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Acid Sustained Release Tablets with Water-Insoluble Gel

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Acid Sustained Release Tablets with Water-Insoluble Gel '1. j Available online at www.sciencedirect.com -.._ ~. - SCll!NCl!@DIRl!CT• 1 : Ü. Kiitüphane v;;ö 1 k ILFARMACO ELSEVIER ;' No M'-ttt-15. .. II Farmaco 58 (2003) 397 - 401 www.elsevier.com/locate/farmac • . ... ····· ····· ..... acid sustained release tablets with water-insoluble gel S. Güngör *, A. Y. Özsoy, E. Cevher, A. Araman Faculty of Pharmacy, Department of Pharmaceutical Technology, /stanbul Istanbul, Turkey Received 24 April 2002; accepted 28 November 2002 Abstract Mefenamic acid (MA) has analgesic, anti-inflammatory and antipyretic properties. Available conventional dosage forms are capsules and film-coated tablets. No commercial sustained release preparation of MA exists in the market. The usual oral dose is 250 or 500 mg and reported half-life is 2 h. Sodium alginate (NaAL) is the sodium salt of alginic acid, a natura! polysaccharide extracted from marine brown algae. it has the ability to forma water-insoluble gel with a bivalent metal ions as calcium. Therefore, NaAL has been studied for preparing sustained release formulations in pharmaceutical technology. In this study, tablet formulations containing different ratios of NaAL and calcium gluconate (CaGL) were prepared by direct compression method. In vitro release studies were carried out using USP 23 basket method and release data were kinetically evaluated. According to release studies, it can be emphasized that NaAL and CaGL can be used for design of sustained release preparation of MA. © 2003 Editions scientifiques et medicales Elsevier SAS. Ali rights reserved. Mefenamic acid; Sodium alginate; Calcium g]uconate; Sustained release 1. Introduction dispersing agent and gelation agent (10]. NaAL has the ability of forming rapid viscous solutions and gels by its Mefenamic acid (MA), 2-((2,3-dimethylphenyl)ami- contacts with aqueous media. lts wide application no]benzoic acid, is a nonsteroidal anti-inflammatory involves the preparation of hydrophilic type agent possessing analgesic and antipyretic activities sustained release oral dosage (11 - 13]. In addition, [1,2]. it is an inhibitor of prostaglandin synthetase. NaAL also has the ability to cause water-insoluble The usual oral dose is 250 or 500 mg, being administered gelation in the presence ofbivalent metal ions as calcium three times daily and reported half-life is 2 h [2]. [14]. Therefore, aAL has been widely used for design Sustained re!ease MA beads based on K-carrageenan of novel drug delivery systems (15 - 18]. [3] and cellulose acetate phthalate [4] and prolonged In this study, tablets containing different ratios and released MA microcapsules prepared with acrylic acid amounts of NaAL and calcium gluconate (CaGL) as a polymers [5,6] have been reported in the literature. bivalent metal were prepared by direct compression However, no commercially long acting product exists method. In vitro release of MA from tablets was in the market. evaluated by using USP 23 basket method and release The use of natura! polymers as drug carriers is one of <lata were to kinetic models. the main objectives of researchers dealing with long acting dosage forms [7 - 9]. Sodium alginate (NaAL), the sodium salt of alginic acid, a natura! polysaccharide 2. Experimental having high biological safety is extracted from brown algae. it has been widely used as a stabilizer, thickener, 2.1. Materials * Corresponding author. Mefenamic acid was kindly supplied from Nobel E-mail address: [email protected] (S. Güngör). Pharm. Comp., Turkey. Sodium alginate (A-2033) was 00l4-827X/03/$ - see front matter © 2003 Editions et medicales Elsevier SAS. All rights reserved. doi: 10.1 O16/SOO l 4-827X(03)00040-5 S. Güngör et al. I Il Farmaco 58 (2003 ) 397- 401 399 3. Results and discussion the release data were evaluated statistically (ANOVA), formulations C and F (P < 0.001) de- The results indicated that ali the tablets prepared in creased the extent of drug release in comparison with this study meet the USP 23 requirements for weight the other formulations (A, B, D and E). variation tolerance [19]. The amounts of MA in the ali As can be seen from Fig. l(b) that formulation A and tablet formulations were found in the range of 98.0- B showed similar release patterns. At the end of 8 h, 102.0%. The friability results showed that ali formula- 69.25 ±2. l and 73.30 ± 1.8% of MA was released from tions the Ph. Eur. fourth ed. requirements [l]. formulations A and B, respectively. On the other hand, The release which represent the percent only 39.76± 1.7% ofMA was released from formulation released of pure drug (MA powder) and MA from the Cin 8 h. Although the ratio ofNaAL and CaGL was 1:1 sustained release tablets as function of time are shown in in the formulations A, B and C, the extent and rate of Fig. l(a and b). It is seen from that figure 96.70±2.2% drug release from formulation C was slower of pure drug was released in 2 h. According to release than from formulations A and B (P < 0.001), this could data, while about 50% of MA from formulations A, B, be attributed to the presence ofhigher amount ofNaAL D and E was released in 5 h, only about 20% of MA was and CaGL in formulation C (Table 1). The decreased in released from formulations C and F (Fig. l(b)). When drug release may be explained by the fact that insoluble 100 80 ---- 60 20 40 60 80 100 120 (a) TiME [min.} 100 __.A 90 _._ B --4,-- C 80 -,.-o 70 -+-E -+-F 'o' 60 o w 50 40 ...Jw o::: 30 /~ 20 10 o o 2 4 6 8 (b) TIME [hours) Fig. In vitro release profiles of: (a) pure drug, and (b) mefenamic acid from sustained release tablets. 398 S. Güngör et al. / Il Farmaco 58 (2003) 397-401 purchased from Sigma, USA. Calcium gluconate 5893). 0.2 ml ofthe was diluted to 100 mi with 0.1 (CaGLJ, magnesium stearate and talc were purchased N NaOH and absorbances were determined spectro- from Merek, Germany. Avicel pH 101 was obtained photometrically at 285 nm. Preliminary studies have from Selectchemie AG, Germany and ali other chemi- shown that the presence of the tablet ingredients has no cals were of analytical grade. interference with the spectrophotometric method. The MA contents of tablets were calculated using standard 2.2. Preparation of tablets curve which was plotted in the range of 1-1 O mcg ml - 1 (r2 = 0.998). The experiment for each formulation was The unit formula of the tablet formulations is given in repeated three times. Table 1. The ratio of NaAL (1% w/v 260±35 cps at 25 C) and CaGL in the formulations A, B and C was 2.4. Dissolution studies 1: l, but these ingredients were used in different amounts for each formulation. Formulation D and E were Dissolution studies of the sustained release tablets in prepared adding NaAL and CaGL at the ratios of 1:2 comparison with pure drug (powder MA) were carried and 2: l, respectively. The formulation F was prepared out employing USP 23 basket method at 37 ±0.5 °C without CaGL to assess the influence of CaGL on the [19]. Basket rotational speed was held at 50 rpm. The release of drug. Avicel pH 101 was used as diluent, dissolution medium was chosen as 900 mi phosphate magnesium stearate and talc as lubricants in the all buffer (0.2 M, pH 7.4) containing 0.5% of Tween 80. formulations. Phosphate buffer containing 27.22 g potassium For tablet preparation, MA ( < 63 mesh) and all the dihydrogene phosphate was prepared according to USP auxiliary ingredients except lubricants were mixed in V- 23 [19]. At predetermined intervals (1-8 h), 1 mi samples type mixer for 15 min. Then, talc and magnesium were taken and diluted to 10 ml with 0.1 N NaOH. stearate were added and mixed for a further 5 min. Subsequently, released amount of MA was determined The mixtures were sieved through ASTM sieve (0.710 spectrophotometrically at 285 nm. Each measurement mm). Then, the blends were directly compressed on a was repeated three times for each formulation. single station tablet machine (Korch, Berlin) using 1.3 cm diameter flat-faced punches, to a weight of 500 mg and such a compression force that give tablets with 2.5. Kinetic assessment minimum 5 kg hardness. Ten tablets were weighed one by one and weight variation of tablets were calculated. Drug release mechanism was investigated in compar- Friability of all tablet formulations was determined ison with modellings according to the equations of zero using 20 tablets by Roche Friability Tester. order, first order and Higuchi's square root of time [20,21]. The following plots were made: Q8 versus t (zero 2.3. Mefenamic acid contents of prepared tablets order kinetic model); log( Q0 - Q1) versus (first order kinetic model), and Q1 versus ,Jt (Higuchi's square of Five tablets were powdered and 500 mg of this root kinetic model), where Q1 is the percentage of drug mixture was accurately weighed. It was suspended in released at time, t and Q0 is the initial amount of drug. 50 mi of O. 1 N NaOH and sonicated in the ultrasonic The release constants (k), determination for 30 min. The volume of the suspension was (,2) and sum the weighed squared deviations (SWSD) adjusted to 100 ml with a 0.1 N NaOH and filtered (S&S were calculated by means of a computer programme which was written in Gw-Basic 3. 10 for the kinetic Table 1 assessment of the dissolution data. The percent of The unit formula of the prepared tablets released drug were input.
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