Low-Viscosity Hydroxypropylcellulose (HPC) Grades SL and SSL: Versatile Pharmaceutical Polymers for Dissolution Enhancement, Controlled Release, and Pharmaceutical Processing

Abstract

Abstract. Hydroxypropylcellulose (HPC)-SL and -SSL, low-viscosity hydroxypropylcellulose polymers, are versatile pharmaceutical excipients. The utility of HPC polymers was assessed for both dissolution enhancement and sustained release of pharmaceutical drugs using various processing techniques. The BCS class II drugs carbamazepine (CBZ), hydrochlorthiazide, and phenytoin (PHT) were hot melt mixed (HMM) with various polymers. PHT formulations produced by solvent evaporation (SE) and ball milling (BM) were prepared using HPC-SSL. HMM formulations of BCS class I chlorpheniramine maleate (CPM) were prepared using HPC-SL and -SSL. These solid dispersions (SDs) manufactured using different processes were evaluated for amorphous transformation and dissolution characteristics. Drug degradation because of HMM processing was also assessed. Amorphous conversion using HMM could be achieved only for relatively low-melting CBZ and CPM. SE and BM did not produce amorphous SDs of PHT using HPC-SSL. Chemical stability of all the drugs was maintained using HPC during the HMM process. Dissolution enhancement was observed in HPC-based HMMs and compared well to other polymers. The dissolution enhancement of PHT was in the order of SE>BM>HMM>physical mixtures, as compared to the pure drug, perhaps due to more intimate mixing that occurred during SE and BM than in HMM. Dissolution of CPM could be significantly sustained in simulated gastric and intestinal fluids using HPC polymers. These studies revealed that low-viscosity HPC-SL and -SSL can be employed to produce chemically stable SDs of poorly as well as highly water-soluble drugs using various pharmaceutical processes in order to control drug dissolution.

Spray-Dried Amorphous Solid Dispersions of Griseofulvin in HPC/Soluplus/SDS: Elucidating the Multifaceted Impact of SDS as a Minor Component

“…Its melting point temperature T m and glass transition temperature T g are 220 • C and 89 • C [42]. Hydroxypropyl cellulose (HPC), which is a semi-crystalline polymer with low crystallinity and amorphous domains of sub-ambient T g [43], was donated by Nisso America Inc. (SSL grade, New York, NY, USA). Soluplus ® (Sol), donated by BASF, is an amphiphilic graft copolymer made of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol.…”

Development and Optimisation of Novel Polymeric Compositions for Sustained Release Theophylline Caplets (PrintCap) via FDM 3D Printing

“…HPC has been widely used in the pharmaceutical industry as a tablet binder, thickening agent, viscosity increasing agent, and coating agent [23]. A study carried out by Sarode et al shows that HPC can be used to produce chemically stable solid dispersions of poorly and highly water-soluble drugs [26]. The polymer HPC can effectively convert the crystalline drug to amorphous form, improving the dissolution and making the drug a sustained release type.…”

Evaluation of Hot-Melt Extrusion and Injection Molding for Continuous Manufacturing of Immediate-Release Tablets

“…Soluble polymers used as carriers for solid dispersions prepared by HME (HPC, HPMC, PVA, KIR, KVA, Soluplus, Eudragit E) and thermoplastic starch were initially considered . Also, PEGs (6000 and 8000), which were the only polymers already proposed for the manufacturing of tablets by IM, were taken into account for comparison purposes .…”

“…Soluble polymers used as carriers for solid dispersions prepared by HME (HPC, HPMC, PVA, KIR, KVA, Soluplus, Eudragit E) and thermoplastic starch were initially considered. [28][29][30][31][32][33][34][35][36][37][38] Also, PEGs (6000 and 8000), which were the only polymers already proposed for the manufacturing of tablets by IM, were taken into account for comparison purposes. 20 In addition, the ability of starch derivatives employed as disintegrants for solid dosage forms (EXP, EXP CLV , VIV) to behave like thermoplastic starch does when processed in the same way, that is, in admixture with plasticizers, under thermal and mechanical stresses, and to maintain hydration/swelling properties, was investigated.…”