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A kind of stable limaprost pharmaceutical composition and preparation method thereof

A technology for limaprost and composition, which is applied in the field of limaprost composition and preparation thereof, can solve problems such as enhancement of hygroscopicity, and achieve the effects of reducing hygroscopicity, increasing selection of species and good stability

Active Publication Date: 2019-03-05
YAOPHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The purpose of the present invention is to provide a limatoprost-containing pharmaceutical composition and a preparation method thereof. While solving the problem of temperature sensitivity by using the freeze-drying method, it focuses on solving the problem that the freeze-dried powder has enhanced hygroscopicity due to the porous structure. problems, and reduce the harsh requirements of finished products on packaging materials; in addition, it is necessary to improve the fluidity of freeze-dried powder, increase the hardness of the product, reduce the brittleness of the product, and ensure that the final product has excellent quality attributes

Method used

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  • A kind of stable limaprost pharmaceutical composition and preparation method thereof
  • A kind of stable limaprost pharmaceutical composition and preparation method thereof
  • A kind of stable limaprost pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] prescription:

[0028]

[0029] Preparation Process:

[0030] Weigh the inclusion compound of chitosan, trehalose, hydrogenated castor oil and limatoprost alfa cyclodextrin in the prescribed amount, disperse with appropriate amount of water, freeze-dry, the pre-freezing temperature is -35 ℃, and the primary drying temperature is - 10°C, the secondary drying temperature is 25°C; the freeze-dried lumps are pulverized and passed through an 80-mesh sieve to obtain a freeze-dried powder; Magnesium acid is mixed evenly and compressed into tablets.

Embodiment 2

[0032] prescription:

[0033]

[0034] Preparation Process:

[0035] Weigh the prescription amount of sucrose, dextrin, silicon dioxide and limatoprost alpha cyclodextrin inclusion compound, disperse with appropriate amount of tert-butanol-water system (volume ratio 1:30), freeze-dry, and pre-freeze the temperature -45°C, the primary drying temperature is -20°C, and the secondary drying temperature is 15°C; the freeze-dried block is pulverized and passed through an 80-mesh sieve to obtain a freeze-dried powder; then mixed with the prescribed amount of mannitol and microcrystalline Cellulose, croscarmellose sodium, pregelatinized starch and talcum powder are evenly mixed and pressed into tablets.

Embodiment 3

[0037] prescription:

[0038]

[0039] Preparation Process:

[0040] Weigh the prescription amount of dextran, silicon dioxide, hydrogenated castor oil and limatoprost alfa cyclodextrin inclusion compound, disperse with appropriate amount of tert-butanol-water system (volume ratio 1:4), freeze-dry, and pre-freeze The temperature is -45°C, the primary drying temperature is -20°C, and the secondary drying temperature is 15°C; the freeze-dried block is crushed and passed through a 80-mesh sieve to obtain a freeze-dried powder; then mixed with the prescribed amount of lactose, microcrystalline Cellulose, croscarmellose sodium and stearic acid are uniformly mixed and compressed into tablets.

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PUM

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Abstract

The invention provides a limaprost-containing pharmaceutical composition. The limaprost-containing pharmaceutical composition contains the following ingredients: a limaprost alfadex clathrate compound, a freeze-drying stabilizer, a freeze-drying stent, a diluent, a disintegrant, an adhesive and a lubricant. The invention further provides a preparation method for the composition. According to the stable limaprost pharmaceutical composition and the preparation method provided by the invention, the problems that the finished products are poor in the capacity of preventing hard matters from pressing in the surfaces thereof (showing as low hardness), and liable to cause crispness, capping, breakage (showing as high friability) after being subjected to vibration or friction due to the high amount of fine powder, poor flowability and poor compressibility of a freeze-dried product after being crushed are solved. Moreover, according to the limaprost pharmaceutical composition and the preparation method provided by the invention, the hygroscopicity of freeze-dried powder is remarkably improved, and strict requirements on environment humidity during a preparation process are lowered, thus the finished limaprost tablets are remarkably superior to commercial products in de-packaging state stability, and the stability is still capable of keeping consistent with that of the commercial products under the condition of no drying agent.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a composition of limatoprost and a preparation method thereof. Background technique [0002] Limaprost as prostaglandin E 1 (Prostaglandin E 1 , referred to as PGE 1 ) derivatives, which are mainly used clinically to improve various ischemic symptoms such as ulcers, pain, and coldness caused by thromboangiitis obliterans, and to improve acquired lumbar spinal stenosis (SLR test is normal, showing bilateral intermittent Subjective symptoms (pain and numbness of lower extremities) and walking ability caused by patients with lameness. [0003] Traditional PGE 1 It is easily catabolized in the gastrointestinal tract and cannot be administered orally; the inclusion complex of limaprost alfa cyclodextrin is PGE 1 Derivatives Limatoprost and alpha cyclodextrin (α-cyclodextrin) inclusion complex. The solubility and safety of the clathrated limaprost alfa cyclodextrin are ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K9/20A61K47/44A61K47/04A61K31/5575A61P9/14A61P17/02A61P29/00
Inventor 段瑞玲熊迎新唐晓欢王小霞
Owner YAOPHARMA CO LTD
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