A kind of freeze-dried oral preparation containing agomelatine and preparation method thereof
An oral preparation and freeze-drying technology, applied in the field of pharmaceutical preparations, can solve the problems of difficulty in taking ordinary tablets, slow drug release, and long absorption process time, achieve pre-gastric absorption and water-free delivery, and speed up the dissolution rate. , the effect of improving compliance
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Embodiment 1
[0041] This example provides a lyophilized oral formulation containing agomelatine, the prescription of which is shown in Table 1 below.
[0042]
[0043] Table 1
[0044] The flavoring agent in the above prescription can be one of aspartame or anhydrous citric acid alone, and the dosage is 0.001mg-0.81mg. Preferably, the flavoring agent includes aspartame and anhydrous citric acid, wherein aspartame is located in the sweetness regulator, and anhydrous citric acid is used as the sourness regulator.
[0045] It is easy to understand that according to the actual use, the above-mentioned excipients of the freeze-dried preparation can also be replaced by other similar excipients, and the dosage of the above-mentioned excipients can be adjusted appropriately to meet the pharmaceutical dosage requirements of the components.
Embodiment 2
[0047] According to the prescription in Example 1, this implementation provides a preparation method of a freeze-dried oral preparation containing agomelatine, comprising the following steps:
[0048] A. Dissolve the prescribed amount of flavoring agent in 300ml of purified water, add the prescribed amount of freeze-dried skeleton proppant and binder, and stir until dissolved; then add agomelatine raw material, and continue to stir until dissolved Add purified water to make the volume to 500ml to obtain the medicinal solution;
[0049] B. The fully stirred medicinal solution in step A is left to stand, and degassed by ultrasound; the degassed medicinal solution is respectively packaged and poured into each aluminum foil blister mold, and heated at -40°C to Quick-frozen and shaped at -120°C, then transferred to a freeze dryer for freeze-drying to make the moisture content <2%, to obtain a freeze-dried oral preparation.
[0050] The above-mentioned freeze-drying includes the fi...
Embodiment 3
[0054] In this example, the quality evaluation of the freeze-dried oral preparation in Example 1 was carried out.
[0055] (1) Disintegration evaluation
[0056] In vitro disintegration ①: Put the product on a glass surface, add 1 drop of water (about 0.02ml) (37°C±0.5°C) at a distance of 0.5cm from the tablet surface of the product and time it accurately. The standard limit is no more than 15 seconds;
[0057] In vitro disintegration ②: Measured by (Chinese Pharmacopoeia 2015 Edition, Part IV General Rule 0921), the standard limit is no more than 10 seconds.
[0058] (2) Taste evaluation: 5 volunteers evaluated the taste, put the product on the tip of their tongues, observed the disintegration situation and recorded the oral disintegration time, whether there is a sandy feeling after complete disintegration, whether the sweet and sour taste is good, etc.
[0059] (3) Character evaluation: the product surface is required to be smooth; the packaging is completely stripped of t...
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