Design and In-vitro Evaluation of a Modified-release Oral Dosage Form of Nifedipine by Hybridization of Hydroxypropyl-β-cyclodextrin and Hydroxypropylcellulose (original) (raw)
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Journal of Inclusion Phenomena and Macrocyclic Chemistry, 2006
ABSTRACT An attempt was made to improve the release property of nifedipine (NP) from Witepsol® H-15, glycerin and polyethylene glycol (PEG) suppository bases by means of the complexation with 2-hydroxypropyl-β-cyclodextrin (HP-β-CyD). The amorphous complexes of NP with HP-β-CyD in molar ratios of 1:1–1:10 (guest:host) were prepared by the spray-drying method. The NP/HP-β-CyD complex was homogeneously dispersed in Witepsol® H-15 suppository base, whereas the drug alone and the physical mixture of the guest and host were sedimented at the bottom of the base. The release rates of NP from Witepsol® H-15 and glycerin suppositories were significantly increased by the complexation with HP-β-CyD. On the other hand, HP-β-CyD gave negligible effect on the release rate of NP from PEG suppository base. The results indicated that Witepsol® H-15 suppository containing NP/HP-β-CyD complex is useful from a viewpoint of the release control and quality assurance.
Asian Journal of Pharmaceutics, 2010
T he aim of the present work was to develop controlled release matrix formulation of nifedipine and investigate the effects of both hydrophilic and hydrophobic polymers on in vitro drug release. Matrix tablets were prepared by wet granulation technique using different concentration of hydroxy propyl methyl cellulose (HPMC), ethyl cellulose (EC), compressible Eudragits (RSpo and RLpo) and their combination in different ratios to examine their influence on tablet properties and drug release profile. Tablets were evaluated by measurement of hardness, friability, content uniformity, weight variation and drug release pattern. Release studies were carried out using USP type II apparatus in 900 ml of sodium phosphate buffer (pH 7.4) with 0.5% (w/v) SDS. The amount of drug released was determined at 238 nm by UV-visible spectrophotometer. In vitro dissolution studies indicated that hydrophobic polymers significantly reduced the rate of drug release compared to hydrophilic ones in 12 hrs and combination of both polymers exhibited the best release profile to sustain the drug release for prolong period of time. As a result, the tablet containing HPMC:EC in ratio of 0.75:1 showed better controlled release pattern over a period of 12 hrs. In selected formulation, the calculated regression coefficients for release models fitted best to zero-order models.
G.Dinesh Babu et al: Design and Evaluation of tablets of Nifedipine
2012
Nifedipine is a calcium channel blocker drug widely used in the treatment of hypertension. However, its extensive first pass metabolism results in poor bioavailability. The objective of present research work is to design and evaluate the controlled release of mucoadhesive buccal tablets of Nifedipine with a goal to increase the bioavailability, reduce dosing frequency and improve patient compliance. The tablets were prepared using Carbopol‐934, Hydroxy propyl methyl cellulose (HPMC), Hydroxy ethyl cellulose (HEC) as mucoadhesive polymers. Six formulations were developed with varying concentration of polymers. The tablets were evaluated for hardness, weight variation, thickness, percentage of drug content, Surface pH, invitro studies like swelling, mucoadhesive strength and drug release. Formulation (F4) containing Carbopol‐934 and HPMC K4M in the ratio of (2 : 4) showed good mucoadhesive strength (36.8) and maximum drug release of 97.1% in 10 hrs. Swelling increase with increase in...
Objective: The aim of the present research is to formulate and evaluate matrix tablet of Nifedipine by using hydrophobic and hydrophilic polymer. Method: The Nifedipine matrix tablets were prepared by wet granulation method. Formulated tablets were characterized by parameters like hardness, friability, content uniformity, weight variation and in- vitro release studies. In vitro drug release studies were carried in dissolution apparatus using 900 ml of 0.1N HCL (pH 1.2 buffer) for first 2 hours and remaining 12 hours in phosphate buffer (pH 6.8) containing 1% w/v sodium lauryl sulfate as dissolution medium. The amount of drug released was determined spectrophotometrically at 235 nm. Result: The results of the present study based on the in- vitro dissolution studies showed that formulation F5 was shown drug release upto 92.53% at 14 hours was selected as the best formulation from Nifedipine formulations. All the formulated tablets were evaluated for various physical parameters such as hardness, thickness, friability weight variation and drug content was found to be within the limit. In selected formulation, the calculated regression coefficients for drug release kinetics follows the Korsemayer-peppas and drug transport mechanism follow anomalous transport and non- fickian diffusion mechanism release. Conclusion: The result of the study demonstrated that combination of both hydrophilic and hydrophobic polymers could be successfully employed for formulating sustained-release matrix tablets of nifedipine.
The purpose of the present investigation was to design and evaluate sustained release tablets of a poorly water soluble drug nifedipine, employing hydrophilic polymers Methocel K15M CR and Methocel K100LV CR and to select the best formulation based on pharmacokinetic studies. Direct compression method was used to prepare matrix tablets. The granules were evaluated for angle of repose, loose bulk density, tapped bulk density, compressibility index and drug content. The tablets were subjected to various tests for their physical parameters such as thickness, hardness and friability. In vitro release study was carried out for 12 hours using USP paddle type dissolution apparatus in phosphate buffer with sodium lauryl sulphate (pH 6.8). Quantitative evaluation by mathematical model indicates that formulation containing HPMC K15M CR and HPMC K100LV CR in a ratio of 1:3 showed better dissolution properties compared to other formulations. Korsmeyer's plot indicated that the drug release mechanisms from the matrix tablet followed Fickian mechanism. The study indicates that the hydrophilic matrix tablets of nifedipine prepared using Methocel K15M CR and Methocel K100LV CR can successfully be employed as twice-a-day oral controlled release dosage form in order to improve patient compliance.
Formulation of solid dispersion and surface solid dispersion of nifedipine: A comparative study
African journal of pharmacy and pharmacology
In this study, an attempt was taken to enhance the solubility and dissolution characteristics of nifedipine, a poorly water soluble calcium channel blocking agent, by preparing solid dispersions (SD) with water soluble carriers; Poloxamer 407, HPMC 5 cPs, polyethylene glycol (PEG) 4000 and 6000 and surface solid dispersions (SSD) with insoluble carriers; sodium starch glycolate (SSG) and croscarmellose sodium (CCS). In vitro dissolution study showed that all the preparations were effective to improve the dissolution of nifedipine to several folds when compared with the drug and physical mixtures (PMs). Drug loading in SDs and SSDs was found uniform and they produced satisfactory results on drug content analysis (95 to 102%), compatibility and thermal analysis. PEG 6000, Poloxamer 407 and SSG were found to be the most effective carriers to enhance the dissolution behavior of nifedipine. SDs with water soluble carriers were found more effective in improving solubility of nifedipine th...
2008
Mr. Shubhrajit Mantry Department of Pharmaceutics Himalayan Pharmacy Institute Majhitar, E. Sikkim, INDIA Email: manu28pharmcy@gmail.com Phone: +91-7384205300 The aim of the present work was to develop sustained release formulation of Nifedipine and evaluate the In-vitro Drug release, a poorly water soluble drug, hydroxy propyl methyl cellulose (HPMC) with different grade as hydrophilic polymers. Tablets were prepared by wet granulation and direct compression technique by using various ratio of different grades of HPMC. Tablets were evaluated for Friability, Hardness, Weight Variation, Content Uniformity, Thickness and In-vitro drug release. By observing dissolution profile it was concluded that the formulation containing HPMC in the ratio of 1:1 showed acceptable dissolution properties compared to other formulation. This study indicates the hydrophilic matrix tablet of Nifedipine prepared using HPMC of different grade can successfully be employed as sustained release matrix tablet ...
Encapsulation and drug release of poorly water soluble nifedipine from bio-carriers
Journal of Non-Crystalline Solids, 2018
Controlled drug delivery is one of the most intruding field in pharmaceutical research. It is desired for most of the drugs due to safety and efficacy reasons. Another emerging field is improving the bioavailability of poorly water-soluble drugs. By encapsulating such drugs into biodegradable polysaccharide materials both, improved bioavailability and controlled drug release is readily expected. Nifedipine, used as a model drug, was encapsulated within polysaccharide gels by the novel ethanol induced gelation method. Wet materials were processed by supercritical technology to retain its form and structure. Swelling and in-vitro dissolution tests were performed to investigate the swelling of aerogels and release behavior of nifedipine within body fluids. It was observed that guar and xanthan are not the best candidates for oral delivery of nifedipine, since the release was prolonged to 14 days. Oppositely, pectin and alginate are both suitable for nifedipine encapsulation as they released 100% of nifedipine within the first 5 h. Higher drug loading was achieved by pectin aerogels most likely due to their higher surface area.