Formulation Development and Evaluation of Fast Disintegrating Sustained Release Pellets Containing Verapamil Hydrochloride Tablets by Fluidized Bed Processor

This study aimed to developed novel fast disintegrating sustained release pellets containing tablet by using Fluidized Bed processor. Verapamil HCl used as a model drug for the formulation. Fluidized bed processor was used for coating of drug and polymer on the sugar spheres. To overcome the problem of swallowing for paediatric, geriatric, psychiatric, bedridden patients, uncooperative patients or for active patients who are busy and travelling and may not access to we aim to formulate the fast-disintegrating tablet. The superdisintigrant are commonly use like cross povidone, sodium starch glycolate which disintegrate tablet rapidly. It is assumed that, after the disintegration of tablets, pellets within tablets which are reside in GIT for several hours and gradually released a drug in controlled way. Eudragit RS 30D and ethyl cellulose were used as a sustained release polymer. Coating of spheres with sustained release film is achieved by bottom spray processor of FBP. Proper pellets coating film thickness, and concentration of polymers’, ensure obtaining desirable VH release profile for extended period of time, was defined. X composition of tablet with pellets were examined in order to obtained formulation, from which VH release would mostly appropriate pellets before compressing. Compression of pellets into tablet, being a modern technological process than enclosing them into hard gelatine capsule. The optimized batch evaluated by studied the effect of compression force, tablet hardness and friability and drug release from the pellets by sustained release manner.

Evaluation of Drug Release from Carboxymethyl Starch-Xanthan Gum-HPMC Matrix

The use of hydrophilic polymers from natural origin. Especially the polysaccharides have been the focus of current research activity in the design of matrix device due to their non toxic, biocompatible, biodegradable nature and broad regulatory acceptance. A large number of polysaccharides such as Carboxymethyl starch, Xanthan gum, Hydroxy propyl methyl cellulose (HPMC), Sodium Alginate etc, have been used as hydrophilic matrices to investigate release behavior of drug. In order to enrich the resources, there is a quest for new polysaccharide owing to their diverse chemical composition and functional groups are amenable to chemical modification and thus tailor made polymeric matrices are obtained which which can be used to modulate oral drug release. The objective of the study is to characterize Verapamil hydrochloride loaded matrix dosage form using hydroxy propyl methyl cellulose (HPMC), xanthan gum, corn starch as rate retarding polymer. Dosage forms were prepared using different polymers along with drug Verapamil hydrochloride. Carboxymethylation was performed. Drug release was evaluated in simulated gastric media. Addition of xanthan gum significantly retarded the burse release of drug. The retardation of drug release was found to be dependent upon the concentration. The formulation composed of HPMC K4M and CS (ARI-ARI3) followed super case transport is swelling controlled, purely relaxation controlled drug delivery. Keywords: Verapamil HCl, Natural gums, xanthan gum, HPMC, sustained release

PENGARUH MATRIKS PEKTIN DAN HPMC K15M TERHADAP DAYA MENGAPUNG DAN MENGEMBANG SERTA DISOLUSI PADA TABLET FLOATING VERAPAMIL HCl DENGAN METODE FACTORIAL DESIGN

Verapamil HCl merupakan penghambat kanal Ca2+ untuk terapi hipertensi dan angina pectoris. Verapamil HCl memiliki bioavabilitas 10-20% dan waktu paruh 4 jam sehingga dapat dibuat sediaan gastroretentive untuk mempertahankan kadar terapi obat. Penelitian ini bertujuan mengetahui pengaruh matriks pektin dan HPMC K15M terhadap kemampuan mengapung, mengembang dan pelepasan obat pada tablet floating verapamil HCl.Penelitian ini menggunakan empat formula variasi konsentrasi matriks pektin dan HPMC K15M dengan metode kempa langsung kemudian dilakukan pengujian terhadap sifat fisik serbuk dan tablet. Pengaruh dan interaksi antara pektin dan HPMC K15M ditentukan dengan metode factorial design menggunakan software Design Expert.Matriks pektin dan HPMC K15M memberikan pengaruh terhadap kemampuan mengapung, mengembang dan pelepasan obat dari tablet floating verapamil HCl. HPMC K15M berpengaruh dominan terhadap floating lag time yang lebih cepat dan floating time yang lebih lama. Peningkatan HPMC K15M dan pektin menurunkan jumlah pelepasan di awal dan kecepatan pelepasan obat, serta meningkatkan kemampuan mengembang. Kombinasi pektin dan HPMC K15 M (1,5:1) mempunyai floating lag time cepat, floating time lama, dan kemampuan mengembang paling besar serta mengikuti orde nol.

Formulation and Evaluation of Novel Sericin Nanoparticles for Buccal Delivery of Antihypertensive Drug

The aim of this study is to prepare and evaluate sericin nanoparticles (NPs) of Verapamil Hcl which are finally formulated as buccal gel. It was envisaged to formulate the nanoparticles with gelatine, sericin and genipin. Nanoparticles incorporated gel was successfully prepared by using carbopol 934. Nanoparticles were prepared by dessolvation followed by crosslinking. Various parameters like drug content, viscosity, pH, spreadability and drug release were used to obtain the optimized formulation. The sericin nanoparticles incorporated gel shows better fast release as compare to API. The obtained results like drug content, % drug release, buccal permeation study confirmed the potential of nanoparticles as good carrier for buccal administration. The optimised sericin nanoparticles range between 100-400 nm with a zeta potential of 29.91mv showing good stability. Later, we proved our hypothesis through In vitro studies for pharmacokinetics, where we found that NPs had better bioavailability than API. NPs showed protective action and maintained normal tissue architecture. We concluded that nanoparticle form of verapamil had better bioavailability and good pharmacological actions, which might be beneficial for future formulation design perspective.

COMPARATIVE EVALUATION OF THE RELEASE PROPERTIES OF VERAPAMIL HCL AND CARBAMAZEPINE FROM MICROCRYSTALLINE CELLULOSE II PELLETS

Objective: To study microcrystalline cellulose II (MCCII) as new pelletization aid for a high and low solubility drugs such as verapamil. HCl and carbamazepine, respectively.Methods: Approximately, 30 g of MCCII and drug mixtures were hydrated passed through a # 20 mesh sieved and spheronizated at a frequency of 6 Hz and residence time of 480 s. A microscopy analysis was used to evaluate the shape and size descriptors. Pellets properties such as compressibility, friability, density, flowability and product yield were also evaluated. Drug release properties were tested according to the USP specifications and compared to those of MCCI.Results: The wetting level of the excipients depended on drug loading and drug solubility. Thus, a high drug loading (>50%) rendered pellets having a low yield, flowability and caused a detriment on size descriptors. Likewise, the regular morphology and strength of MCCII-based pellets was highly affected by increasing drug loads. Verapamil. HCl pellets were less friable and compressible and showed better flowability than carbamazepine pellets. Regardless of drug loading and drug solubility, MCCII-based pellets released more than 80% of verapamil. HCl within 10 min, whereas released more than 75% of carbamazepine within 15 min. Conversely, MCCI pellets had a satisfactory verapamil. HCl release, but ~30% carbamazepine release within 1h.Conclusion: MCCII proved to be a better excipient than MCCI to yield beads having optimal pellet characteristics and rendered an immediate release profile for verapamil. HCl and carbamazepine.