In the recent years, great efforts are being directed towards the refabrication of existing drug molecules in a fashion, capable of solving problem related to poor water solubility, poor bioavailability, dosing problem, stability, toxicity etc. This trend of working has led to the development of new drug delivery system. Eye, as a portal for drug delivery is generally used for the local therapy as against systemic therapy in order to avoid the risk of eye damage from high blood concentrations of drug, which are not intended for eye. 1)Most of the ocular treatments call for the topical administration of ophthalmically active drugs to the tissues around the ocular cavity. Several types of dosage forms can be applied as the delivery systems for the ocular delivery of drugs. The most prescribed conventional ocular dosage forms for the delivery of drugs are eye drops, eye ointments and suspensions have major disadvantages like poor bioavailability due to rapid precorneal elimination, normal tears turnover and conjunctiva absorption, frequent instillation of concentrated medication, side effects due to systemic absorption of drugs, blurred vision due to presence of viscous vehicles.2) The present study aims at formulating ocular inserts using biodegradable polymers to overcome the drawbacks of conventional eye preparations.The ocular insert presents valuable assets such as increasing contact time, reduced number of administrations, possibility of providing a prolonged drug release and thus a better efficacy, reduction of systemic side effects and thus reduced adverse effects.3) In order to improve drawbacks associated with conventional dosage form, it is desired that an alternative way of administration is needed to enhance the bioavailability of drug. Ocular inserts of polymeric materials which can release the drug at preprogrammed rate 4) without interference with the normal vision can serve this purpose. Ophthalmic drug delivery is one of the most interesting and challenging endeavors facing the pharmaceutical scientists. Although very few ophthalmic formulations containing bioadhesive or penetration enhancer are commercially available in the market, research in this area has provided a new impetus and dynamism, as never before, for the development of modified or novel ophthalmic formulations, with the promise of new and exciting directions in the field of formulations technology.5) Eye is a unique organ and drug administration is a challenging task. Eye is prone to number of diseases; some of them are blepharitis, conjunctivitis, ophthalmia neonatorum, trachoma, iritis, and corneal ulceration. Bacteria are the causative pathogens for a large number of eye disorders. The anatomy and physiology of the eye render this organ exquisitely impervious to foreign substances.6) The challenge to the formulator is to circumvent the protective barriers of the eye without causing permanent tissue damage. The development of newer, more sensitive diagnostic techniques and therapeutic agents render urgency to the development of ma...
A simple, specific, accurate and precise stability-indicating reversed-phase high-performance liquid chromatographic method was developed for simultaneous estimation of olmesartan medoxomile (OLME), amlodipine besylate (AMLO) and hydrochlorothiazide (HCTZ) in tablet dosage form. The method was developed using an RP C18 base deactivated silica column (250 × 4.6 mm, 5 µm) with a mobile phase consisting of triethylamine (pH 3.0) adjusted with orthophosphoric acid (A) and acetonitrile (B), with a timed gradient program of T/%B: 0/30, 7/70, 8/30, 10/30 with a flow rate of 1.4 mL/min. Ultraviolet detection was used at 236 nm. The retention times for OLME, AMLO and HCTZ were found to be 6.72, 4.28 and 2.30, respectively. The proposed method was validated for precision, accuracy, linearity, range, robustness, ruggedness and force degradation study. The calibration curves of OLME, AMLO and HCTZ were linear over the range of 50-150, 12.5-37.5 and 31-93 µg/mL, respectively. The method was found to be sensitive. The limits of detection of OLME, AMLO and HCTZ were determined 0.19, 0.16 and 0.22 µg/mL and limits of quantification of OLME, AMLO and HCTZ were determined 0.57, 0.49 and 0.66, respectively. Forced degradation study was performed according to International Conference on Harmonization guidelines.
Reversed-phase High-Performance Liquid-Chromatography (RP-HPLC) method was successfully developed for the simultaneous determination of quaternary mixture consisting of chlorpheniramine maleate (CPM), phenylephrine hydrochloride (PE), paracetamol (PCM) and caffeine in pharmaceutical preparation. The method was found to be simple, sensitive and rapid. The separation of the drugs was carried out using Inertsil ODS C18 column using 0.05M dibasic phosphate buffer: acetonitrile (93: 07; v/v) as mobile phase. The flow rate of mobile phase was adjusted to 1.5 ml/min and column oven temperature was kept at 30ᴼC. All these drugs were resolved successfully with retention times 2.74 (CPM), 3.48(PE), 9.5(PCM) and 26.32(Caffeine) minutes when detection was carried out at 215 nm. Correlation coefficient was found 0.999, 0.998, 0.999 and 0.999 respectively for CPM, PE, PCM and Caffeine. The relative standard deviation in the tablets was found less than 2% for six replicates. The method was validated for precision and accuracy. Thus, proposed method can be successfully applicable to the pharmaceutical preparation containing the above mentioned drugs without any interference of excipients
The eye presents unique opportunities and challenges when it comes to the delivery of pharmaceuticals. In the present study, ocular inserts of levofloxacin were prepared using chitosan and gelatin by solvent casting technique with an aim to improve therapeutic efficacy in the treatment of conjunctivitis. Prepared ocular inserts were then evaluated for film thickness, weight variation, content uniformity, percentage moisture loss and absorption. In vitro drug release studies were carried out using flow through apparatus that simulated the eye conditions. Optimized formulations were subjected to in vivo and stability studies to assess the effectiveness of the formulations. Finally in vitro in vivo correlation was established. Plasticizer like PEG was found to influence their effect on drug release. Prepared ocular inserts exhibited zero order kinetics which was confirmed by strong and positive correlation. The in vitro and in vivo drug release studies revealed that the formulations provide a best alternative to prolong the drug release at the end of 24 h and remained stable with intact at ambient conditions.
Millions of people around the world suffers from the fever, effective treatment is essential by formulating Transdermal patch. Paracetamol IP traditionally considered as a NSAID, is an effective analgesic and antipyretic fully sold without prescription. The conventional formulations containing high dose as well as required to take the medication frequently so increase the risk factor associated with drug. The present study is an attempt to develop suitable matrix type patch of Paracetamol using blends of Xanthan Gum and HPMC K4M with polyethylene glycol (PEG-400) as a plasticizer. To get better effect permeation enhancers such as Linseed oil and oleic acid was also incorporated and their optimum concentration was determined. Prepared formulations were evaluated for compatibility, drug content, moisture loss and absorption, thickness, weight variation, adhesion, folding endurance etc. In vitro permeation study was performed by using Franz diffusion cell. Formulations were found to be uniform in physicochemical parameter with a fewer variations and there was no significant interaction between drug and polymer used. Formulation of HPMC K4M along with Linseed oil showed faster release of drug from developed formulations. Based on the observation, No burst effect but HPMC K4M are better for faster release with linseed oil and xanthan gum for prolonged release for the development of patch. Stability studies indicated the formulations were remained stable both physically and chemically. All developed formulations showed desired properties of an ideal TDDS and followed zero order rate profile. Thus, the study achieved targets by reduction in frequency of administration and systemic toxicity.
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