[Isobutane driven salbutamol sulfate metered dose inhaler: formulation selection and respiratory tract absorption in guinea pigs].

This paper is to study the iso-butane (A-31)-driven salbutamol sulfate (SS) metered dose inhaler (MDI) formulations and inhaling status in guinea pigs. Solubility determination and orthogonal design were used to screen non-chlorofluorocarbon (CFC) SS MDI formulations. Intubation inhalation of MDI in guinea pigs was used as a main administration method. Fluorescence HPLC detection method was testified as a potential method in assaying the concentration of SS in plasma of guinea pigs after inhaling various SS MDI formulations. Analysis of the data was executed with statistical moment calculation from which pharmacokinetic parameters were obtained. The results show that A-31 based on SS MDI formulations were screened and the guinea pigs in vivo determination method after inhaling SS MDI was established. The zero-moment rations of SS/A-31 MDI formulation to contrast sample and CFC SS MDI was 143.26% and 147.01%, respectively. The first moment value of SS/A-31 MDI formulation was the highest. It is a preliminary conclusion that the absorption result of SS/A-31 MDI formulation inhaled by guinea pigs is equivalent to HFA-134a formulation in sale and better than CFC formulation. A-31 could be used as a potential substitute candidate for CFC MDI propellant.

Calcium pectinate capsules for colon-specific drug delivery.

The calcium pectinate (CaP) capsule, a novel, colon-specific delivery system, was designed and developed using 5-fluorouracil (5-FU) as a model drug. Technically, CaP capsules were prepared by dipping a glass or stainless steel rod successively into pectin and calcium chloride solutions, followed by subsequent air-drying and coating. In vitro studies showed that the release of 5-FU from CaP capsules markedly increased in the presence of rat cecal contents, and the release characteristic was mainly associated with some capsule parameters such as calcium content, shell thickness, and coat amount. Gamma scintigraphic studies demonstrated that CaP capsules could pass through the stomach and small intestine intact and could release drug in colon. The 5-FU releasing characteristics acquired both from in vitro biomimic dissolution experiments and from healthy volunteers indicated that the newly developed CaP capsule possessed the ideal colon-specific drug delivery characteristic.