Polyphenols constitute a family of natural substances distributed widely in plant kingdom. These are produced as secondary metabolites by plants and so far 8000 representatives of this family have been identified. Recently, there is an increased interest in the polyphenols because of the evidence of their role in prevention of degenerative diseases such as neurodegenerative diseases, cancer, and cardiovascular diseases. Although a large number of drugs are available in the market for treatment of these diseases, however, the emphasis these days is on the exploitation of natural principles derived from plants. Most polyphenols show low <i>in vivo</i> bioavailability thus limiting their application for oral drug delivery. This low bioavailability could be associated with low aqueous solubility, first pass effect, metabolism in GIT, or irreversible binding to cellular DNA and proteins. Therefore, there is a need to devise strategies to improve oral bioavailability of polyphenols. Various approaches like nanosizing, self-microemulsifying drug delivery systems (SMEDDS), microencapsulation, complexation, and solid dispersion can be used to increase the bioavailability. This paper will highlight the various methods that have been employed till date for the solubility enhancement of various polyphenols so that a suitable drug delivery system can be formulated.

Harkiran Kaur

Gurpreet Kaur

A Critical Appraisal of Solubility Enhancement Techniques of Polyphenols

Recent developments in fast disintegrating tablets have brought convenience in dosing to pediatric and elderly patients who have trouble in swallowing tablets. The objective of the present study was to prepare the fast disintegrating tablet of Cetirizine Hydrochloride for allergic and respiratory disorders. As precision of dosing and patient&#x27;s compliance become important prerequisite for a long-term treatment, there is a need to develop a formulation for this drug which overcomes problems such as difficulty in swallowing, inconvenience in administration while travelling, and patient&#x2019;s acceptability. Hence, the present investigation was undertaken with a view to develop a fast disintegrating tablet of Cetirizine Hydrochloride which offers a new range of products having desired characteristics and intended benefits. Superdisintegrants such as Sodium Starch Glycolate were optimized. Different binders were optimized along with optimized superdisintegrant concentration. The tablets were prepared by direct compression technique. The tablets were evaluated for hardness, friability, weight variation, wetting time, disintegration time and uniformity of content. Optimized formulation was evaluated by in vitro dissolution test, drug excipient compatibility and accelerated stability study. It was concluded that fast disintegrating tablets of Cetirizine Hydrochloride were formulated successfully with desired characteristics which disintegrated rapidly, provide rapid onset of action, and enhance the patient convenience and compliance.

Deepak Sharma

Mankaran Singh

Dinesh Kumar

Gurmeet Singh

Formulation Development and Evaluation of Fast Disintegrating Tablet of Cetirizine Hydrochloride: A Novel Drug Delivery for Pediatrics and Geriatrics

<i  >Aim</i>. The aim of this study was to establish population pharmacokinetic models of tacrolimus in Chinese adult liver transplantation patients. <i  >Methods</i>. Tacrolimus dose and concentration data <svg     style="vertical-align:-2.3205pt;width:64.324997px;" id="M1" height="15.0875" version="1.1" viewBox="0 0 64.324997 15.0875" width="64.324997"  xmlns:xlink="http://www.w3.org/1999/xlink" xmlns="http://www.w3.org/2000/svg">
	
		
			<g transform="matrix(.017,-0,0,-.017,.062,12.138)"><path id="x28" d="M300 -147l-18 -23q-106 71 -159 185.5t-53 254.5v1q0 139 53 252.5t159 186.5l18 -24q-74 -62 -115.5 -173.5t-41.5 -242.5q0 -130 41.5 -242.5t115.5 -174.5z" /></g><g transform="matrix(.017,-0,0,-.017,5.944,12.138)"><path id="x1D45B" d="M495 86q-46 -47 -87 -72.5t-63 -25.5q-43 0 -16 107l49 210q7 34 8 50.5t-3 21t-13 4.5q-35 0 -109.5 -72.5t-115.5 -140.5q-21 -75 -38 -159q-50 -10 -76 -21l-6 8l84 340q8 35 -4 35q-17 0 -67 -46l-15 26q44 44 85.5 70.5t64.5 26.5q35 0 10 -103l-24 -98h2&#xA;q42 56 97 103.5t96 71.5q46 26 74 26q9 0 16 -2.5t14 -11.5t9.5 -24.5t-1 -44t-13.5 -68.5q-30 -117 -47 -200q-4 -19 -3.5 -25t6.5 -6q21 0 70 48z" /></g><g transform="matrix(.017,-0,0,-.017,19.186,12.138)"><path id="x3D" d="M535 323h-483v50h483v-50zM535 138h-483v50h483v-50z" /></g><g transform="matrix(.017,-0,0,-.017,33.89,12.138)"><path id="x34" d="M456 178h-96v-72q0 -51 12.5 -62.5t72.5 -16.5v-27h-256v27q65 5 78 17t13 62v72h-260v28q182 271 300 426h40v-407h96v-47zM280 225v295h-2q-107 -148 -196 -295h198z" /></g><g transform="matrix(.017,-0,0,-.017,42.049,12.138)"><path id="x33" d="M285 378v-2q65 -13 102 -54.5t37 -97.5q0 -57 -30.5 -104.5t-74 -75t-85.5 -42t-72 -14.5q-31 0 -59.5 11t-40.5 23q-19 18 -16 36q1 16 23 33q13 10 24 0q58 -51 124 -51q55 0 88 40t33 112q0 64 -39 96.5t-88 32.5q-29 0 -64 -11l-6 29q77 25 118 57.5t41 84.5&#xA;q0 45 -26.5 69.5t-68.5 24.5q-67 0 -120 -79l-20 20l43 63q51 56 127 56h1q66 0 107 -37t41 -95q0 -42 -31 -71q-22 -23 -68 -54z" /></g><g transform="matrix(.017,-0,0,-.017,50.209,12.138)"><path id="x35" d="M153 550l-26 -186q79 31 111 31q90 0 141.5 -51t51.5 -119q0 -93 -89 -166q-85 -69 -173 -71q-32 0 -61.5 11.5t-41.5 23.5q-18 17 -17 34q2 16 22 33q14 9 26 -1q61 -50 124 -50q60 0 93 43.5t33 104.5q0 69 -41.5 110t-121.5 41q-53 0 -102 -20l38 305h286l6 -8&#xA;l-26 -65h-233z" /></g><g transform="matrix(.017,-0,0,-.017,58.368,12.138)"><path id="x29" d="M275 270q0 -296 -211 -440l-19 23q75 62 116.5 174t41.5 243t-42 243t-116 173l19 24q211 -144 211 -440z" /></g>

		
	
</svg> were obtained from 47 Chinese adult liver transplant recipients, and the data were analyzed using a nonlinear mixed-effect modeling (NONMEM) method. <i  >Results</i>. The structural model was a two-compartment model with first-order absorption. The typical population values of tacrolimus for the pharmacokinetic parameters of apparent clearance (<svg     style="vertical-align:-2.22495pt;width:38.150002px;" id="M2" height="14.85" version="1.1" viewBox="0 0 38.150002 14.85" width="38.150002"  xmlns:xlink="http://www.w3.org/1999/xlink" xmlns="http://www.w3.org/2000/svg">
	
		
			<g transform="matrix(.017,-0,0,-.017,.062,12.012)"><path id="x43" d="M614 175l29 -10q-33 -109 -57 -154q-121 -26 -184 -26q-90 0 -160.5 29t-112.5 77t-63.5 105.5t-21.5 119.5q0 157 108 253t277 96q36 0 71.5 -5t69 -13.5t36.5 -8.5q15 -102 20 -150l-29 -8q-20 79 -66.5 114t-128.5 35q-119 0 -187.5 -86t-68.5 -207&#xA;q0 -140 73.5 -227.5t188.5 -87.5q73 0 119.5 37.5t86.5 116.5z" /></g><g transform="matrix(.017,-0,0,-.017,11.367,12.012)"><path id="x4C" d="M495 163l30 -6q-19 -99 -36 -157h-453v28q63 5 77.5 20t14.5 78v400q0 63 -13 77t-75 19v28h261v-28q-61 -5 -74.5 -19t-13.5 -77v-395q0 -41 5 -59t18 -25q24 -13 96 -13q85 0 112 31q30 33 51 98z" /></g><g transform="matrix(.017,-0,0,-.017,20.512,12.012)"><path id="x2F" d="M368 703l-264 -866h-60l265 866h59z" /></g><g transform="matrix(.017,-0,0,-.017,27.515,12.012)"><path id="x1D439" d="M599 650l-18 -160l-30 -2q-2 70 -11 94q-5 16 -26 24t-75 8h-94q-27 0 -33.5 -6.5t-12.5 -32.5l-43 -226h108q52 0 72.5 5t31 18t28.5 52h28l-40 -200h-28q-1 42 -6 56.5t-24.5 21t-70.5 6.5h-108l-32 -177q-13 -65 1 -80.5t88 -22.5l-8 -28h-279l6 28q61 5 77.5 20.5&#xA;t29.5 81.5l72 387l7.5 40.5t1 26.5t-4 18t-15.5 10t-24 6t-37 4l8 28h461z" /></g>

		
	
</svg>), apparent distribution volume of the central compartment (<svg     style="vertical-align:-3.27605pt;width:36.650002px;" id="M3" height="16.15" version="1.1" viewBox="0 0 36.650002 16.15" width="36.650002"  xmlns:xlink="http://www.w3.org/1999/xlink" xmlns="http://www.w3.org/2000/svg">
	
		
			<g transform="matrix(.017,-0,0,-.017,.062,12.012)"><path id="x1D449" d="M730 650l-8 -28q-52 -4 -72 -18t-64 -77q-79 -113 -321 -539h-33l-119 541q-13 59 -29.5 73t-66.5 20l7 28h245l-8 -28l-28 -5q-33 -6 -40.5 -15.5t-0.5 -38.5l102 -450h2q191 320 246 430q21 42 15.5 56t-43.5 19l-31 4l7 28h240z" /></g>

			<g transform="matrix(.012,-0,0,-.012,12.675,16.087)"><path id="x32" d="M412 140l28 -9q0 -2 -35 -131h-373v23q112 112 161 170q59 70 92 127t33 115q0 63 -31 98t-86 35q-75 0 -137 -93l-22 20l57 81q55 59 135 59q69 0 118.5 -46.5t49.5 -122.5q0 -62 -29.5 -114t-102.5 -130l-141 -149h186q42 0 58.5 10.5t38.5 56.5z" /></g>

			<g transform="matrix(.017,-0,0,-.017,19.013,12.012)"><use xlink:href="#x2F"/></g><g transform="matrix(.017,-0,0,-.017,26.016,12.012)"><use xlink:href="#x1D439"/></g>

		
	
</svg>), intercompartmental clearance (<svg     style="vertical-align:-2.2932pt;width:30.762501px;" id="M4" height="14.925" version="1.1" viewBox="0 0 30.762501 14.925" width="30.762501"  xmlns:xlink="http://www.w3.org/1999/xlink" xmlns="http://www.w3.org/2000/svg">
	
		
			<g transform="matrix(.017,-0,0,-.017,.062,12.013)"><path id="x1D444" d="M745 361q0 -134 -83.5 -233t-214.5 -130l16 -11q97 -67 250 -132l-8 -23q-76 3 -131 16q-81 19 -242 125l-20 13q-129 8 -209 91t-80 208q0 160 116 271t289 111q136 0 226.5 -83t90.5 -223zM645 356q0 127 -57.5 201.5t-169.5 74.5q-126 0 -210.5 -104.5t-84.5 -248.5&#xA;q0 -97 46 -166.5t129 -87.5l84 15l29 -19q104 21 169 121.5t65 213.5z" /></g><g transform="matrix(.017,-0,0,-.017,13.118,12.013)"><use xlink:href="#x2F"/></g><g transform="matrix(.017,-0,0,-.017,20.121,12.013)"><use xlink:href="#x1D439"/></g>

		
	
</svg>), apparent distribution volume of the peripheral compartment (<svg     style="vertical-align:-3.3907pt;width:36.650002px;" id="M5" height="16.299999" version="1.1" viewBox="0 0 36.650002 16.299999" width="36.650002"  xmlns:xlink="http://www.w3.org/1999/xlink" xmlns="http://www.w3.org/2000/svg">
	
		
			<g transform="matrix(.017,-0,0,-.017,.062,12.013)"><use xlink:href="#x1D449"/></g>

			<g transform="matrix(.012,-0,0,-.012,12.675,16.088)"><use xlink:href="#x33"/></g>

			<g transform="matrix(.017,-0,0,-.017,19.013,12.013)"><use xlink:href="#x2F"/></g><g transform="matrix(.017,-0,0,-.017,26.016,12.013)"><use xlink:href="#x1D439"/></g>

		
	
</svg>), and absorption rate (<svg     style="vertical-align:-3.3907pt;width:15.3125px;" id="M6" height="16.450001" version="1.1" viewBox="0 0 15.3125 16.450001" width="15.3125"  xmlns:xlink="http://www.w3.org/1999/xlink" xmlns="http://www.w3.org/2000/svg">
	
		
			<g transform="matrix(.017,-0,0,-.017,.062,12.162)"><path id="x1D458" d="M480 416q0 -21 -18 -41q-9 -11 -17 -7q-20 9 -42 9q-62 0 -140 -78q23 -69 88 -192q17 -31 27 -42t20 -11q16 0 62 46l17 -20q-64 -92 -119 -92q-35 0 -70 66q-41 73 -84 187q-36 -30 -62 -61q-27 -115 -35 -172q-41 -8 -78 -20l-6 6l140 612q7 28 0.5 34t-37.5 7l-34 1&#xA;l5 26q38 4 74 13.5t57 17t25 7.5q12 0 4 -32l-104 -443h2q35 38 97 93q39 35 65.5 56t62 41.5t58.5 20.5q19 0 30.5 -10t11.5 -22z" /></g>

			<g transform="matrix(.012,-0,0,-.012,8.612,16.25)"><path id="x1D44E" d="M483 97q-42 -50 -88.5 -79.5t-68.5 -29.5q-37 0 -17 93l22 102h-2q-54 -79 -144 -149q-59 -46 -100 -46q-24 0 -43 29t-19 86q0 78 34.5 153t94.5 120q41 31 94 51.5t98 20.5q29 0 72 -9q26 -6 39 -6l2 -4q-30 -117 -67 -323q-8 -41 2 -41q16 0 79 58zM374 387&#xA;q-32 15 -73 15q-52 0 -83 -23q-48 -36 -78 -108.5t-30 -152.5q0 -33 8.5 -50.5t20.5 -17.5q31 0 107 79t99 132q15 40 29 126z" /></g>

		
	
</svg>) were 11.2&#x2009;L/h, 406&#x2009;L, 57.3&#x2009;L/h, 503&#x2009;L, and 0.723&#x2009;h<sup  >&#x2212;1</sup>, respectively. The interindividual variabilities of these parameters were 16.2&#x25;, 163&#x25;, 19.7&#x25;, 199&#x25;, and 74.3&#x25;, respectively, and the intraindividual variability of observed concentration was 26.54&#x25;. The covariates retained in the final models were postoperative days (POD) and dosage per day (DOSE) on <svg     style="vertical-align:-2.22495pt;width:38.150002px;" id="M7" height="14.85" version="1.1" viewBox="0 0 38.150002 14.85" width="38.150002"  xmlns:xlink="http://www.w3.org/1999/xlink" xmlns="http://www.w3.org/2000/svg">
	
		
			<g transform="matrix(.017,-0,0,-.017,.062,12.012)"><use xlink:href="#x43"/></g><g transform="matrix(.017,-0,0,-.017,11.367,12.012)"><use xlink:href="#x4C"/></g><g transform="matrix(.017,-0,0,-.017,20.512,12.012)"><use xlink:href="#x2F"/></g><g transform="matrix(.017,-0,0,-.017,27.515,12.012)"><use xlink:href="#x1D439"/></g>

		
	
</svg>. <i  >Conclusion</i>. Population pharmacokinetic models of tacrolimus were developed in Chinese adult liver transplant patients. These results could provide the interpretation of the outcome of pharmacokinetics modeling and the impact of covariate tested on individualized tacrolimus therapy.

Liqin Zhu

Hao Wang

Xiaoye Sun

Wei Rao

Wei Qu

Yuan Zhang

Liying Sun

The Population Pharmacokinetic Models of Tacrolimus in Chinese Adult Liver Transplantation Patients

Approximately 34 million people were living with human immunodeficiency virus (HIV-1) at the end of 2011. From the last two decades, researchers are actively involved in the development of an effective HIV-1 treatment, but the results intended are still doubtful about the eradication of HIV. The HIV-1 virus has gone from being an &#x201c;inherently untreatable&#x201d; infectious agent to the one liable to be affected by a range of approved therapies. Candidate microbicides have been developed to target specific steps in the process of viral transmission. Microbicides are self-administered agents that can be applied to vaginal or rectal mucosal surfaces with the aim of preventing, or reducing, the transmission of sexually transmitted infections (STIs) including HIV-1. The development of efficient, widely available, and low-cost microbicides to prevent sexually transmitted HIV infections should be given high priority. In this review, we studied the various forms of microbicides, their mechanism of action, and their abundant approaches to control the transmission of sexually transmitted infections (STIs).

Onkar Singh

Tarun Garg

Goutam Rath

Amit K. Goyal

Microbicides for the Treatment of Sexually Transmitted HIV Infections

Drugs from nitroimidazole category are generally bitter in taste. Oral formulation with bitter taste is not palatable. Geriatrics and pediatrics patients usually suffer from swallowing difficulties. Many other patients in some disease conditions avoid swallowing tablets. Satranidazole is a new nitro-imidazole derivative with bitter taste and is available in market as film coated tablet. The purpose of this research was to mask the bitter taste of Satranidazole by coating complexation with low melting point wax and Eudragit EPO. Different types of wax (glyceryl monostearate, stearic acid and cetyl alcohol) were tried for taste masking. The drug to stearic acid ratio 1&#x2009;:&#x2009;2 was found to be optimum on the basis of taste evaluation and <i>in vitro</i> release. The formulated granules were found to possess good flow property. FTIR studies confirmed that there was no interaction between drug and excipients. Scanning Electron Microscopy of drug and the optimized batch of granules was performed. The <i>in vitro</i> release of drug from granules was compared with marketed tablet formulation. The taste masked granules of optimized batch showed 87.65&#x25; release of drug in 1&#x2009;hr which is comparable to that of marketed tablet formulation.

Harshal Ashok Pawar

Pooja Rasiklal Joshi

Development and Evaluation of Taste Masked Granular Formulation of Satranidazole by Melt Granulation Technique

Nanosizing is a suitable method to enhance the dissolution rate and therefore the bioavailability of poorly soluble drugs. The success of the particle size reduction processes depends on critical factors such as the employed technology, equipment, and drug physicochemical properties. High pressure homogenization and wet bead milling are standard comminution techniques that have been already employed to successfully formulate poorly soluble drugs and bring them to market. However, these techniques have limitations in their particle size reduction performance, such as long production times and the necessity of employing a micronized drug as the starting material. This review article discusses the development of combinative methods, such as the NANOEDGE, H 96, H 69, H 42, and CT technologies. These processes were developed to improve the particle size reduction effectiveness of the standard techniques. These novel technologies can combine bottom-up and/or top-down techniques in a two-step process. The combinative processes lead in general to improved particle size reduction effectiveness. Faster production of drug nanocrystals and smaller final mean particle sizes are among the main advantages. The combinative particle size reduction technologies are very useful formulation tools, and they will continue acquiring importance for the production of drug nanocrystals.

Jaime Salazar

Rainer H. M&#xfc;ller

Jan P. M&#xf6;schwitzer

Combinative Particle Size Reduction Technologies for the Production of Drug Nanocrystals

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<p><em>Journal of Pharmaceutics</em> publishes original research articles, review articles, and clinical studies on the design and preparation of new drugs, with a focus on drug dosage forms and safety and efficacy in humans.</p>


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Journal of Pharmaceutics ceased publication in 2020 and is no longer accepting submissions.

description

Journal of Pharmaceutics publishes original research articles, review articles, and clinical studies on the design and preparation of new drugs, with a focus on drug dosage forms and safety and efficacy in humans.

Journal of Pharmaceutics