Gliclazide tablet prescription and Preparation Process
Author: Xu Jun PENG Wang Lu Hua Zhao Defang
【Abstract】 Objective To study and selection of gliclazide Preparation of dispersible tablets and prescription. Methods
filter through a series of experiments the collapse of auxiliary agents to determine the prescription and preparation process, compared dispersible tablets and ordinary tablets in the dissolution of the main drugs. The results determined in order to cross-linked carboxymethyl cellulose sodium, cross-
linked polyvinylpyrrolidone as a disintegrant in tablet prescription; tablet dissolution rate as compared with ordinary tablets. Conclusion Gliclazide tablet prescription reasonable and technology is feasible, in line with the
requirements of dispersible tablets.
Key words gliclazide tablet prescription Preparation
Abstract: ObjectiveTo optimize the preparation technology and the formula of Gliclazide dispersible tablets. MethodsThe formula and preparation process were optimized by a series of experiments. The dissolution rates of the principal agent in dispersible tablets and conventional tablets were determined and compared. ResultsSodium carboxymethyl starch and crospolyvinylpyrrolidone were optimized as the disintegrants
of the dispersible tablet formula; the dissolution rates of the dispersible tablets were faster than those of the conventional tablets. ConclusionThe prepared gliclazide dispersible tablet is reasonable in formula, feasible in technology and it meets the quality standards.
Key words: Gliclazide; Dispersible tablets; Formula; Preparation technologies
Gliclazide is a second-generation oral sulfonylurea
hypoglycemic agents, the role of strong, its mechanism is selectively acts on islet β-cells, promoting insulin
secretion, and increase insulin release after the consumption of glucose, so that glycogen formation and the output is inhibited, for non-insulin-dependent diabetes mellitus (?)
At present, gliclazide tablets listed species are mainly , capsules [4,5] and so on. Dispersible tablets in recent years developed an oral immediate-release dosage forms, which
can rapidly collapse into a uniform viscous suspension. Because of its convenient to take, especially suitable for
old, young, and patients with difficulty swallowing solids, coupled with the absorption of its fast and high bioavailability , the preparation process the same as ordinary tablets, which have become an increasing concern.
This experiment, the author appearance, hardness, disintegration time, uniformity and dissolution rate dispersion as an indicator of the composition and preparation process prescriptions were screened studies to determine the tablet of the prescription and preparation process.
1 Materials and equipment
1.1 Materials gliclazide (Tianjin Zhongxin Pharmaceutical Group, New New pharmaceutical); lactose (Shanghai dairy products factory); powder silica gel (Zhejiang Huzhou foods & chemicals); cross-linked carboxymethyl cellulose sodium
(Shanghai Chemical Yuan-hong Co., Ltd.); cross-linked
polyvinylpyrrolidone (Shanghai Yuan Wang Chemical Co., Ltd.); Poloxamer (Shenyang Pharmaceutical University Pharmaceutical Factory); magnesium stearate (Shanghai Pharmaceutical
1.2 Instrument Dissolution Tester (Tianjin Guo-ming
Medical Equipment Co., Ltd.); high-speed milling machine
(Zhangjiagang City, New Electrical and Mechanical Co., Ltd.); Smart collapse Instrument (Fa Technology Co., Ltd. Tianjin,
Tianjin University and Tianjin); TDP Single Punch Tablet Press (Shanghai United Pharmaceutical Equipment Co., Ltd.); tablet hardness tester (Shanghai Yellow doping Instruments Co.,
Ltd.); electronic balance (Beijing Sartorius Instrument Systems Co., Ltd.).
2 Methods and Results
2.1 The prescription and Technology
2.1.1 Prescription Gliclazide 40 g, lactose 80 g, powder silica gel 39 g, microcrystalline cellulose 95 g, cross-linked
sodium carboxymethyl cellulose 20 g, cross-linked
polyvinylpyrrolidone 20 g, parking losha Beam 5 g, magnesium stearate 1 g, 30% ethanol amount.
2.1.2 process the original, auxiliary backup over 100 mesh sieve, according to the amount of said prescription to take the original, auxiliary materials, will gliclazide and
lactose mixing, and placing high-speed milling machine crushed
1 min, were added to silica gel powder, microcrystalline cellulose, crosslinked polyvinylpyrrolidone and crosslinked sodium carboxymethyl cellulose, so that mixing, poloxamer 30%
ethanol solution of the system of soft material, 18 mesh sieve system of particles, the wet granules at 80 ? for drying 4 h,
16 Whole mesh sieve, add lubricant magnesium stearate mixing, tabletting, that is too.
2.2 Prescription and screening to determine
2.2.1 formulation design according to "Chinese Pharmacopoeia" on the requirements of dispersible tablets: dispersible tablets must be within 3 min and can collapse on the 2nd through the sieve (24 mesh). In addition, the need to have better dissolution. According to these requirements, I designed using a prescription comparison of different combinations of prescription trial to compare tablets disintegrated within 3 min in the case, as well as the determination of dissolution results of screening to determine
the best use of prescription combination. Reposted elsewhere in the paper for free download http://
The author according to the requirements of dispersible tablets and this product characteristics, design of this product on-chip weight about 300 mg, the appropriate
combination of accessories to take the same preparation technique to observe the preparation process and the collapse
of the problems in a decentralized situation, formulation design Table 1. Table 1 Prescription Design (abbreviated)
Trial during the following problems: 1 ~ 3 by adding a prescription wetting agent 90% ethanol, granulating effect is better, but fragile particles after drying, it should lower the ethanol concentration; prescription by adding 90% ethanol
at 4 dry granulation, powder more particles less pressure films hat serious phenomenon tablet machine is unable to continue operating, thus, the formulation design is unreasonable to be eliminated.
Four kinds of prescription tablets to suppress the
determination of disintegration time and the tablet hardness testing. The results in Table 2. Table 2 Prescription test results (omitted)
From Table 2 experimental results, the prescription of two better. Prescription a longer disintegration time, its
hardness, one-sided finish is poor, needs to be improved.
2.2.2 Prescription adjustment and to determine the appropriate adjustment of prescription, preparation ibid, prescription design in Table 3. Table 3 Adjusted prescription Design (abbreviated)
Prescriptions for more than five groups, forming after the disintegration time, hardness, dissolution test and other tests, the results in Table 4. Table 4 prescriptions designed to test results (omitted)
The results we can see from table 4: two sets of
prescription prescription 8,9 suppression of its
disintegration time and hardness of tablets, dissolution have better results. In particular, the combination of nine prescription only an increase in the solvent also reached a good dissolution, film-sided light, and the prescription of a minimum of components in components. Taking all factors, after selection and choose a prescription prescription prescription for the final nine.
Gliclazide of raw materials and excipients lactose mixed
high-speed milling, the powder fine grind (through 200 mesh sieve), conducive to gliclazide drug dissolution may be related to the formation of solid melts were related, need to be further validation.
In this study, using the poloxamer dissolved in 30%
ethanol solution (Lueke heated to accelerate dissolution), the soft material is conducive to the system will be fully poloxamer solubilizer uniformly distributed in soft materials, the increased glibenclamide Qi Special drug dissolution.
Through the above analysis of experimental results can be seen, the prescription preparation of dispersible tablets of gliclazide rapid disintegration, dissolution high, in line with dispersible tablet formulation requirements, and its
preparation process is simple, suitable for industrial mass production, has good prospects for development and application of .
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