What's New

Get Adobe Acrobat You need the free Adobe Acrobat to view the PDFs. Download it here.

Technical Newsletter

13 April 2016

Continuous Hot Melt Extrusion with Neusilin®

Neusilin® 's high specific surface area, increased surface adsorption, porosity, anticaking, flow enhancing properties and its ability to keep drugs stable under amorphous state has made Neusilin® the best choice inorganic carrier for development of free flowing powder of solid dispersion and directly compressible tablets. One-step continuous dry granulation via Hot Melt Extrusion (HME) provides one path forward to reduce cost of manufacturing, increase efficiency and allow real time assurance of activity via innovative processing strategies. We previously reported manufacture of Sulindac-Neusilin® amorphous drug complex using HME.1)2) .
In this newsletter, we introduce a collaborative study by Dr. Douroumis research group at University of Greenwich and Fuji Chemical Industries to evaluate the performance of Neusilin® (NEU) as an inorganic carrier in HME processing of indomethacin (INM).3)HME was explored as a continuous one-step hot granulation process for the development of solid-state dispersions.

 

Read More 

13 November 2014

Neusilin® - The Optimal Method to Expand Your Dosage Forms for Your SEDDS

In developing Self Emulsifying Drug Delivery System (SEDDS) or Self Nano-Emulsifying Drug Delivery System (SNEDDS), optimization study of formulation is conducted and evaluated with the emulsified liquid. However, in order to expand the dosage forms, the liquid SEDDS/SNEDDS needs to be converted into solid one. With so many choices available for the conversion, the carrier adsorption may be the preferred method since it is energy-efficient and does not require special equipment.
In this newsletter, we introduce two case studies with Berberine and Cilostazol from recently published papers.

 

Read More

10 November 2013

Neusilin® - The Most Competent Adsorbent Carrier for your SMEDDS

We introduced in previous issues of Pharmaceutical Technical Newsletter that Neusilin® is an excellent adsorbent carrier for solid dispersion via hot melt granulation1(Neusilin featured article #1), and preparation of liquidsolid tablets of Self Emulsifying Drug Delivery Systems(SEDDS)2,3,4,5 (Issue27/Issue28/Issue29). intended for improving dissolution profile of poorly water soluble APIs . The physical and chemical stability of amorphous state of drug-Neusilin® complexes for long periods have been well established. In this Newsletter, we introduce two recent studies published by independent research groups as further examples of Neusilin®'s ability to support development of solid dispersion of a wide variety of active pharmaceutical ingredients.

 

Read more

19 February 2013

pH independent bi-layer self-microemulsifying tablets (SMETs) of Candesartan cilexetil with Fujicalin® and Neusilin®

 

Candesartan cilexetil (CDC), an angiotensin II receptor antagonist is a prodrug which gets converted to active drug Candersartan during absorption from the gastrointestinal tract. The conventional CDC tablets have a significantly low bioavailability of approximately 14% after oral administration.

Self-microemulsifying drug delivery system (SMEDDS) approach is becoming a common practice to enhance oral bioavailability of poorly water soluble drugs. To produce tablets of SMEDDS and to have a desired dissolution profile is considered one of the most difficult tasks for a formulator. Through several publications and commercial products, Neusilin® and Fujicalin® have proved to be one of the best adsorbent carriers available in the industry today. In this newsletter, we summarized a recent study by Sohn et al. where a-pH-independent fast release bi-layer self-microemulsifying tablets (SMETs) of Candesartan cilexetil were prepared using Neusilin® and Fujicalin® as adsorbent carriers.


22 January 2013

Oral Self Emulsifying Powder (SEP) of Lercanidipine hydrochloride with Neusilin®

Self-Emulsifying Drug Delivery Systems (SEDDS) improve the oral bioavailability of poorly water soluble drugs. However, the traditional SEDDS as liquid dosage forms has limitations such as low drug loading capacity, drug leakage, low stability, excipient-capsule incompatibility and possibility of irreversible drugs/excipients precipitation. To overcome these complications, the liquid SEDDS are adsorbed on to inert carriers to produce solid SEDDS. Neusilin®'s high specific area, increased surface adsorption, porosity, anticaking flow enhancing properties and its ability to keep the drug stable under amorphous state make it one of the best choice carriers today.
Lercanidipine hydrochloride (LCH: a highly lipophilic calcium channel antagonist used in treatment of hypertension) has the oral bioavailability of approximately 10% and shows erratic absorption from gastrointestinal tract which is attributed to extensive first pass metabolism and low solubility.
The liquid SEDDS of LCH was formulated into solid SEDDS as Self-Emulsifying Powder (SEP) by adsorbing on to Neusilin® as carrier.
High dissolution efficiency value of SEP compared with pure drug indicated the increase in dissolution characteristics of LCH in SEP.

30 November 2012

Solid Self Emulsifying DDS of Paliperidone with Neusilin®

Self-Emulsifying Drug Delivery Systems (SEDDS) have proved to be the promising technology for improving bioavailability of poorly water soluble drugs. The commercialization of a few SEDDS such as Fortovase (saquinavir), Norvir (Ritonavir), and Neoral (cyclosporine) established interest in the commercial viability of these formulation systems. To overcome some complications in SEDDS, the liquid SEDDS are adsorbed on to inert carriers to produce solid SEDDS.
Neusilin®'s high specific area, increased surface adsorption, porosity, anticaking, flow enhancing properties and its ability to keep the drug stable under amorphous state make it one of the best choice carriers today.
Paliperidone (9-hydroxyrisperidone, an active metabolite of risperidone a second-generation antipsychotic for the treatment of schizophrenia) has limited bioavailability of 28%.
Paliperidone loaded SEDDS was formulated into solid SEDDS by adsorbing on to Neusilin® as carrier. The in vitro dissolution study indicates improved dissolution characteristics with higher dissolution efficiency for solid SEDDS (SEDDS-N) compared to pure drug.

30 October 2012

Self-Nano Emulsifying Powders (SNEPs) of Zaleplon with Neusilin�®

Enhancing the oral bioavailability of poorly water soluble drugs is one of the biggest challenges facing formulators. Solid dispersions and in particular Self-(nano)Emulsifying Drug Delivery Systems (SEDDS/SNEDDS) have proved to be the most practical route to commercialization. Successof Fortovase® (Saquinavir), Norvir® (Ritonavir) and Neoral® Cyclosporine) as lipid suspensions have prompted formulators to develop more stable forms by converting these suspensionsinto powder. Neusilin®'s high specific area, increased surface adsorption, porosity, anticaking, flow enhancing properties and its ability to keep the drug stable under amorphous state make
it one of the best choice among adsorbents available today.
Zaleplon (a nonbenzadiazepine sedative and hypnotic drug used in treatment of insomnia) has bioavailability of only 30%. Janga et al 2012 demonstrated that Zaleplon SNEP-Neusilin® powder formulation had higher predicted human permeability coefficient and percentage fraction oral dose adsorption in model systems.

The authors chose Neusilin® over Aerosil® 200, Maltodextrin and Pearlitol® SD200 due to it's improved performance.

09 July 2012

Improvement in Dissolution Property of Poorly Water-Soluble Drugs by Mechanofusion System

Improvement in dissolution property of poorly water-soluble drugs is an extremely important subject in recent drug development. Various methods have been reported to improve the dissolution property of poorly water-soluble drugs, such as micronization (co-grinding), amorphization, and solid dispersion.
The Mechanofusion system  developed in Japan in the mid-1980s is another approach to improve dissolution. The system is  based on a high-powered mechanical energy device to dry coating powders without using any liquids[1,2]. In a dry coating process, tiny, submicron or nanosized (guest or fine) particles are coated onto relatively larger, micron-sized (host or core) particles in order to create value-added composite particulate materials. In contrast to wet-particle coating, the guest particles are brought into close contact with the host particles through the application of mechanical forces.

 

Read More

15 November 2011

Manufacture of Sulindac-Neusilin® Amorphous Drug Complex using Hot Melt Extrusion

Hot Melt Extrusion (HME) offers several advantages over traditional pharmaceutical processing techniques such as, few processing steps, continuous operation, little or no solvents and commercial scale production of solid dispersions with improved bioavailability. New Chemical Entities (NCEs) with solubility problems are prime candidates for HME. HME allows dispersion of poorly water soluble drugs in a given matrix at the molecular level via the formation of solid solution. The most exciting part of using Neusilin® in HME is that solid dispersions can be prepared without any addition of solvents or polymers.

In this newsletter, we report a summary from a recent publication by Maclean et al on manufacture of Sulindac-Neusilin® amorphous drug complex via HME.

 

Read more

14 January 2011

Liquid loadable tablets of Neusilin® US2 - A new approach to tabletting lipid formulations, the case of Cyclosporine A

In this newsletter we present a new research of Camella Sander and Per Holm in 2009 showing that liquid loadable tablets of Neusilin US2 could be a promising approach to achieve oral solid dosage forms from formulations of self-microemulsifying drug delivery system (SMEDDS).

 

Read more (PDF)

Back to top