An Investigation into the Factors Influencing Drug Release from Hydrophilic Matrix Tablets Based on Novel Carbomer Polymers

Parojčić, Jelena; Đurić, Zorica; Jovanović, Milica; Ibrić, Svetlana

doi:10.1080/10717540490265379

Cited by 42 publications

(24 citation statements)

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“…[10] Many polymers have been used in the formulation of matrix based CR drug delivery systems. Reports are found on the use of hydrophilic polymers such as hydroxypropyl methylcellulose, methylcellulose, sodium carboxymethylcellulose (Na CMC), [11] carbopols, [12] and polyvinyl alcohol [13] for the preparation of CR formulations of different drugs. Hydrophilic polymer matrix systems [14][15][16][17][18][19] are widely used for designing oral controlled drug delivery dosage forms because of their flexibility to provide a desirable drug release profile, cost-effectiveness, and broad regulatory acceptance.…”

Section: Original Articlementioning

confidence: 99%

Untitled

Das¹

2017

AJP

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Aim: To design and characterize oral controlled release matrix tablets of lamivudine to improve efficacy and patient compliance. Materials and Methods: Lamivudine matrix tablets were prepared by wet granulation method using various proportions of hydrophilic polymers such as sodium carboxymethylcellulose (Na CMC), hydroxypropyl methylcellulose (HPMC), Eudragit-L155, and xanthan gum alone or in combination with hydrophobic polymer ethyl cellulose (EC). In-vitro release studies were performed using USP Type II dissolution apparatus 900 ml of pH -6.8 phosphate buffer at 100 rpm. Drug release kinetics was analyzed using zero-order, first-order, Higuchi and Hixon equation. No chemical interaction between drug and the polymer was seen as confirmed by Fourier transform infrared studies. Results and Discussion: All the formulations showed good results which were compliance with pharmacopeial standards. Formulations X 2, X 3 , X 4 , X 5 , X 7 , X 9 , X 12 , and X 14 containing a combination of two polymers, i.e., xanthan gum, combine with EC, Na CMC, HPMC, and Eudragit-L155 in the different ratios shows zero-order kinetic of release with 80-97% of drug released. But in the presence of Na CMC in the formulation X 4 , X 9 , and X 14, the drug released in 12 h was in the range of 75-85% and shows zero-order kinetics. Mathematical analysis of the release kinetics indicated that the nature of drug release from the matrix tablets was dependent on drug diffusion and therefore followed non-Fickian or anomalous release. The formulation X 4 containing xanthan gum with Na CMC gave more sustaining action, i.e., 79.16% in 12 h. Conclusion: Based on the in-vitro drug release study, it can be concluded that among the prepared formulations, X4 is the optimized formulation and can overcome the demerits of conventional lamivudine tablet.

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Section: Original Articlementioning

confidence: 99%

Untitled

Das¹

2017

AJP

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“…Parojčić et al described the use of second-order derivative UV spectrophotometry for direct determination of PCT in urine without preliminary extraction or prior derivatization. 36) Criado et al have investigated the use of an evaporative light scattering detector (ELSD) for the determination of PCT in urine samples. 37) However, most of these methods have detection limits close to the urinary levels of PCT while urinary clearance of the drug after a certain time may reduce the concentrations to such low levels that preconcentration/detection of the toxic agent may be necessary.…”

Section: Spectrophotometric Determination Of Paracetamol In Urine Witmentioning

confidence: 99%

Spectrophotometric Determination of Paracetamol in Urine with Tetrahydroxycalix[4]arene as a Coupling Reagent and Preconcentration with Triton X-114 Using Cloud Point Extraction

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et al. 2006

CHEMICAL & PHARMACEUTICAL BULLETIN

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Paracetamol (N-acetyl-p-aminophenol; abbreviated as PCT) has been widely used as analgesic and antipyretic drug. Paracetamol is a weak acid (pK a ϭ9.5) which is rapidly absorbed and distributed after oral administration and excreted largely in urine: 45-55% as glucuronide conjugates, 20-30% as sulphate, 15-55% as cysteine and mercapturic acid conjugates and only 1-5% unchanged.1) Although PCT is usually well tolerated when used at the recommended dose, large doses have been associated with lethal hepatic necrosis and renal failure.2) Various methods have been proposed for the determination of PCT in biological fluids (urine, plasma and serum). Relatively few reports describe high-performance liquid chromatographic (HPLC) methods for the estimation of urine and serum concentrations of PCT using spectrophotometric, 2-10) fluorescence 11) and electrochemical detection.12) Other methods such as nuclear magnetic resonance (NMR), 13) capillary electrophoresis (CE), 14) and gas chromatography (GC) 15) have also been reported. There are many reliable methods for assaying urinary PCT levels, but they are often time-consuming, technically demanding, and requires the use of costly, highly specialized instruments.In the first practical spectrophotometric method developed, 16) PCT was extracted with ether and hydrolyzed with acid to p-aminophenol, which was then coupled with phenol in the presence of sodium hypobromite to form an indophenol dye. Since then, other spectrophotometric methods for PCT assay in biological fluids have been described. [17][18][19][20][21][22][23][24][25] The majority of published spectrophotometric methods are based on ring-nitration, 23) diazotization, [17][18][19] differential absorbance measurement, 18) direct acid reduction, 21) and oxidative coupling with some phenolic reagent to form an indophenol dye. 24,25) Generally, urinary PCT is not directly assayed, and requires preliminary hydrolysis of PCT to paminophenol (abbreviated as PAP) for final determination. Urinary screening of PCT is mostly based on acidic [25][26][27][28][29][30] or enzymatic [31][32][33] hydrolysis of PCT to PAP, the latter requiring 17-20 h. In most of the conventional spectrophotometric procedures, the hydrolysis product (PAP) reacts with a special chromogenic reagent in basic medium to form an indophenol blue dye. A number of chromogenic reagents including phenol, 30) o-cresol, 25,26,28) Heirwegh and Fevery,29) in strongly acidic medium, PAP resulting from differential extraction and acid hydrolysis of total PCT in urine is diazotized and the diazonium salt cou- In the present paper, conventional spectrophotometry in conjunction with cloud point extraction-preconcentration were investigated as alternative methods for paracetamol (PCT) assay in urine samples. Cloud point extraction (CPE) was employed for the preconcentration of p-aminophenol (PAP) prior to spectrophotometric determination using the non-ionic surfactant Triton X-114 (TX-114) as an extractant. The developed methods were based on acidic hydrolysis of ...

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“…9 Many polymers have been used in the formulation of matrix-based CR drug delivery systems. Reports were found on usage of hydrophilic polymers such as hydroxypropyl methylcellulose (HPMC), methylcellulose, sodium carboxymethylcellulose, 10 carbopols, 11 and polyvinyl alcohol 12 for the purpose of CR formulations of different drugs. HPMC, a semisynthetic derivative of cellulose, is a swellable and hydrophilic polymer.…”

Section: Introductionmentioning

confidence: 99%

Design and study of lamivudine oral controlled release tablets

2007

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The objective of this study was to design oral controlled release matrix tablets of lamivudine using hydroxypropyl methylcellulose (HPMC) as the retardant polymer and to study the effect of various formulation factors such as polymer proportion, polymer viscosity, and compression force on the in vitro release of drug. In vitro release studies were performed using US Pharmacopeia type 1 apparatus (basket method) in 900 mL of pH 6.8 phosphate buffer at 100 rpm. The release kinetics were analyzed using the zero-order model equation, Higuchi's square-root equation, and the RitgerPeppas empirical equation. Compatibility of the drug with various excipients was studied. In vitro release studies revealed that the release rate decreased with increase in polymer proportion and viscosity grade. Increase in compression force was found to decrease the rate of drug release. Matrix tablets containing 60% HPMC 4000 cps were found to show good initial release (26% in first hour) and extended the release up to 16 hours. Matrix tablets containing 80% HPMC 4000 cps and 60% HPMC 15 000 cps showed a first-hour release of 22% but extended the release up to 20 hours. Mathematical analysis of the release kinetics indicated that the nature of drug release from the matrix tablets was dependent on drug diffusion and polymer relaxation and therefore followed non-Fickian or anomalous release. No incompatibility was observed between the drug and excipients used in the formulation of matrix tablets. The developed controlled release matrix tablets of lamivudine, with good initial release (20%-25% in first hour) and extension of release up to 16 to 20 hours, can overcome the disadvantages of conventional tablets of lamivudine.

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An Investigation into the Factors Influencing Drug Release from Hydrophilic Matrix Tablets Based on Novel Carbomer Polymers

Cited by 42 publications

References 12 publications

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Spectrophotometric Determination of Paracetamol in Urine with Tetrahydroxycalix[4]arene as a Coupling Reagent and Preconcentration with Triton X-114 Using Cloud Point Extraction

Design and study of lamivudine oral controlled release tablets

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