Evaluation of various properties of alternative salt forms of sulfobutylether-β-cyclodextrin, (SBE)7M-β-CD (original) (raw)
Related papers
Journal of Pharmaceutical Sciences, 2007
The objective of this work was to demonstrate that the incorporation of sulfobutylether-b-cyclodextrin, (SBE) 7M-b-CD, results in the complete and sustained release of a sparingly water-soluble drug, prednisolone (PDL) from controlled porosityosmotic pump pellets (CP-OPP). PDL and CD were prepared in various formulations (physical mixtures and presumed preformed complex). Several factors influencing drug and CD release were explored, and the probable mechanisms of drug release were probed and discussed. A significant improvement in the release of PDL from the CP-OPPs was observed by the incorporation of CD relative to the coated pellet formulation containing lactose in place of the CD. The release profiles of PDL depend on the molar ratio of CD to PDL, thickness of the microporous membrane, and osmotic pressure difference across the membrane. PDL appears to be released as an in situ complex with CD via mainly osmotic pumping during at least the initial portion of the release profiles. ß 2007
Journal of Pharmaceutical Sciences, 2009
The purpose of this work is to delineate the release mechanisms of a sparingly water-soluble drug, prednisolone (PDL), from a microporous or controlled porosity-osmotic pump pellet (CP-OPP) using sulfobutylether-b-cyclodextrin (CD) as both a solubilizing and osmotic agent. All factors, osmotic and diffusional, influencing drug release as described by the Theeuwes and Zentner equation were partially demonstrated in an earlier paper 1 and are further quantitatively evaluated here to determine whether the equation may be applied to CP-OPPs. The PDL release rate from the CP-OPPs containing precomplexed PDL follows the zero-order kinetics for up to 30-40% of drug release during the first 1-2 h and subsequently nonzero order kinetics. The zero-order drug release phase reveals the main contribution is from osmotic pumping with a negligible diffusion component, resulting from the nearly constant driving forces in the system. The nonzero order drug release phase is associated with the dynamic changes in the system (e.g., declining osmotic driving force and greater diffusion component with time). In addition, the parameters related to membrane characteristics were determined, and the effect of viscosity was evaluated for the pellet system. The membranes coated on the CP-OPPs are less permeable to water or solutes than the membranes coated on the previously reported tablets. The viscosity due to the CD decreases as a function of CD concentration, which partly affects the observed drug release profiles. The viscosity effect of CD is significant and captured in a hydraulic permeability term.
Journal of Controlled Release, 1999
The purpose of this study was to define membrane controlling factors responsible for drug release from a controlled-porosity osmotic pump tablet (OPT) that utilizes a sulfobutyl ether-beta-cyclodextrin, (SBE)(7m)-beta-CD, as both a solubilizing and osmotic agent. The OPT was spray coated with cellulose acetate solutions varying the amount and size of micronized lactose, the amount of triethyl citrate (TEC) and the composition ratio of dichlormethane to ethanol. Chlorpromazine (CLP) was used as a model drug. The release of CLP from the OPTs was studied using the Japanese Pharmacopoeia dissolution method. The membrane surface area of the OPTs were measured with multi-point analysis by the gas absorption method. The release rate of CLP from OPTs containing (SBE)(7m)-beta-CD increased with increasing amounts of micronized lactose and decreasing amounts of TEC and lactose particle size in the membrane. Also, the CLP release rates from the spray-coated OPTs using mixtures of varying ratios of dichlormethane to ethanol were almost identical. The membrane surface area of the OPTs following release of membrane components had a linear relationship to CLP release rates from the OPTs. The present results confirmed that the membrane controlling factors responsible for the drug release were the amount and size of micronized lactose and the amount of TEC in the membrane.
Effect of Cyclodextrin Derivatization on Solubility and Efficacy of Drugs
Colloid Science in Pharmaceutical Nanotechnology [Working Title]
Cyclodextrins (CDs) possess cyclic structure having (α-1,4)-linked glucopyranose units making them less vulnerable to enzymatic degradation as than the linear dextrins. Commonly used natural CDs are α-CD, β-CD, and ɣ-CD with truncated cone-like appearance having lipophilic central cavity and hydrophilic exterior surface. The problem of low aqueous solubility of natural CDs can be addressed by reacting them with various reagents to produce water-soluble derivatives. CD derivatives can be categorized in many ways depending upon their substituents, biological activity, polarity, and size. The derivatization of natural CDs produces noncrystalline and amorphous forms with higher water solubility that are physically and microbiologically stable for prolonged time period. Variety of methods can be used to determine average degree of substitution for a modified CD. Dissociation by dilution is considered as major release mechanism of drugs from complex. It is essential to optimize the amount of CDs for a given preparation because they can either retard or promote drug delivery through biological membrane.
Recent Aspect of Cyclodextrin-Based Drug Delivery System
Journal of Inclusion Phenomena and Macrocyclic Chemistry, 2006
The pharmaceutically useful cyclodextrins (CyDs) are classified into hydrophilic, hydrophobic, and ionic derivatives. These CyDs can serve as multi-functional drug carriers, through the formation of inclusion complex or the form of CyD/drug conjugate. In addition, the combined use of different CyDs and/or pharmaceutical excipients is capable of alleviating the undesirable properties of drug molecules, improving efficacy and reducing side effects. This contribution outlines the potential use of CyDs in the design and evaluation of CyD-based drug formulation, focusing on their ability to enhance the drug absorption across biological barriers, the ability to control the rate and time profiles of drug release, and the ability to deliver a drug to targeted site.
Cyclodextrin in Drug Delivery Application: A Review
Journal of Drug Discovery And Therapeutics
The cyclodextrins have a wide range of applications in various areas of drug delivery and pharmaceutical industry due to their complexation ability and other versatile characteristics. The most popular pharmaceutical application of cyclodextrin is to increase the solubility, stability, safety and bioavailability of drug molecules. The idea of this review article is to solve and study any of the findings and application of cyclodextrin (CD) and their derivatives in different areas of drug delivery. This review article introduce the molecular structure, properties like complexation, solubility etc. of cyclodextrins and targeted on its use for parenteral, oral, ophthalmic and nasal drug delivery. Other routes including dermal, rectal, sublingual and pulmonary delivery are again briefly addressed. The aim of this contribution is to focus on the potential application of chemically altared cyclodextrins as high-performance drug carriers in drug delivery systems with emphasis on the other ...
Cyclodextrins – A Review on Pharmaceutical Application for Drug Delivery
Cyclodextrins are widely used and are among the most acceptable pharmaceutical excipients. These are cyclic oligosaccharides compounds with a hydrophilic outer surface and a lipophilic inner/central cavity. This unique property makes them popular excipient in pharmaceutical field. In pharmaceutical industry, Cyclodextrins are mainly been used as a complexation agent to increase aqueous solubility, bioavailability and to stability of drugs. A number of cyclodextrin based products have reached to the market based on their ability to camouflage undesirable physiochemical properties of drugs. This review article aims to asses the properties of cyclodextrin and their use in drug delivery, Complexation techniques, characterization of complex, regulatory status and future scope for their usage in advanced drug delivery. 107 107 determining factor in dermal drug delivery, then cyclodextrin can acts as a permeation enhancer . However, if the drug permeation through the lipophilic Stratum Corneum is the main rate determining factor then cyclodextrins are unable to enhance the delivery. Thus a suitable vehicle must be selected so that cyclodextrin fully exert their functions.
Formulation & evaluation of cyclodextrin complexed tablets by enhancing the dissolution rate
Journal of Innovations in Applied Pharmaceutical Science (JIAPS)
In the present work, studies design, formulation development and evaluation of immediate release tablets of Lercanidipine inclusion complex with a view to improve its aqueous solubility, dissolution rate and oral bioavailability.The inclusion complexes of Lercanidipine were prepared with β-cyclodextrin by physical mixture, Kneading method and solvent evaporation method. The complexes were prepared in different molar ratios of drug and β-cyclodextrin namely 1:1M, 1:2M with β-cyclodextrin.The phase solubility diagram for the complex formation between Lercanidipine and β-cyclodextrin in water are AL type. Phase solubility diagram of Lercanidipine with β-cyclodextrin illustrate the solubility enhancement capacity of cyclodextrin. The aqueous solubility of Lercanidipine increased linearly (R2=0.989) as the function of β-cyclodextrin concentration. The stability constant “Kc” was found to be 164.557M-1.Invitro dissolution studies for pure drug and inclusion complexes and prepared tablets...