Volume 7

October-December 2015

Review Articles

Meenakshi Kandwal, G Gnanarajan, Preeti Kothiyal

Floating drug delivery system are designed to prolong the gastric residence time after oral administration at particular site and controlling the release of drug for achieving the controlled plasma level as well as improving bioavailability. They provide local delivery to specific regions like stomach and proximal small intestine and shows better bioavailability and improved therapeutic activity and substantial benefit to patients. They offer several advantages over conventional dosage forms. Effervescent and Non-effervescent are two classes of floating drug delivery system and can formulate either in single unit dosage form or in multiple unit dosage form.

Keywords: Floating Drug Delivery System, Effervescent, Non-Effervescent.

Rewar S, Bansal B K, Singh C J, Sharma A K, Pareek R

Pulsatile drug delivery systems (PDDS) are gaining importance as these systems deliver the drug at specific time as per the pathophysiological need of the disease, resulting in improved patient therapeutic efficacy and compliance. A Pulsatile drug release, where the drug is released rapidly after a well-defined lag-time, could be advantageous for many drugs or therapies. A pulse has to be designed in such a way that a complete and rapid drug release is achieved after the lag time so as to match body’s circadian rhythms with the release of drug which increases the efficacy and safety of drugs by proportioning their peak plasma concentrations during the 24 hours in synchrony with biological rhythm. Various techniques are available for the pulsatile delivery like pH dependent systems, time dependent systems, etc. Pulsatile release systems can be classified in multiple-pulse and single-pulse systems. A popular class of single-pulse systems is that of rupturable dosage forms. Advantages of the Pulsatile drug delivery system are reduced dose frequency; reduce side effects, drug targeting to specific site like colon and many more. Now in market varies technologies of pulsatile drug delivery system like Pulsincap, Diffucaps etc. are launched by pharmaceutical companies.

Keywords: Pulsatile Drug Delivery System, Circadian Rhythm, Lag Time and Technologies.

Research Articles

Nidhimalviya, Nagaraju Patro M, Kusumvalli Somisetty, Kusumdevi Vemula

Transmucosal patches of Lignocaine were developed and evaluated so as to achieve complete release and permeation of the drug within early minutes of application. Permeability of Lignocaine base (LB) and Lignocaine HCl salt (LH) were accessed through porcine buccal mucosa and dialysis membrane. Patches were prepared with mucoadhesive film forming polymers Sodium Carboxy Methyl Cellulose (SCMC), Hydroxy Propyl Cellulose (HPC, Grades JF, LF, LXF and MF), Hydroxy Propyl Methyl cellulose (HPMC) Labrafac PG (LPG) as permeation enhancer by solvent casting method over the dried ethyl cellulose (EC) backing. Permeation was further enhanced by addition of natural permeation enhancer clove oil and olive oil individually. Patches were evaluated for appearance, weight and thickness and content uniformity, surface pH, folding endurance, in vitro residence time, in vitro release, ex vivo permeation, mucoadhesive and tensile strength, FTIR, DSC, XRD, SEM. The release and permeation of LB from HPC-LF patch with clove oil was promising. Also the in vitro residence time, mucoadhesion and tensile strength was satisfactory. FTIR and DSC confirmed compatibility between the drug and the polymer.

Keywords: Lignocaine, Transmucosal Patch, Mucoadhesive Strength, In Vitro Release, Ex Vivo Permeation.

Kanika Bahuguna, Ganarajan, Preeti Kothiyal

Mucoadhesive buccal patch of rosuvastatin were prepared by solvent casting technique using 1% hydroxypropylmethylcellulose, and variable amount of polymer sodium carboxymethylcellulose, polyvinyl alcohol (PVA) and polyvinyl pyrrolidine using propylene glycol as plasticizer as well as penetration enhancer. Prepared patch were evaluated for weight uniformity, thickness, surface pH, swelling index, percent moisture absorption, percent moisture lose, folding endurance, in vitro release, and drug content uniformity. The mean thickness of buccal polymeric patches increased with an increase amount of polymer percent. Percent swelling index determined at 5, 10, 30 and 60 minutes increased with time and with increase in hydrophilic polymer. HPMC-SCMC buccal patches show better swelling index because of presence of more hydroxyl group. The increase in the amount of polymer retarded the release of rosuvastatin. F1 (HPMC –SCMC) showed the maximum and faster release. From the study it was concluded that the films exhibited satisfactory swelling, and promising drug release. The formulation was found to be suitable candidate for the development of buccal patches for therapeutic use.

Keywords: Mucoadhesive, Buccal Patch, Rosuvastatin, In Vitro Studies.

Shittu AO, Okoh M

A research was carried out to study the effect of increasing concentration of grewia gum in a binary-binder mixture on granules properties of a composite directly compressible excipient made with local primary materials and to formulate Ibuprofen (IBF) and metronidazole (MNZ) tablets with the best granules. This research was designed based on a fixed amount of Nigerian Tapioca Starch (NTS), while varying ratio of grewia gum (GG), and local acacia sieberiana gum (LASG) in the following percentage ratio: 80:0:20, 80:5:15, 80:10:10, 80:15:5, and 80:20:0 respectively. Slurry of physical mixture of GG and LASG was made using mixture of isopropranol and water (2:1) as granulation fluid. Slurry of NTS was also made and was triturated with the binder slurry. The resultant mixture was stirred vigorously until a semi solid mass was formed which was air dried for 72 h. The dried granules were size reduced by passing through 500 µm sieve size. The granules percent(%) cummulative distribution for various batches showed that the batch A with 20 % LASG showed weaker compact granules than every other batch containing binary binder mixture. The granule compactness increases from 20 % LASG and picked at 20 % GG. In between the batches, granules with 10 % GG and 10 % LASG possessed hybrid compactness which was consistent for particles retained on 180 µm, 250 µm and 355 µm. the average granule size was found to greater than 250 µm and less than 355 µm. It was observed that as the proportion of GG increases while LASG decreases, the granules became stronger, flow rate increases, compressibility decreases and viscosity increases. GrewStarag granules containing 80 % NTS, 10 % GG, and 10 % LASG with the following physicochemical properties was chosen: FR, 15.8 g/s; AR, 14.7°; CI, 8.0 %; HR, 1.08; viscosity, 115 mPa.S-1. This was employed for the formulation of IBF and MNZ tablets. The tablet target weight was 505 mg, compressed at 7.5 KN. Evaluation of IBF tablets shows acceptable dilution potential for tablets made with 200 mg of GrewStarag and 300 mg of IBF, having crushing strength (CR), disintegration time (DT), and friability (F) values: 58.2+2.4 N, 2 h 20 min., and 1.2 % respectively. Evaluation of MNZ tablets revealed acceptable compacts for dilution potential: 300 mg GrewStarag granules and 200 mg MNZ, having CS, 7.0 +1.0 N; DT, 2 h. 21 min., and 1.10 %. GrewStarag, a new filler-binder can be employed to extend or modified the release of moisture sensitive and poorly compressible active pharmaceutical ingredients for non- disintegrating colon targeted drugs.

Keywords: Directly Compressible Excipient, Coprocessed Filler-binder, Binary-based Filler-binder, Controlled Release Filler-binder, Ibuprofen Tablets, Metronidazole Tablets.

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