Iodomethane reacted in vacuo with lyophilized alpha-chymotrypsin to give an inactive enzyme in which the active-site imidazole was dimethylated. However, alpha-chymotrypsin co-lyophilized with the competitive inhibitors, N-acetyl-L-tryptophan or N-acetyl-D-tryptophan, was fully protected from such inactivation. In contrast, indole by itself not only did not protect the lyophilized enzyme from i...

CONTEXT AND OBJECTIVES The buccal mucosa presents a unique surface for non-invasive drug delivery and also avoids first-pass metabolism. The objective of this study was the formulation development of polymeric mucoadhesive lyophilized wafers as a matrix for potential buccal drug delivery. MATERIALS AND METHODS Differential scanning calorimetry (DSC) was used to develop an optimum freeze-cycle...

Introduction To induce sufficient new bone formation, high doses of bone morphogenetic protein-2 (BMP-2) are applied in regenerative medicine that often induce serious side effects. Therefore, improved treatment strategies are required. Here, we investigate whether the delivery of BMP-2 lyophilized in the presence of trehalose reduced the dose of BMP-2 required for bone regeneration. Material...

BACKGROUND Vaccinia immune globulin (VIG) administered via the intramuscular route has historically been used for the treatment of complications of smallpox vaccination. Intravenous formulations of VIG are required to improve tolerability and pharmacokinetic profile. METHODS We conducted 2 separate studies to evaluate the feasibility of administration of an intravenous formulation of antivacc...

Chitosan (CS) floating lyophilized formulations (L) for gastric drug delivery of acyclovir (ACV) have been developed. The freeze-dried formulations were obtained from acidic aqueous suspensions prepared with different ACV/CS ratios. No changes in ACV crystallinity were observed during X-ray diffraction powder studies as a consequence of the manufacturing process. Considering that fed and fasted...

A case study is presented in which a tert-butanol (TBA)/water cosolvent system was found to be a useful means of producing freeze-dried tobramycin sulfate that readily forms a loose powder upon agitation in a specialized application in which a critical quality attribute is the ability to pour the sterile powder from the vial. Both formulation and processing variables are important in achieving ...

Development of a lyophilized orally disintegrating tablet (ODT) that enhanced the in vitro dissolution and in vivo absorption of nimesulide (NM), a drug with poor solubility and poor bioavailability, is presented. The ODTs were prepared by freeze-drying an aqueous dispersion of NM containing a matrix former, a sugar alcohol, and a collapse protectant. In addition, different disintegration accel...

Abstract: The trend of using peptides, short chains amino acids, as therapeutic agents has been increasing in recent decades. Therapeutic peptides usually use the parenteral route systemic delivery system, requiring an aqueous formulation. However, formulation, are often unstable. most stable form peptide is a lyophilized powder. Unfortunately, for tropical and developing countries such Indones...

Background: Microcrystalline cellulose (MCC) is a popular dry binder in tablet formulation. Differences its processing methods can significantly affect tableting properties. Aim: Assessment of the and in-vitro release properties diazepam tablets formulated with Gossypiumherbaceum (GH) derived MCC that was dried by two different methods. Methods: G.herbaceum bolls were de-lignified sodium hydrox...