Pharmaceutical Development of Solid Dispersion Based Osmotic Drug Delivery System for Nifedipine

Kanagale, Pritam; Patel, Vineetkumar; Venkatesan, Natarajan; Jain, Mukul; Patel, Pankaj S.; Misra, Ambikanandan

doi:10.2174/156720108785914998

Cited by 13 publications

(3 citation statements)

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“…Micellar nanoparticles incorporating paclitaxel or cisplatin are in their clinical trials [177]. There are also oral dosage formulation commercial products for which osmotic pressure is the major driving force in release mechanism, including Procardia XL ® for nifedipine (Figure 2) and Glucotrl XL ® for glipizide [47,48,178].…”

Section: Marketed Controlled Release Polymeric Pharmaceutical Prodmentioning

confidence: 99%

Materials for Pharmaceutical Dosage Forms: Molecular Pharmaceutics and Controlled Release Drug Delivery Aspects

Mansour

Sohn

Al-Ghananeem

et al. 2010

IJMS

181

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Controlled release delivery is available for many routes of administration and offers many advantages (as microparticles and nanoparticles) over immediate release delivery. These advantages include reduced dosing frequency, better therapeutic control, fewer side effects, and, consequently, these dosage forms are well accepted by patients. Advances in polymer material science, particle engineering design, manufacture, and nanotechnology have led the way to the introduction of several marketed controlled release products and several more are in pre-clinical and clinical development.

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Section: Marketed Controlled Release Polymeric Pharmaceutical Prodmentioning

confidence: 99%

Materials for Pharmaceutical Dosage Forms: Molecular Pharmaceutics and Controlled Release Drug Delivery Aspects

Mansour

Sohn

Al-Ghananeem

et al. 2010

IJMS

181

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“…A monolithic osmotic system or a single core osmotic tablet (SCOT) based on SD offers this flexibility. Literature reports incorporation of solubility enhanced form into osmotic system for many drugs like 10-hydroxycamptothecan [5] , nifedipine [6,7] , glipizide [8] , atenolol [9] and diltiazem [10] . However, the reports about polymer level and type screening through glass transition temperature (T g ) approach and statistical evaluation of factors affecting design of monolithic osmotic dosage forms were scarce.…”

Section: Development Of a Single Core Osmotic Tablet Containing Thermmentioning

confidence: 99%

Development of a Single Core Osmotic Tablet Containing Thermodynamically Stable Solid Dispersion of Nisoldipine

Kumar¹,

Singh²

2017

pharmaceutical-sciences

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Kumar, et al.: Thermodynamically Stable Solid Dispersion in an Osmotic TabletThe main aim of the research work was to investigate the type and level of the polymer for solubility enhancement of nisoldipine by solid dispersion approach, followed by study of the formulation factors affecting design of a single unit, solid dispersion containing osmotic controlled release tablet. Solid dispersions with copovidone and Soluplus ® were manufactured by hot melt extrusion technique, which offered possibility of scale up and commercialization. Dynamic vapour sorption and differential scanning calorimetry were used to characterize solid dispersions. Based on the glass transition temperature and dynamic vapour sorption data, nisoldipine-Soluplus ® , at 1:1 ratio was selected to make dissolution enhanced solid dispersion system. The formulation factors affecting the drug release from the osmotic tablets such as type of dispersant, level of osmogen, %plasticizer in film coat and %coating, were studied by full factorial design. The drug release was found to increase with the increase in sodium chloride concentration in the core and polyethylene glycol level in the coating. The coating weight gain was found to decrease the drug release. Scanning electron microscopy revealed that the drug release occurred through the drilled hole and not through the extended release coating membrane. An interesting observation was found with respect to the dispersant type in the core. The high viscosity dispersant (Polyox) was found to facilitate complete release from the tablets compared to highly soluble, low viscosity dispersant (lactose). A design space was generated indicating that 36% osmogen in the core, a %polyethylene glycol level of 10-15% and weight gain at 5-7% can provide for a single core osmotic dosage form releasing ~80% drug in 12 h. The drug release from the monolithic tablets followed the Korsenmeyer-Peppas kinetics.

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“…In solid dispersions, cyclosporine is dispersed with polymers such as hydroxypropyl cellulose–SSL [13], dimethyl-β-cyclodextrin [13], hydroxypropyl methylcellulose phthalate and polyoxyethylene hydrogenated castor oil [14], polyoxyethylene (40) stearate [15], dimyristoyl phosphatidylcholine [16], and sodium lauryl sulfate and dextrin [17] in order to reach a better intrinsic solubility, dissolution rate, absorption rate, and thus, its oral bioavailability in vivo.…”

Section: Introductionmentioning

confidence: 99%

Enhanced Dissolution and Oral Bioavailability of Cyclosporine A: Microspheres Based on αβ-Cyclodextrins Polymers

et al. 2018

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Cyclosporine (CsA) has a selective property of suppressing various T-lymphocyte functions. This is of utmost importance in preventing allograft rejection by several organ transplantations, as well as in the treatment of systemic and local autoimmune disorders. However, the poor water solubility of CsA can be a major hurdle for its absorption into the blood stream, which leads to low bioavailability and thus less efficacy. The aim of this study was to prepare, characterize, and evaluate in vitro as well as in vivo, the potential of the innovative CsA drug delivery system. The latter contains CsA in spherical amorphous solid dispersion (SASD) which is embedded in an original α-cyclodextrin and β-cyclodextrin polymer mixture (Poly-αβ-CD) as a multifunctional amorphous carrier. The new developed SASD formulation showed that CsA was molecularly dispersed in αβ-cyclodextrins in an amorphous form, as was confirmed by physicochemical characterization studies. Interestingly, the peptide secondary structure, and thus, the drug activity was not impacted by the preparation of SASD as was shown by circular dichroism. Furthermore, the in vitro CsA release profile kinetics was almost identical to the commercially available product Neoral®. This study presents the first in vivo proof-of-concept for a novel drug delivery system based on Poly-αβ-CD containing CsA, with SASD allowing for increased bioavailibility. The pharmacokinetic parameters of cyclosporine A from the spherical spray-dried dispersion formulation was demonstrated in a “rat” animal model. For comparison, the commercially available Neoral® was studied. Importantly, the pharmacokinetic parameters were improved by extending Tmax from 2 to 3 h after the oral administration in rats, and eventually preventing the enterohepatic circulation. All these results clearly demonstrate the improved pharmacokinetic parameters and enhanced bioavailability of CsA in the new developed drug delivery system. These data demonstrated the superiority of the newly developed Poly-αβ-CD formulation for oral administration of the poorly soluble CsA in vivo without altering its secondary structure. Poly-αβ-CD can be a very useful tool for the oral administration of poorly water-soluble drugs.

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Pharmaceutical Development of Solid Dispersion Based Osmotic Drug Delivery System for Nifedipine

Cited by 13 publications

References 0 publications

Materials for Pharmaceutical Dosage Forms: Molecular Pharmaceutics and Controlled Release Drug Delivery Aspects

Materials for Pharmaceutical Dosage Forms: Molecular Pharmaceutics and Controlled Release Drug Delivery Aspects

Development of a Single Core Osmotic Tablet Containing Thermodynamically Stable Solid Dispersion of Nisoldipine

Enhanced Dissolution and Oral Bioavailability of Cyclosporine A: Microspheres Based on αβ-Cyclodextrins Polymers

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