Impact of superdisintegrants on efavirenz release from tablet formulations

Abstract

EFV is a non-nucleoside reverse transcriptase inhibitor and is used as part of the highly active antiretroviral therapy for the treatment of human immunodeficiency virus type 1 (HIV) infection. It is also used in combination with other antiretroviral agents as part of an expanded post-exposure prophylaxis regimen to prevent HIV transmission for those exposed to materials associated with a high risk of HIV transmission.EFV has poor aqueous solubility and is a BCS class II drug (1). EFV tablets of 600 mg are available, while lower doses (50, 100 and 200 mg) are generally available as capsules and are prepared by a wet granulation process (2, 3). 185Acta Pharm. 60 (2010) [185][186][187][188][189][190][191][192][193][194][195] Original research paper DOI: 10.2478/v10007-010-0019-6 Impact of superdisintegrants on efavirenz release from tablet formulations Efavirenz (EFV) tablets of different doses were prepared by a wet granulation process using different superdisintegrants such as crosscarmellose sodium (CCS), sodium starch glycollate (SSG) and crosspovidone (CP) to evaluate the role of different disintegrants on the in vitro release of EFV. Further, the mode of addition of disintegrants on EFV dissolution from tablets containing 600 mg of the drug was evaluated by incorporating the disintegrants extragranularly (EG), intragranularly (IG) or distributing them equally (IG and EG). In vitro dissolution of the prepared tablets was conducted using the recommended medium and a dissolution medium developed in-house, which had the ability to discriminate between the formulations.The t 50 and t 80 values were indicative of the fact that the drug release was faster from tablet formulations containing CP. CP was able to release the drug faster than the other two disintegrants in both dissolution media and the drug release was unaffected by the mode of CP addition.Keywords: efavirenz, superdisintegrants, granulation * Correspondence; e-mail: rajeshyelchuri@rediffmail.com Brought to you by | MIT Libraries Authenticated Download Date | 5/12/18 2:48 PM Superdisintegrants generally improve disintegration efficiency compared to traditional disintegrants. They are generally used at low levels in solid dosage forms, typically 1-10 % of mass relative to the total mass of the dosage unit (4). Examples of superdisintegrants are crosscarmellose sodium (CCS), sodium starch glycollate (SSG) and crosspovidone (CP), which are cross-linked cellulose, a cross-linked starch and a cross--linked polymer (polyvinyl pyrrolidone), respectively. Wet granulation is one of the frequently used techniques to prepare blends to be compressed into tablets. The disintegrant can be incorporated in the blend before granulation, referred to as intragranular addition (IG), or after granulation, referred to as extragranular addition (EG), or it can be distributed both intra and extragranularly. EXPERIMENTAL MaterialsEfavirenz (Aurbindo Pharma Ltd., India) was purchased from the source indicated. Crosscarmellose sodium (Ac-di-sol ® , FMC biopolymer) and SS...

Cyclodextrin-Efavirenz Complexes Investigated by Solid State and Solubility Studies

“…EFV belongs to class II of Biopharmaceutical Classification System (BCS); that is, it is poorly water-soluble and highly permeable [1]. Several approaches to improve efavirenz dissolution are reported, namely the manipulation of polymorphs [1], the use of superdisintegrants [2], solid dispersions [3,4], nano-sized polymeric micelles [5] and complexation with two chemically modified β-cyclodextrins, RAMEB and HPβCD [6].…”

In Vivo Wound‐Healing Effects of Novel Benzalkonium Chloride‐Loaded Hydrocolloid Wound Dressing

“…A novel HCD, composed of 1% drug (BC), 27% sodium alginate, 2% crospovidone, 8% polyisobutylene, 25% styrene–isoprene–styrene copolymer, 25% petroleum hydrocarbon resin, and 12% liquid paraffin, was prepared using a hot melting method. Sodium alginate, crospovidone, and liquid paraffin were used as a hydrocolloid forming base [Balakrishnan et al, ; Devi et al, ], drug release‐controlling agent [Rajesh et al, ] and plasticizer [Jones et al, ], respectively and polyisobutylene, styrene–isoprene–styrene copolymer and petroleum hydrocarbon resin were used as the pressure‐sensitive adhesives and elastomers [Zohuriaan‐Mehr and Omidian, ]. These materials impart chemical inertness and excellent resistance to weathering, higher temperatures, and chemicals.…”

Review : Superdisintegran dalam Sediaan Oral

“…Bagian pertama ditambahkan sebelum serbuk dibasahi dengan cairan granulasi (intra) dan sisanya ditambahkan ke granul (ekstra) sebelum tablet dicetak. Mekanisme kerja metode ini yaitu tablet dipecah menjadi granul oleh baian ekstragranular selanjutnya granul terdisintegrasi oleh bagian intragranular untuk melepaskan zat obat ke dalam larutan serta metode ini lebih efektif (Rajesh, et al, 2010).…”