Current Issue : July-September Volume : 2013 Issue Number : 3 Articles : 15 Articles
The objective of this article is to review research works carried for development of topical biodegradable dermal patch including a biodegradable biopolymers to accelerate wound healing. Delays occurred in acute cutaneous wound healing leads to local infections, and transition toward chronic and non-healing wounds. Wound repair and regeneration is a highly complex combination of matrix destruction and reorganization. The aim of this study is to hasten and improve the wound healing activity. Topical applications of compounds with free radical scavenging properties have shown to improve wound healing significantly and protect tissues from oxidative damage. Natural polymers are preferred candidates for designing wound healing patches of therapeutic drugs in treatment of different types of ailments. Chitosan collagen and gelatin are few important biodegradable ingredients that find place in wound healing formulation designing and technology. The polymers that render wound healing properties, the combination of such polymers display desired results....
A cocrystals can be described as a crystalline structure formed by two different or more molecular entities wit weak attractive forces. In crystal engineering, cocrystals technology is an efficient way to modify the character of drugs in solid state and has great potential for improving the physicochemical inadequacies of a drug, such as poor aqueous solubility. Cocrystallization is an emerging stratagem to produce drug substances with desirable preoperties and has remained largely unexplored till recent times. This review go over this highly up-and-coming cocrystals technology, covering basic concepts, cocrystal design and screening, conformer selection, methods of cocrystal preparation and charecterization, applications, scaleup and IPR issues....
The purpose of the current study was to develop a novel taste masked mouth dissolving tablets of Tramadol HCl. Tramadol HCl is an opioid analgesic used for the treatment of moderate to severe pain. Mouth dissolving tablets offer substantial advantages but its crucial aspect is to mask the bitter taste and to minimize the disintegration time. In the present investigation, the bitter taste of Tramadol HCl was masked by three different approaches- solid dispersion, inclusion complex and ion exchange resin. The mouth dissolving tablets were prepared by sublimation technique using camphor as subliming agent. The result revealed faster release profile of Tramadol HCl using sublimation technique. Out of the three approaches utilized, ion exchange resin (Kyron T314) exhibited highest taste masking of Tramadol HCl. Hence it can be concluded that ion exchange resin with sublimation technique demonstrated potentials for taste masking, rapid absorption, improved bioavailability, effective therapy and patient compliance....
Olmesartan medoxomil is an antihypertensive agent which belongs to the class of medicines called angiotensin II receptor antagonists. It acts rapidly to lower high blood pressure. One of the major problems with this drug is its low solubility in biological fluids, which results into poor bioavailability after oral administration. The present study is an attempt to enhance the dissolution rate of olmesartan medoxomil by solvent evaporation techniques using olmesartan medoxomil and β-cyclodextrine and Hydroxypropyl-β-cyclodextrin as carrier in the ratios of 1:1, 1:2, 1:3 and 1:4 respectively. The prepared solid dispersions were characterized for bulk density, tapped density, Carr’s Index, Hausner’s ratio, angle of repose, saturation solubility study, drug content, drug dissolution, hardness, friability, thickness. The solvent evaporation techniques were found to be efficient method to obtained good yield solid dispersions with good flow properties. The drug content was found in the ranges of 99.2±0.28 to 100.8±0.19 %. Dissolution study revealed that there is marked enhancement in the dissolution rate of olmesartan medoxomil from all the solid dispersions when compared to pure olmesartan medoxomil itself. From the in-vitro drug release profile, it can be seen that formulation F8 (1:4 ratio of drug: HP β-cyclodextrine, prepared by solvent evaporation technique) shows higher dissolution rate compared with other formulations....
The aim of the study was to develop extended release matrix tablets of Phenytoin sodium comprising hydrophilic and hydrophobic polymers in different ratios. The matrix tablets were formulated by incorporating combination of Hydroxypropyl methylcellulose K-100 and Ethyl cellulose (7-22 cps) in the concentration range of 2-6%w/w and 6-10%w/w respectively. The optimized formulation was obtained with Hydroxypropyl methyl cellulose (4%w/w) and Ethyl cellulose (8%w/w) in the formulation of matrix tablets. Physical and chemical parameters were evaluated and found within the acceptable limits. In-vitro drug release studies were carried out and mechanism of drug release was predicted using different kinetic models. The optimized formulation showed drug release profile which was within the acceptance criteria specified in USP for Phenytoin sodium extended release dosage forms i.e. less than 30% drug release at 30 mins, 30 - 60 % drug release at 60 mins and more than 60% drug release at the end of 120 mins. Moreover, drug release profiles of all the formulations were compared with the market product and similarity between formulated products and marketed product was determined....
Parenteral antibiotic formulations are sterile formulation to be administered through pierced skin to sufficient depth having advantages of free from hepatic first pass, total bioavailability and fast action but have number of major disadvantages that makes it less susceptible to patients including real/psychological pain, requirement of trained technical person for administration. In comparison to parenteral formulations; most natural, easy and safe route of administration is oral route that haves additional advantages including self-administration, patient compliance, economical. In market, a number of parenteral antibiotics (piperacillin, tazobactam, cephalothin, ceftazidime, cefotaxime, ceftriaxone, cefepime, ceftaroline, ceftobiprole, cefaloridine, cefoxitin, cefazolin) are available that are used in case of life threatening situation or severe emergency cases but does not have alternate oral formulations that can be given in post-operative recovery that will have better patient compliance, self-medication. Therefore extensive research works is needed for development of alternative oral formulations for these life-saving parenteral antibiotics....
In the present investigation, bi-layer tablets containing Olmesartans Medoxomil as calcium channel blocker and Metoprolol Succinate as beta blocker were formulated in which tablets containing Olmesartan Medoxomil designed to release immediately while release rate of tablets containing Metoprolol Succinate were retarded. Immediate release attributed due to presence of sodium starch glycolate ranging from 2 to 4 % while xanthan gum in concentration from 30 to 35% and Hydroxyl propyl methyl cellulose K15M in concentration from 25 to 30% in different tablet formulations responsible for retard the release of Metoprolol Succinate. Amount of sodium starch glycolate, xanthan gum and Hydroxyl propyl methyl cellulose K15M were optimized to achieve desire release profile....
The study was carried out to develop an emulgel formulation of antifungal drug Bifonazole. The drug had the poor solubility and poor permeability (BCS Class-IV). So to enhance the solubility and permeability of the drug, it was first incorporated in emulsion and then emulsion was mixed with the gel. The polymer used in the gel was Carbopol 934 and HPMC K4M. The 23 factorial design was used for the study. The evaluation parameters were Physical Properties, Viscosity, spreadability and %drug release, antifungal activity and stability study was done. Commercially available Bifonazole cream was used for the comparison. It was found that the emulsifying agent had prominent effect of the drug release in emulgel followed by the oil phase as well as the gelling type. Stability studies shows that the physical appearance, viscosity, drug content, % drug release were unchanged upon three months of the storage. At the end of the investigation it was observed that the Carbopol 934 was the choice of polymer as it has shown higher drug release and good antifungal activity....
The present manuscript describes stable, cost effective immediate release tablets of Losartan Potassium (LTK) in combination with Hydrochlorthiazide (HCTZ) which simplified treatment of hypertension particularly in older patients with renal insufficiency. The addition of Hydrochlorthiazide to Losartan Potassium will potentiate the antihypertensive action. Tablets were prepared by direct compression method. Ac-Di-Sol was selected for the formulation from Crospovidone and Sodium starch Glycolate. Prepared tablets were evaluated for weight variation, uniformity of content, disintegration time and dissolution. Total nine batches were punched and B8 batch was taken optimized batch which had highest similarity with reference produce....
The objective of present investigation was to study and evaluate the individual and combined effects of solubilizers on drug release from pioglitazone controlled release matrix tablets. Controlled release matrix tablets of pioglitazone were developed for better control of blood glucose levels by prolonging its duration of action and to reduce GI disturbances with improved patient compliance. The tablets were prepared by wet granulation technique employing 50% w/w Hydroxy propyl methyl cellulose K-15M as release controlling agent. Polyvinyl pyrrolidone and polyethylene glycol 6000 at 2% w/w were used as solubilizers to study the individual and combined effects of solubilizers on drug release from pioglitazone matrix tablets. Different dissolution models were applied to drug release data in order to evaluate release mechanisms and kinetics. All Pioglitazone matrix tablets followed first order, Higuchi drug release kinetics with diffusion as the dominant mechanism of drug release. As per Korsmeyer-Peppas equation, the release exponent ''n'' ranged 0.669-0.892 indicating that drug release from all the batches was by non-Fickian diffusion mechanism. Polyethylene glycol 6000 gave relatively higher release than polyvinyl pyrrolidone. A combination of Polyvinyl pyrrolidone and polyethylene glycol 6000 gave slow, controlled and complete release of pioglitazone over 24 hours....
The objective of the present investigation is to characterize physicochemical properties of MFD Formulations. The interactive mixture of powder sample was characterized in terms of compressibility characteristics, Differential Scanning Calorimetry (DSC) and Fourier Transformed Infra Red Spectroscopy (FTIR). Fast dissolving tablets were then formulated by direct compression method. The tablets were evaluated for the disintegration time, hardness, friability, tensile strength, weight variation and in vitro release studies. FTIR indicated the absence of any chemical reaction between the two species (drug and excipients) during the process of MFD tablets. DSC studies showed there is no interaction between the drug and excipients. Hausner’s ratio & Carr’s index value of interactive mixture suggested excellent flowability. The interactive mixture was found to be effective at all the concentrations tested in the fast dissolving tablet formulation. Disintegration time (DT) of less than 30 seconds was observed in case of interactive mixture. MFD can be utilized as a better option in the pharmaceutical applications....
The present study was undertaken with a view to prepare a colon targeted matrix tablets of azathioprine and evaluating in vitro drug release in presence and absence of rat ceacal. Matrix tablets containing various proportions of guar gum were prepared by wet granulation technique with the help of starch paste as a binder. The tablets were evaluated for drug content uniformity and were subjected to in vitro drug release studies. The amount of azathioprine released from the matrix tablets was estimated by UV-visible spectrophotometer at regular time intervals. Guar gum matrix tablets released 10-16% of the azathioprine in the physiological environment of stomach and small intestine depending on the proportion of guar gum used in the formulation. When the dissolution study was performed in simulated colonic fluids the matrix tablets containing 20% of guar gum released total about 96% of azathioprine in 24 hour after degradation of tablet into 2ââ?¬â??3 pieces. The matrix tablets containing 30% of guar gum also released about 62% of azathioprine in simulated colonic fluids indicating the susceptibility of the guar gum formulations to the rat caecal contents. The results of the study show that matrix tablets containing 30% of guar gum are most likely to provide targeting of azathioprine for local action in the colon....
The oral Bioavailability of BCS (Bio Pharmaceutical Classification System) class II drug with poor solubility and reasonable permeability is limited by drug dissolution. The purpose of this research was to obtain enhancement of the dissolution profile and Flow Properties of Loratadine using solid dispersion technique with hydrophilic polymers such as Beta-cyclodextrin. Solid dispersions were prepared by the method of solvent evaporation. Prepared dispersion was evaluated for physical appearance, flow property (Angel of repose, Bulk and Tapped density, Compressibility index, Hausner ratio), Drug content, Dissolution studies using the USP paddle method were performed for solid dispersions of Loratadine & pure drug. The resulting systems were subjected to Infrared (IR) spectroscopy to identify the physicochemical interaction between drug and carrier, hence its effect on dissolution. IR spectroscopy, showed no change in the chemical structure of Loratadine. The solid dispersion technique can be successfully used for improvement of dissolution of Loratadine. The Dissolution rates & Dissolution efficiency of Loratadine from the Solid Dispersions exhibited higher values over that of pure drugs....
Captopril, an effective anti hypertensive drug, faced various limitations in preparation of sustained or controlled delivery system due to the fact that the drug is not stable in intestine. Thus the objective of the present study was to prepare gastro retentive microspheres using poly methacrylate polymers to retain the drug in the stomach for longer period. Microspheres prepared by solvent evaporation method were analyzed to sustain the release of captopril in gastric region. The drug and polymer compatibility analysis were done to determine possible interactions between them using FTIR, DSC and TG analysis. The compatible polymers were selected for further formulations. Microspheres of captopril were prepared using Eudragit RLPO, RL100, RSPO and RS100 and its combinations. The process was optimized for the drug polymer ratio, speed of rotation and concentration of surfactant. The various parameters such as percentage yield, drug content, buoyancy percentage, particle size analysis and bulk density was determined. The in vitro release study was carried out for the prepared microspheres. The bulk density of the microspheres were less than one and the results of buoyancy showed that the prepared microspheres float in the acidic medium upto 8h.The microspheres gave sustained release of drug upto 24h. The kinetic modeling showed that release follows first order and the mechanism was by both dissolution and diffusion. Thus the formulation and in vitro evaluation of captopril loaded microspheres using eudragit polymers found to retain in the gastric region upto 8 h and the drug release was also found to sustained upto 24h....
The data collection of the present work is carried out to prepare a document on SUPAC. We have incorporated the changes in base formulation and prepared documentation for Eplerenone-immediate release solid oral dosage form as per USFDA guideline. Scale up and post approval change (SUPAC) classified changes according to “LEVELS” and provided requirements to support each level. The reporting category for the change was determined by the “LEVELS” classification. Aldosterone Antagonists such as Eplerenone is used in immediate release for Batch level changes and composition level changes. Ac-Di-SolTM excipient is used as disintegrating agents which was able to decrease disintegration time upto 7 minutes while increasing the concentration of Ac-Di-SolTM excipients. These combinations of active compound and carrier material have been found to possess improved bioavailability, chemical stability, physical stability, dissolution profiles, disintegration times, safety, as well as other improved pharmacokinetic, chemical and/or physical properties....
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