The aim of the study was to improve the solubility of aceclofenac, which is poorly water soluble drug belongs to BCS class-II. Aceclofenac appears to be particularly well tolerated among the NSAIDs, with a lower incidence of gastrointestinal adverse effects. For poorly soluble orally administered drugs, the rate of absorption is often controlled by the rate of dissolution. To improve the solubility of drug by solid dispersions were prepared with different methods like physical mixture, kneading method and solvent evaporation method with various carriers like poloxamer188, poloxamer407 and PEG 6000 in different ratios from 1:1 to 1:5. The prepared formulations were evaluated for physicochemical characteristics, characterized by differential scanning calorimetry (DSC), X-ray diffraction (XRD), in-vitro dissolution studies and saturation solubility. Based on the evaluation parameters poloxamer407 in ratio of 1:5 through solvent evaporation method was optimized and formulated into tablets by direct compression method.These tablets showed a higher in-vitro dissolution drug release which is 99.62% in 30 minutes when compared with pure drug which showed 26.62% in 60 minutes, whereas marketed tablet (Hifenac) shows 99.64±0.10% in 40 minutes. Hence it was concluded that solid dispersion of aceclofenac drug by using polaxamer 407 with solvent evaporation method enhances solubility, absorption rate and increase bioavailability of the aceclofenac drug.

Objectives: In present investigation, an attempt was made to develop bilayered floating tablets of clopidogrel bisulfate and aspirin using natural gums as release retarded material. Clopidogrel bisulfate and aspirin are anti-platelet agents. Methodology: Clopidogrel bisulfate is a suitable candidate for formulating as gastro retentive dosage form as it has absorption window in stomach and solubility in the acidic pH. Sodium bicarbonate and citric acid were used to get desired floating properties. The effect of formulation variables on floating properties and drug release were investigated. Results: The tablets so designed were evaluated and found to have acceptable physicochemical properties, floating lag time, floating time and drug release. Among all the bilayered formulations, CBXA with susutained.release layer containing xanthan gum (2 ratio with drug), sodium bicarbonate (15% w/w) and citric acid (1.2% w/w) and immediate release layer containing sodium bicarbonate (10% w/w) and guar gum (4% w/w) has shown optimum results. Sustained release layer has shown dissolution of 99.03±0.42 % in 12 hrs whereas immediate release layer has shown 99.4±0.44 % in 30mins.CBXA has shown optimum floating properties with in vitro floating lag time of 4 min and floating time of >12 hr. In vivo buoyancy study revealed that the floating time of CBXA was greater than 6 hr. The in vitro release data of optimized formulation was treated with mathematical equations and was evident that drug release followed zero order kinetics with case II transport mechanism. Conclusion: Based on the results it can be found that bilayered floating tablets of clopidogrel bisulfate and aspirin containing xanthan gum provides a better approach for sustained release and improved bioavailability.

Amaç: CP'nin, keçiboynuzu zamkını salım kontrol edici bir materyal olarak kullanımıyla sinterlenmiş yüzen tabletler geliştirmektir. CP, sefalosporin sınıfının oral yolla uygulanan genişletilmiş spektrumlu, yarı sentetik bir antibiyotiğidir. Gereç ve Yöntemler: CP, kısa bir eliminasyon yarı ömrüne sahiptir, asidik pH'da yüksek çözünürlük, kimyasal, enzimatik stabilite ve absorpsiyon profillerine sahiptir, bu da, biyoyararlanımın iyileştirilmesi için midede kalan dozaj formuna uygun bir aday olmasını sağlar. İstenen yüzme özelliklerini elde etmek için kafur kullanıldı. Hazırlanan CP yüzen tabletler, sinterlemeye tabi tutuldu; burada polimerik yapı içindeki çapraz bağlantı, tabletleri aseton buharlarına maruz bırakarak arttırıldı. Sinterlemenin avantajı, uzun süreli etkin madde salımının düşük sertlikte ve düşük konsantrasyonlarda polimerlerle elde edilebilmesidir. Bulgular: Hazırlanan tabletler değerlendirildi ve kabul edilebilir fizikokimyasal özelliklere sahip olduğu bulundu. Altı saat süre ile aseton buharlarına maruz bırakılan keçiboynuzu zamkı: etkin madde (0.3:1.0) ve kafur (%10 a/a) içeren formülasyon S2, optimum yüzme özellikleri ve 12 saatte %97.3 gibi daha iyi bir çözünme profili gösterdi. Bunun sonucu olarak formülasyon S2 optimize edilmiş formülasyon olarak kabul edildi. Optimize edilmiş formülasyonun in vitro salım verileri, matematiksel denklemlere uygulandı ve etkin madde salımı, anomalous transport mekanizması (0.991) ile sıfır derece kinetiğe (0.9599) uyum gösterdi. Sonuç: Sonuçlara göre, sefpodoksim proksetilin keçiboynuzu içeren sinterlenmiş yüzen matriks tabletlerinin kontrollü salım için daha iyi bir seçenek sağladığı sonucuna varılabilir. Anahtar kelimeler: Sefpodoksim proksetil, kontrollü materyal, midede kalan yüzen tabletler, sinterleme tekniği Objectives: To develop sintered floating tablets of CP using locust bean gum as a release-controlling material. CP is an orally-administered, extended-spectrum, semi-synthetic antibiotic of the cephalosporin class. Materials and Methods: CP has a short elimination half-life, possesses high solubility, chemical, enzymatic stability and absorption profiles in acidic pH, which makes it a suitable candidate for formulation in a gastro-retentive dose form for improved bioavailability. Camphor was used to get the desired floating properties. The prepared CP floating tablets were subjected to sintering, where the cross linkage within the polymeric structure was increased by exposing the tablets to acetone vapors. The advantage with sintering is that prolonged drug release can be attained at low hardness and low concentrations of polymers. Results: The prepared tablets were evaluated and found to have acceptable physicochemical properties. Formulation S2 containing locust bean gum: drug (0.3:1.0) and camphor (10% w/w), which was exposed to acetone vapors for a period of 6 hrs showed optimum floating properties and a better dissolution profile i.e. 97.3% in 12 hrs. Hence, formulation S2 was considered as the optimized formulation. The in vitro release data of...

The objective of this investigation is to study the applicability of gum karaya, the natural gum for the preparation and in vitro evaluation of losartan potassium, as Chronotherapeutic Drug Delivery System (ChDDS). The compression-coated timed-release tablets (CCT) containing losartan potassium in the core tablet were prepared by dry coating technique with different ratios of gum karaya as the outer coat. The parameters investigated were tensile strength, friability, in vitro dissolution studies and drug concentration. The optimized formulation was further characterized by powder XRD and FTIR to investigate interactions and no interactions observed. The tensile strength and friability of all the CCT were between 1.06-1.23 MN/m 2 and < 0.3% respectively. All the CCT showed a clear lag time before a burst release of drug. However, the lag time of drug release increased as the amount of gum karaya in the outer layer increased. For instance, the lag time of LGK1, LGK2, LGK3, LGK4, LGK5, LGK6 and LGK7 were 16, 10.5, 5.5, 3, 2, 1.5 and 0.5 hrs respectively. The drug content of all the CCT was >98%. Formulation LGK3 was taken as an optimized formulation which can be exploited to achieve ChDDS of losartan potassium for the treatment of hypertension.

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