Roshan Issarani, Roshan
Lachoo Memorial College of Science and Technology, Pharmacy Wing, Jodhpur – 342 003, Rajasthan, India

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DESIGN AND EVALUATION OF GUARGUM - BASED TIMOLOL MALEATE OCULAR INSERT Kumar, Sunil; Issarani, Roshan; Nagori, B P
INDONESIAN JOURNAL OF PHARMACY Vol 26 No 4, 2015
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (15.106 KB) | DOI: 10.14499/indonesianjpharm26iss4pp177

Abstract

The objective of this study was to prepare ocular inserts of timolol maleate using guar gum as a polymer. Timolol maleate ocular inserts were prepared by solvent casting method using guar gum in different proportions (0.25% w/v, 0.50% w/v , 75 % w/v and 1.0% w/v). The prepared formulations were evaluated for thickness, weight variation, percentage drug content, surface pH, folding endurance, percentage moisture absorption and loss, percentage swelling, mechanical strength and in vitro transcorneal permeation. In-vitro transcorneal permeation study was performed on goat cornea using modified Franz diffusion cell. The inserts were found to be of uniform thickness (ranging from 41.12±0.04µm to 79.90±0.03µm) and weight (0.84±0.07 mg to 2.11±0.09 mg). The % drug content in the inserts was found to be varied between 98.69±0.58to 96.37±0.58. The cumulative % drug releases from the formulation ranged from 50.22±1.41 to 97.72±0.67over a period of 24 h. In-vitro transcorneal study revealed that an increase in concentration of polymer slows down the release of timolol maleate from the formulation. Ocular inserts using guar gum as a polymer were successfully prepared and can be effectively used for sustain ocular delivery over a period of 24 h.Key words: Guar gum, in vitro transcorneal permeation study, ocular insert, timolol maleate, sustained release
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
Ocular Insert: Dosage Form for Sustain Opthalmic Drug Delivery Thakral, Sunil Kumar; Nagori, Badri P.; Issarani, Roshan; Ahuja, Munish
Indonesian Journal of Clinical Pharmacy Vol 1, No 2 (2012)
Publisher : Indonesian Journal of Clinical Pharmacy

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (1167.891 KB)

Abstract

Except for skin, the eye is the most easily accessible site for topical administration of a medication. Traditional topical ophthalmic formulations (eye drops and ointments) have poor bioavailability because of rapid pre-corneal elimination, conjunctival absorption, solution drainage by gravity, induced lacrimation and normal tear turnover. This leads to frequent  installations of concentrated medication to achieve a therapeutic effect. The typical “pulse-entry” type drug release observed with ocular aqueous solutions (eye drops), suspensions and ointments can be replaced by more controlled, sustained, and continuous drug delivery, using a controlled-release ocular drug delivery system. Ocular inserts are solid or semisolid sterile preparations, of appropriate size and shape, designed to be inserted behind the eyelid or held on the eye and to deliver drugs for topical or systemic  effect. These are polymeric systems into which the drug is incorporated as a solution or dispersion. They are better tolerated as to drainage and tear flow compared with other ophthalmic formulation and produce reliable drug release in the conjunctival cul-de-sac.Key words: Eye, ocular inserts, films simulated tear fluid, cul-de-sac Penyisipan Okular: Sediaan untuk Penghantaran Obat Mata DiperlambatAbstrakMata adalah organ yang paling mudah dijangkau untuk pengobatan topikal selain kulit. Formulasi sediaan topikal tradisional untuk mata (tetes mata dan salep) memiliki ketersediaan hayati yang rendah karena cepat dieliminasi sebelum mencapai kornea, absorpsi konjungtiva, kekeringan cairan mata karena gravitasi, lakrimasi terinduksi, dan pergantian normal air mata. Hal ini mengarahkan pada penggunaan obat yang pekat secara berulang untuk menghasilkan efek terapi. Tipe obat pulse-entry seperti tetes mata, suspensi, dan salep dapat digantikan dengan penghantaran obat yang lebih terkontrol, diperlambat, dan berkelanjutan menggunakan sistem penghantaran obat okular yang pengeluarannya dikontrol. Sediaan penyisipan okular merupakan sediaan steril berbentuk solid dan semisolid, dengan ukuran dan bentuk yang sesuai, serta didesain untuk dapat disisipkan di belakang kelopak mata atau diletakkan di atas mata untuk menghantarkan efek obat secara topikal atau sistemik. Sediaan ini  merupakan sistem polimer yang tidak larut atau terdispersi. Sediaan ini lebih baik dalam hal pengeringan dan aliran air mata dibandingkan formulasi sediaan mata yang lain dan menghasilkan pengeluaran obat yang reliabel pada konjungtiva kuldesak.Kata kunci: Mata, penyisipan okular, simulasi cairan air mata film, kuldesak