Development of Dispersible Self-microemulsifying Tablet of Atorvastatin

Abstract

Aim: The aim of this study was to develop dispersible self-microemulsifying (SMEDDS) tablet of atorvastatin for promoting its solubility and thus its oral bioavailability. Materials and Methods: The liquid SMEDDS were prepared by water titration method using oil, surfactant and co-surfactant and converted into solid-SMEDDS (S-SMEDDS) by adsorption on solid carriers (Neusilin US2). The S-SMEDDS were blended with sodium starch glycolate (disintegrant) and tablet excipients and compressed into tablets that were dispersible and self-microemulsifying in nature. All these formulations were assessed for various physicochemical parameters viz. weight variation, hardness, friability, disintegration test. In vitro studies of pure drug, SMEDDS, S-SMEDDS and dispersible SME-tablets were carried out. Results: Pure drug released only 29.84 ± 0.16% upto 60 minutes and all the SMEDDS formulations (i.e. SMEDDS. S-SMEDDS and dispersible SME-tablets) released 100% of drug in comparatively lesser time. Formulations containing atorvastatin, 30% oleic acid, 65% tween 80 and 5% co-surfactant came out to show the best results in in vitro studies. But, FB1 (tablet) was considered to be the best since it released 100% drug in 35 min and also has advantages over SMEDDS and S-SMEDDS in terms of stability and patient compliance. Conclusion: The study revealed the potential use of dispersible SMEDDS tablet for the oral delivery of hydrophobic drugs, such as atorvastatin.

Solubility and Dissolution Enhancement of Atorvastatin Calcium using Solid Dispersion Adsorbate Technique

“…The poor oral bioavailability is attributed to presystemic clearance in the gastrointestinal mucosa and high hepatic first-pass metabolism (6) . Many authors have worked to improve the solubility and dissolution rate of ATR by preparing microsphere, emulsion, nanosuspension, self-microemulsion, solid dispersion (7) . Solid dispersion (SD) is the most generally used technique for bioavailability enhancement of poorly water-soluble drugs, as the drug dispersed in freely soluble carrier (8) .…”

Development and Characterization of Oro-Dispersible Tablets of Metformin Hydrochloride Using Cajanus Cajan Starch as a Natural Superdisintegrant

“…Orodispersible tablets (ODTs) signify a rapidly evolving method of drug delivery with higher patient's compliance. For individuals that have swallowing problems, ODTs are very beneficial [2][3][4]. The disintegrate time of ODTs is within a minute and is suitable for patients with dysphasia [5,6].…”

Formulation Development of Albendazole-Loaded Self-Microemulsifying Chewable Tablets to Enhance Dissolution and Bioavailability

“…Although albendazole has been developed as SEDDS [4] and SMEDDS [13] to enhance the dissolution and bioavailability of drugs, liquid dosage forms are inconvenient to carry and difficult to administer as compared to solid dosage forms. In addition, solid pharmaceutical preparations are more stable than liquid preparations and their portability is convenient during the manufacturing process [14]. In fact, SMEDDS does not contain water in their composition, which enhances their chemical and physical stability.…”

“…The major disadvantage of conventional SMEDDS is the high manufacturing cost as they have to be filled in soft gelatin capsules and they can interact with the shell components of the capsule in the SMEDDS. In addition, precipitation of either active ingredient and/or oil constituents can also be influenced by storage temperature [14,15]. Therefore, attention has been given to transform liquid into solid SMEDDS by several techniques such as spray drying, spray cooling, super critical fluid technology, and using adsorption carriers [14,16].…”

“…In addition, precipitation of either active ingredient and/or oil constituents can also be influenced by storage temperature [14,15]. Therefore, attention has been given to transform liquid into solid SMEDDS by several techniques such as spray drying, spray cooling, super critical fluid technology, and using adsorption carriers [14,16]. Colloidal silica, a successful inexpensive hydrophobic carrier, requires common laboratory instruments to formulate as a vehicle for the preparation of solid SMEDDS [16,17].…”