Volume 9

July-Septembet 2017

Review Articles

Vivek P Chavda, Sanjay Desai, Moinuddin Soniwala

Bioavailability (BA) has an important role in new drug discovery and product development in pharmaceutical field. The solubility and permeability are important parameters of biopharmaceutics and have central role in lead optimization by controlling the pharmacokinetic parameters to give better therapeutic activity. Biopharmaceutical classification system (BCS) is a drug development tool that is based on correlation of solubility and permeability with bioavailability of drug in human body. The principles of BCS are widely applicable in development of new drug and new drug product as the scientific approach for testing of waiver on clinical study and bioavailability of drug and in regulatory approvals of drug. This review article gives an overview of BCS with special emphasis on concept, classification, class boundaries determination, extension and BDDCS with brief idea on applications. Finally, future prospect and limitations are pointed out.

Keywords: Biopharmaceutical Classification System, Solubility, Bioavailability, Intestinal Permeability, Bioequivalence, Product Development, BDDCS.

Prasad M Potekar, Jameel Ahmed S Mulla, Rajendra C Doijad

Orally administered drugs having poor Absorption window in the proximal gut can limit the bioavailability. Gastro-retention is one of the approaches to retain drug in GI tract for several hours gives prolong residence time and drug release. GRDDS is helps to improve bioavailability and polymer concentration gives sustained drug delivery. Gastro-retentive dosage forms (GRDF) has received significant interest in the past few decades as they can improve the limitation of most conventional and oral controlled release drug delivery system related to fast gastric-emptying time. Recently oral controlled release drug delivery has been of great interest in pharmaceutical field to achieve improved therapeutic advantages. In recent years, gastro-retentive drug delivery has gained abundant importance for medicine acting regionally within the proximal a part of digestive tract. Various approaches such as floating and non-floating system. GRDDS which are further classified are cited in this review. This article gives an overview on advantages & disadvantages of gastro-retentive drug delivery systems.

Keywords: Gastro-retentive, GRDDS, Floating, Bioadhesion, Hydrodynamically balanced system, Effervescence.

Research Articles

Nnamani P O, Kenechukwu F C, Okoye Onyeka, Akpa P A

Sustained-release microcapsules of mebendazole were prepared using Prosopis africana peel powder (PAPP), a novel biopolymer, in the ratios of 1:1, 1:2 and 1:3 by the emulsification method. The microcapsules were evaluated for particle size, morphology, encapsulation efficiency, thermal property, in vitro drug release and larvicidal activity on 20 active mosquito larvae. The results show that particle size and encapsulation efficiency (EE%) of the mostly irregularly shaped microcapsules were independent of polymer concentrations, yet the 1:3 (inner coat) and 1:2 (outer coat) microcapsules gave the highest EE% of 72 and 81 % respectively. Thermograms of the microcapsules generally revealed lower melting temperatures suggesting total disappearance of mebendazole peak, indicating that mebendazole was molecularly dispersed in the polymeric microcapsules. The in vitro release study indicates that drug release in simulated intestinal fluid (SIF, pH 7.2) followed a pattern: 1:1>1:2>1:3 (for the inner coat microcapsule) and 1:1>1:3>1:2 (for the outer coat) better than in simulated gastric fluid (SGF, pH 1.2). Microcapsules (1:3 outer coat) recorded 65% death of mosquito larvae in 24 h while mebendazole recorded 100 % death in 24 h; microcapsules made with the inner coat recorded death of 50 % of the mosquito larva in 24 h. The larvicidal activity of mebendazole was sustained for up to 3 days in all the formulations unlike the reference standard. This study suggests that PAPP could be employed in sustained delivery of mebendazole for improved patient compliance thus reducing the frequency of drug administration with associated side effects of mebendazole.

Keywords: Mebendazole, Microcapsule, Prosopis africana Peel Powder (PAPP), Sustained Drug Release, Larvicidal Activity.

Vishal V Pande, Surekha Jamdhade, Gayatri V Dusane, Priyanka P Salunke, Nikita A Borawake, Prakash N Kendre

The aim of present study was to increase the solubility and dissolution of poorly water soluble Febuxostat by mechanochemical approach. Initially the drug was milled in planetary ball mill and then particle size of milled Febuxostat was measured by Malvern zetasizer, hence the particle size of milled Febuxostat was reduced 4.4% as compare to plain unmilled drug 2%. The solid dispersions of poorly water soluble Febuxostat was prepared with water soluble carrier such as gelucire 44/14 and aeroperl 300 was added as adsorbent to improve its solubility and dissolution properties. The solid dispersions of different ratios i.e., 1:1, 1:2, 1:3 and 1:4 of milled and unmilled Febuxostat were prepared by particle size reduction by planetary ball mill and melt method. Characterization of solid dispersions of milled and unmilled was performed using FTIR, DSC, PXRD, SEM, solubility and dissolution study.

Keywords: Febuxostat, Mechanochemical Approach, Solid Dispersions.

Radhika B, Vilasini S

Tabernaemontana divaricata is traditionally used for various ailments. The young stems are used as dental caries, latex of leaves used as anti-inflammatory and infusion of roots are used as antipyretic. In the present study leaves were collected from Husnabad village of Karimnagar district which were dried and made into the fine powder then subjected to maceration and soxhlation by chloroform and methanol as solvents. The preliminary phytochemical screening was performed for those extracts and results showed the presence of carbohydrates, alkaloids, glycosides, terpenoids, phenols, tannins, flavonoids, steroids, proteins and amino acids. These extracts were screened for their antibacterial activity against 4 pathogens bacteria by well diffusion method. The pattern of inhibition varied with the solvent used for extraction and microorganism tested. A comparative study had been done between the maceration and soxhlation extracts of leaves by using chloroform and methanol as solvents. Among these extracts, methanol soxhlation extract showed significant antibacterial activity against most tested bacteria. The most susceptible microorganism was Proteus vulgaris (ZOI-22mm) followed by Staphylococcus aureus (ZOI-17).

Keywords: Tabernaemontana divaricata, Antibacterial, Maceration, Soxhlation, Staphylococcus aureus, Lacto bacillus, Proteus vulgaris, Enterobacter aerogenes, ZOI.

Ofokansi K C, Kenechukwu F C, Ezugwuro, Reginald-Opara J, Agbo C P, Attama A A

The purpose of this study was to improve the dissolution and absorption rate of ibuprofen, a hydrophobic non-steroidal anti-inflammatory drug (NSAID), via polyethylene glycol 8000 (PEG 8000) solid dispersions. Ibuprofen-PEG 8000 solid dispersions (SDs) were prepared by fusion method using varying combination ratios of ibuprofen and polyethylene glycol (PEG) 8000 i.e. 1:1, 1:2, 1:3, and 1:4 (1 g :1 g, 1 g : 2 g, 1 g : 3 g, and 1 g : 4 g). Characterization based on surface morphology, particle size, absolute drug content, Fourier transform infrared (FT-IR) spectroscopy and micromeritic properties were carried out on the SDs. The in vivo release of ibuprofen from the SDs was performed using rats. Greenish brown, discrete, flowable and irregularly shaped SDs of mean particle size range 113.5 ± 2.5 to 252.5 ± 1.9 µm, which were stable over 3 months, were obtained. The higher the polymer (PEG 8000), the smaller the particle sizes of the SDs, which were less than the mean particle size of the physical mixture. The encapsulation efficiency (EE %) of the SDs ranged from 73.4 ± 2.9 % to 83.5 ± 2.7%. The encapsulation efficiency of the physical mixture (67.0 ± 1.8) was lower than those of the SDs. While the EE % increased with increased concentration of PEG 8000 in the SDs the mean particle size decreased with increased concentration. The FT-IR results indicate no strong chemical interaction of ibuprofen and PEG 8000 in the SDs. Administration of the SDs to rats resulted in much higher plasma concentration compared to the pure ibuprofen and the physical mixture (p<0.05), an indication of enhanced absorption rate of ibuprofen in the SDs systems. This study has shown that ibuprofen-PEG 8000 SDs could offer a better and more effective approach of increasing the dissolution and absorption rate of the drug.

Keywords: Ibuprofen, Solid Dispersion, PEG 8000, Plasma Concentration, Non-Steroidal Anti-inflammatory Drug (NSAID).

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