Sunil Thakral, Sunil
Akal College of Pharmacy and Tecchnical Educaiton, Mastuana Sahib, Sangrur, Punjab, 148001, India

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Formulation of the Model Fluconazole Eye Drop and Its Comparison with the Available Fluconazole Eye Drops Thakral, Sunil; Ahuja, Munish
Indonesian Journal of Clinical Pharmacy Vol 1, No 1 (2012)
Publisher : Indonesian Journal of Clinical Pharmacy

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (631.595 KB)

Abstract

The aim of the study was to formulate the model formulation of fluconazole eye drop and then compare it with the available eye drops. The corneal permeation studies were conducted using freshly excised sheep cornea, mounted between donor and receptor. The receptor cell had an internal volume of 11 mL, containing ringer bicarbonate (pH 7.4, 34±1 0C). At appropriated intervals 2 ml. samples were withdrawn from the side arm and were analyzed spectrophotometrically by measuring absorbance at λmax of 260 nm. Each experiment was continued for about 2.0 hrs (triplicate). At the end of the experiment, each cornea (freed from sclera) was weighed, soaked in 1 mL. methanol, dried overnight at 90 °C and reweighed. From the difference in weights corneal hydration was calculated. Even though, the marketed formulation (Zocon) comprised of 0.3% w/v of fluconazole and our model formulation contained only 0.2% w/v of fluconazole, the amount of fluconazole permeated from model formulation and the marketed formulation was respectively 78.34±4.26 and 22.14±1.3. The permeation from model formulation was much greater than other preparations and shows less corneal hydration (80.29±0.47) than others available preparations.Key words: Fungal kerititis, fluconazole, in vitro permeation, corneal hydration, model formulationsFormulasi Tetes Mata Fluconazole dan Perbandingannya dengan Tetes Mata Fluconazole di PasaranAbstrakPenelitian ini bertujuan untuk melakukan formulasi tetes mata flukonazol dan membandingkannya dengan tetes mata yang beredar di pasaran. Studi permeasi kornea dilakukan dengan menggunakan kornea biri-biri yang telah dikeluarkan, disatukan antara donor dan reseptor. Sel reseptor memiliki volume internal 11 mL, mengandung ringer bicarbonate (pH 7,4, 34±1 0C). Sampel diambil pada interval 2 mL sampel dari bagian lengan bejana dan dianalisis menggunakan spektrofotometri dengan pengukuran absorbansi pada λmax 260 nm. Percobaan dilanjutkan selama dua jam (triplikat). Pada akhir percobaan, setiap kornea (dipisahkan dari sklera) ditimbang, direndam dalam metanol, dikeringkan pada suhu 90 C dan ditimbang ulang, perbedaan berat dari hidrasi korena dihitung. Formulasi yang dipasarkan (Zocon) terdiri atas 0,3% w/v flukonazol sedangkan model formulasi dari penelitian ini hanya mengandung 0,2% w/v flukonazol, jumlah flukonazol yang mengalami permeasi dari model formulasi dan formulasi dipasarkan masing-masing sebesar 78,34±4,26 and 22,14±1,3. Permeasi dari model formulasi lebih besar dibandingkan dengan sediaan dan menunjukkan nilai hidrasi korneal lebih kecil (80,29±0,47) dibandingkan dengan sediaan di pasaran.Kata kunci: Fungal kerititis, fluconazole, permeasi in vitro corneal hydration, model formulations
Formulation and In Vitro-In Vivo Correlation of Timolol Maleate Ocular Insert Thakral, Sunil; Issarani, Roshan; Nagori, Badri P.
Indonesian Journal of Clinical Pharmacy Vol 4, No 4 (2015)
Publisher : Indonesian Journal of Clinical Pharmacy

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (442.511 KB) | DOI: 10.15416/ijcp.2015.4.4.281

Abstract

The concept of in-vitro and in-vivo correlation studies was used in pharmaceutical research because a simple in-vitro release study on a drug product will be insufficient to predict its therapeutic efficiency. Therefore, correlation between in-vitro release behavior of a drug and its in-vivo absorption in rabbits must be demonstrated experimentally to reproduce therapeutic response. Aim of the study was to study the in vitro and in vivo evaluation and correlation of timolol maleate ocular insert. Timolol maleate ocular inserts were prepared by solvent casting method using guar gum in different proportions (0.25% w/v, 0.50% w/v, 0.75 % w/v, and 1.0% w/v). In vitro transcorneal permeation study was performed on goat cornea using modified Franz diffusion cell. The in vivo study was done using New Zeland albino rabbits and the in vitro invivo correlation (IVIVC) was determined by plotting a graph of in vivo drug release was plotted against in vitro release to determine the correlation. The cumulative % drug releases from the formulation ranged from 50.22±1.41 to 97.72±0.67over a period of 24 h. In vivo release of the timolol maleate from the optimized ocular inserts F2, through conjunctival cul-de-sac of rabbits was 76.03±1.43 at the end of 24 h. A high value of correlation coefficient (r2=0.9965) suggested good correlation between the in vitro-in vivo data of the timolol maleate ocular insert.Keywords: Guar gum, IVIVC, in vitro transcorneal permeation study, ocular insert, timolol maleate Formulasi dan Korelasi In vitro-In vivo pada Timolol Maleat dengan Penyisipan OkularKonsep studi korelasi in-vitro dan in-vivo telah digunakan dalam penelitian farmasi karena studi invitro yang sederhana pada produk obat tidak cukup untuk memprediksi efisiensi terapi. Oleh karena itu, korelasi antara pelepasan in vitro obat dan penyerapan secara in vivo pada kelinci harus dapat didemonstrasikan secara eksperimental untuk menghasilkan respons terapi. Tujuan penelitian ini adalah mengevaluasi formulasi dan korelasi in vitro dan invivo pada timolol maleat dengan penyisipan okular. Penyisipan okular timolol maleat disiapkan dengan metode pemilihan pelarut menggunakan guar gum pada proporsi berbeda (0,25% w/v, 0,50% w/v, 0,75 % w/v, dan 1,0% w/v). Permeasi transkorneal in vitro dilakukan pada kornea kambing menggunakan modifikasi difusi sel Franz. Studi in vivo dilakukan pada kelinci albino New Zeland dan korelasi invitro invivo (IVIVC) ditentukan dengan pelepasan in vivoobat yang diplot pada grafik yang dihubungkan dengan pelepasan in vitro untuk menentukan korelasi. Pelepasan kumulatif obat (%) dari formulasi memiliki rentang antara 50,22±1,41 sampai 97,72±0,67 pada lebih dari periode 24 jam. Pelepasan in vivo timolol maleat dari penyisipan okular teroptimasi F2, melalui konjungsi kul-de-sak pada kelinci yaitu 76,03±1,43 pada akhir periode 24 jam. Nilai yang tinggi dari koefisien korelasi (r2=0,9965) menunjukkan korelasi yang baik antara invitro dan invivo data penyisipan okular pada timolol maleat.Kata kunci: Guar gum, IVIVC, penyisipan okular, studi permeasi transkorneal in vitro, timolol maleat