Particle Design for Taste-Masking Using a Spray-Congealing Technique.

Yajima, Toshio; Nogata, Akemi; Demachi, Miki; Umeki, Nobuo; Itai, Shigeru; Yunoki, Nobuo; Nemoto, Masami

doi:10.1248/cpb.44.187

Cited by 57 publications

(31 citation statements)

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“…5) Our formulation was comprised of a wax matrix agglomerated using a spray-congealing technique. 6) In the manufacturing process, GM, one of the components of the wax matrix, is transformed from the b-form to the a-form and gradually transformed back to the b-form at ambient temperature.…”

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confidence: 99%

Determination of Optimum Processing Temperature for Transformation of Glyceryl Monostearate.

Yajima

Itai

Takeuchi

et al. 2002

CHEMICAL & PHARMACEUTICAL BULLETIN

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Glyceryl monostearate (GM), a mixture of glyceryl esters of fatty acids, is composed of glyceryl monostearate (65%), glyceryl monopalmitate (30%) and glyceryl monomyristate (5%). It has been widely used as an emulsifying agent in food preparations.Maruyama et al. carried out precise studies of the polymorphism of GM, 2,3) and reported that four crystal forms of GM exist. Rapid cooling of melted GM yields the a-form, which is successively transformed to the b-form via the bЈ-form under ambient conditions. Since the a-form is dispersible and foamy, it is often used as an emulsifying agent, foaming agent and preservative for bread, ice cream, cookies, etc.4) On the other hand, the b-form of GM having higher melting point, higher density, is poorer in foaming and wetting than the a-form.We have applied b-form of GM to the pediatric formulation of clarithromycin (CAM) and succeeded in masking the bitter taste. 5) Our formulation was comprised of a wax matrix agglomerated using a spray-congealing technique.6) In the manufacturing process, GM, one of the components of the wax matrix, is transformed from the b-form to the a-form and gradually transformed back to the b-form at ambient temperature. The bitterness of taste of the formulation diminishes due to increase in the ratio of the b-form of GM, which has poor wettability. The objective of this study was to find the optimum conditions for rapid formation of b-form of GM during the manufacturing process of the formulation. For this purpose, we focused on the transformation of a-form of GM to b-form under the congealing conditions. ExperimentalMaterial Glyceryl monostearate of b-form (GM, Taiyo Kagaku Co., Ltd.) was of the grade specified in the Japanese Pharmaceutical Excipients Directory. Preparation of Polymorphs of GMIn preparing the a-form of GM, GM melted at 120°C was dropped on the rotating wing of a stirring machine with an approximately 5 cm blade at 1500 rpm. Dripped GM was micronized, solidified, and recovered on the bed under room temperature.GM with various ratios of polymorphs a and b was prepared by mixing the a-form immediately after preparation and the commercially available GM (b-form) at the ratios of 25 : 75, 50 : 50 and 75 : 25.Method of Heat-Treatment About 2 mg of GM was placed in the differential scanning calorimeter (DSC) pan and stored for fixed times and temperatures.Measurement of Powder Characteristics Thermal analysis was carried out using a differential scanning calorimeter (DSC-7, Perkin Elmer). About 2 mg of GM was heat-treated in the opened pan in the DSC and, after cooling the sample to 30°C at the rate of 10°C/min, the first run of thermal analysis was carried out at a heating rate of 10°C/min in the temperature range of 30°C to 90°C. After cooling, the second run of thermal analysis was carried out under the same conditions. Enthalpies of first and second thermal analyses were expressed by the enthalpy change, DH 1 and DH 2 , respectively.Powder XRD patterns were obtained using a Rigaku Geigerflex RAD powder X-ray diffractometer und...

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confidence: 99%

Determination of Optimum Processing Temperature for Transformation of Glyceryl Monostearate.

Yajima

Itai

Takeuchi

et al. 2002

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…This is thought to be due to promotion of the dissolution of an acidsoluble polymer, aminoalkyl methacrylate copolymer E, which is present in the dry syrup to aid dissolution of CAM in stomach (below pH 5), and the fact that acid jellies enhance the solubility of basic CAM itself. 16) On the other hand, the concentration of CAM in the solution extracted from the mixture of CAMD and chocolate jelly was lower than the control. It was suggested that dissolution of CAM from the jelly was suppressed by the jelly network structure.…”

Section: Resultsmentioning

confidence: 92%

“…3, the pH of the chocolate jelly was 6.4, almost neutral, while in mixtures of CAMD (or AZMD) and chocolate jelly the pH shifted to 7.3 (or 8.2), respectively, because of the basic components in the dry syrup product. 16,17) This fact suggests that the solubility of CAM or AZM in chocolate jelly was low, since solubility of basic drugs increases as pH decreases.…”

Section: Resultsmentioning

confidence: 99%

Evaluation of Bitterness Suppression of Macrolide Dry Syrups by Jellies

Tsuji

Uchida

Fukui³

et al. 2006

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…3) Various methods such as drug particle coating, 4,5) encapsulation, 6) complexation 7) and chemical modiˆcation 8) have been utilized to mask the bitterness. However, these techniques are complex and extensive optimization is required for their practical application and, therefore, cost eŠective and simple taste masking technology needs to be developed.…”

Section: Introductionmentioning

confidence: 99%

Investigation of Organoleptic Characteristics in the Development of Soft Chews of Calcium Carbonate as Mineral Supplement

2009

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The present study was aimed at developing a soft chewable dosage form for calcium carbonate for nutraceutical application. Two diŠerent types of the formulations viz., sugar based and sugar free soft chews were prepared. The eŠect of various ingredients on the diŠerent organoleptic characteristics (grittiness, sweetness, hardness and mouthfeel) and the emulsion stability of the dosage form were checked and evaluated on the basis of an in-house numerical scale on healthy human volunteers. The study revealed that the type of emulsifying agent, heating temperature, particle size of the drug, ratio and quantity of sugars were found to have signiˆcant impact on the organoleptic characteristics of the dosage form. The study also indicates that the proper selection of packaging material is important in order to maintain the long term integrity of the formulation.

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Particle Design for Taste-Masking Using a Spray-Congealing Technique.

Cited by 57 publications

References 0 publications

Determination of Optimum Processing Temperature for Transformation of Glyceryl Monostearate.

Determination of Optimum Processing Temperature for Transformation of Glyceryl Monostearate.

Evaluation of Bitterness Suppression of Macrolide Dry Syrups by Jellies

Investigation of Organoleptic Characteristics in the Development of Soft Chews of Calcium Carbonate as Mineral Supplement

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