Hot- Melt Extrusion
Hot-melt extrusion (HME) technology is an established solid dispersion technology for improving dissolution rate and solubility, and a component of our premier bioavailability enhancement services. HME has broad applicability across poorly soluble (BCS II and IV) compounds and the resultant extrudate can be readily formulated in either tablets or capsules. We offer our customers flexible end-to-end solutions for bioavailability challenged compounds from concept to commercial, and from API to finished drug products.
Effective delivery of many BCS class II compounds with low solubility can be enabled with amorphous dispersions made by HME. HME manufacture of amorphous dispersion involves the melting of a drug substance with an appropriate polymeric excipient in a co-rotating twin-screw extruder. Functional excipients, such as surfactants, may be added to aid in the extrusion process or to improve dissolution performance upon administration. When cooled, the extrudate generally consists of a single-phase amorphous glassy matrix that can be milled to the desired particle size and incorporated into traditional tablet or capsule dosage forms.
Resultant extrudate is typically milled and directly filled into capsules, or formulated with excipients and compressed into tablet formats. We are fully equipped to produce the hot-melt extrudate and finished dosage form for feasibility assessments, clinical trials and commercial scale applications.
Spray drying technology
A spray dried dispersion (SDD) is a single-phase, amorphous molecular dispersion of a drug in a polymer matrix. It is a solid solution with the compound molecularly “dissolved” in a solid matrix. As the name suggests, SDDs are obtained by dissolving drug and polymer in an organic solvent and then spray drying the solution. The formulation and process conditions are chosen so that the solvent quickly evaporates from the droplets, allowing insufficient time for phase separation or crystallization. In addition to their proven performance in enhancing solubility, SDDs have demonstrated long-term stability, facile scale-up and excellent manufacturability.
Our SDD technology platform incorporates compositions, processes and finished dosage forms designed to meet performance, stability and manufacturing requirements for a diverse range of compounds.
Micro-dosing for powder-in-capsule / powder-in-bottle studies
Micro-dosing is the process of dispensing a precise amount of drug substance into a container – typically capsules, but also bottles or vials – for use in early phase human clinical studies. These “powder in capsule” (PIC) or “powder in bottle” (PIB) studies generally avoid the use of excipients – and the compatibility and stability studies associated with their use – thereby accelerating early phase product development timelines. Accelerating these initial studies to determine if the drug substance should receive further investment is critical in cost-effective product development.
Micro-dosing for PIC evaluations is a key component of our early stage product development offering aimed at accelerated feasibility and first-in-human (FIH) studies. Precision micro-dosing is an increasingly effective tool given the trend towards highly potent compounds requiring very small and precise dose levels.
By combining our market-leading experience in micro-dosing and Lonza Xcelodose® Precision Powder Micro-Dosing Systems, we provide premier PIC evaluations and services for preclinical studies in support of client projects. Our experience indicates that PIC programs are generally completed approximately 50% faster than traditional formulation development approaches using excipients, resulting in time savings of 13-17 weeks. Our micro-dosing services – performed across non-GMP and GMP conditions – are complemented by a full range of clinical supply services including primary and secondary packaging, labeling, kitting, distribution and overall clinical supply management.
Our Xcelodose Precision Powder Micro-dosing Systems are the industry standard for enabling accurate and rapid PIC/PIB studies. These systems allow for precision weighing of drug substances into capsules or bottles from 0.1mg to 200 mg per dose dependent upon the physical characteristics of the API and capsule size. Best-in-class filling accuracy (2% RSD) is achieved at typical speeds of 200-250 capsules per hour dependent upon dose specifics.
Spray drying technology
Pioneered for pharmaceutical applications by Bend Research (now Lonza), spray drying has emerged as a primary technology for addressing poor dissolution rate, solubility and bioavailability. Spray-dried dispersions represent an established approach in bringing an increasing number of BCS II compounds to market. we have premier expertise and capability in spray drying, with integrated capabilities in place to support proof-of-concept through commercial scale manufacture of spray-dried dispersions or finished drug products based on these intermediates.
The majority of today’s drug candidates have low aqueous solubility (BCS II), and require an enabling technology to enhance oral bioavailability. Amorphous solid dispersion approaches utilizing spray dried dispersion (SDD) technology offer a proven and highly flexible approach to significantly improve the bioavailability of promising BCS ll compounds.
Spray drying is also increasingly utilized for dry powder inhaler (DPI) applications, providing particle engineered formulations in the required particle size distribution to meet target product profiles.
Our Bend (OR) site is our Center of Excellence for solid dispersions. The site is equipped with a full range of processing capabilities for spray drying, as well as hot-melt extrusion. Bend also has extensive capabilities in developing and manufacturing finished drug products in monolithic or multiparticulate formats.
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