Current Issue : April - June Volume : 2010 Issue Number : 1 Articles : 15 Articles
Pulsatile systems are gaining a lot of interest as they deliver the drug at the right site of action at the right time and in the right amount, thus providing spatial and temporal delivery and increasing patient compliance. The basic design of pulsatile drug delivery system consists of formaldehyde treated hard gelatin capsule body, filled with Eudragit microspheres of doxofylline and plugged with a hydrogel polymer. Microspheres were prepared using combination of Eudragit L-100 and S-100 with different core: coat ratios by solvent evaporation technique. Different plugging materials like Xanthan gum, Locust bean gum and Psyllium husk were used in the design of pulsatile capsule. The insoluble hard gelatin body was cap sealed by 5% ethanolic solution of ethylcellulose and then the entire capsule was enteric coated with HPMCP to render the system insoluble in gastric pH. Dissolution studies of the pulsatile drug delivery system revealed the absence if drug release in first three hours and negligible release in the fourth hour and thus a lag time of 3-4 hrs was achieved. In conclusion, time and pH dependent pulsatile drug delivery system was successfully designed, evaluated for various parameters and found satisfactory with respect to the desired lag time which is needed in the chronotherapeutic delivery of doxofylline in the treatment of nocturnal asthma....
The present study was performed to design the sustained release muco-adhesive oral tablet of propranolol HCl. The study was aimed to increase the residence time of the drug in to the stomach and release for extended period of time in order to increase bioavailability of the drug, reduce dosing frequency, improve patient compliance and optimization of drug release profile. The study was performed on three different polymer i.e. Hydroxy propyl methyl cellulose (HPMC), Sodium carboxy methyl cellulose (Na CMC) and Carbopol. All the 13 formulations (F1 to F13) were evaluated for their physical parameters with regard to thickness uniformity, hardness, friability, weight variation and drug content determination. All the prepared formulation had shown the satisfactory results. The muco-adhesion force for all the prepared formulations was found in the range of 0.58 N to 3.43 N. Formulation containing combination of polymer shows greater muco-adhesion as compare to other formulations. The linear relationship was found between concentration of polymer & swelling index. Dissolution studies revealed that release rate was inversely related to polymer concentration down the dissolution rate. Statistical data shows drug release occurred via diffusion mechanism from hydrophilic polymers like Carbopol and HPMC. Stability study performed according to ICH guideline shows negligible changes in drug release and drug content after the period of three months....
The objective of study was to develop and evaluate a stable lyophilized formulation of antihypertensive agent SNP4027. SNP4027 is a metabolite of arachidonic acid, is a naturally occurring prostaglandin with potent vasodilator activity and inhibitory activity of platelet aggregation. SNP4027 gets rapidly hydrolyzed at neutral pH in blood and is also subject to enzymatic degradation. SNP4027 is unstable at pH lower than 10.5, so stable bulk solution of formulation was prepared by adjusting pH at 13 with sodium hydroxide. Based on these preformulation observations, a lyophilized formulation containing 1.5 mg/ml of SNP4027 was prepared in a buffer solution of pH at 13. To minimize the degradation, 1N (4%) sodium hydroxide solution was included to prepare stable formulation. Rubber closures, filter membranes and liquid transfer tubing were selected on the basis of compatibility studies and absence of loss of drug due to adsorption of these components. The lyophilized formulation was reconstituted with 5 ml of sterile diluent for SNP4027 and subjected to accelerated and long term stability studies. Lyophilized formulation of SNP4027, when administered chronically, should be prepared in a drug delivery reservoir appropriate for the infusion pump with a total reservoir volume of at least 100 ml. Lyophilized formulation of SNP4027 should be prepared using 2 vials of sterile diluent for use during a 24 hour period without drug precipitation and degradation. Accelerated stability studies suggested that the product should be kept at 2�°C to 8�°C for long term storage....
The effects of sodium lauryl sulphate (SLS), a surfactant widely used as a wetting agent on the in vitro release of ciprofloxacin hydrochloride (CPF) embedded in four different polymers; ethylcellulose (Etcell), hydroxyethylcellulose (HEC), eudragit l-100 (EUD) and hydroxy propylmethyl cellulose (HPMC) were investigated. The wet granulation method of massing and screening using hydro alcoholic medium was used. CPF tablets of all the polymers were of good physical quality with respect to appearance, drug content uniformity, hardness, weight variation and friability. In vitro release studies show that, ethylcellulose extended drug release more than the other polymers, while the fastest release was obtained from eudragit. The presence of sodium lauryl sulphate (SLS) led to about 2 ââ?¬â?? 3 fold increase in the rate of drug dissolution from HPMC matrices while further decreasing dissolution rate in Etcell matrices. The overall result demonstrates that drug release was found to be dependent on both polymer type and concentration of the surfactant. Kinetic studies show that, drug release was both by diffusion and erosion of polymers depending on polymer type, with the presence of SLS only significantly affecting HPMC matrices....
Concomitant consumption of alcoholic beverages along with sustained release products might be expected to have the potential to induce dose dumping. No concrete research has been taken to evaluate the role of various beverages and drinks on the drugs ââ?¬â?? specifically sustained release dosage forms. The literature review definitely points to the lacunas in the field of this area of research. Hence, the objective of present study is to correlate in vitro drug release pattern of sustained released dosage forms in presence of alcoholic beverages with ex vivo drug absorption pattern. Reliable and predictive in vitro methods to quantify drug transport across the intestinal epithelium are required at an early stage in the drug development process for oral solid dosage forms. Several approaches have been used to obtain the most representative model of the intestinal epithelium. The everted intestine model presents many advantages relative to other methods. In this work, an attempt has been made to develop an ex vivo continuous dissolutionââ?¬â??absorption system to study the effect of alcohol consumption on sustained release formulation of metformin and diclofenac. The studies yielded a dissolutionââ?¬â??absorption relationship that can be used to predict dissolution or permeation-rate-limited absorption for two marketed formulations. Thus, the dissolutionââ?¬â??absorption system may prove to be a valuable tool in formulation development. Broader evaluation of such a system is warranted....
Amlodipine besylate, {2-[(2-Aminoethoxy)methyl]-4-(2-chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-1,4-dihydropyridine benzenesulfonate} is an antihypertensive drug of dihydropyridine calcium channel blocker class, administered orally as a long acting antihypertensive agent that is used in the treatment of acute and chronic hypertension and as prophylactic treatment of angina pectoris. Fast-dissolving tablets (FDTs) of amlodipine besylate were prepared by direct-compression method. Nine formulae having three subliming agents at three different concentration levels were prepared to assess the most efficiency and critical concentration level. Twelve formulae having three subliming agents at the predetermined level and two superdisintegrants at two different concentration levels were prepared to assess the efficiency of superdisintegrants and their critical concentration level. Six formulae having three subliming agents at the most efficient level and coprocessed superdisintegrant at different concentrations levels were prepared to assess the efficiency of coprocessed superdisintegrants and its critical concentration level. The prepared tablets were evaluated with respect to their shape, size, organoleptic properties, drug content uniformity, weight variation, mechanical strength, water absorption ratio, wetting time, dissolution behavior and disintegration time. All the prepared powder blends showed passable to excellent flowability. The prepared tablets were of acceptable drug content and weight variation according to USP specifications. \r\nTablets containing Camphor (15%) and Ac- Di- Sol (8%) showed superior organoleptic properties, mechanical properties, water absorption ratio, wetting time, along with excellent in-vivo disintegration time and drug release, as compared to other formulae....
The purpose of the study was to develop the sustained release of bilayered tablets. Bilayered tablets are preferred when the release profile of the drugs are different from one another. In this studies combination of Salbutamol sulphate and Theophylline are used which shows synergistic effect in producing bronchodilation. The formulations were prepared by using HPMC-P, Ethyl cellulose and HPMCK100M as polymers at various concentrations. The bilayered matrix tablets were prepared by wet granulation method. The prepared tablets were evaluated for hardness, drug content and Invitro dissolution studies. All the formulations showed good matrix integrity and sustained release of drug for 8hrs. In F13 formulation theophylline release was 13.20% in the 1st hour and in 8th hour 99.62% and Salbutamol sulphate release was 46.6%in the 1st hour and only 96.26% in the 8th hour. So it can be concluded that the formulation (F13) which containing HPMC-P polymer is suited for the sustained release matrix tablets of Salbutamol sulphate and Theophylline....
Present research work describes emulsion non solvent addition technique for microencapsulation of tinidazole using dichloromethane and cyclohexane as solvent and nonsolvent respectively. Liquid Paraffin was used as the liquid dispersion medium, tween 80 as an emulsifying agent. The process variables included variations in core: coat ratios. Microcapsules obtained were evaluated for flow properties, particle size, taste masking efficiency, drug content and in vitro release studies. Results of the study revealed that microcapsules obtained from 1: 2 ratio (core: coat) were spherical in shape with an average particle size of 343 microns. The encapsulation efficiency was found to be 75 ââ?¬â?? 85 % w/w depending on the stirring speed. Taste masking evaluation was done by time intensity method and it showed that taste of Tinidazole was masked successfully. Dissolution studies revealed that complete drug was released in 3 hrs. Thus, it can be concluded that effective taste masking of Tinidazole was achieved by microencapsulation technique using Eudragit RSPO polymer....
The aim of the present study was to prepare PharmagumTM based chlorpheniramine maleate chewable tablets for the treatment of rhinitis, urticaria, allergy, common cold, asthma and hay fever. Chewable tablets containing CPM was prepared by a direct compression technology. The indigenously fabricated and standardized flat faced toolings used for the preparation of chewing gum formulations. The effect of varying the concentration PharmagumTM as a gum base on release of chlorpheniramine maleate (CPM) from chewable tablets was investigated. Differential scanning calorimetry and X-ray powder diffraction spectroscopy were used for physicochemical characterization. The drug content was estimated by UV spectrophotometer at 261 nm. In vitro drug release studies of chewing gum formulations were performed in artificial saliva pH 6.8 at 37�±1oC....
It is believed that most of the modern drugs which are therapeutically active are derived synthetically. This in fact is not true. Actually plant itself is a chemical laboratory. It synthesizes biologically active secondary metabolites. Most of the modern medicines have originated from plant metabolites. Herbal formulations may contain single or several plant materials. These can be in any dosage form like Capsules, Tablets, Pills, Syrups, and Avaleha etc. Selection of Herbal product depending upon pharmacological action is required and it can be done by phytochemical investigation of each part of plant and/or by clinical traits of extract of different plant parts. The objective is to formulate and evaluate quality control study, pharmacological study and stability studies of herbal anti-inflammatory tablets. Herbal drugs were taken and the active ingredients were extracted. Then it was formulated as a tablet dosage of 100mg by adding the additives and excepients. Further the tablet undergone quality control studies, stability studies, pharmacological study etc. The study sample tablets were formulated according to the standard procedure. The tablets also comply all the tests done for quality control, stability studies and pharmacological study. Various plant chemicals found in plants and herbal sources all have different properties as they go about their business of reducing inflammation. Many herbs also possess anti-inflammatory (also known as antiphlogistic) characteristics. Herbs can be used as the sole therapy in autoimmune disease or as complementary corticosteroid-sparing therapies allowing patients to take smaller doses or shorter courses of corticosteroids. Thus this study also confirms the anti-inflammatory action by controlling the release of inflammatory mediators by using different herbals which were not tried before....
The purpose of this study was to improve the solubility and dissolution rate of very\r\npoor water soluble drug Nitazoxanide by solid dispersions. Solid dispersions of\r\nNitazoxanide prepared with polyethylene glycol (PEG 6000) by hot-melt method. Physical properties and dissolution behavior of solid dispersions as well as physical mixtures were determined. Nitazoxanide was evaluated for the compatibility studies with the polymer PEG 6000 at 40�°C temperature and 75% relative humidity. Evaluation of the properties of the dispersions and physical mixtures were performed using dissolution studies, Fourier transform infrared spectroscopy (FTIR), X-ray powder diffraction (XRD) and differential scanning calorimetry (DSC). In Vitro dissolution study of pure drug, solid dispersions and physical mixtures were performed after filling in the hard gelatin capsules (transparent) in phosphate buffer pH-7.5 at 37�°C. Dissolution measurements demonstrated a significantly increased dissolution rate from the solid dispersions compared to physical mixtures. From the FTIR it was cleared that there was no any interaction between drug and polymer in case of solid dispersions as well as physical mixtures. The results from DSC and XRD analysis showed the decrease in the crystallinity of the drug in solid dispersions as compared to that of physical mixtures and pure drug. \r\nKeywords: Nitazoxanide, PEG 6000, Solid dispersions, Physical mixtures, Hot-Melt method....
Since conventional ophthalmic solutions are rapidly eliminated and cannot provide and maintain an adequate concentration of the drug in the cul-de-sac. To solve these problems, we developed a thermo sensitive in situ gelling and mucoadhesive ophthalmic drug delivery system containing moxifloxacin HCl based on poloxamer analogs (15 %w/v poloxamer 407/15 %w/v poloxamer 188) and PEO (X2) (0.3 or 0.5% w/v Polyox WSR 301). The combined formulation would easily converted to stiff gel at physiological conditions and exhibited sufficient mucoadhesion force and gel strength to provide ocular bioavailability of the drug for a long period of time. A 32 full factorial design was employed in formulating the IODDS (In situ Ophthalmic Drug Delivery System) with two polymers: PF68 (Pluronic F 68) (X1) and PEO (Polyox WSR 301) (X2) as independent variables. Formulations were prepared and analyzed for the dependent variables i.e., gelation temperature (GT), gel strength (GS) and bio-adhesion force (BF) etc. Drug permeation data was fitted to different kinetic models. PF 68 loading was found to be significant for gelation temperature, PEO loading showed positive effect on the bio-adhesion force and found helpful to control the release rate of drug. It was found significant effect of both the polymers on gel strength and bioadhesion force properties but PF 68 was important for gel formation at temperature range 33-36 �°C. The quadratic mathematical model developed could be used to predict and to have the formulations with desired gelation temperature, gel strength, bioadhesion force to obtained proper drug release properties....
A number of characteristic properties of pharmaceuticals and biopharmaceuticals have been obtained by Differential Scanning Calorimetry (DSC) technique that is considered as a universal pharmaceuticals and biopharmaceuticals product development monitor. This review relates to DSC development and applications within pharmaceutical and biopharmaceuticals research areas. DSC is a rapid and accurate thermo-analytical technique for a wide variety of transitions [e.g. glass transition, detection of amorphous material in semi-crystalline compounds, melting and crystallization, purity, polymorphs, drug-excipient interaction, drug-receptor interaction, protein denaturation, freeze drying, thermal behavior of lipid bilayers and of lipidic drug delivery systems] in the pharmaceutical industry. In addition, DSC thermally characterize proteins, DNA and RNA and is commonly used in conjunction with other biophysical techniques to link thermodynamics, structure and function to fully characterize biopharmaceutical products. The development of sophisticated, modulated temperature programs and high scan rates provided additional benefits over DSC while introduction of hyphenated thermal techniques provided a more insight view of solid-state properties along with thermal characterization. Researchers are of the opinion that DSC will retain its place at the forefront of the pharmaceutical and biopharmaceuticals thermal analytical sciences in coming years.\r\n\r\nKeywords: DSC, thermal methods, pharmaceutical, biopharmaceutical...
Photodynamic therapy (PDT) is a proven clinical tool for the treatment of non-malignant and malignant cancers. PDT is a treatment with a drug that makes the skin cells sensitive to light. It combines the preferential accumulation of the chemical photosensitizer in the target tissue with defined illumination, to give the selectivity of the treatment. The light penetrates the tissue and causes excitation of the photosensitizer to produce cytotoxic singlet oxygen (1O2) species from surrounding tissue dissolved oxygen (3O2). PDT is an alternative to surgery and is best used in cases where a lot of surgery is needed. It is normally not suitable for deeper skin cancers because the light cannot penetrate far enough into the skin. Compared to complete excision of tumours by surgery; PDT is advantageous in cancer treatment and is much less invasive. Compared to chemotherapy, its penetration limitations make it much less likely to damage underlying healthy cells. Success has been achieved especially for surface cancers of the skin and esophagus, by targeting tumour cells directly, their supporting vasculature, and activating the immune system....
In the present study has been focused to increase solubility and to prepare rapidly disintegrating tablets of cilostazol using superdisintegrant Doshion P544, croscarmellose sodium by direct compression. The solid complexes of Cilostazol & �Ÿ-CD (1:1 molar ratio) were prepared by different techniques. Phase solubility showed stability constant 747.03M-1. The saturation solubility showed increase in the solubility. Prepared inclusion complexes were characterized by I.R, UV, XRD, and DSC. Cilostazol tablets were prepared and evaluated. 4 % Doshion and 4 % CCS showed D.T, 0.36 and 0.58 min respectively. Formulation Dosh II and CCS II were selected for stability study....
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