Development of an Oral Curcumin Nanocrystal Formulation

During the last ten years, the formulation of drugs as nanocrystals has rapidly evolved into a mature drug delivery strategy, with currently five products on the market. The major characteristic of these systems is the rapid dissolution velocity, enabling bioavailability enhancement after oral administration. This study describes the preparation of a solid dosage capsule form of spray-dried curcumin nanocrystal and compares its dissolution behavior with market capsule in different media. The aim was to obtain a stable nanocrystal loaded drug capsule with an increased drug saturation solubility and dissolution velocity. The solubility and dissolution experiments were performed to verify the obvious improvement of the dissolution behavior compared with commercial product. Improved dissolution behavior in drug nanocrystal-loaded solid dosage forms should lead to better bioavailability of poorly soluble drugs in the body.

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Enhancement of solubility of poorly soluble drugs by solid dispersion: An Overview

Indian Journal of Pharmaceutical and Biological Research ◽

10.30750/ijpbr.5.4.4 ◽

2017 ◽

Vol 5 (04) ◽

pp. 17-23

Author(s):

Katta Manogna ◽

P. Nagaveni ◽

K. Thyagaraju

Keyword(s):

Solid Dispersion ◽

Oral Absorption ◽

Water Soluble ◽

Poorly Soluble Drugs ◽

Drug Solubility ◽

Solid Dosage Forms ◽

Preparation Methods ◽

Solid Dosage ◽

Poorly Soluble ◽

Poorly Water Soluble

Most of the newly invented chemical drug moieties are poorly water soluble. According to BCS classification, class II and IV drugs are considered as poorly water soluble. So enhancement of oral absorption and bioavailability of solid dosage forms remains a challenge to formulation scientists due to their solubility criteria. Therefore many techniques are being explored to enhance the solubility of poor soluble drugs. Solid dispersion is one of the most important method for enhance the solubility (dissolution rate) and hence oral bioavailability of poorly soluble drugs. In solid dispersion the particle size of drug is reduced or a crystalline pure drug is converted into amorphous form and hence the solubility is increased. Polymer incorporating in solid dispersion technology is usually hydrophilic in nature and also showing compatibility with the drug to enhance the drug solubility. This review mainly discus about solid dispersion, preparation methods, and finally characterization.

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Dissolution Advantage of Nitazoxanide Cocrystals in the Presence of Cellulosic Polymers

Pharmaceutics ◽

10.3390/pharmaceutics12010023 ◽

2019 ◽

Vol 12 (1) ◽

pp. 23 ◽

Cited By ~ 7

Author(s):

Reynaldo Salas-Zúñiga ◽

Christian Rodríguez-Ruiz ◽

Herbert Höpfl ◽

Hugo Morales-Rojas ◽

Obdulia Sánchez-Guadarrama ◽

...

Keyword(s):

Hydroxypropyl Methylcellulose ◽

Dissolution Behavior ◽

Dissolution Profile ◽

Solid Dosage ◽

Dissolution Studies ◽

Key Factor ◽

Pharmaceutical Powder ◽

Poorly Soluble ◽

Fast Dissolution ◽

Cellulosic Polymer

The effect of hydroxypropyl methylcellulose (HPMC) and methylcellulose (Methocel® 60 HG) on the dissolution behavior of two cocrystals derived from nitazoxanide (NTZ), viz., nitazoxanide-glutaric acid (NTZ-GLU, 1:1) and nitazoxanide-succinic acid (NTZ-SUC, 2:1), was explored. Powder dissolution experiments under non-sink conditions showed similar dissolution profiles for the cocrystals and pure NTZ. However, pre-dissolved cellulosic polymer in the phosphate dissolution medium (pH 7.5) modified the dissolution profile of NTZ when starting from the cocrystals, achieving transient drug supersaturation. Subsequent dissolution studies under sink conditions of polymer-based pharmaceutical powder formulations with NTZ-SUC cocrystals gave a significant improvement of the apparent solubility of NTZ when compared with analogous formulations of pure NTZ and the physical mixture of NTZ and SUC. Scanning electron microscopy and powder X-ray diffraction analysis of samples recovered after the powder dissolution studies showed that the cocrystals undergo fast dissolution, drug supersaturation and precipitation both in the absence and presence of polymer, suggesting that the solubilization enhancement is due to polymer-induced delay of nucleation and crystal growth of the less soluble NTZ form. The study demonstrates that the incorporation of an appropriate excipient in adequate concentration can be a key factor for inducing and maintaining the solubilization of poorly soluble drugs starting from co-crystallized solid forms. In such a way, cocrystals can be suitable for the development of solid dosage forms with improved bioavailability and efficacy in the treatment of important parasitic and viral diseases, among others.

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Solubility Enhancement of Poorly soluble Drugs by using Novel Techniques : A Comprehensive Review

International Journal of PharmTech Research ◽

10.20902/ijptr.2019.130211 ◽

2020 ◽

Vol 13 (2) ◽

pp. 80-93 ◽

Cited By ~ 1

Author(s):

Abikesh P.K. Mahapatra ◽

Vinod Patil ◽

Ravindra Patil

Keyword(s):

Dissolution Rate ◽

Class Ii ◽

Systemic Circulation ◽

Poorly Soluble Drugs ◽

Formulation Development ◽

Solid Dosage ◽

Bcs Class Ii ◽

Pharmacological Response ◽

Poorly Soluble ◽

Low Solubility

The primary aim of this review was to improve the solubility and Bioavailability of BCS Class-II drugs because of their low solubility and dissolution rate. Solubility is one of the imp parameter to achieve desired concentration of drug in systemic circulation for pharmacological response to be shown. Hence the class- II drugs require enhancement in solubility and dissolution rate in there formulation development particularly in solid dosage form such as in tablet and capsule. So because of this there are several methods and newer emerging technologies have been developed for increasing the solubility as well as Bioavailability of class –II drugs. In this article review on literature on newer techniques or methods as well as recent research on formulation development of class- II drugs was done.

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A comparative in vitro dissolution study of generic moxifloxacin immediate-release film coated tablets and referent pharmaceutical product

Macedonian Pharmaceutical Bulletin ◽

10.33320/maced.pharm.bull.2018.64.02.003 ◽

2019 ◽

Vol 64 (02) ◽

pp. 27-34

Author(s):

Emilija Janeva ◽

Liljana Anastasova ◽

Irena Slaveska Spirevska ◽

Tatjana Rusevska ◽

Tanja Bakovska Stoimenova ◽

...

Keyword(s):

Immediate Release ◽

Dosage Forms ◽

Pharmaceutical Product ◽

Generic Product ◽

In Vitro Dissolution ◽

Dissolution Behavior ◽

Solid Dosage Forms ◽

Solid Dosage ◽

Similarity Factor

Dissolution testing of generic immediate release solid dosage forms represents a valuable tool to obtain dissolution profiles and to establish the similarity/dissimilarity between tested dosage forms. In this study, the in vitro dissolution profiles of generic immediate-release moxifloxacin (MOX) film coated tablets and a referent pharmaceutical product were compared and evaluated. The dissolution behavior of the generic product was investigated in three different dissolution media (pH=1.2, 4.5 and 6.8). The amount of dissolved MOX was determined using validated UV spectrophotometric method. For comparison of the dissolution behavior, the similarity factor, f2, was used. The dissolution profile of the generic product showed a release of >85 % MOX in the time frame of 30 min, in all the tested dissolution media. The similarity factor, f2, calculated from the comparison of the dissolution profiles of the generic and the referent pharmaceutical product in pH=1.2 dissolution medium was 50, 58, thus the products were established as similar. Based on the results of our study, the dissolution similarity between the generic MOX immediate-release film coated tablet and the referent product could be successfully used as a part of the approach to ensure their in vivo bioequivalence. Keywords: moxifloxacin, immediate-release solid dosage forms, dissolution, in vitro similarity

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LIQUISOLID TECHNIQUE FOR DISSOLUTION AND BIOAVAILABILITY ENHANCEMENT OF POORLY SOLUBLE DRUGS

Universal Journal of Pharmaceutical Research ◽

10.22270/ujpr.v2i5.rw3 ◽

2017 ◽

Vol 2 (5) ◽

pp. 46-53

Author(s):

Shrikant S. Magdum ◽

Keyword(s):

Poorly Soluble Drugs ◽

Bioavailability Enhancement ◽

Poorly Soluble

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Application of Drug Nanocrystal Technologies on Oral Drug Delivery of Poorly Soluble Drugs

Pharmaceutical Research ◽

10.1007/s11095-012-0889-z ◽

2012 ◽

Vol 30 (2) ◽

pp. 307-324 ◽

Cited By ~ 116

Author(s):

Lei Gao ◽

Guiyang Liu ◽

Jianli Ma ◽

Xiaoqing Wang ◽

Liang Zhou ◽

...

Keyword(s):

Drug Delivery ◽

Oral Drug Delivery ◽

Oral Drug ◽

Poorly Soluble Drugs ◽

Poorly Soluble ◽

Drug Nanocrystal

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Amorphous drug nanoparticle complex as bioavailability enhancement strategy of poorly soluble drugs

Proceedings of the 4th World Congress on Recent Advances in Nanotechnology ◽

10.11159/nddte19.3 ◽

2019 ◽

Author(s):

Kunn Hadinoto Ong

Keyword(s):

Poorly Soluble Drugs ◽

Bioavailability Enhancement ◽

Poorly Soluble ◽

Amorphous Drug ◽

Nanoparticle Complex

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Potent dried drug nanosuspensions for oral bioavailability enhancement of poorly soluble drugs with pH-dependent solubility

International Journal of Pharmaceutics ◽

10.1016/j.ijpharm.2011.04.034 ◽

2011 ◽

Vol 413 (1-2) ◽

pp. 237-244 ◽

Cited By ~ 86

Author(s):

Dongsheng Mou ◽

Huabing Chen ◽

Jiangling Wan ◽

Huibi Xu ◽

Xiangliang Yang

Keyword(s):

Oral Bioavailability ◽

Poorly Soluble Drugs ◽

Bioavailability Enhancement ◽

Poorly Soluble ◽

Ph Dependent

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Enhancement of Aqueous Solubility and Dissolution of Celecoxib through Phosphatidylcholine-Based Dispersion Systems Solidified with Adsorbent Carriers

Pharmaceutics ◽

10.3390/pharmaceutics11010001 ◽

2018 ◽

Vol 11 (1) ◽

pp. 1 ◽

Cited By ~ 11

Author(s):

Kanghee Jo ◽

Jae Min Cho ◽

Hyunjoo Lee ◽

Eun Kyung Kim ◽

Hong Chul Kim ◽

...

Keyword(s):

Aqueous Solubility ◽

Drug Dissolution ◽

Dissolution Behavior ◽

X Ray Diffraction ◽

Hydrophobic Property ◽

Scanning Calorimetry ◽

Solid Dosage ◽

Poorly Soluble ◽

Highly Hydrophobic ◽

Hydrophilic Materials

This study aimed to design phosphatidylcholine (PC)-based solid dispersion (SD) systems for enhancing the apparent aqueous solubility and dissolution of celecoxib (CLC), a selective cyclooxygenase-2 inhibitor with a highly hydrophobic property. Although PC-based dispersion formulations considerably increased solubilities of CLC, the lipidic texture of PC was not appropriate as a solid dosage form for oral administration of CLC. To mask the lipidic texture of PC-based matrices, Neusilin® US2, an adsorbent material with a porous structure and large surface area widely used in the pharmaceutical industry, was employed and thereby fully powderized PC-based dispersion formulations could be fabricated. However, PC matrices containing CLC strongly adsorbed to the pores of Neusilin® US2 was not able to be rapidly released. To address this problem, different hydrophilic materials were examined to promote the release of the CLC-dispersed PC matrices from Neusilin® US2. Among tested hydrophilic materials, croscarmellose sodium was the most suitable to facilitate fast drug dissolution from Neusilin® US2 particles, showing significantly enhanced apparent aqueous solubility and dissolution behavior of CLC. Through differential scanning calorimetry, X-ray diffraction, and Fourier transform infrared spectroscopy (FT-IR) analysis, a considerably reduced crystallinity of CLC dispersed in the PC-based dispersion formulations was demonstrated. The PC-based SD formulations developed in this study would be useful for improving the oral bioavailability of poorly soluble drugs such as CLC.

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