CN1302772C - Orally disintegrated sodium ferulate tablet and its prepn process - Google Patents

Abstract

The present invention relates to a sodium ferulate orally disintegrating tablet and a preparation method thereof, which belongs to the technical field of medicinal preparations. The table contains 10 to 50 wt% of sodium ferulate active ingredient and 50 to 90 wt% of pharmaceutically acceptable auxiliary materials, wherein the auxiliary materials comprise 2 to 30 wt% of disintegrating agent, 10 to 90 wt% of filling agent, 1 to 5 wt% of adhesive, at most 5 wt% of lubricating agent and 0.1 to 20 wt% of corrigent; the preparation method can adopt a freeze drying method, a direct powder compression method and a wet granulation and tabletting method; according to different preparation methods, relevant auxiliary materials in the components can be selected; the preparation of the present invention overcomes the defects of slow dissolution, inconvenient swallow, etc. of common sodium ferulate tablets; the tablet has the advantages of no stimulation to the feelmouth mucosa, good taste and no sand feel and is especially suitable for senile patients with dysphagia.

Description

Sodium ferulate orally disintegrating tablet and preparation method thereof

Technical field

The invention relates to the technical field of pharmaceutical preparations, and relates to a sodium ferulate orally disintegrating tablet and a preparation method thereof.

Background technique

Sodium ferulate (sodium ferulate) is the sodium salt of ferulic acid, the main component of traditional Chinese medicine extracts such as angelica and chuanxiong. disease treatment. The curative effect is definite, and its marketed oral dosage form is common tablet. However, sodium ferulate tablets are insoluble in the stomach. According to the dissolution test of sodium ferulate tablets in the 2005 edition of "Chinese Pharmacopoeia", it is found that commercially available sodium ferulate tablets (Chengdu Hengda Pharmaceutical Co., Ltd., batch number 040804) Only 10% of the drug dose is dissolved in the artificial gastric juice in 45 minutes, which affects the absorption of the drug in the body, and the drug takes effect slowly. It is worth noting that the clinical users of sodium ferulate tablets are mostly special groups such as the elderly and bedridden who need long-term medication. These patients often have difficulty swallowing, and the tablets are prone to physical blockage. According to the latest epidemiological findings, only about 35% of ordinary elderly patients will have difficulty swallowing medicine.

Orally disintegrating tablet is a new type of solid preparation researched and developed abroad in the past ten years. It refers to a tablet that can quickly disintegrate or dissolve within 1 minute in the oral cavity without additional water or with very little water. This dosage form mainly selects a disintegrant with excellent disintegration performance. The tablet is placed on the patient's tongue, and it dissolves or disintegrates quickly when it meets saliva, and the drug enters the stomach to take effect by swallowing. Compared with ordinary tablets, orally disintegrating tablets provide a new method of taking medicine, which is convenient for patients to take medicine, especially for the elderly and other patients with dysphagia, and prevents suffocation due to physical blockage of the tablet. At the same time, due to the use of a disintegrant with excellent disintegration performance, the tablet disintegrates rapidly in the oral cavity, which accelerates the dissolution of the drug and makes the drug quickly absorbed and effective. But at present, there is no relevant research report on sodium ferulate orally disintegrating tablets.

Contents of Invention

The invention provides an orally disintegrating sodium ferulate tablet which is convenient to swallow and has a quick effect and a preparation method thereof.

The sodium ferulate orally disintegrating tablet of the present invention, the component comprises sodium ferulate active ingredient and pharmaceutically acceptable adjuvant, the weight percentage of sodium ferulate is 10-50%, the weight percentage of adjuvant is 50-90% %, auxiliary materials include disintegrants, fillers, and may also contain binders, lubricants, and flavoring agents. The weight percentage of the disintegrant is 2-30%, the weight percentage of the filler is 10-90%, the weight percentage of the binder is 1-5%, the weight percentage of the lubricant is not more than 5%, and the weight percentage of the flavoring agent The percentage is 0.1 to 20%. Depending on the preparation method, relevant auxiliary materials can be selected.

The disintegrating agent is selected from crospovidone, croscarmellose sodium, sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose, microcrystalline cellulose, and one or more of them can be selected at the same time. Several kinds.

The filler is selected from lactose, pregelatinized starch, mannitol, sorbitol, xylitol, and erythritol, and one or more of them can be selected simultaneously.

The binder is selected from syrup, starch slurry, sodium carboxymethylcellulose, hydroxypropylmethylcellulose, povidone, and one or more of them can be selected simultaneously.

Described lubricant is selected from micropowder silica gel, magnesium stearate, talcum powder, can select wherein one or more simultaneously.

The flavoring agents include sweeteners, flavoring agents and effervescent agents. The sweetener is selected from sodium saccharin, sucrose, aspartame, and cyclamate, and one or more of them can be selected at the same time, and the weight percentage is 1 to 5%; the flavoring agent is selected from vanilla, cherry, grape, orange, Lemon, mint, blueberry, banana, pineapple, peach, caramel essence, the percentage by weight is 0.1-1%; effervescent agent is selected from the mixture of sodium bicarbonate and tartaric acid or citric acid or fumaric acid, the percentage by weight is not more than 15% .

The preparation method of the sodium ferulate orally disintegrating tablet can be selected from a freeze-drying method, a powder direct compression method or a wet granulation tablet compression method.

1. Freeze-drying method: the step is to mix sodium ferulate with disintegrant, filler, and flavoring agent according to the proportion, add appropriate amount of water to dilute, mix well, place in the corresponding tablet mold, and freeze-dry Freeze drying in the machine until the material is completely dry and shaped.

2. Powder direct compression method: the step is to sieve sodium ferulate, disintegrant, filler and flavoring agent according to the proportion, mix evenly, add lubricant and mix evenly, and directly compress into tablets.

3. Wet granulation and tabletting method: the step is to mix sodium ferulate with filler, flavoring agent and part of disintegrating agent evenly according to the proportion, add binder to make soft material, granulate, dry, Granules, and finally add the remaining amount of disintegrant and lubricant, and compress into tablets.

According to the dissolution rate test, the dissolution rate of the sodium ferulate in the orally disintegrating tablet of the present invention is greater than 90% within 5 minutes, so the medicine takes effect quickly after oral administration. The orally disintegrating tablet of the present invention does not need water when taken, and disintegrates within 1 minute only by saliva in the oral cavity, has no irritation to the oral mucosa, has good taste, suitable acidity and sweetness, and has no gritty feeling, and is especially suitable for swallowing difficult elderly patients. The preparation method of the orally disintegrating tablet of the invention is simple and suitable for industrial scale production.

Description of drawings

Fig. 1 is the dissolution curve of sodium ferulate orally disintegrating tablets and commercially available common tablets in artificial gastric juice

Fig. 2 is the dissolution curve in water of sodium ferulate orally disintegrating tablets and commercially available common tablets

Detailed ways

The present invention will be described in detail below in conjunction with the embodiments and accompanying drawings, but the present invention is not limited thereto.

In specific implementation, different auxiliary materials can be used in the components according to different requirements and preparation methods.

Embodiment 1 freeze-drying method prepares sodium ferulate orally disintegrating tablet

Components and ratio (w/w%)

Sodium Ferulate 40

Sodium Carboxymethyl Starch 5

Microcrystalline Cellulose 10

Lactose 23

Sucrose 20

Aspartame 1.5

Orange flavor 0.5

Preparation:

Suspend sodium ferulate, sodium carboxymethyl starch, microcrystalline cellulose, lactose, sucrose, aspartame, and orange essence in appropriate amount of water, stir for 1 hour to make a suspension, and pour it into tablet molds , carry out freeze-drying, freeze-drying and forming, pressing and sealing, and packaging.

The resulting freeze-dried product has a loose structure, suitable acidity and sweetness on the tongue, no gritty feeling, a disintegration time of 5 seconds, and a 100% dissolution time of 4 minutes.

Embodiment 2 freeze-drying method prepares sodium ferulate orally disintegrating tablet

Components and ratio (w/w%)

Sodium Ferulate 15

Low-substituted hydroxypropyl cellulose 10

Microcrystalline Cellulose 20

Lactose 33.8

Pregelatinized starch 20

Cyclamate 1

Cherry flavor 0.2

Preparation:

Suspend sodium ferulate, low-substituted hydroxypropyl cellulose, microcrystalline cellulose, lactose, pregelatinized starch, cyclamate, and cherry essence in appropriate amount of water, stir for 1 hour to make a suspension, and pour it into In the tablet mold, freeze-drying is carried out, and after freeze-drying and molding, it is compressed and sealed, and packed.

The resulting freeze-dried product has a loose structure, suitable acidity and sweetness on the tongue, no gritty feeling, a disintegration time of 5 seconds, and a 100% dissolution time of 4 minutes.

Embodiment 3 powder direct compression method prepares sodium ferulate orally disintegrating tablet

Components and ratio (w/w%)

Sodium Ferulate 25

Crospovidone 8

Microcrystalline Cellulose 20

Lactose 19

Mannitol 23.5

Micropowder silica gel 2

Magnesium stearate 1

Aspartame 1

Orange flavor 0.5

Preparation:

Pass sodium ferulate, crospovidone, microcrystalline cellulose, lactose, and mannitol through an 80-mesh sieve, and mix them with micropowder silica gel, magnesium stearate, aspartame, and orange essence in equal amounts, and directly Tablet forming, packaging.

The obtained orally disintegrating tablet has a cooling sensation on the tongue, suitable acidity and sweetness, and no gritty feeling. The disintegration time is 47 seconds, and the 100% dissolution time is 10 minutes, all of which meet the requirements of the Pharmacopoeia.

Embodiment 4 powder direct compression method prepares sodium ferulate orally disintegrating tablet

Components and ratio (w/w%)

Sodium Ferulate 22

Sodium Carboxymethyl Starch 3

Microcrystalline Cellulose 18

Lactose 20

Mannitol 28

Sodium bicarbonate 2

Citric acid 2.5

Micropowder silica gel 2

Magnesium stearate 0.5

Aspartame 1.5

Lemon essence 0.5

Preparation:

Pass sodium ferulate, sodium carboxymethyl starch, microcrystalline cellulose, lactose, mannitol, sodium bicarbonate, citric acid through an 80-mesh sieve, and micronized silica gel, magnesium stearate, aspartame, lemon essence, etc. The amount is added and mixed evenly, directly compressed into tablets, and packaged.

The obtained orally disintegrating tablet had effervescent and cooling sensations on the tongue, suitable acidity and sweetness, and no gritty feeling. The disintegration time was 32 seconds, and the 100% dissolution time was 8 minutes, all of which met the requirements of the Pharmacopoeia.

Embodiment 5 powder direct compression method prepares sodium ferulate orally disintegrating tablet

Components and ratio (w/w%)

Sodium Ferulate 30

Sodium Croscarmellose 5

Microcrystalline Cellulose 10

Lactose 11.5

Mannitol 28

Sodium bicarbonate 5

Tartaric acid 6

Micropowder silica gel 2

Magnesium stearate 0.5

Aspartame 1.5

Lemon essence 0.5

Preparation:

Pass sodium ferulate, croscarmellose sodium, microcrystalline cellulose, lactose, mannitol, sodium bicarbonate, and tartaric acid through an 80-mesh sieve, and mix with micronized silica gel, magnesium stearate, aspartame, and lemon The essence is added in equal amounts and mixed evenly, directly compressed into tablets and packaged.

The obtained orally disintegrating tablet has an effervescent and cool feeling on the tongue, suitable acidity and sweetness, and no gritty feeling. The disintegration time is 30 seconds, and the 100% dissolution time is 8 minutes, all of which meet the requirements of the Pharmacopoeia.

Example 6 Preparation of Sodium Ferulate Orally Disintegrating Tablets by Wet Granulation and Tablet Compression

Components and ratio (w/w%)

Sodium Ferulate 30

Sodium Croscarmellose 5

Microcrystalline Cellulose 15

Lactose 10

Mannitol 30

Sodium bicarbonate 2

Fumaric acid 2.5

Micropowder silica gel 2

Magnesium stearate 2

Aspartame 1

Orange flavor 0.5

Preparation:

Mix sodium ferulate with croscarmellose sodium, microcrystalline cellulose, lactose, mannitol, sodium bicarbonate, fumaric acid, micronized silica gel, aspartame, and use 1% povidone ethanol The solution is granulated, dried at 50°C, sprayed with orange essence after granulation, added with magnesium stearate, compressed into tablets, and packaged.

The obtained orally disintegrating tablet had effervescent and cooling sensations on the tongue, suitable acidity and sweetness, and no gritty feeling. The disintegration time was 49 seconds, and the 100% dissolution time was 10 minutes, all of which met the requirements of the Pharmacopoeia.

The orally disintegrating tablet that embodiment 3 makes is compared with the commercially available sodium ferulate tablet (Chengdu Hengda Pharmaceutical Co., Ltd., batch number 040804) by "Chinese Pharmacopoeia" 2005 edition, and the dissolution rate in artificial gastric juice and water is compared respectively, and the result See Figure 1 and Figure 2. It can be seen from the figure that the dissolution rate of the orally disintegrating tablet of the present invention in artificial gastric juice and water is significantly higher than that of the ordinary tablet. Therefore, in vitro experiments show that the orally disintegrating tablet of the present invention is convenient to take orally and has quick effect.

Claims (5)

1. an Orally disintegrated sodium ferulate tablet comprises sodium ferulate active component and medicinal acceptable auxiliary, and adjuvant comprises disintegrating agent, filler, correctives; Wherein disintegrating agent is selected from carboxymethyl starch sodium, microcrystalline Cellulose, can select wherein a kind of or two kinds simultaneously for use; Filler is a lactose; Correctives comprises sweeting agent and flavouring agent, and sweeting agent is sucrose and aspartame, and flavouring agent is an orange flavor, it is characterized in that component and proportioning (w/w/%) are as follows:

Sodium ferulate 40

Carboxymethyl starch sodium 5

Microcrystalline Cellulose 10

Lactose 23

Sucrose 20

Aspartame 1.5

Orange flavor 0.5.

2. an Orally disintegrated sodium ferulate tablet comprises sodium ferulate active component and medicinal acceptable auxiliary, and adjuvant comprises disintegrating agent, filler, lubricant, correctives; Wherein disintegrating agent is selected from polyvinylpolypyrrolidone, microcrystalline Cellulose, can select wherein a kind of or two kinds simultaneously for use; Filler is lactose and mannitol; Lubricant is micropowder silica gel and magnesium stearate; Correctives comprises sweeting agent and flavouring agent, and sweeting agent is an aspartame, and flavouring agent is an orange flavor, it is characterized in that component and proportioning (w/w/%) are as follows:

Sodium ferulate 25

Polyvinylpolypyrrolidone 8

Microcrystalline Cellulose 20

Lactose 19

Mannitol 23.5

Micropowder silica gel 2

Magnesium stearate 1

Aspartame 1

Orange flavor 0.5.

3. an Orally disintegrated sodium ferulate tablet comprises sodium ferulate active component and medicinal acceptable auxiliary, and adjuvant comprises disintegrating agent, filler, binding agent, lubricant, correctives; Wherein disintegrating agent is selected from cross-linking sodium carboxymethyl cellulose, microcrystalline Cellulose, can select wherein a kind of or two kinds simultaneously for use; Filler is lactose, mannitol; Lubricant is micropowder silica gel, magnesium stearate; Correctives comprises sweeting agent, flavouring agent, effervescent, and sweeting agent is an aspartame, and flavouring agent is a Fructus Citri tangerinae essence, and effervescent is sodium bicarbonate and fumaric acid, it is characterized in that component and proportioning (w/w/%) are as follows:

Sodium ferulate 30

Cross-linking sodium carboxymethyl cellulose 5

Microcrystalline Cellulose 15

Lactose 10

Mannitol 30

Sodium bicarbonate 2

Fumaric acid 2.5

Micropowder silica gel 2

Magnesium stearate 2

Aspartame 1

Fructus Citri tangerinae essence 0.5.

4. the preparation method of the described Orally disintegrated sodium ferulate tablet of claim 1, step is as follows: by proportioning with sodium ferulate and disintegrating agent, filler, correctives mix homogeneously, and add suitable quantity of water dilution, abundant mixing, place the respective tablets mould, put into the freeze dryer lyophilization, be shaped to the material bone dry.

5. the preparation method of the described Orally disintegrated sodium ferulate tablet of claim 2, step is as follows: by proportioning sodium ferulate, disintegrating agent, filler, correctives are sieved, mix homogeneously adds the lubricant mixing again, and direct compression is shaped.

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