S(-)-Carvedilol

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HPLC Method Development and Validation of S( ) Carvedilol from API and Formulations

HPLC Method Development and Validation of S( ) Carvedilol from API and Formulations

like heart, lungs, liver, kidneys and is metabolized faster than R(+)-enantiomer [4]. It possesses calcium channel blocking effect by inhibiting voltage-dependent L-type Ca 2+ in vascular smooth muscle cells [5]. It is also used to treat ischemic heart disease and congestive heart failure [1]. Cardiac hypertrophy is the most dominant pre- dictor for the heart failure and is a homeostatic response to elevate after load which develops due to pressure overload. This can be significantly regressed by S(-)-Carvedilol with less effect on normal heart and liver while the R(+)-Carvedilol possesses significant risk of hepatotoxicity. Therefore the overall cardioprotective action of S(-)-Carvedilol is more and hepatotoxicity is less when compared to that of racemic and R(+)-Carvedilol [6]. In most of the cases, racemic mixtures are more preferred for oral administration than those of the enantiomer be- cause of high cost and difficulty in selective synthesis of one optical isomer [7]. Hence there is a need to develop a validated method for the analysis of S(-)-Carvedilol from API and marketed formulations.
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SPECTROPHOTOMETRIC QUANTIFICATION OF CARVEDILOL IN BULK DRUG AND TABLETS

SPECTROPHOTOMETRIC QUANTIFICATION OF CARVEDILOL IN BULK DRUG AND TABLETS

A sensitive and rapid extractive spectrophotometer method has been developed for the assay of carvedilol in bulk drug and tablets. The method is based on the formation of a chloroform soluble ion-pair complex between carvedilol and bromophenol blue in an acidic medium. The complex shows maximum absorbance at 414 nm. Beer’s law was obeyed in the concentration range of 5-20 μg /ml. Results of analysis were validated statistically and by recovery studies. The proposed method is now simple, new, reproducible, and accurate and successfully employed in routine analysis of carvedilol bulk drug and tablet dosage forms.
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Formulation Development and  In-vitro Evaluation of Sustained Release Tablets of Carvedilol Solid Dispersion

Formulation Development and In-vitro Evaluation of Sustained Release Tablets of Carvedilol Solid Dispersion

In the present work, an attempt was made to formulate sustained release tablets of Carvedilol by solid dispersion technique for improving solubility of Carvedilol using Poloxamer 407 and PVP K30. The carvedilol tablets were prepared by direct compression method using HPMC K15 as sustained release polymer in different concentrations. The prepared tablets were evaluated for various physicochemical parameters, In-vitro drug release study was carried out in simulated gastric fluid (0.1 N HCl) for the first 2 hr and in phosphate buffer (pH 6.8) for the next 12 hr following USP Type II paddle apparatus. Increase in HPMC concentrations resulted in a significant decrease in Carvedilol release. For instance, the tablets containing 20mg of HPMC K15 (F1 and F4) shows 97% drug releaseupto12hr when compared to 40mg and 60mg 0f HPMC K15 (F2, F3, F5 and F6)shows 98% drug release upto 14hr. The in-vitro data is fitted in to different kinetic models like Zero order, First order, Korsmeyer and Higuchi’s plot. The release of Carvedilol from tablets containing solid dispersions of Poloxamer 407 and PVP K30 were shown early t 50%
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FORMULATION AND EVALUATION OF FLOATING OSMOTIC DELIVERY SYSTEM OF CARVEDILOL

FORMULATION AND EVALUATION OF FLOATING OSMOTIC DELIVERY SYSTEM OF CARVEDILOL

Floating osmotic delivery system is a combination of floating and osmotic systems that provides site specific and controlled drug release. Carvedilol is non- selective β blocker under bio pharmaceutical classification system (BCS) class II is widely used in the treatment of hypertension. Half-life of model drug is 6-8 h. The model drug showed promising pharmacokinetics and physico - chemical properties required for controlled releases dosages. Therefore this drug was selected for present investigation. Floating drug delivery system was developed initially by formulating the osmotic core tablet followed by multilayer coating for floating the system. Core tablet comprised of Carvedilol, Mannitol, and sodium bicarbonate which was coated with cellulose acetate (osmotic layer), followed by coating of floating layer with Hydroxyl propyl Methyl cellulose (E15 / E50) and sodium bicarbonate and further coated with entrapment layer composed of Eudragit RL30D.The drug and polymers were characterized by DSC and pre-compression like bulk density, tapped density and Hausner’s ratio. The prepared tablets were evaluated for physical properties like floating lag time, duration of floatation. Invitro studies revealed that drug release depends on concentration of polymer, agitation speed and pH of the medium. From the results, it indicated that formulation were intact. Floating lag time and floating time were dependent on hydroxyl propyl methyl cellulose grade used in floating layer and coating percentage on entrapment layer. Drug release was controlled by changing the amount of mannitol in the core tablets.
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CARDIOPROTECTIVE EFFECT OF IVABRADINE VERSUS CARVEDILOL IN RATS

CARDIOPROTECTIVE EFFECT OF IVABRADINE VERSUS CARVEDILOL IN RATS

ABSTRACT: The discovery of the f-channel and its role in regulating pacemaker activity lead to the development of new pharmacological agents such as ivabradine, which target these f-channels causing a reduction in heart rate by inhibiting the /fcurrent. The aim of the present work was designed to evaluate the cardioprotective effect of ivabradine on experimentally- induced myocardial infarction and adrenaline-induced arrhythmia in rats. In addition, the present work studied the effect of ivabradine on isolated rabbit's aortic spiral strip and isolated rabbit's heart. Acute myocardial infarction in rats was induced by isoperameline (150mg/kg subcutenous injection, once) 24 rats were divided into the following groups: group (1) control normal rats, group (II) myocardial infarction – induced rats with no previous treatment, group (III) myocardial infarction – induced rats pretreated with ivabradine (10mg/kg/day) for one week and group (IV)) myocardial infarction – induced rats pretreated with carvedilol (1mg/kg/day) for one week. Electrophysiological, biochemical and histopathological parameters were estimated. pretreatment with either ivabradine or carvedilol show significant improvement in all these parameters with insignificant difference between them. In the current work 20 rats were used to investigate the protective effects of ivabradine (10mg/kg) and carvedilol (1mg/kg) on adrenaline- induced arrhythmia in anaesthetized rats and the results revealed that both drugs had a prophylactive effect. Also data obtained in the present work pointed out that ivabradine in gradually increasing doses produce no significant effect on the isolated rabbit's aortic strip and basal myocardial contractility of isolated rabbit's heart. Both ivabradine and carvedilol have cardioprotective effect against acute MI as well as adrenaline- induced arrhythmia with no significant difference between them, also ivabradine has no effect on contractility of the heart. So, the choice of either drug in these disease states depend on which of them has low side effects.
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A New and Alternate Synthesis of Carvedilol: An Adrenergic receptor

A New and Alternate Synthesis of Carvedilol: An Adrenergic receptor

Preparation of 4-(oxiran-2-ylmethoxy)-9H-carbazole, (4). To a stirred solution of (300 mL)water and sodium hydroxide (22.9 g, 0.573 Mole), 9H-carbazol-4-ol, 3 (100 g, 0.546 Mole) was added over 10 min followed by drop wise addition of (150 mL) DMSO over 30 min at 15 °C. After 10 min, to this solution is added epichlorohydrin (75.7 g, 0.818 mole) at 15 °C over 1 hr. The suspension is placed in a constant temperature bath at 50 °C and the mixture is stirred for 8.0 hr. After completion of the reaction, water (400 mL) was added, filtered and washed with water. The crude product was recrystallised in isopraponal gave glycidyl aryl ether, 4 as a pale brown solid; yield 76.6%; mp 121-126°C; 1 H NMR (DMSO): δ 11.3 (s, 1H), 8.16 (d,1H), 7.3 (m, 1H), 7.3 (m, 1H), 7.46 (d,1H), 7.18 (t, 1H), 7.1 (d, 1H), 6.9 (d, 1H), 4.1 (m, 2H), 3.3 (m, 1H), 3.0 (m, 2H). MS: m/z (M + +1) 240; IR (KBr): ν 3296, 2928, 1609, 1509, 1099, 725 cm -1 .
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FORMULATION DEVELOPMENT AND EVALUATION OF BUCCAL FILMS OF CARVEDILOL

FORMULATION DEVELOPMENT AND EVALUATION OF BUCCAL FILMS OF CARVEDILOL

Carvedilol is a non-selective and - adrenergic antagonist with no intrinsic sympathomimetic activity widely used to treat essential hypertension and angina pectoris. Although it is completely absorbed from the gastrointestinal tract, the systemic availability is approximately 25-35% because of high first-pass metabolism. Carvedilol was selected as a model drug for the present investigation because of its oral therapeutic dose is low (6.25 - 25 mg), it’s having low molecular weight (406.48) 5, 6 . A suitable buccal drug delivery system should be flexible and possess good bioadhesive properties, so that it can be retained in the oral cavity for the desired duration. In addition, it should release the drug in a predictable manner to elicit the required therapeutic response.
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DEVELOPMENT AND EVALUATION OF NANOEMULSION FORMULATIONS FOR IMPROVED ORAL DELIVERY OF CARVEDILOL

DEVELOPMENT AND EVALUATION OF NANOEMULSION FORMULATIONS FOR IMPROVED ORAL DELIVERY OF CARVEDILOL

The higher pH value in the formulations of carvedilol nanoemulsions was (6.23) for NEA3 and this pH value is suitable for oral administration. Zeta potential of different formulations was calculated to explain the electro kinetic potential in colloidal dispersions. The results of zeta potential of carvedilol nanoemulsions were in range -18.34 mV to -26.47 mV). According to rule of thumb, the values of zeta potential which are: range -5 mV to +5 mV indicate fast aggregation, about -20 mV or +20 mV provide short term stability, above +30 mV or below -30 mV indicate a good stability and above +60 mV or below -60 mV offers excellent stability 24 . The results of drug content in nine formulations of carvedilol loaded nanoemulsions were in range (92.1- 98.9%). The higher percent of drug content (99.04 %) was found in NEA4 that has S mix (1:1), and the lowest percent of drug content (96.48 %)
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 VALIDATED SPECTROPHOTOMETRIC METHODS FOR THE DETERMINATION OF CARVEDILOL IN TABLETS

 VALIDATED SPECTROPHOTOMETRIC METHODS FOR THE DETERMINATION OF CARVEDILOL IN TABLETS

Carvedilol bulk powder was kindly gifted by Ipca Lab. Ltd. Mumbai, India. The pharmaceutical formulation was procured from the local market.Millipore’s distilled water (Millipore, USA), Concentrated Hydrochloric Acid (AR Grade, S. D. Fine Chemicals Lts., Mumbai, India) and Whatman filter paper no. 41 (Whatman International Ltd., England) were used in the study.

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FORMULATION AND EVALUATION OF MOUTH DISSOLVING TABLETS OF CARVEDILOL

FORMULATION AND EVALUATION OF MOUTH DISSOLVING TABLETS OF CARVEDILOL

Preformulation Study: The objective of pre formulation studies are to develop a portfolio of information about the drug substance, so that this information useful to Develop formulation. Organoleptic Characteristics, Solubility, Bulk Density, Tapped Density, % Compressibility, Identification of drug Sample, Drug Excipients Compatibility study. Carr‟s Index [Compressibility Index] And Hausner‟s Ratio- Carr‟s index and Hausner‟s ratio measure the propensity of powder to be compressed and the flow ability of powder. Carr‟s index and Hausner‟s ratio can be calculated from the bulk and tapped density.
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Effect of particle size on oral absorption of carvedilol nanosuspensions: in vitro and in vivo evaluation

Effect of particle size on oral absorption of carvedilol nanosuspensions: in vitro and in vivo evaluation

A pharmacokinetic study was performed in beagle dogs to assess the absorption efficiency of carvedilol suspensions. Following oral administration, there were significant differ- ences in pharmacokinetic profiles among the commercial tablets, the microsuspension and nanosuspension capsules. The plasma concentration–time profiles of carvedilol are presented in Figure 6, and the pharmacokinetic parameters are displayed in Table 2. As expected, significant increase in absorption was observed with the nano- and micro- suspensions. In contrast with carvedilol coarse suspen- sions (the commercial tablets), the nanosuspensions and microsuspensions had higher C max (2.09- and 1.48-fold), AUC 0–t (2.11- and 1.51-fold), and shorter T max (0.34- and 0.48-fold) (all P,0.05). Furthermore, enhanced absorption was observed with the nanosuspensions as compared with the microsuspensions. These findings were in accordance with the results from the in vitro dissolution and the in situ single-pass perfusion tests, indicating that the differences in carvedilol absorption are primarily attributed to the dissolu- tion and intestinal absorption behavior of carvedilol with different particle sizes. Meanwhile, the direct uptake of the nanoparticles by mechanisms involving M-cells in Peyer’s patches of the gastrointestinal lymphoid tissue, thus avoid the first-pass metabolism effect, which is primarily responsible for the low bioavailability of carvedilol. Furthermore, the rapid absorption could attribute to the increased aqueous solubility and the size effect of carvedilol.
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FORMULATION AND EVALUATION OF BUCCOADHESIVE BILAYERED TABLETS OF CARVEDILOL

FORMULATION AND EVALUATION OF BUCCOADHESIVE BILAYERED TABLETS OF CARVEDILOL

Carvedilol (99.96% purity), were gift samples from Dr.Reddy’s Labs Ltd, Hyderabad, India. Hydroxy propyl methyl cellulose (HPMC K4M), Sodium carboxymethylcellulose (SCMC, 400 cps), Carbopol-934 (CP), ethyl cellulose and D-mannitol (S.D. Fine Chemicals, Mumbai, India) were obtained from commercial sources. All other reagents and chemicals used were of analytical reagent grade.

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 FORMULATION DEVELOPMENT AND EVALUATION OF CARVEDILOL TABLET

 FORMULATION DEVELOPMENT AND EVALUATION OF CARVEDILOL TABLET

According to USP 32-NF27, Conventional compressed tablets that loose less than 0.5 to 1 % of their weight are generally considered acceptable. In all batches (B01-B09), core and coated tablets were disintegrated within 2 minutes (Figure 4). Formulation Batch 04 showed the lowest disintegration time (15 sec) where as formulation batch 09 showed the highest disintegration time (1 min. 50 Sec). After coating the weight gain achieved was 3.11 % w/w with 1 minute 32 seconds as the disintegration time of coated tablets. The dissolution performance of the tablets in batch B09 was similar to that of the RLD where the formulation with 1.51 % crospovidone was used. Stability showed that, there was no change in product’s physical properties with little bit change in disintegration time. Dissolution also reduced in some batches insignificantly. The drug content remained almost same after 3 and 6 months. The assay of Carvedilol 25 mg tablet found 25.06 mg to 24.092 mg / tablet for accelerated condition which is under pharmacopoeias limit.
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“Solubility and Dissolution Enhancement of Carvedilol by Solid Dispersion Technique Using Gelucire 50/13” by Shinkar Dattatraya Manohar, Dhake Avinash Shridhar, Setty Chitral Mallikarjuna, India.

“Solubility and Dissolution Enhancement of Carvedilol by Solid Dispersion Technique Using Gelucire 50/13” by Shinkar Dattatraya Manohar, Dhake Avinash Shridhar, Setty Chitral Mallikarjuna, India.

Solid dispersions in water-soluble carriers have attracted considerable interest as a means of improving the dissolution rate and hence possibly bioavailability, of a range of hydrophobic drugs. Inclusion behavior of gelucire 50/13 was studied towards carvedilol, an antihypertensive agent in order to develop mucoadhesive oral dosage form with enhanced dissolution rate and bioavailability, following gelucire carvedilol solid dispersion. The present work was investigated to examine the release of carvedilol from various molecular weight fractions of gelucire solid dispersions. Solid dispersions of carvedilol were prepared in different molar ratios of drug: carrier by using solvent evaporation and melting methods. The physical mixture and solid dispersion (s) were characterized for drug-carrier interaction, drug content, solubility and dissolution rate. The release rate of carvedilol from the resulting complexes was determined from dissolution studies by use of USP dissolution apparatus 2 (paddle method). The physical state and drug: gelucire interaction of solid dispersions and physical mixtures were characterized by X-ray diffraction (XRD), Infra Red Spectroscopy (IR) and Differential Scanning Calorimetry (DSC). The dissolution rate of carvedilol was increased significantly in all of the solid dispersion systems compared to that of the pure drug and physical mixtures. The solid dispersion prepared in the molar ratio of 1:2 by the solvent evaporation method was found to have the fastest dissolution profile.
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FORMULATION AND EVALUATION OF IMMEDIATE RELEASE TABLET OF CARVEDILOL WITH NATURAL SUPERDISINTEGRANT AND SYNTHETIC DISINTEGRANTS

FORMULATION AND EVALUATION OF IMMEDIATE RELEASE TABLET OF CARVEDILOL WITH NATURAL SUPERDISINTEGRANT AND SYNTHETIC DISINTEGRANTS

From the present research it was concluded that formulatedimmediate release tablets of Carvedilol with Fenugreek seed mucilage exhibited good physical parameters. The overall results indicated that formulation F6 and F3with (Fenugreek seed mucilage and Crospovidone) (7.5%) had a higher edge compared to other formulations containing superdisintegrants. They satisfy all the criteria for immediate release tablets. With the progress in the formulation of rapid disintegrating tablets, now it is possible to formulate these tablets with reduced quantity of superdisintegrants. Rapidly disintegrating dosage forms have been effectively commercialized by using numerous types of super disintegrating agents. By the use of many and different types of super disintegratingagent’s patient compliance, commercial and therapeutic benefits have enhanced. At a time when researchers are faced with increasing amounts of poorly soluble drugs, it is very important to select super disintegrating agents that maximize drug dissolution. Due to fast acceptance of RDTs by patients and pharmaceutical companies, the market of this dosage form is growing and the product pipeline quickly, but without the field of super disintegrating agents it would not have been possible.
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PREPARATION AND PHYSICO-CHEMICAL CHARACTERIZATION OFCARVEDILOL- POLY (LACTIDE-CO-GLYCOLIC ACID) LOADED NANOPARTICLES.

PREPARATION AND PHYSICO-CHEMICAL CHARACTERIZATION OFCARVEDILOL- POLY (LACTIDE-CO-GLYCOLIC ACID) LOADED NANOPARTICLES.

The entrapment efficiency (EE) and loading capacity (LC) were estimated by reverse phase High performance liquid chromatography (RP- HPLC) method. The drug loaded nanoparticles solution of 1 mg/ml was prepared in mobile phase and 20 µl of the sample was injected manually to HPLC equipped with Shimadzu LC-20AD PLC Pump and SPD-M 20 A PDA detector. The output signal was monitored and integrated using Shimadzu Class-VP version 6.12 SPI software. The chromatographic separation was achieved by using Phenomenex 150 x 4.6 mm, 5µm (X-Terra; C18) analytical Column. The mobile phase used to consist of acetonitrile: acetate buffer pH 3.0: water (75:600:325) was passed through 0.45 µm membrane filter and degassed by ultrasonication. The flow rate was maintained at 1.0 mL/min and the measurement was made at 240 nm. The column was maintained in ambient condition using thermostat. The amount of the carvedilol in the sample was determined from the peak area correlated with the standard curve. The standard curve was prepared under the same identical condition.
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 FORMULATION AND EVALUATION OF BUCCAL PATCHES OF CARVEDILOL PHOSPHATE

 FORMULATION AND EVALUATION OF BUCCAL PATCHES OF CARVEDILOL PHOSPHATE

Infra red spectroscopy can be used to investigate and predict any possible physicochemical interactions between different components in a formulation and therefore, it can be applied to the selection of suitable, chemically compatible excipients. The aim of the present study was to find out the possible interaction between the selected polymer chitosan and the drug carvedilol and also to identify the compatibility between the drug and the polymer.

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The evaluation of β-adrenoceptor blocking agents in patients with COPD and congestive heart failure: a nationwide study

The evaluation of β-adrenoceptor blocking agents in patients with COPD and congestive heart failure: a nationwide study

β -Blocker nonusers were defined as patients who used any β -blocker ,90 days after the index date. β -Blocker users were defined as patients who used any β -blocker .90 days after the index date. The study subjects were further assigned to groups according to the average daily dose of β -blockers in each 90-day period, which was treated as a time-dependent covariate. Patients were classified into three categories according to their medication dose. The group of nonusers was further divided into carve- dilol ,3.125 mg/day, bisoprolol ,0.625 mg/day, and metoprolol ,25 mg/day subgroups. The low-dose groups consisted of the carvedilol $3.125 and ,6.25 mg/day, bisoprolol $0.625 and ,1.25 mg/day, and metoprolol $25 and ,50 mg/day subgroups. The high-dose groups included the carvedilol $6.25 mg/day, bisoprolol $1.25 mg/day, and metoprolol $50 mg/day subgroups. Baseline characteristics included age, sex, number of HF and COPD exacerbation patients in the past year, HF and COPD exacerbation rate in the past year, comorbidities, and co-medications. Comor- bidities were identified if two diagnoses were coded for an outpatient visit or if one diagnosis was coded during an inpatient visit 1 year before the index date. Co-medications were identified if they were used longer than 30 days.
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Controlled release tablet formulations of carvedilol

Controlled release tablet formulations of carvedilol

The present investigation was undertaken with an objective of formulating controlled release (CR) oral matrix tablet formulations of Carvedilol (CAR), an antihypertensive using cellulose ether polymer, Hydroxy Propyl Methyl Cellulose (HPMC K4M, HPMC K15M) of different viscosity grades as drug release retardants. The tablets were prepared by direct compression technique and evaluated for various physico-chemical/mechanical parameters. Based on the viscosity and gel formation during dissolution, HPMC K4M was selected as release retardant. The effect of different fillers like Avicel PH 101, Avicel PH 105 and Avicel PH 200 (microcrystalline cellulose), pre gelatinized starch (PGS), maize starch with spray dried lactose (FLOWLAC) on CAR release was studied and percent release of CAR at the end of 24h is in the order of FLOWLAC > Avicel PH 101 > Avicel PH 105 > Avicel PH 200 > PGS. Based on the dissolution data obtained with different fillers and keeping in view of the results from the pre-compression studies, and gel layer retaining with the matrix tablets, Avicel PH 105 was selected to carry out further formulation development. The formulation containing 25%w/w HPMC K4M as release retardant and Avicel PH 105 gave 96.59 ± 3.1% release at the end of 24h and fulfils regulatory requirement. The dissolution data was also evaluated for drug release kinetics and mechanism.
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FORMULATION AND EVALUATION OF CARVEDILOL TRANSDERMAL PATCHES WITH HYDROPHILIC POLYMERS

FORMULATION AND EVALUATION OF CARVEDILOL TRANSDERMAL PATCHES WITH HYDROPHILIC POLYMERS

The purpose of this research work was to develop and evaluate transdermal patches of Carvedilol employing different ratios of hydrophilic polymers by solvent evaporation technique. The main objective is to avoid first pass effect and to improve bioavailability. The physicochemical compatibility of the drug and the polymers was studied by infrared spectroscopy. The results suggested no physicochemical incompatibility between the drug and the polymers. Nine formulations consisting of Hydroxy propyl methyl cellulose k4M, Sodium c mc, xant han gum, in the ratios 1:1, 1:2, 1:3 were prepared. The prepared TDDS were evaluated for in vitro drug release, moisture absorption, moisture loss and mechanical properties. The patches coded as F 1 , F 2 , F 3 (HPMCk4m) showed maximum
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