Current Issue : July-September Volume : 2011 Issue Number : 3 Articles : 11 Articles
Development of oral controlled-release systems has been a challenge to formulation scientists because of their inability to restrain and localize the system in the targeted area of the gastrointestinal tract. Controlled/sustained release preparations using alternating routes have also been formulated but oral route still remains preferable. Bi-layer tablets are novel drug delivery systems where combination of two or more drugs in a single unit having different release profiles which improves patient compliance, prolongs the drug(s) action, avoid saw tooth kinetics resulting in effective therapy along with better control of plasma drug levels....
The purpose of this study is to prepare fast dissolving tablets of Metoclopramide hydrochloride by direct compression. In the present research study, Sodium Starch Glycolate, Ac-di-sol and crosspovidone was taken as a super disintegrants. Here the Metoclopramide hydrochloride (anti-emetic) is taken as the model drug for the study and direct compression as a method for preparation of the Fast Dissolving Tablet. The comparison was done for different super disintegrants concentration and it was found that Ac- di-Sol was the best super disintegrants, and disintegrates the tablet from 15 to 22 sec. F3 batch was the best formulation and shown all the parameters like hardness, friability and disintegrating time within limit. F3 batch shown good onset of action (71.38% release of drug in 5min) and good release (98.87%) by 30 min as compared to other formulation....
The aim of present investigation was to evaluate the potential use of mucoadhesive Carbopol 934P microspheres for gastroretentive delivery of Cefuroxime Axetil. Microspheres were prepared by spray drying technique using 32 Full factorial design. Independent variables chosen were Drug: Polymer ratio and Feed flow rate. The formulated Microspheres were characterised for Mucoadhesion time, Encapsulation Efficiency, Particle size analysis, DSC, XRD, IR and In-vitro drug release. The result of mucoadhesion study shows better retention (320±15 min) of formulation in upper part of GIT. The formulation technique shows higher encapsulation efficiency (97.21±1.09). The Particle size analysis shows better particle size (4to7 µm). The result of surface topography shows formation of matrix of drug & polymer with spherical particles. The IR spectroscopic study reveals that no structural changes during formulation. DSC thermogram shows the thermal behaviour of formulations. The release of the drug was prolonged up to 10 hrs (96.46±0.76)....
Mucoadhesive buccal films of nifedipine were prepared by solvent casting technique using Hydroxyl propyl methyl cellulose, Eudragit RLPO, Eudrgit RSPO, Eudragit E100, and Ethyl cellulose. FT-IR interaction studies revealed that there was no interaction between nifedipine and polymers. Cumulative in vitro drug release in PBS pH 6.6 was in the range of 66.57% to 98.61% at the end of 12 h. Formulations F1, F2, F4, F5 followed first order kinetics and the formulation F3 followed zero order kinetics. The mechanism of drug release followed diffusion controlled rate process through a swollen matrix and water filled pores in the formulations. Optimized formulation, F3, containing nifedipine 10 mg in 41.09% w/v Hydroxy propyl methyl cellulose and 41.09% w/v Eudragit RLPO exhibited satisfactory swelling, adequate tensile strength and promising drug release for a period of 12 h. In vivo bioavailability in rabbits increased to 90% for formulation F3 as compared to 30 – 60% for pure drug nifedipine. A good correlation between in vitro release and in vivo absorption (R2= 0.8131) was observed. The films were evaluated for their physical characteristics like weight variation, drug content uniformity, thickness uniformity, folding endurance, content uniformity, swelling behaviour, tensile strength and surface pH. The films were found to be stable with respect to the amount of drug content and physical stability in both accelerated as well as at room temperature conditions for the period of study....
The purpose of this study was to develop a nanosuspension of a poorly soluble drug by nanomilling process using pearl milling technique to achieve superior in vitro dissolution and high in vivo absorption of drug. A promising simvastatin nanosuspension was formulated with poloxamer-407 as a stabilizer and Zirconium Oxide beads as a milling media. The obtained nanosuspension having particle size in the nano range (333nm) which is characterized by particle size , Zeta potential and Screening Electron Microscopy (SEM) method. This formed nanosuspension was lyophilized. Although the formulation showed significant improvement during in vitro dissolution as compared to pure drug and its marketed formulations. The in vivo study revels that the decrease in the total cholesterol level increases high-density lipoprotein cholesterol. Probably due the formation of nanoparticles which absorbs rapidly. The stability study was carried out at two different temperature and its shows that the lyophilized simvastatin nanosuspension was stable up to six month....
Atenolol is a cardio selective β-blocker, widely used in the management of hypertension. The present research work shows a relatively simple method to design and develop control release hydrogels base Atenolol microspheres drug delivery system. The hydrogels base microparticles can be prepared by using solvent evaporation technique which mainly depends on the nature and quantity of the polymer used, the drug, the quantity of emulsifier as well as cross linker like Polyvinyl Alcohol and the duration of the therapy. In the present research work, a Control release Atenolol microparticles synthesized by solvent evaporation method in which the different concentration ranges of biodegradable polymer like Polycaprolactone and an emulsifier like Polyvinyl Alcohol was taken while the amount of Atenolol was taken standard throughout the study. The formulated microspheres were also evaluated for their drug loading properties, swelling index and in vitro drug release which was justified by mathematical models like factorial design studies....
Propranolol (CAS 525-66-6), designated chemically as (RS)-1-(1-methylethylamino)-3-(1-naphthyloxy) propan-2-ol, is cheap and commercially available chemical. Propranolol is a β1-selective (cardioselective) β-adrenergic receptor blocking agent which was discovered in 1988 by the scientists Scottish and James W. Black. They achieved Nobel prize for their discovery of Propranolol molecules.1 One of the most widely prescribed as sympatholytic non selective β-blockers in the long term treatment of hypertension and cardiovascular diseases is usually taken orally, although an intravenous form is available for acute administration. Propranolol is rapidly absorbed from gastrointestinal tract, but the oral bioavailability is low nearer to 30% due to significant first pass metabolism. Propranolol is rapidly and completely absorbed, with peak plasma levels achieved approximately 1–3 hours after ingestion. Effective plasma concentrations are between 10–100 ng/mL. Toxic levels are associated with plasma concentrations above 2000 ng/ml. 2 the present work was attributed to the formation of injection having hydrogels base control drug delivery system of Propranolol. The formulations contain microparticles were prepared by using biodegradable polymer like Polycaprolactone....
Pharmaceutical invention and research are increasingly focusing on delivery systems which enhance desirable therapeutic objectives while minimising side effects. Recent trends indicate that multiparticulate drug delivery systems are especially suitable for achieving controlled or delayed release oral formulations with low risk of dose dumping, flexibility of blending to attain different release patterns as well as reproducible and short gastric residence time. The release of drug from microparticles depends on a variety of factors including the carrier used to form the multiparticles and the amount of drug contained in them. Consequently, multiparticulate drug delivery systems provide tremendous opportunities for designing new controlled and delayed release oral formulations, thus extending the frontier of future pharmaceutical development....
Amongst the various routes of drug delivery, oral route is perhaps the most preferred to the patient and the clinician alike. Review provides knowledge for the patient who cannot swallow, such as the elderly, stroke victims, bedridden patients, patients affected by renal failure and patients who refuse to swallow such as paediatric, geriatric and psychiatric patients. In this review is a collection of mouth drug delivery that avoid first pass mechanism so it can avoid the drug loss, potent drug use and better therapeutic efficiency with improving the patient compliance. Bypass of the gastrointestinal tract and hepatic portal system, increasing the bioavailability of orally administered drugs that otherwise undergo hepatic first-pass metabolism. In addition the drug is protected from degradation due to pH and digestive enzymes of the middle gastrointestinal tract so patient get idea about this route and how to administer. Within the oral mucosal cavity, the buccal region offers an attractive route of administration for systemic drug delivery. The mucosa has a rich blood supply and it relatively permeable. The objective of this article is to review oral drug delivery system by discussing the anatomy and physiology of mouth, various roots like buccal, sublingual and forms of various dose like tablet, film, gel, chewing gum as drug delivery in mouth and various method to preparation the dose and its evaluation of dose, drug which use as active substance and its polymer for oral drug delivery....
Mucoadhesive buccal drug delivery of drugs provides an attractive alternative to the oral route of drug administration, particularly in overcoming deficiencies associated with the latter mode of administration problems such as high first pass metabolism. Mucoadhesive buccal drug delivery systems offer many advantages over conventional systems such as ease of administration, rapid termination of therapy and administration to unconscious patients. Buccal mucosa makes a more appropriate choice of site if prolonged drug delivery is desired because buccal site is less permeable than the sublingual site.\r\nBuccal bioadhesive tablet formulations enable a delivery with a plasma drug level of the desired therapeutic response for a defined period of time, and also provides a means of confining the drug and penetration enhancer to a defined region of the mucosa....
The objective of the present study is to prepare sustained-release ketorolac tromethamine microspheres of bovine serum albumin in different ratios by the emulsion cross-linking method using epichlorohydrin. The prepared microspheres were subjected to various physicochemical evaluation and in vitro release studies. The drug release from microspheres of 1:5 ratio is the most constant and prolonged drug release is diffusion followed by erosion. The characteristics of the prepared microspheres are conducive to the formulation of the sustained release drug delivery system....
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