Asymmetric Membrane Capsules of Phenylephrine Hydrochloride: An Osmotically Controlled Drug Delivery System

Abstract

The aim of the current study was to develop osmotically controlled release system of freely water soluble drug phenylephrine hydrochloride by use of asymmetric membrane capsules to reduce the dosing frequency and consequently improve the patient compliance. Ethyl cellulose asymmetric membrane capsules were developed by phase inversion process and solubility modulation was accomplished by common ion effect wherein sodium chloride was included in the formulation that also served as an osmogen. The effect of formulation variables namely level of polymer (ethyl cellulose), level of pore former (glycerol) and level of osmogen (sodium chloride) on the in vitro release of the drug was evaluated by 2(3) factorial design. Effects of environmental factors on the release rate of the drug from asymmetric membrane capsules were also evaluated. Membrane characterization by scanning electron microscopy showed an outer dense region with less pores and inner porous region for the prepared asymmetric membrane. The dimensional analysis of asymmetric membrane capsule documented the capsules to be of uniform cap and body size comparable to commercial hard gelatin capsules. In vitro release studies results showed that incorporation of higher amount of osmogen not only increased the osmotic pressure but also controlled the drug release for a period of 12 hr. The drug release was inversely proportional to the level of polymer in asymmetric membrane capsule but directly related to the level of pore former in the membrane. The optimized asymmetric membrane capsule (F5) was able to provide zero order release of phenylephrine hydrochloride independent of agitation rate, intentional defect in the membrane and pH of dissolution medium but was dependent on the osmotic pressure gradient between inside and outside of the delivery system.

Osmotically Regulated Floating Asymmetric Membrane Capsule for Controlled Site-Specific Delivery of Ranitidine Hydrochloride: Optimization by Central Composite Design

“…The results concluded that, when osmogen and pore former were at high levels in FAMC6 and FAMC8, higher release (average release,~92%) was observed than FAMC1 and FAMC2 (average release,~85%), having lower levels of both variables. The effect is attributable to the combined result of increased perforation of the capsular wall and osmotic gradient that has been documented in our previous studies (8)(9)(10)(11). Fig.…”

“…Hence, a solubility modulator (coated NaCl) was used. This approach (based on the common ion effect) has been utilized by us in the development of AMCs of highly water-soluble drugs-phenylephrine hydrochloride (10) and triprolidine hydrochloride (11).…”

“…Research inputs from our group have resulted in the successful development of AMCs of drugs with varying water solubility, namely, ketoprofen (6,7), flurbiprofen (8), promethazine hydrochloride (9), phenylephrine hydrochloride (10), and triprolidine hydrochloride (11), thus proving the efficacy of the system for both poorly water-soluble and highly watersoluble drugs. The present work aims at exploring the feasibility of AMCs for site-specific osmotically regulated delivery of ranitidine hydrochloride (RHCl) as a floating single-unit device.…”

Cellulose Acetate 398-10 Asymmetric Membrane Capsules for Osmotically Regulated Delivery of Acyclovir

“…The results are consistent with the literature report on acyclovir as “slightly soluble in water” at room temperature (22–25°C) and solubility values range from 1.2 to 1.6 mg/mL [ 17 , 18 ]. The solubility is a prominent factor in governing the drug release from an osmotically controlled drug delivery system [ 19 ]. A poorly soluble drug (<10 mg/mL) will be governed by first-order release kinetics rather than zero-order kinetics.…”

Preparation, Properties and Potential of Carrageenan-Based Hard Capsules for Replacing Gelatine: A Review

“…Based on Ridgway [ 20 ], the size of a capsule is classified into five different classes, with size 00 as the biggest and size 3 as the smallest. Kumar et al [ 35 ] developed an osmotically controlled release system of phenylephrine hydrochloride in an ethyl cellulose capsule. Their results showed that the lengths of the cap and body of the capsule were 10.45 ± 0.34 mm and 17.42 ± 0.22 mm, respectively.…”