Method of composition in solid form

专利摘要:
Solid shaped articles, particularly pharmaceutical dosage forms, are prepared by freezing in a mould a composition comprising a predetermined amount of chemical (eg. pharmaceutical) and a solution of carrier material and then subliming solvent from the frozen composition. The side wall or walls of the mould make an angle with the vertical of at least 5° at the surface of the composition. This enables shaped articles of constant thickness to be produced with minimum sublimation times.
公开号:SU1514239A3
申请号:SU823520359
申请日:1982-12-01
公开日:1989-10-07
发明作者:Dzhordzh Kejt Emerson Gregori
申请人:Wyeth John & Brother Ltd；
IPC主号:

专利说明:

The invention relates to the chemical-pharmaceutical industry. To ensure a uniform thickness of the product, the medicinal substance in a volume of 0.25-3 ml is poured into a mold having the correct shape, and the cross-sectional area at the base is smaller than the cross-sectional area at the top. The slope of the lateral surface of the walls of the form is 5-40 °, and the depth of the substance in the form is 1.5-4 mm. Substance sublimated.
1514239
one
The invention relates to the chemical-pharmaceutical industry and concerns a method for preparing the composition.
in solid form. five
The purpose of the invention is to provide a uniform thickness of the product.
The ingredients of the composition can be formulated separately or in a mixture, preferably in the form of a mixture containing the entire composition.
The volume in the form of the composition is preferably 3 ml or less (for example, about 0.25 “
1 ml), especially when the molded from-15 product is a pharmacological dosage form for oral administration. The depth of the composition in the form, the cross-sectional area of the form, and the angle of the side wall 20 or walls affect the volume of the composition. The shape may have a regular shape, such as a circle or a polygon (for example, a rectangle, in particular a square), in cross section, and the cross-sectional area at the base of the shape is smaller than the area closer to the open top, taking into account the inclined walls. It is advisable to use a shape having a circular cross section. Molded products are a flat disk having inclined side walls. Preferably, the side walls of the mold are 35 vertical.
angle from 9 to 20 °.
In order for the drying time in the freeze dryer to be minimal, it is advisable that the depth of the composition in the form be less than 3.5 mm, for example, 1.5 (or 22.5 mm). If the depth is less than 1.5 mm, the molded product is difficult to remove.
'Example 1. Pharmacological dosage forms, oxaepam, composition,
Oxazepam Twin-80 HRV Mannitol BP
3% Hydrated Gelatin Up to 0.5 3% hydrolyzed gelatin is prepared by suspending 30 g of powdered gelatin in 800 ml of cold distilled water in a one-liter flask and autoclaved at 121 ° C for 60 minutes. After cooling, the final volume is adjusted to 1 l.
containing mg mg:
15
0.25
15
2
Prepare a suspension of oxazepam (30 g) in a solution of 3% hydrolyzed gelatin containing dissolved mannitol (30 g) and Tween-80 (0.5 g) using ultrasound for 5 minutes, and the suspension is diluted to I l 3% - Nym solution of gelatin. This solution is dosed in 0.5 ml portions using an automatic casting machine and poured into the nests in cellular PVC trays. Each nest is an inverted truncated cone depth
3.5 mm, the diameter of the bottom is 14.5 mm, and the diameter of the upper part is 16 mm (that is, the side walls form an angle with the vertical of about 12 °). The contents of the nests are then frozen by passing the pallets through a special freezing tunnel, which is supplied with liquid nitrogen.
Pallets containing frozen compositions are then transported to a freeze dryer. The pressure is 0.5 mm Hg. The temperature of the shelves of the freeze-dryer is set to 60 ° C for and then drops to 40 ° C. After 2 hours, the trays are removed from the freeze dryer. Removable aluminum foil is then sealed onto the cellular packaging in recesses containing pharmacological dosage form. The latter have the same thickness and quickly collapse, for example 2 seconds or less when taken orally.
Examples 2-11. Analogously to Example 1, pharmacological preparations are prepared.
ical dosage forms containing the following active ingredients (by example), mg: (2) Oxazepam 30 and 50 (3) Lorazepam 1,2,2,5 and four (four) Temazepam 10 and 20 (five) Lormetazepam one (6) Frusemide 40 (7) Bendrofluazide five (eight) Cyclopentia zid 0.5 (9) Dinitrat iso - sobida 2.5, 5 and ten (YU) Indomethacin 25 and 50 (AND) Prochlorpera zine maleate 50
Example 12. Composition, mg:
Indolyl acetic
acid 1
1514239
Mannitol BP 15
3% hydrolyzed gelatin To 0.5 ml
The operation of Example I, 5 is repeated.
but instead of 30 g of oxazepam, 2 g of indolylacetic acid are used, and Tween-80 is excluded. Each product obtained by freeze-drying is added to 1 liter of water. At the same time, a composition is obtained that can serve as a plant growth accelerator.
Example 13. The operation of Example 12 is repeated, but instead of indole acetic acid, indolyl-15 butyric acid is used. Each of the products obtained by freeze-drying is added to 1 l of water. You get a composition that is useful for use as a growth accelerator 20 roots of cuttings of plants.
The proposed method provides a uniform thickness of the product, while by a known method molded products usually have a minimum thickness near their central part and maximum thickness near their edges, and this change is due to the influence of the meniscus of the composition at the side walls of the form.

权利要求:
Claims (1)
[1]
Claim
A method of making a composition in solid form by adding to the form a composition consisting of a given amount of a chemical substance and! carrier solution inert with respect to the substance used, followed by freezing and freeze-drying, characterized in that, in order to ensure a uniform thickness of the product, the depth of the composition in the mold is 1.54.0 mm, the angle of inclination of the side surface of the forca wall is 5- 40 °, and the volume of the composition is not more than 3 MP.

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法律状态:

优先权:

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申请号 | 申请日 | 专利标题

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GB8136360|1981-12-02|

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