In situ-formed asymmetric membrane capsule for osmotic release of poorly water-soluble drug.
A non-disintegrating, in situ-formed, asymmetric membrane, polymeric capsular system, offering improved osmotic effect, was used to deliver poorly water-soluble drug in a controlled manner. The poorly water-soluble drug ketoprofen was selected as a model drug to demonstrate how controlled release characteristics can be manipulated by design of in situ-formed polymeric capsule with an asymmetric membrane and core formulations. In situ-formed, asymmetric membrane capsule was made by dry method via precipitation of asymmetric membrane on the walls of hard gelatin capsule. Resulting asymmetric membrane composed of a dense outer region with fewer pores and a lighter inner porous region. The present study evaluates the influence of variables based on two-factor composite design, namely, ethylcellulose and osmogen (sodium chloride), apart from studying effect of varying osmotic pressures of dissolution medium and level of pore-former concentration (glycerol) on drug release. Statistical significance was tested at P < 0.05. Results showed the best formulation (F-5) to closely corresponded to extra design checkpoint formulation by a similarity (f2) value of 95.41 and capsules made with 15% w/v EC, 50 mg sodium chloride, 8% w/v glycerol and 30 mg citric acid (F-11), to achieve therapeutic concentration within first hour of dissolution not observed with any other formulations used in the study. Drug release followed Fickinan diffusion and was independent of pH but dependent on the osmotic pressure of the dissolution medium.
Philip
Anil
A
Department of Pharmaceutics, Rajiv Academy for Pharmacy, Mathura- 286001, Uttar Pradesh, India. anilphilip@sancharnet.in
Pathak
Kamla
K
D002214:Capsules; D002851:Chromatography, High Pressure Liquid; D016503:Drug Delivery Systems / Q000379:methods*; D005780:Gelatin / Q000737:chemistry; D008567:Membranes, Artificial; D008855:Microscopy, Electron, Scanning; D009995:Osmosis; D010539:Permeability; D004364:Pharmaceutical Preparations / Q000008:administration & dosage* / Q000737:chemistry; D016062:Porosity; D012995:Solubility; D013056:Spectrophotometry, Ultraviolet; D014867:Water / Q000737:chemistry*
D002214:Capsules; D008567:Membranes, Artificial; D004364:Pharmaceutical Preparations; D014867:Water; D005780:Gelatin