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.
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...
In present investigation, an attempt was made to develop gastro retentive tablets of cefpodoxime proxetil (CP) using locust bean gum as release retarded material. CP is an orally administered, extended spectrum, semi-synthetic antibiotic of cephalosporin class. CP has a short elimination half-life and also possesses high solubility, chemical, enzymatic stability and absorption profiles in acidic pH which makes CP suitable candidate for formulating it as gastro retentive dosage form for improved bioavailability. Sodium bicarbonate and citric acid were used as effervescent agents to get desired floating properties. The tablets prepared were evaluated and found to have acceptable physicochemical properties. The in vitro release data of optimized formulation was treated with mathematical equations and was concluded that drug release followed zero order kinetics with anomalous transport mechanism. Based on the results it can be concluded that floating tablets of cefpodoxime proxetil containing locust bean gum provides a better option for controlled release action and improved bioavailability.
Topical drug delivery has been used for the treatment of local skin disorders. Emulgel have emerged as one of the most interesting topical delivery systems as it has dual control release system i.e. gel and emulsion form. One side the topical applications of the drug offer the potential advantages of delivering the drug directly to the site of action and secondly delivering the drug for extended period of time at the effected site. The major objective behind this formulation is enhancing the topical delivery of hydrophobic drug (flurbiprofen) by formulating flurbiprofen emulgel using high molecular weight water soluble polymer of hydroxy propyl methyl cellulose (HPMC K100M), carbopol 940, carbopol 941 and xanthan gum. Oleic acid and propylene glycol were used as permeation enhancers. The influence of the type of the gelling agent on the drug release from the prepared emulgel was investigated. The prepared emulgels were evaluated for their physical appearance, pH determination, viscosity, spreadability, extrudability, in-vitro drug release, ex-vivo drug release and stability. All the prepared emulgels showed acceptable physical properties, homogeneity, consistency, spreadability, viscosity and pH value. The in-vitro release rate of emulgel was evaluated using diffusion cell containing dialysis membrane with phosphate buffer pH 7.4 as the receptor medium. FOA4, FOA1, FPG4 and FOA3 have shown more than 75% drug release for 8 h respectively. Ex-vivo studies indicated that the FOA4 formulated with xanthan gum in the concentration of 2% have shown superior drug release of 56.63 % compared with the other formulations. The emulgels were found to be stable with respect to physical appearance, pH, rheological properties and drug content at all temperature and conditions for one month.
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