Evaluation of Weight Variation in Mini-Tablets Manufactured by a Multiple-Tip Tool.

Abstract:

:Recently, owing to their pharmaceutical and clinical utility, mini-tablets have been well studied by researchers. Mini-tablets are usually manufactured by compression molding using a multiple-tip tool in a rotary tableting machine. Owing to their special structure, ensuring uniformity is a very important challenge in the manufacturability of mini-tablets using the multiple-tip tool. In this study, we aimed to evaluate the weight variation in mini-tablets produced by a multiple-tip tool, which is considered to be the root cause affecting the uniformity, and to investigate the physical properties of drug granules and tableting conditions in a rotary tableting machine that could reduce this weight variation. In addition, the relationship between these factors and response was visualized using response surface analysis. It was shown that the weight variation in mini-tablets produced by a multiple-tip tool was reduced when using a forced feeder compared with an open feeder. Furthermore, in the case of an open feeder, the optimal range of the average particle size diameter of drug granules and the rotational speed of the rotating disc in the rotary tableting machine were determined from response surface analysis. It was suggested that it is possible to reduce the weight variation in the mini-tablets by selecting drug granules with an average particle size diameter of 100-150 µm and using tableting conditions with a rotational speed of 40-60 rpm. This study elucidated the factors that affect uniformity and determined their optimal range for the manufacture of mini-tablets.

authors

Kurashima H,Uchida S,Kashiwagura Y,Tanaka S,Namiki N

doi

10.1248/cpb.c20-00460

subject

Has Abstract

pub_date

2020-01-01 00:00:00

pages

981-988

issue

10

eissn

0009-2363

issn

1347-5223

journal_volume

68

pub_type

杂志文章
  • Spectroscopic analysis of charge transfer complex formation between neuroleptics and iodine.

    abstract::Molecular interactions between iodine and various neuroleptics were investigated by UV/Vis spectroscopy. Iodine was found to form charge transfer complexes in a 1:1 stoichiometry and of n-sigma type with these molecules. The values of the formation constants Kc of these iodinated complexes indicate a strong donor-acce...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.37.151

    authors: Comby F,Jambut-Absil AC,Buxeraud J,Raby C

    更新日期:1989-01-01 00:00:00

  • Transport to intestinal lumen and peritoneal cavity of intravenously administered aprinidine in rats.

    abstract::Transfer of aprindine from the blood into the intestinal lumen or into the peritoneal cavity was examined after intravenous administration of the drug at a dose of 5 mg/kg in rats. The amount of the drug transferred from the blood into the intestinal lumen was much greater than into the peritoneal cavity. The average ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.39.3359

    authors: Arimori K,Hashimoto Y,Nakano M

    更新日期:1991-12-01 00:00:00

  • Hyosgerin, a new optically active coumarinolignan, from the seeds of Hyoscyamus niger.

    abstract::Hyosgerin, a new optically active coumarinolignan, has been isolated and characterized along with three other coumarinolignans, venkatasin, cleomiscosin A and cleomiscosin B, from the seeds of Hyoscyamus niger L. The structure was determined on the basis of spectroscopic analysis and chemical conversion. The optical p...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.54.538

    authors: Sajeli B,Sahai M,Suessmuth R,Asai T,Hara N,Fujimoto Y

    更新日期:2006-04-01 00:00:00

  • Synthesis of biologically active acycloAZT derivatives and related compounds.

    abstract::The synthesis of optically active acyclic analogues of 3'-azido-3'-deoxythymidine, which lack only the 2'-CH2 of the sugar, is described. The synthesis of some nucleoside analogues that contain the N-acetyl-D-neuraminic acid moiety is also described. ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.38.836

    authors: Murata M,Achiwa K

    更新日期:1990-03-01 00:00:00

  • Evaluation of new pasty-type implantable devices consisting of poly(epsilon-caprolactone/delta-valerolactone) and Estracyt or estramustine.

    abstract::Biodegradable pasty-type copolyesters with a relatively low molecular weight of 4500 were synthesized by direct copolycondensation of epsilon-caprolactone (CL) and delta-valerolactone (VL) in the absence of catalysts to evaluate in vivo capabilities of the polymer for implantable controlled release devices in drug del...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.39.2096

    authors: Imasaka K,Yoshida M,Fukuzaki H,Asano M,Kumakura M,Mashimo T,Yamanaka H,Nagai T

    更新日期:1991-08-01 00:00:00

  • Synthetic studies on (+)-biotin, part 15: A chiral squaramide-mediated enantioselective alcoholysis approach toward the total synthesis of (+)-biotin.

    abstract::An efficient stereocontrolled total synthesis of (+)-biotin (1) has been achieved via the intermediacy of Roche's lactone 5 starting from cis-1,3-dibenzyl-2-imidazole-4,5-dicarboxylic acid (2). The bifunctional cinchona alkaloid-derived squaramide-promoted enantioselective alcoholysis was utilizing as a tool for the c...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.59.488

    authors: Chen XX,Xiong F,Fu H,Liu ZQ,Chen FE

    更新日期:2011-01-01 00:00:00

  • Fasciculic acids A, B and C as calmodulin antagonists from the mushroom Naematoloma fasciculare.

    abstract::Three new fasciculol esters, fasciculic acids A (1), B (2) and C (3), having potent calmodulin antagonistic activity were isolated from the toxic mushroom Naematoloma fasciculare (Fr.) Karst. Their structures were elucidated on the basis of spectral and chemical evidence. ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.37.3247

    authors: Takahashi A,Kusano G,Ohta T,Ohizumi Y,Nozoe S

    更新日期:1989-12-01 00:00:00

  • Modeling the entrainer effects on solubility of solutes in supercritical carbon dioxide.

    abstract::Applicability of a previously published equation for calculating the solubility of solutes in supercritical carbon dioxide was extended to calculate the solubility in entrained supercritical carbon dioxide employing 42 experimental data sets collected from the literature. The accuracy of the proposed model was evaluat...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.53.290

    authors: Jouyban A,Khoubnasabjafari M,Chan HK

    更新日期:2005-03-01 00:00:00

  • A new method to modify the C-4 position of 10-deacetylbaccatin III.

    abstract::We have developed a new method to modify the C-4 position of 10-deacetylbaccatin III (5) using the C-4 acetoxy anion of the 13-keto derivative (7) and various alkyl halides. The method developed herein should be very useful for the preparation of C-4 modified taxoid analogs. ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.45.2093

    authors: Uoto K,Takenoshita H,Ishiyama T,Terasawa H,Soga T

    更新日期:1997-12-01 00:00:00

  • Synthesis and antitumor activity of 20(S)-camptothecin derivatives: A-ring modified and 7,10-disubstituted camptothecins.

    abstract::20(S)-Camptothecin derivatives having nitro, amino, chloro, bromo, hydroxyl and methoxyl groups in the A-ring were synthesized. B-Ring hydrogenated camptothecin (2a) was converted into 10-hydroxycamptothecin (6e) by treatment with lead tetraacetate in trifluoroacetic acid. 10-Substituted derivatives (6) were obtained ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.39.3183

    authors: Sawada S,Matsuoka S,Nokata K,Nagata H,Furuta T,Yokokura T,Miyasaka T

    更新日期:1991-12-01 00:00:00

  • Revised structures of gambiriins A1, A2, B1, and B2, chalcane-flavan dimers from gambir (Uncaria gambir extract).

    abstract::Gambir, the aqueous extract from Uncaria gambir (Rubiaceae), has been used as an astringent medicine in Asian countries. Investigation of the constituents in the extract led to the isolation of four chalcane-flavan dimers, gambiriin A1 (6), A2 (7), B1 (8), and B2 (9), in addition to (+)-catechin (1), (+)-epicatechin (...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.55.268

    authors: Taniguchi S,Kuroda K,Doi K,Tanabe M,Shibata T,Yoshida T,Hatano T

    更新日期:2007-02-01 00:00:00

  • Separation and purification of uridine diphosphate-glucuronosyltransferases by chromatofocusing on a high-performance liquid chromatograph.

    abstract::A rapid method for the separation and purification of uridine diphosphate-glucuronosyltransferases (GT) was developed with the use of chromatofocusing on a high-performance liquid chromatograph. GT isoenzymes solubilized from hepatic microsomes of Wistar rats were separated on a Mono P column, a pre-packed column for ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.37.1583

    authors: Takanashi H,Homma H,Matsui M

    更新日期:1989-06-01 00:00:00

  • Quaternary isoquinoline alkaloids from Stephania cepharantha.

    abstract::From the quaternary alkaloidal fraction of the dried tubers of Stephania cepharantha, two new isoquinoline alkaloids, stecepharine and tetradehydroreticuline have been isolated along with the known compounds, magnoflorine, menisperine, steponine, cyclanoline, oblongine, cis-N-methylcapaurine and 2'-N-methylisotetrandr...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.48.370

    authors: Tanahashi T,Su U,Nagakura N,Nayeshiro H

    更新日期:2000-03-01 00:00:00

  • Detection and identification of loline and its analogues in horse urine.

    abstract::Several kinds of loline-type alkaloids, norloline, loline, N-acetylnorloline, N-acetylloline, N-formylnorloline, N-formylloline and N-methylloline were detected in the urine of race-horses. Furthermore, a new compound of the alkaloids, N-senecioylnorloline, was also found and identified. These compounds were mainly id...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.39.964

    authors: Takeda A,Suzuki E,Kamei K,Nakata H

    更新日期:1991-04-01 00:00:00

  • Lobenzarit disodium (CCA) inhibits in vitro immunoglobulin production via direct interaction with B lymphocytes.

    abstract::The regulatory effects of lobenzarit disodium (CCA), a therapeutic agent for treating rheumatoid arthritis (RA), on polyclonal immunoglobulin production by human lymphocytes were investigated in vitro. CCA inhibited the production of immunoglobulin in all the classes examined at a clinically relevant concentration. Mo...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.40.177

    authors: Takeda Y,Urakawa K,Sakamoto A,Nakano T,Sugawara Y,Ohsugi Y,Morita M,Kasahara T

    更新日期:1992-01-01 00:00:00

  • Synergistic action of phenolic signal compounds and carbohydrates in the induction of virulence gene expression of Agrobacterium tumefaciens.

    abstract::Virulence (vir) gene expression of Agrobacterium tumefaciens is activated by plant phenolic compounds such as alpha-hydroxyacetosyringone (HOAS), acetosyringone (AS), methyl syringate, coniferyl alcohol and sinapyl alcohol. Inositol was found to be a potentiating factor of vir-inducing activity, which enhanced the vir...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.39.2613

    authors: Song YN,Shibuya M,Ebizuka Y,Sankawa U

    更新日期:1991-10-01 00:00:00

  • Syntheses of taxuspine C derivatives as functional inhibitors of P-glycoprotein, an ATP-associated cell-membrane transporter.

    abstract::UV-Irradiation of taxinine and related compounds in acetonitrile induced a smooth transannulation between the C-3 and C-11 positions without any influence from the C-2, C-9 and C-10 substituents to give tetracyclic taxuspine C derivatives in almost quantitative yields. Photochemical transannular reaction of taxoids po...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.46.1135

    authors: Sako M,Suzuki H,Hirota K

    更新日期:1998-07-01 00:00:00

  • Catalytic activity of anion-exchange resins modified with metal-porphine in oxidative reactions of phenols.

    abstract::Anion-exchange resins modified with metal-porphine (M-Pr) have been investigated to develop a solid catalyst in the oxidative reaction of phenols by O2 in air. Co-Pr, which is easily prepared and separable from the reaction mixture, has been proved to accelerate the oxidative reaction of phenols such as 3,5-di-tertbut...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.48.1831

    authors: Iwado A,Mifune M,Kato J,Oda J,Chikuma M,Motohashi N,Saito Y

    更新日期:2000-11-01 00:00:00

  • Angiotensin-converting enzyme inhibitors: synthesis and biological activity of N-substituted tripeptide inhibitors.

    abstract::A new series of highly potent angiotensin-converting enzyme (ACE) inhibitors, 1-(N2-substituted L-lysyl-gamma-D-glutamyl)octahydro-1H-indole-2-carboxylic acids, was synthesized; various acyl groups were introduced at the alpha-amino group of the N-terminal P1 Lys. The effect of the N2-acyl groups on in vitro inhibitor...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.38.110

    authors: Sawayama T,Tsukamoto M,Sasagawa T,Nishimura K,Deguchi T,Takeyama K,Hosoki K

    更新日期:1990-01-01 00:00:00

  • Total synthesis of (+/-)-acetomycin and design of esterase-resistant analogs.

    abstract::The synthesis of acetomycin and related analogs was investigated. Acetomycin was synthesized from diethyl allyl(methyl)malonate in 6.5% yield over 18 steps. The total number of steps was improved compared to our previous synthesis; i.e., four steps shorter, and the total yield was 4.5% greater than the previous synthe...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.47.517

    authors: Uenishi J,Kobayashi N,Komine S,Okadai T,Yonemitsu O,Sasaki T,Yamada Y

    更新日期:1999-04-01 00:00:00

  • Change of ras-transformed NRK-cells back to normal morphology by mycalamides A and B, antitumor agents from a marine sponge.

    abstract::Mycalamide A and mycalamide B, isolated as antiviral and antitumor agents from a New Zealand sponge of the genus Mycale, converted the morphology of ras-transformed NRK-cells to normal morphology at 10 and 1 ng/ml, respectively. The effect on protein synthesis suggests that these agents converted the morphology by pre...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.39.2152

    authors: Ogawara H,Higashi K,Uchino K,Perry NB

    更新日期:1991-08-01 00:00:00

  • Characterization of secondary structure of neocarzinostatin apoprotein.

    abstract::Characteristics of the secondary structure of neocarzinostatin apoprotein (apo-NCS) were examined by various means. Gaussian analysis of the Fourier-transform infrared (FT-IR) curve and curve-fitting of the circular dichroism (CD) spectrum for apo-NCS revealed that this peptide was abundant in beta-structures. In the ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.37.3078

    authors: Saito K,Sato Y,Edo K,Akiyama-Murai Y,Koide Y,Ishida N,Mizugaki M

    更新日期:1989-11-01 00:00:00

  • Synthesis, characterization, cytotoxic activities, and DNA-binding studies of ternary copper(II) complexes with new coumarin derivatives.

    abstract::In this study, two novel complexes [Cu(MCVH)phen(H(2)O)].ClO(4) (1) and [Cu(MCLH)phen(H(2)O)].ClO(4) (2) (here, MCVH(2)=(7-hydroxy-4-methyl-8-coumarinyl) valine, MCLH(2)=(7-hydroxy-4-methyl-8-coumarinyl) leucine) have been synthesized and characterized by elemental analyses, molar conductance, infrared spectra (IR), (...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.58.1003

    authors: Jia L,Xu XM,Xu J,Chen LH,Jiang P,Cheng FX,Lu GN,Wang Q,Wu JC,Tang N

    更新日期:2010-08-01 00:00:00

  • Triterpenoid saponins from Ardisia crenata and their inhibitory activity on cAMP phosphodiesterase.

    abstract::Two novel triterpenoid saponins, ardisicrenoside C (1) [3 beta-O-(alpha-L-rhamnopyranosyl-(1-->2)-beta-D-glucopyranosyl-(1-->4)- [beta-D-glucopyranosyl-(1-->2)]-alpha-L-arabinopyranosyl)-16 alpha, 28-dihydroxy-olean-12-en-30-oic acid 30-O-beta-D-glucopyranosyl ester] and ardisicrenoside D (2) [3 beta-O-(beta-D-xylopyr...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.42.2309

    authors: Jia Z,Koike K,Nikaido T,Ohmoto T,Ni M

    更新日期:1994-11-01 00:00:00

  • Design, synthesis, and cytotoxic activity of Michael acceptors and enol esters in the benzo[b]acronycine series.

    abstract::A series of 2-acyl-6-methoxy-3,3,14-trimethyl-3,14-dihydro-7H-benzo[b]pyrano[3,2-h]acridin-7-ones (4-6) was prepared by treatment of 6-methoxy-3,3,14-trimethyl-3,14-dihydro-7H-benzo[b]pyrano[3,2-h]acridin-7-one (3) with an excess of an appropriate acyl chloride in the presence of aluminum chloride. Treatment of (+/-)-...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.53.919

    authors: Doan Thi Mai H,Gaslonde T,Michel S,Koch M,Tillequin F,Bailly C,David-Cordonnier MH,Pfeiffer B,Léonce S,Pierré A

    更新日期:2005-08-01 00:00:00

  • Synthesis, in Vivo Anti-inflammatory, and in Vitro Antimicrobial Activity of New 5-Benzofuranyl Fused Pyrimidines.

    abstract::Chalcone (3) has been synthesized as a new chalcone derivative bearing benzofuran moiety at 1 position. Such chalcone was used as a model dielectrophile applied to react with some nucleophiles such as 5-amino pyrazoles, 5-amino-1,2,4-triazole, 2-aminobenzimidazole, and 6-uraciles under Michael reaction conditions and ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.c15-00922

    authors: Nassar E,El-Badry YA,El Kazaz H

    更新日期:2016-01-01 00:00:00

  • Synthesis of macromolecular prodrugs of procaine, histamine and isoniazid.

    abstract::The attachment of various drugs bearing -NH2 groups to poly-alpha,beta-aspartic acid as a biodegradable carrier afforded in good yields macromolecular prodrugs which were characterized with respect to composition and drug load by spectroscopic and analytical methods. N-Ethyl-N'-(3-dimethylaminopropyl)carbodiimide hydr...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.37.2245

    authors: Giammona G,Giannola LI,Carlisi B,Bajardi ML

    更新日期:1989-08-01 00:00:00

  • Synthesis and antiproliferative evaluation of amide-containing anthraquinone, xanthone, and carbazole.

    abstract::Certain amide-containing anthraquinone, xanthone, and carbazole derivatives have been synthesized and evaluated in vitro for their antiproliferative activities against a panel of human cancer cell lines including nasopharyngeal carcinoma (NPC-TW01), lung carcinoma (NCI-H661), and leukemia (Jurkat). Among them, 2-(9,10...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.c13-00617

    authors: Chen LC,Juang SH,Chang KM,Tzeng CC,Chen JJ,Chen IL,Wang TC

    更新日期:2014-01-01 00:00:00

  • The new method for introduction of an allyl group into the angular position of 2-(TBS-oxymethyl)-2,3,4,6,7,8-hexahydro-1-benzopyran-5-one and its application to chiral Wieland-Miescher type compound synthesis.

    abstract::The stereoselective introduction of an allyl group into the angular position of 2-(TBS-oxymethyl)-2,3,4,6,7,8-hexahydro-1-benzopyran-5-one was accomplished using Birch reduction and an enolate trapping reaction. It was determined that the allyl group was introduced via an unexpected conformation-flipped from the initi...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.53.207

    authors: Hiroya K,Takahashi T,Shimomae K,Sakamoto T

    更新日期:2005-02-01 00:00:00

  • False HDAC Inhibition by Aurone Compound.

    abstract::Fluorescence assays are useful tools for estimating enzymatic activity. Their simplicity and manageability make them suitable for screening enzyme inhibitors in drug discovery studies. However, researchers need to pay attention to compounds that show auto-fluorescence and quench fluorescence, because such compounds lo...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.c16-00123

    authors: Itoh Y,Suzuki M,Matsui T,Ota Y,Hui Z,Tsubaki K,Suzuki T

    更新日期:2016-01-01 00:00:00