Determinants of Increasing Trend of Self-Medication in a Pakistani Community

Purpose: To determine the major reasons, sources, diseases and drugs responsible for increasing trend of self-medication.Method: A community-based cross-sectional survey was carried out in the district of Faisalabad in Pakistan. Respondents (1488) were classified on the basis of age, sex, education, lifestyle and their economical level. A questionnaire was distributed among the sample population to collect data.Results: Majority of respondents involved in self-medication were aged between 15 and 20 years. Family members (N = 717, 48 %) were considered the major source of information for self-medicated drugs. Lack of time (N = 504, 37 %) while economic issues (N = 485, 33 %) were the major reasons for self-medication. Medical stores were the source of drug purchase by 1087 (73 %) respondents. Headache (N = 772, 52 %) and fever (N = 600, 40 %) were the main indications for self-medication while 694 respondents reported that they engage in single-dose self-medication. Paracetamol (N = 689, 46 %), other analgesics (N = 488, 33 %),  non-steroidal anti-inflammatory (N = 680, 46 %) were reported to be used frequently for self-medication.Conclusion: Self-medication is prevalent in the Pakistani community due to easy access to over the counter (OTC) and prescription-only medicines  (POM). This may lead to untoward effects in consumers of the products. Special interventions by relevant regulatory agencies regarding the sale of the drugs are therefore required.Keywords: Self-medication, OTC drugs, Pharmacist

Development and in-vitro Evaluation of Once Daily Tablet Dosage Form of Loxoprofen Sodium

Purpose: To formulate and characterize once daily controlled release tablet of loxoprofen sodium.Methods: Eudragit RS-100, hydroxylpropyl methylcellulose (HPMC) and pectin were used as release retarding polymers. All the formulations were prepared by direct compression method. Various precompression studies were carried out to determine Hausner’s ratio, Carr’s index, angle of repose, bulk density and tapped density Differential scanning calorimetry (DSC) studies and also post-compression studies to evaluate hardness, friability, weight variation, drug content, in-vitro drug release were conducted on the tablets. The drug release data were subjected to kinetic models, including zero order, first order, Hixon Crowell, Higuchi and Korsmeyer-Peppas.Results: Compressibility index (7.6 ± 1.32 - 12.5 ± 1.43%), Hausner’s ratio (1.08 ± 0.04 - 1.14 ± 0.03), angle of repose (27.78 ± 0.47 - 30.49 ± 0.46°), hardness (6.25 ± 0.27 - 7.21±0.21 kg/cm2), friability (0.14 ± 0.06 - 0.28 ± 0.0 %), weight variation (249.5 ± 2.09 - 251.35 ± 2.41 mg) and drug content  (97.30 ± 0.28 - 103.70 ± 0.31 %) were within generally accepted limits for the pre-and post-compression formulations, respectively. The tablets having the maximum amount of among the three polymers tested as matrix materials, HPMC, represented by F3 tablets, exerted better sustained release properties after 12 h. Release pattern was more of Fickian diffusion followed by Higuchi mechanism.Conclusion: The release of the loxoprofen sodium was optimized up to 12 h.Keywords: Loxoprofen, Sustained release, hydroxypropyl methylcelluose, Pectin, Eudragit, Matrix tablet

Development of β-cyclodextrin-based hydrogel microparticles for solubility enhancement of rosuvastatin: an in vitro and in vivo evaluation

Rai Muhammad Sarfraz,1 Mahmood Ahmad,2 Asif Mahmood,3 Muhammad Rouf Akram,1 Asad Abrar2 1Faculty of Pharmacy, University of Sargodha, Sargodha, 2Faculty of Pharmacy and Alternative Medicines, The Islamia University of Bahawalpur, Bahawalpur, 3Institute of Pharmacy, Physiology and Pharmacology, University of Agriculture Faisalabad, Faisalabad, Pakistan Abstract: The aim of this study was to enhance the solubility of rosuvastatin (RST) calcium by developing β-cyclodextrin-g-poly(2-acrylamido-2-methylpropane sulfonic acid [AMPS]) hydrogel microparticles through aqueous free-radical polymerization technique. Prepared hydrogel microparticles were characterized for percent entrapment efficiency, solubility studies, Fourier transform infrared spectroscopy, differential scanning calorimetry, thermal gravimetric analysis, powder X-ray diffraction, scanning electron microscopy, zeta size and potential, swelling and release studies. Formulations (HS1–HS9) have shown entrapment efficiency between 83.50%±0.30% and 88.50%±0.25%, and optimum release was offered by formulation HS7 at both pH levels, ie, 1.2 (89%) and 7.4 (92%). The majority of microparticles had a particle size of less than 500 µm and zeta potential of –37 mV. Similarly, optimum solubility, ie, 10.66-fold, was determined at pH 6.8 as compared to pure RST calcium, ie, 7.30-fold. In vivo studies on fabricated hydrogel microparticulate system in comparison to pure drug were carried out, and better results regarding pharmacokinetic parameters were seen in the case of hydrogel microparticles. A potential approach for solubility enhancement of RST calcium and other hydrophobic moieties was successfully developed. Keywords: hydrogel microparticles, rosuvastatin calcium, polymerization, β-cyclodextrin solubilit

Formulation design and development of matrix diffusion controlled transdermal drug delivery of glimepiride

Muhammad Rouf Akram,1 Mahmood Ahmad,1 Asad Abrar,1 Rai Muhammad Sarfraz,2 Asif Mahmood3 1Faculty of Pharmacy & Alternative Medicine, The Islamia University of Bahawalpur, Bahawalpur, Pakistan; 2Faculty of Pharmacy, University of Sargodha, Sargodha, Pakistan; 3Faculty of Pharmacy, University of Lahore, Lahore, Pakistan Background: The present work was conducted to prepare and evaluate transdermal patches with optimization of suitable polymeric blend of poly(meth) acrylates (Eudragit®) (Ammonio Methacrylate Copolymer Ph Eur) for sustained transdermal delivery of glimepiride. Method: Polymeric matrix transdermal films were prepared by using Ammonio Methacrylate Copolymer Ph Eur RL 100 and Ammonio Methacrylate Copolymer Ph Eur RS 100 as the film former, and dibutyl phthalate (30% w/w) as the plasticizer. Patches were characterized by physical appearance, thickness, weight variation, folding endurance, percentage erosion, swelling index, moisture content, and moisture uptake capacity. Fourier transform infrared spectroscopic studies and differential scanning calorimetry analysis of physical mixtures of contents were performed to identify any chemical and physical interaction between drug and excipients. Five different enhancers (isopropyl myristate [IPM], Span® 80, Tween® 20, eucalyptus oil, and limonene) were employed at three different concentrations of polymer (2%, 5%, and 10% w/w) in order to enhance permeation through rabbit skin. In vitro drug release studies were performed at pH 7.4, and scanning electron microscopy was conducted to elucidate surface morphology before and after the drug release. In vitro permeation studies through rabbit skin were performed on Franz diffusion cells and permeation kinetics followed the Higuchi model. Results: Results of in vitro permeation studies revealed that these enhancers not only increased drug release but also augmented the skin permeation of glimepiride. Conclusion: IPM was the most effective enhancer with the highest permeation flux of 51.763 μg/cm2/hr, and the enhancement effect of different enhancers on glimepiride permeation through rabbit skin was in the rank order of IPM > eucalyptus oil > Span® 80 > Tween® 20> limonene. Keywords: transdermal patches, polymers, transdermal, permeation enhancers, glimepirid

Formulation and evaluation of mouth disintegrating tablets of atenolol and atorvastatin

In this study, mouth-disintegrating tablets of atenolol and atorvastatin combination were formulated using superdisintegrants to impart fast disintegration. Fifteen formulations were prepared based on different concentrations of two superdisintegrants, croscarmellose sodium and Kyron-T 134 . Three different techniques such as direct compression, effervescent and sublimation were used to study the effect of manufacturing processes, nature and concentration of superdisintegrants on various features of these tablets. Five formulations were made using each method. Precompression studies like bulk density, tapped density, angle of repose, Carr′s compressibility index, Hausner′s ratio and compatibility studies such as Fourier transform infrared spectroscopy and differential scanning calorimetry were performed. Various features such as hardness, thickness, diameter, weight variation, friability, disintegration time, dissolution studies, wetting time, wetting volume, water absorption ratio, modified disintegration, uniformity of contents and stability were evaluated. Finally results were statistically analyzed by the application of one way ANOVA test. Formulation F 13 containing Kyron-T 134 (6%) and croscarmellose sodium (2%) was found to be the best among all fifteen formulations prepared in all aspects evaluated. Sublimation method is found to be the best among three methods of preparation used