The objective of the present study was to develop theophylline and salbutamol sulphate matrix tablet for sustained release combined dosage form, for treatment of chronic obstructive pulmonary disease. Simultaneous equations were formed to calculate the concentration values of theophylline and salbutamol sulphate and drug compatibility studies were established through Infrared and Differential Scanning Calorimetry studies. The matrix tablets were prepared by wet granulation method using hydroxypropyl methylcellulose K4M and K15M in various percentages. The granules showed satisfactory flow properties and compressibility. All the five tablet formulations showed acceptable pharmacotechnical properties and complied with the in-house specifications for tested parameters. The results of formulation FH-3 (20% hydroxypropylmethylcellulose of grade K15M and K4M in 1:2 ratio) could extend the release of theophylline and salbutamol sulphate up to 12 h and was found comparable to marketed sustained release tablet. Model fitting analysis for formulation FH-3, theophylline fitted in the Zero order and Korsmeyer-Peppas model, while salbutamol sulphate fitted in the Zero order model. Scanning Electron Microscopy studies of FH-3 indicates good swelling and gel formation property of hydroxy propyl methyl cellulose, supporting the drugs release followed both diffusion and erosion mechanism. Successful formulation was found stable after evaluation for physicochemical parameters, kept for 30 d at 25° /60% RH and 40°/75% RH.

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Two simple, accurate and precise methods for simultaneous estimation of pioglitazone hydrochloride and glimepiride in combined dosage form have been described. First method employs formation and solving of simultaneous equation using 268.6 nm and 227.6 nm as two analytical wavelengths. Second method is absorbance ratio method, 268.6 nm for estimation of pioglitazone hydrochloride and 251.5 nm, isobestic point, where two drugs shows equal absorptivity, for the estimation of glimepiride. Both the methods allow the simultaneous determination of pioglitazone hydrochloride and glimepiride in the concentration ranges employed for this purpose. The result of analysis has been validated statistically and by recovery studies and assay of tablets with standard deviation < 1.0% was found.

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Two simple, fast, convenient, precise, reproducible UV spectrophotometric methods have been developed for the determination of carvedilol in pure form in tablets using methanol (method A) and polyethylene glycol-400: water (2:1) (method B). The UV spectrum of carvedilol showed absorption maxima at 242 nm and 245 nm, respectively in methanol and PEG-400:water (2:1). Good agreement with Beer's law was found in the range of 2 to 20 μg/ml for method A and 1 to 10 μg/ml for method B.

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Simple UV and first derivative spectrophotometric methods have been developed for the determination of etoricoxib in bulk drug and its pharmaceutical formulations. In simple UV spectrum of etoricoxib in 0.1 N sodium hydroxide, it exhibits absorption maxima (λmax) at 284 nm where as in first derivative spectrum it shows maxima at 301.0 nm and minima at 266.8 nm. Both the methods were found to be simple, economical, accurate, reproducible and can be adopted in routine analysis of etoricoxib in bulk drug and its pharmaceutical formulations.

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Mucoadhesive buccal films of diltiazem hydrochloride were prepared by solvent casting technique using sodium carboxymethylcellulose, polyvinyl pyrrolidone K-30 and polyvinyl alcohol. Prepared films were evaluated for their weight, thickness, surface pH, swelling index, in vitro residence time, folding endurance, in vitro release, permeation studies and drug content uniformity. Films exhibited controlled release over more than 6 h. From this study it was concluded that the films containing 20 mg diltiazem hydrochloride in polyvinyl alcohol 10% and polyvinyl pyrrolidone 1% w/v (formulation F5), showed moderate swelling, a convenient residence time and promising drug release, thus can be selected for the development of buccal film for potential therapeutic uses.

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Total alkaloids (calculated as reserpine) from various samples of Rauwolfia serpentina root powder and its marketed formulation were estimated by spectrophotometric method using ion-pair complexation of acid dye (methyl orange) with the alkaloids. The complex was selectively extracted in to chloroform and by treatment with hydrochloric acid, the dye was liberated from the complex. The pink colour of the liberated dye is proportional to the amount of alkaloids which was measured at 530nm. The method adopted for extraction of alkaloids from samples has the advantage of extraction of mainly the alkaloids and not the other interfering substances. All the alkaloids extracted in this method were found to form complexes with the dye under the experimental conditions. Beer's law was obeyed between 5-40 μg/ml. The method was found to be simple, sensitive and accurate. It could be applied to formulations containing Rauwolfia and found suitable for routine quality control purposes.

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Leaves of Cadaba indica, family Capparidaceae were extracted with petroleum ether, chloroform, ethanol and water. The crude extracts were investigated for its antibacterial activity against Escherichia coli, Staphylococcus aureus, Bacillus subtilis and antifungal activity against Candida albicans, Candida krushi. The extracts showed significant antibacterial and antifungal activity in the order ethanol, water, chloroform, petroleum ether against all the microorganisms tested and the effect so produced was compared with the standard drugs ampicillin and cotrimoxazole. However, the antibacterial, antifungal activity of the ethanol extract of the leaves was found to be most effective against all the organisms.

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The study was undertaken with an aim to investigate the ability of native sugars (e.g. glucose, fructose and sucrose) to induce crosslinking of gelatin for the preparation of modified release microspheres of diclofenac sodium. The microspheres were prepared by emulsion crosslinking method and they were evaluated for drug content, in vitro drug release and size analysis. The results of preliminary trials revealed that the parameters such as drug to gelatin ratio, volume of light liquid paraffin and stirring rate were found to affect the morphology and in vitro drug release, of microspheres. The microspheres crosslinked with glucose showed highest drug content, good yield and lowest burst effect. The evidence of glucose mediated crosslinking of gelatin was confirmed by DSC. A 32 fuII factorial design was adopted to investigate the joint influence of two variables, amount of glucose (X1; 1,1.5 or 2 g) and concentration of gelatin (X2; 10,15 or 20% w/v) on the percentage drug released in 60 min (Y60) and the time required for 80% drug dissolution (t80) while keeping the other variables constant. The results of multiple linear regression analysis revealed] that for obtaining modified drug release up to 12 h, the microspheres should be prepared using higher level of glucose and middle level of gelatin. Response surface plots are presented to show the effects of X1 and X2 on Y60 and t80. The drug release pattern fitted well to Korsmeyer and Peppas model indicating anomalous diffusion. An equation was generated by adopting multiple linear regression analysis, for predicting the drug dissolution profile for a check point. Good agreement was observed between the predicted and observed drug dissolution profiles. The results suggest that native glucose could be an interesting agent to crosslink gelatin for obtaining modified release of diclofenac sodium from the microspheres.

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A new spectrophotometric method for the simultaneous and individual estimation of amoxycillin and cloxacillin in binary tablet formulations has been described. The method based on the estimation of one drug in presence of another drug by absorbance difference method.

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A simple, accurate and reproducible HPLC method for the determination of betacarotene in the ripe fruit juice of Passiflora edulis Sims was developed. The method involves separation of betacarotene using an isocratic mobile phase consisting of acetonitrile, methylene chloride and methanol in the ratio of 82:12:16 at 436 nm using photo diode assay detector. The sensitivity was found to be 0.25 mg. The betacarotene content of 3.21%w/v was observed in test sample. The calibration curve was linear in the range of 0.25 mg to 2.50 mg with correlation co-efficient of 0.987998 indicating good linearity between concentration and area. The method provides good resolution and separation of betacarotene from other constituents of total carotenoids. An average recovery of 99.08% w/w shows the reliability and suitability of the method.

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Chitosan has been chemically modified by treating with two different aldehydes viz acetaldehyde and propionaldehyde to form Schiff's bases. Schiff bases of chitosan with acetaldehyde and propionaldehyde were named as polymer-l and polymer-II, respectively. FTIR confirmed the reaction carried out on chitosan. Chemically-modified chitosan and plain chitosan were compared for the film forming capacity, swelling property and water permeability rate. Further, the films were incorporated with antiasthmatic drug, salbutamol sulphate by mixing with polymer solution during casting. Drug loading and permeation characteristics were compared for plain chitosan and chemically modified chitosan. Films produced were transparent, smooth and flexible without plasticization. Water permeability for chitosan was 1.13X10-4 g.cm2/day. It was found to be 8.10x10-4 and 5.18x10-4 g.cm2/day for polymer-I and polymer-II, respectively. Percentage entrapment of salbutamol sulphate in the membranes of plain chitosan, polymer-I and polymer-II was 1.22, 1.83 and 1.40 mg/cm2, respectively. The time taken for permeation of 50 % of drug (T50) through excised rat skin was 118, 62 and 88 min for chitosan, polymer-l and polymer-ll, respectively.

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Celecoxib, a COX-2 inhibitor, useful in the relief of symptoms of rheumatoid arthritis, suffers from the draw back of poor aqueous solubility, thereby giving problems during formulations and in achieving good oral bioavailability. The present paper attempts at preparing three formulations of celecoxib in conjunction with β-cyclodextrin for the purpose of solubility enhancement of the drug. The formulations were tested in different media (water, 0.1 N HCI, phosphate buffer pH 7.4). Phosphate buffer was found to be the most suitable amongst the three with good discriminating power. The formulations were compared with two marketed capsule samples of celecoxib. A marked enhancement in the dissolution of celecoxib from the laboratory made formulations was observed as compared to the marketed preparations.

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The ethanol extract of dried leaves of Artocarpus heterophyllus Lam. and different crude fractions such as petroleum ether (40-60°), butanol, butanone and methanol were tested for various phytoconstituents and screened for wound healing properties using incision, excision and dead space (granulation) wound models in albino rats. The methanol fraction had exhibited the most significant wound healing property followed by butanol, butanone fractions and ethanol extract, where as petroleum ether fraction was least effective.

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The fresh as well as dried rhizome of ginger, Zingiber officinale Roscoe is widely used in the traditional system of medicine. We have studied the effect of fresh juice of Z.officinale (4 ml/kg) and methanolic extract (0.5 g/kg ) administered orally daily for 6 w on streptozotocin induced noninsulin dependent diabetic rats (90 mg/kg, i.p. single dose). Diabetes produced a significant increase in fasting glucose levels that was associated with increase in insulin levels. Treatment with Z.officinale produced a significant decrease in fasting glucose and increase in insulin levels levels in non-insulin dependent type diabetes mellitus rats. In oral glucose tolerance test treatment with Z. officinale was found to significantly (P<0.05) decrease Area Under the Curveglucose and increase Area Under the CurveInsulin values in diabetic rats. Treatment with Z.officinale also produced decrease in serum cholesterol, serum triglyceride levels and decrease in blood pressure in diabetc rats. Our data suggest a potential antidiabetic activity of the Z.officinale in non-insulin depaendent diabetes mellitus model of diabetic rats.

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To investigate the therapeutic applications of immuno microspheres containing cytotoxic agent in affinity-chemotherapy, Methotrexate-loaded microspheres of size ranging from 1 to 3 pm were prepared by emulsion cross-linking method. The drug-incorporated microspheres were conjugated with mouse monoclonal antibodies. In vitro cytotoxicity studies using Hep-2 cells were done and it was found that the Methotrexate immuno microspheres had more affinity towards recognizing and binding to the Hep-2 cells when compared to methotrexate microspheres. In vivo studies were done using mice and the targeting efficiency of the formulations to lungs, liver and kidney was studied. The efficacy of the formulations for their anti-tumour activity was also studied against the Dalton as cites lymphoma cell-induced tumour in mice. Various parameters like weight gain, percentage tumour weight inhibition, and packed cell weight were studied. Our results showed that the methotrexate immuno microspheres group was more therapeutically efficient in terms of better affinity and binding capacity than methotrexate microspheres and free methotrexate in protecting the mice from carcinoma.

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The simple, accurate and precise Vierodt's and Q-analysis UV Spectrophotometric method has been developed for the simultaneous determination of valdecoxib and tizanidine in combined tablet dosage form. Shimadzu UV-1601 instrument was used and the λmax of valdecoxib and tizanidine was found to be 237 nm and 319 nm, respectively. In Q-analysis, the isoabsorptive point for both the drugs was found at 289.5 nm. The linearity range lies between 5-30 μg/ml for valdecoxib and 0.5-3 μg/ml for tizanidine at their respective wavelengths.

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Nimesulide sustained release suppositories were formulated by 23 full factorial design using polymers such as agar, polyethylene glycol-6000 and sodium carboxymethylcellulose. The unconventional non-melting, non-disintegrating suppositories were prepared using fusion method and their in vitro release kinetics were studied. Physical characteristics such as dimensions, homogeneity, crushing strenyth and drug content uniformity were evaluated. Among the various formulations, formulation (N3) with agar (6%), polyethylene glycol-6000 (4%) and sodium carboxymethylcellulose (1.5%) showed maximum drug release (93.69%) by concentration independent manner.

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Supercritical fluid extraction is two-step process, comprising of feed of fluid into extraction vessel at above its critical temperature and critical pressure and depressurization of fluid after extraction. Supercritical fluid has both gas like properties (diffusivity, viscosity and surface tension) and liquid like properties (density and solvating power), which are favorable for diffusion coefficient as well as mass transfer. Carbon dioxide is most useful supercritical fluid (Tc=31° and Pc=74 bars) as it is safe, inexpensive, non-toxic, non-inflammable, inert to materials and solvating strength is adjusted by modifier (methanol) as well as extraction parameters (time, temperature and pressure). Supercritical fluid extraction is useful in extraction, separation and refining, cleaning and disinfection, synthesis and processing, optimization of drug particles and environmental application such as soil remediation and treatment of municipal waste.

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A simple Reverse phase liquid chromatographic method has been developed and subsequently validated for simultaneous determination of metoprolol tartrate and hydrochlorthiazide in combination. The separation was carried out using a mobile phase consisting of acetate buffer of pH 5.0 and acetonitrile in the ratio 80:20.The column used was Lichrosphere C-18 with flow rate of 1.0 ml/ min and UV detection at 254 nm. The described method was linear over a concentration range of 300-700 μg/ml and 40-80 μg/ml for the assay of metoprolol tartrate and hydrochlorothiazide, respectively. The mean recovery was found to be in the range of 99-102%. The obtained results confirmed that the method is highly suitable for its intended purpose of separation of metoprolol tartrate and hydrochlorthiazide and its simultaneous determination in formulation.

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The leaf callus of Convolvulus microphyllus was initiated and developed in Murashige and Skoog medium supplemented with 2,4-dichlorophenoxyacetic acid, 6-benzyl adenine, indole acetic acid and kinetin (1 ppm each). High pressure liquid chromatographic method using UV detector has been developed for the estimation of scopoletin in methanolic extracts of leaf and its calli. The method is simple, precise, accurate, specific and less time consuming for the estimation of scopoletin in crude drugs.

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The study was carried out to assess prescribing practice and general trend of hypertension among patients at Orange City Hospital and Research Institute, a tertiary critical care hospital, Nagpur. Prescription and complete records of hypertensive patients were monitored and data was filled as per WHO prescription auditing proforma. The study revealed that hypertension was mild (diastolic pressure 90-104 mm of Hg) in maximum number of patients (80.0%). Both monotherapy (55.0%) and combination therapy (45.0%) were employed for the patients. Among monotherapy β-blockers and calcium channel blockers were mainly prescribed. Among combination therapy, two-drug combination (23.33%) was most often prescribed and combination of β-blockers and calcium channel blockers was common. Highest prevalence of disease was found in the age group of 50-59 years. The study highlighted the current trend of prescribing antihypertensive drugs in Orange City Hospital and Research Institute, Nagpur.

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A study was initiated with the development and collection of background, structural, process and outcome indicators for a South lndian Jagadguru Sri Shivarathreeshwara Hospital as suggested in the WHO manual, which focuses on the availability, accessibility, and affordability of essential medicines. The information on diseases that are commonly treated in the hospital (key diseases) and medicines that are used to treat such diseases (key medicines) were collected and the availability of these key medicines was assessed. Based on this study it was found that, excess numbers of analgesics, antipyretics, and non-steroidal antiinflammatory drugs (367% more), antiallergics (340% more), anti-bacterials (80% more), antimigraine medicines (75% more), cardiovascular medicines (135% more), dermatological medicines (59% more), diuretics (75% more), gastrointestinal medicines (157% more), psychotherapeutic medicines (322% more), and hormones and other endocrine medicines (58% more) were available in drug store of the hospital. Medicines such as antidotes (64% less), antiinfective (40% less), antiviral (62% less) and immunologicals (50% less) were not available in adequate numbers. However, the availability of key medicines was good (94%). Comparison of affordability of the treatment of enteric fever was performed between ceftriaxone and ciprofloxacin drugs, and basket of food. The cost of treatment using ceftriaxone (Rs.65.4) was 2.1 fold more where as it was 2.3 fold less for cost of treatment using ciprofloxacin (Rs.13.83) when compared to the cost of basket of food (Rs.30.87). In addition to the availability, accessibility and affordability study, cost minimisation and cost effectiveness study was also performed between three medicines viz., atenolol, amlodipine and enalapril which are used in the treatment of hypertension. It was found that atenolol was found to be cost effective drug when compared to amlodipine and enalapril for hypertension.

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Poloxamers/Pluronic block copolymers are recognized pharmaceutical excipients listed in US and British Pharmacopeias. Because of the thermo-reversible gelation property and low toxicity they are widely used in a variety of pharmaceutical formulations including delivery of low molecular weight drugs and high molecular weight polypeptides. This review describes recent reports of applications of poloxamers in drug delivery, gene therapy, tissue engineering and in neuroprotection.

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Two new specific, selective, simple, rapid and inexpensive spectofluorophotometric methods have been developed for the determination of rofecoxib and mosapride citrate in their individual dosage forms. Spectra of rofecoxib in 0.1 N sulphuric acid and mosapride in methanol showed excitation wavelength to be 282 nm and 331 nm while emission wavelength to be 406 nm and 360 nm respectively. Method for rofecoxib was found to be linear over an analytical range of 10-50 ng/ml with correlation coefficient of 0.9990. Limit of detection and limit of quantitation were found to be 1.71 ng/ml and 5.69 ng/ml, respectively for the same method. Method for mosapride was found to be linear over an analytical range of 2-10 ng/ml with correlation coefficient of 0.9996. Limit of detection and limit of quantitation were found to be 0.32 ng/ml and 1.05 ng/ml, respectively for the same method. Both the methods were validated and found to be suitable for estimation of rofecoxib and mosapride from their individual pharmaceutical formulations. Satisfactory recovery from the spiked samples of standard drugs suggests no interference of any excipients present in the formulations.

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A series of some novel compounds 2-(un) substituted-3-amino-5-aryl-6-phenylpyrazolo [3,4-d] pyrimidine-4 (5H)-ones were synthesized by condensation of 2-phenyl-3-aryl-5-cyano-6- thiomethyl pyrimidine-4(3H)-ones independently with hydrazine hydrate/methyl hydrazine/phenyl hydrazine in presence of dimethyl formamide and catalytic amount of anhydrous potassium carbonate. These derivatives were characterized by their spectral data. When evaluated for analgesic activity by hot plate method, compounds 4e, 4i, 4I and 4m exhibited superior activity than Pentozocin hydrochloride at dose of 10 mg/kg. The ED50 values of all thirteen synthesized compounds were determined.

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The in vitro antibacterial activity of the extracts and isolates of Cocculus hirsutus (root) has been studied against Bacillus subtilis and Escherichia coli. The total methanol extract, total alkaloid mixture and the two isolates have shown significant activity against the organisms used, almost comparable with the standard antibiotics, benzyl penicillin and streptomycin: This in vitro testing also resulted in activity guided isolation of two antibacterial principles from the root.

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A quick and reproducible method for radiolabeling of ethionamide, an antitubercular drug, with radioisotope of tecnetium, 99mTc was developed. The radiotracer was evaluated for radiochemical purity, stability, and tissue distribution in normal mice. The 99mTc labeled ethionamide, prepared by using reduced 99mTc demonstrated good labeling efficiency (>85%) and reproducibility. The procedure offers minimum radiation exposure to the radiochemist as handling time is also less. Stannous chloride was used as reducing agent at a concentration of 15 μg/ml at pH 2.0. The radiocomplex was stable till 6 h at 37°. In vitro uptake study of 99mTc labeled ethionamide in Mycobacteria tuberculosis H37RV showed higher uptake in live bacteria. The pharmacokinetic parameters of 99mTc labeled ethionamide, calculated by blood clearance studies in normal New Zealand white rabbits, were found to differ considerably from the native drug. 99mTc labeled ethionamide has low plasma protein binding of approximately 35% and it showed no organ specific accumulation. The radiotracer was f o h d to be a widely and rapidly distributed molecule in the body similar to native drug. Radio labeled ethionamide penetrated all the organs and got cleared off due to short elimination half-life. The scintigraphic studies in infected rabbits confirmed that 99mTc-labeled ethionamide was preferentially taken up by the tubercular lesion.

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Gout is an age-old disease for clinicians, still having many secrets that need to be explored for improving knowledge with respect to uric acid metabolism and monosodium urate crystal-induced inflammation. Despite centuries of study of gout and availability of effective treatment for most patients, the proper diagnosis and treatment are still problematic. In the present review attempts are made to understand various aspects of gout in terms of causes, epidemiology, pathophysiology, site of action for antigout agents, diet, management, treatment, recent innovation and scope for further research.

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Various 4-(substituted aryl)-1-(N-indolyl acetamidyl)-3-chloro-2-azetidinones were prepared by condensing N-(arylidine hydrazidomethyl)-indoles with chloroacetyl chloride. Their structures were established by chemical tests, IR and 1HNMR spectral data. These synthesized compounds were tested for their antibacterial, antifungal, antitubercular and antiinflammatory activities.

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A simple, accurate and sensitive spectrophotometric method has been developed for the estimation of rofecoxib in commercial preparations. The lactone ring in the drug is converted to hydroxy acid by sodium carbonate. 1,4-Napthoquinosulphonic acid acts as oxidizing agent and abstracts hydrogen ion from the hydroxy acid to form brown colored chromogen measured at the wavelength of maximum absorption 440 nm against reagent blank. The chromogen obeyed linearity over 20 to 120 μg/ml (r=0.9998). The method is satisfactorily applied for the analysis of pharmaceutical preparations containing rofecoxib. The results of the analysis were validated statistically and by recovery studies. The recovery ranged between 98.6 and 101.8%.

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