Effect of preparation method on properties of orally disintegrating tablets made by phase transition

Kuno, Yusuke; Kojima, M.; Ando, Shuichi; Nakagami, Hiroaki

doi:10.1016/j.ijpharm.2007.11.046

Cited by 24 publications

(17 citation statements)

References 9 publications

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“…Formulation E had the highest score and was significantly different from the other formulations. The effectiveness of sucralose in masking bitter taste can be explained by its powerful sweetness, which is 600-1,000 times sweeter than sucrose (25,26). The taste of formulation H (contained only flavouring agent), was not significantly different when compared with formulation A (control).…”

Section: Palatability Evaluationmentioning

confidence: 99%

Characterization of Oral Disintegrating Film Containing Donepezil for Alzheimer Disease

2011

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Abstract. The aim of this study was to develop a taste-masked oral disintegrating film (ODF) containing donepezil, with fast disintegration time and suitable mechanical strength, for the treatment of Alzheimer's disease. Hydroxypropyl methylcellulose, corn starch, polyethylene glycol, lactose monohydrate and crosspovidone served as the hydrophilic polymeric bases of the ODF. The uniformity, in vitro disintegration time, drug release and the folding endurance of the ODF were examined. The in vitro results showed that 80% of donepezil hydrochloride was released within 5 minutes with mean disintegration time of 44 seconds. The result of the film flexibility test showed that the number of folding time to crack the film was 40 times, an indication of sufficient mechanical property for patient use. A single-dose, fasting, four-period, eight-treatment, double-blind study involving 16 healthy adult volunteers was performed to evaluate the in situ disintegration time and palatability of ODF. Five parameters, namely taste, aftertaste, mouthfeel, ease of handling and acceptance were evaluated. The mean in situ disintegration time of ODF was 49 seconds. ODF containing 7 mg of sucralose were more superior than saccharin and aspartame in terms of taste, aftertaste, mouthfeel and acceptance. Furthermore, the ODF was stable for at least 6 months when stored at 40°C and 75% relative humidity.

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Section: Palatability Evaluationmentioning

confidence: 99%

Characterization of Oral Disintegrating Film Containing Donepezil for Alzheimer Disease

2011

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“…According to the description of Kuno et al, 21 the preliminary test in volunteers was carried out previously. The oral disintegration time of an ODMT put into the mouth of a healthy male adult volunteer without water was recorded as the time until the volunteer felt that the tablet had disappeared in his mouth.…”

Section: Disintegration Time Of Odtsmentioning

confidence: 99%

A novel spray-dried nanoparticles-in-microparticles system for formulating scopolamine hydrobromide into orally disintegrating tablets

Li¹,

Cheng²,

Bi³

et al. 2011

IJN

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Scopolamine hydrobromide (SH)-loaded microparticles were prepared from a colloidal fluid containing ionotropic-gelated chitosan nanoparticles using a spray-drying method. The spray-dried microparticles were then formulated into orally disintegrating tablets (ODTs) using a wet granulation tablet formation process. A drug entrapment efficiency of about 90% (w/w) and loading capacity of 20% (w/w) were achieved for the microparticles, which ranged from 2 μm to 8 μm in diameter. Results of disintegration tests showed that the formulated ODTs could be completely dissolved within 45 seconds. Drug dissolution profiles suggested that SH is released more slowly from tablets made using the microencapsulation process compared with tablets containing SH that is free or in the form of nanoparticles. The time it took for 90% of the drug to be released increased significantly from 3 minutes for conventional ODTs to 90 minutes for ODTs with crosslinked microparticles. Compared with ODTs made with noncrosslinked microparticles, it was thus possible to achieve an even lower drug release rate using tablets with appropriate chitosan crosslinking. Results obtained indicate that the development of new ODTs designed with crosslinked microparticles might be a rational way to overcome the unwanted taste of conventional ODTs and the side effects related to SH’s intrinsic characteristics.

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“…Rapid penetration of water into the tablet can be a mechanism of disintegration in rapidly disintegrating tablets. 10,[24][25][26] The fact that VE is a fat-soluble drug suggests that the prolongation of disintegration time seen with VE-OI ODTs and VE-PO ODTs is attributable to decreased hydrophilicity of the tablet surface. In contrast, VE-FL ODTs and VE-SD ODTs did not show prolongation of disintegration time, which was thought to be attributable to the increased hydrophilicity of the tablet surface owing to the particle design of oily VE.…”

Section: Physicochemical Properties Of Ve Odts With Various Amounts Omentioning

confidence: 99%

“…For example, ODTs can be prepared by several manufacturing methods, e.g., lyophilization, 7) granulation, 8) the cotton candy process, 9) and phase transition of sugar alcohols by direct compression. 10,11) The oily type of fat-soluble drugs have generally been produced and marketed commercially in soft capsule form, 12) though some prescription and over-the-counter drugs, e.g., tablets and granules as therapeutic agents for gastric ulcer, have already been marketed. A tablet preparation of oily drugs can be expected to improve the compliance and utility of the medicine for patients.…”

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confidence: 99%

Preparation and Evaluation of Orally Disintegrating Tablets Containing Vitamin E as a Model Fat-Soluble Drug

Ikematsu

Uchida

Namiki

2015

CHEMICAL & PHARMACEUTICAL BULLETIN

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The purpose of the present study was to develop orally disintegrating tablets (ODTs) containing fatsoluble drugs that disintegrate rapidly while having appropriate tablet strength. We chose vitamin E (VE) as a model drug; d-α-tocopheryl acetate, as the oily VE (VE-OI), and d-α-tocopheryl acid succinate, as the powder VE (VE-PO), were used. The oily VE was added directly to ODTs (VE-OI ODTs) and also used for the preparation of two types of VE granule, i.e., granules prepared using adsorption to calcium silicate (VE-FL granules) and granules prepared using spray-drying with gelatin (VE-SD granules); each type of granule was added to ODTs (VE-FL ODTs and VE-SD ODTs). Powder VE was added directly to ODTs (VE-PO ODTs). Various VE ODTs were prepared using these four additional methods with varying amounts of VE per tablet and were evaluated with respect to their manufacturability, physicochemical characteristics, and stability. It was demonstrated that a tablet porosity of 30% to 35% and tensile strength of 7 kg/cm 2 or greater are required to provide VE ODTs with rapid disintegration and appropriate tablet strength, and that VE-SD granules and powder VE are suitable forms of VE to be added. When stability tests of VE-SD ODTs and VE-PO ODTs were performed, VE-PO ODTs exhibited prolongation of disintegration time and increased tensile strength, whereas VE-SD ODTs showed none of these changes. These changes were thought to be attributable to a decrease in the pore size of VE-PO ODTs resulting from the softening and migration of powder VE under hot storage conditions. Key words orally disintegrating tablet; fat-soluble drug; vitamin E; disintegration; tensile strength; porosity Most pharmaceutical dosage forms for oral administration are developed for drug delivery after swallowing. In particular, tablets and capsules are the most common oral solid dosage forms, because they are convenient to carry, the duration of action of the contained drugs can be controlled, 1) and their taste or smell can be improved. 2)However, many geriatric and pediatric patients often have difficulties swallowing conventional tablets or capsules.3) It is estimated that 50% of the population experiences this problem, which results in a high prevalence of non-compliance and ineffective therapy. 4,5) To overcome this issue, a variety of pharmaceutical studies have been conducted to develop new dosage forms. Among the dosage forms developed to facilitate ease of medication, the orally disintegrating tablet (ODT) is one of the most widely employed in commercial products. 6)Numerous studies have therefore been performed on the various compositions of and manufacturing methods for ODTs. For example, ODTs can be prepared by several manufacturing methods, e.g., lyophilization, 7) granulation, 8) the cotton candy process, 9) and phase transition of sugar alcohols by direct compression. 10,11) The oily type of fat-soluble drugs have generally been produced and marketed commercially in soft capsule form, 12) though some prescription and over-the-counter d...

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Effect of preparation method on properties of orally disintegrating tablets made by phase transition

Cited by 24 publications

References 9 publications

Characterization of Oral Disintegrating Film Containing Donepezil for Alzheimer Disease

Characterization of Oral Disintegrating Film Containing Donepezil for Alzheimer Disease

A novel spray-dried nanoparticles-in-microparticles system for formulating scopolamine hydrobromide into orally disintegrating tablets

Preparation and Evaluation of Orally Disintegrating Tablets Containing Vitamin E as a Model Fat-Soluble Drug

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