Development of directly compressible metformin hydrochloride by the spray-drying technique

Abstract

Direct compression, although simple in terms of the unit operations involved, is highly influenced by powder characteristics such as flowability, compressibility and dilution potential. Tablets consist of active drugs and excipients, and no drug substance or excipient possesses all the desired physico-mechanical properties required for the development of a robust direct-compression manufacturing process, which could be smoothly scaled from the laboratory to production scale. Most formulations (70-80 %) contain ex- Metformin hydrochloride exhibits poor compressibility during compaction, often resulting in weak and unacceptable tablets with a high tendency to cap. The purpose of this study was to develop directly compressible metformin hydrochloride by the spray-drying technique in the presence of polymer. Metformin hydrochloride was dissolved in solutions containing a polymer, namely polyvinylpyrrolidone (PVP K30), in various concentrations ranging from 0-3 % (m/V). These solutions were employed for spray-drying. Spray-dried drug was evaluated for yield, flow property and compressibility profile. Metformin hydrochloride spray-dried in the presence of 2 % PVP K30 showed an excellent flow property and compressibility profile. From the calculated Heckel's parameter (Py = 2.086), it was demonstrated that the treated drug showed better particle arrangement in the initial compression stage. Kawakita analysis revealed better packability of the treated drug compared to the untreated drug. Differential scanning calorimetry and Fourier transform infrared spectroscopy experiments showed that the spray-dried drug did not undergo any chemical modifications. Tablets made from the spray-dried drug (90 %, m/m) were evaluated for crushing strength, friability and disintegration time and the results were found satisfactory.

Untitled

“…The true density was calculated as the density of compacts formed when maximum pressure (here 60 MPa) was applied on the powder/ agglomerates. [35] The results indicated notable improvement in the compactibility of agglomerates compared to pure drug crystals. The linearity in the Heckel plot [ Figures 4 and 5] was a suggestion of plastic deformation.…”

Dissolution enhancement of chlorzoxazone using cogrinding technique

“…Larger the value of ‘K’, greater was the plasticity in coground sample compared to pure drug. [ 51 52 ] Initial nonlinear region followed by linearity in the graph [ Figure 3 ] was a sign of plastic deformation in case of coground sample. Lower “A” value compared to pure drug suggested that, low compression pressure was required to obtain closest packing, fracturing its texture and densifying the fractured particles in case of coground sample.…”

Influence of excipients and processing conditions on the development of agglomerates of racecadotril by crystallo-co-agglomeration

“…[40] The optimized agglomerates exhibited a significant improvement in the packability compared to the pure drug [Figure 8]. The improvement in true density in the agglomerates compared to the pure drug was also an indication of enhanced compaction.…”