyclodextrin. Triamterene has been reported to show low bioavailability after oral administration, with wide intersubject variation. This s...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt050119

    authors: Mukne AP,Nagarsenker MS

    更新日期:2004-03-29 00:00:00

  • Direct pelletization in a rotary processor controlled by torque measurements. III. Investigation of microcrystalline cellulose and lactose grade.

    abstract::The aim of the present study was to investigate the use of different grades of microcrystalline cellulose (MCC) and lactose in a direct pelletization process in a rotary processor. For this purpose, a mixed 2- and 3-level factorial study was performed to determine the influence of the particle size of microcrystalline...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt060362

    authors: Kristensen J

    更新日期:2005-10-24 00:00:00

  • Characterization and in vitro drug release studies of a natural polysaccharide Terminalia catappa gum (Badam gum).

    abstract::The main objective of the present study is the physicochemical characterization of naturally available Terminalia catappa gum (Badam gum [BG]) as a novel pharmaceutical excipient and its suitability in the development of gastroretentive floating drug delivery systems (GRFDDS) to retard the drug for 12 h when the dosag...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-012-9873-5

    authors: Meka VS,Nali SR,Songa AS,Kolapalli VR

    更新日期:2012-12-01 00:00:00

  • Ultra rapidly dissolving repaglinide nanosized crystals prepared via bottom-up and top-down approach: influence of food on pharmacokinetics behavior.

    abstract::The present work was undertaken with the objectives of improving the dissolution velocity, related oral bioavailability, and minimizing the fasted/fed state variability of repaglinide, a poorly water-soluble anti-diabetic active by exploring the principles of nanotechnology. Nanocrystal formulations were prepared by b...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-014-0267-8

    authors: Gadadare R,Mandpe L,Pokharkar V

    更新日期:2015-08-01 00:00:00

  • Improvement of aripiprazole solubility by complexation with (2-hydroxy)propyl-β-cyclodextrin using spray drying technique.

    abstract::Due to the fact that the number of new poorly soluble active pharmaceutical ingredients is increasing, it is important to investigate the possibilities of improvement of their solubility in order to obtain a final pharmaceutical formulation with enhanced bioavailability. One of the strategies to increase drug solubili...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-012-9786-3

    authors: Mihajlovic T,Kachrimanis K,Graovac A,Djuric Z,Ibric S

    更新日期:2012-06-01 00:00:00

  • Thermal Magnetic Field Activated Propolis Release From Liquid Crystalline System Based on Magnetic Nanoparticles.

    abstract::Intra-periodontal pocket drug delivery systems, such as liquid crystalline systems, are widely utilized improving the drug release control and the therapy. Propolis is used in the treatment of periodontal diseases, reducing the inflammatory and infectious conditions. Iron oxide magnetic nanoparticles (MNPs) can improv...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1163-4

    authors: de Alcântara Sica de Toledo L,Rosseto HC,Dos Santos RS,Spizzo F,Del Bianco L,Montanha MC,Esposito E,Kimura E,Bonfim-Mendonça PS,Svidzinski TIE,Cortesi R,Bruschi ML

    更新日期:2018-10-01 00:00:00

  • Kinetic modelling for the assay of nortriptyline hydrochloride using potassium permanganate as oxidant.

    abstract::Kinetic methods for accurate determination of nortriptyline hydrochloride have been described. The methods are based on the oxidation of nortriptyline hydrochloride with KMnO4 in acidic and basic media. In acidic medium, the decrease in absorbance at 525.5 nm and in basic medium, the increase in absorbance at 608.5 nm...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-014-0230-8

    authors: Rahman N,Khan S

    更新日期:2015-06-01 00:00:00

  • Preparation and characterization of salmon calcitonin-biotin conjugates.

    abstract::This study was performed to prepare and characterize the biotinylated Salmon calcitonin (sCT) for oral delivery and evaluate the hypocalcemic effect of biotinylated-sCTs in rats. Biotinylated sCTs was characterized by using high performance liquid chromatography (HPLC) and MALDITOF-MS. The effect of biotinylation on p...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-008-9165-2

    authors: Cetin M,Youn YS,Capan Y,Lee KC

    更新日期:2008-01-01 00:00:00

  • Elucidation of spheroid formation with and without the extrusion step.

    abstract::Spheroid formation mechanisms were investigated using extrusion-spheronization (ES) and rotary processing (RP). Using ES (cross-hatch), ES (teardrop), and RP (teardrop), spheroids with similar mass median diameter (MMD) and span were produced using equivalent formulation and spheronization conditions. During spheroniz...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt0801010

    authors: Liew CV,Chua SM,Heng PW

    更新日期:2007-02-09 00:00:00

  • Membrane Rigidity Determined by Atomic Force Microscopy Is a Parameter of the Permeability of Liposomal Membranes to the Hydrophilic Compound Calcein.

    abstract::We determined the permeability coefficient of a model hydrophilic drug, calcein, encapsulated within saturated lipid-based nano-sized liposomes of various lipid profiles. We demonstrated that the addition of cholesterol to liposomes containing saturated lipids increased the permeability of the liposomal membrane to ca...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-016-0624-x

    authors: Takechi-Haraya Y,Sakai-Kato K,Goda Y

    更新日期:2017-07-01 00:00:00

  • In Vivo Evaluation of Taste-Masked Fast-Disintegrating Sublingual Tablets of Epinephrine Microcrystals.

    abstract::In community settings, IM injection of 0.3 mg epinephrine (Epi) using an auto-injector is the drug of choice for treatment of anaphylaxis. Previously, a taste-masking (TM) formulation of fast-disintegrating sublingual tablets (FDSTs) was developed in our lab. Also, Epi was micronized (Epi-MC) successfully and reduced ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1171-4

    authors: Rachid O,Simons KJ,Rawas-Qalaji M

    更新日期:2018-11-01 00:00:00

  • Advances in metered dose inhaler technology: hardware development.

    abstract::Pressurized metered dose inhalers (MDIs) were first introduced in the 1950s and they are currently widely prescribed as portable systems to treat pulmonary conditions. MDIs consist of a formulation containing dissolved or suspended drug and hardware needed to contain the formulation and enable efficient and consistent...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章,评审

    doi:10.1208/s12249-013-0062-y

    authors: Stein SW,Sheth P,Hodson PD,Myrdal PB

    更新日期:2014-04-01 00:00:00

  • Mechanical Characterization and Dissolution of Chewing Gum Tablets (CGTs) Containing Co-compressed Health in Gum® and Curcumin/Cyclodextrin Inclusion Complex.

    abstract::Curcumin chewing gums could be therapeutically beneficial if used by the head and neck cancer patients. High curcumin loading in chewing gums however is needed to achieve desired therapeutic effect. Preparing gums with high drug load is nonetheless challenging because of the negative impact of solids on their masticat...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1174-1

    authors: Al Hagbani T,Altomare C,Kamal MM,Nazzal S

    更新日期:2018-11-01 00:00:00

  • Formulation and stability testing of itraconazole crystalline nanoparticles.

    abstract::Itraconazole (ITZ) crystalline nanoparticles were prepared using relatively simple, low-cost sonoprecipitation technique, in which both the solvent and antisolvent were organic in nature. The effect of stabilizer type (hydroxypropyl methylcellulose, hydroxypropyl cellulose, Inutec SP1®, and pluronic F127), drying meth...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-011-9651-9

    authors: Badawi AA,El-Nabarawi MA,El-Setouhy DA,Alsammit SA

    更新日期:2011-09-01 00:00:00

  • An investigation into the effect of fine lactose particles on the fluidization behaviour and aerosolization performance of carrier-based dry powder inhaler formulations.

    abstract::The effect of milled and micronized lactose fines on the fluidization and in vitro aerosolization properties of dry powder inhaler (DPI) formulations was investigated, and the suitability of static and dynamic methods for characterizing general powder flow properties of these blends was assessed. Lactose carrier pre-b...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-014-0119-6

    authors: Kinnunen H,Hebbink G,Peters H,Shur J,Price R

    更新日期:2014-08-01 00:00:00

  • 3D-Printed Isoniazid Tablets for the Treatment and Prevention of Tuberculosis-Personalized Dosing and Drug Release.

    abstract::The aim of the present work was to produce 3D-printed oral dosage forms with a sufficient drug dose displaying various release profiles. Hot-melt extrusion was utilized to produce drug-loaded feedstock material that was subsequently 3D-printed into 6, 8, and 10 × 2.5 mm tablets with 15% and 90% infill levels. The prep...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-018-1233-7

    authors: Öblom H,Zhang J,Pimparade M,Speer I,Preis M,Repka M,Sandler N

    更新日期:2019-01-07 00:00:00

  • Process optimization of a novel immediate release film coating system using QbD principles.

    abstract::This work describes a quality-by-design (QbD) approach to determine the optimal coating process conditions and robust process operating space for an immediate release aqueous film coating system (Opadry® 200). Critical quality attributes (CQAs) or associated performance indicators of the coated tablets were measured w...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-013-9935-3

    authors: Teckoe J,Mascaro T,Farrell TP,Rajabi-Siahboomi AR

    更新日期:2013-06-01 00:00:00

  • Effect of oppositely charged polymer and dissolution media on rheology of spray-dried ionic complexes.

    abstract::The purpose of this research was to address the utility of rheological study in understanding the influence of oppositely charged polymers on release of naproxen sodium encapsulated in chitosan particles. The interaction between oppositely charged kappa-carrageenan (kappa-Ca) and chitosan leads to relatively higher ge...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-010-9379-y

    authors: Bhise KS,Dhumal RS,Shailesh B,Paradkar AR,Kadam SS

    更新日期:2010-03-01 00:00:00

  • Considerations in developing a target product profile for parenteral pharmaceutical products.

    abstract::A target product profile (TPP) describes how a product will be utilized by the end user. A systematically developed TPP can ensure alignment of objectives across company departments, accelerate development timelines, minimize development risks, and eventually lead to an optimal product. A TPP is particularly important...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章,评审

    doi:10.1208/s12249-010-9521-x

    authors: Lambert WJ

    更新日期:2010-09-01 00:00:00

  • Quantification of mass transfer during spheronisation.

    abstract::Spherical granules (pellets) are quite useful in many pharmaceutical applications. The extrusion spheronisation technique is well established as a method of producing pellets of a spherical shape and narrow size distribution. After the extrusion, the cylindrical extrudates are transformed to spherical pellets by spher...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-012-9770-y

    authors: Koester M,Thommes M

    更新日期:2012-06-01 00:00:00

  • Studies on formulation development of mucoadhesive sustained release itraconazole tablet using response surface methodology.

    abstract::The purpose of this research was to prepare and evaluate sustained release mucoadhesive tablets of Itraconazole. It is practically insoluble in aqueous fluids hence its solid dispersion with Eudragit E100 was prepared by spray drying. This was formulated in matrix of hydrophilic mucoadhesive polymers Carbopol 934P (CP...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-008-9119-8

    authors: Madgulkar A,Kadam S,Pokharkar V

    更新日期:2008-01-01 00:00:00

  • EGFR Targeted Paclitaxel and Piperine Co-loaded Liposomes for the Treatment of Triple Negative Breast Cancer.

    abstract::Triple-negative breast (TNBC) cancer that is upregulated with epidermal growth factor receptor (EGFR), and devoid of both the hormonal receptors and epidermal growth factor receptor 2 (HER 2), has led to a concept of treating TNBC with EGFR-targeted therapeutics. The combination of paclitaxel (PTX) and piperine (PIP) ...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/s12249-020-01671-7

    authors: Burande AS,Viswanadh MK,Jha A,Mehata AK,Shaik A,Agrawal N,Poddar S,Mahto SK,Muthu MS

    更新日期:2020-05-21 00:00:00