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Skin external-use patch containing calcium-sensing receptor stimulant

A calcium-sensitive receptor and agonist technology, applied in the field of pharmaceutical preparations, to avoid the first-pass effect of the liver, good safety, and reduce toxic and side effects

Inactive Publication Date: 2017-06-09
BEIJING TIDE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no effective way to prevent and alleviate its side effects on the gastrointestinal tract clinically.

Method used

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  • Skin external-use patch containing calcium-sensing receptor stimulant
  • Skin external-use patch containing calcium-sensing receptor stimulant
  • Skin external-use patch containing calcium-sensing receptor stimulant

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] prescription composition

[0027] materials Amount added (g) percentage% Cinacalcet hydrochloride 2.5 1.39 active vitamin D 0.2 0.11 SIS 84.3 46.83 liquid paraffin 47.8 26.55 polymer polyisobutylene 10．0 5.56 Low Molecular Polyisobutylene 10.0 5.56 Terpene resin 18.0 10.00 Menthol 0.9 0.50 Azone 0.9 0.50 Butylated hydroxytoluene 3.6 2.00 Zinc stearate 1.8 1.00 batch 100 stickers

[0028] Preparation method: heat and stir SIS, part of liquid paraffin, high-molecular polyisobutylene, low-molecular polyisobutylene, terpene resin, and dibutyl hydroxytoluene; add menthol and Azone to the above liquid and mix evenly; add hard After zinc fatty acid and part of liquid paraffin are mixed evenly, add them to the above liquid and stir evenly; after the paste cools down, add the prescribed amount of cinacalcet hydrochloride and active vitamin D and stir evenly; Clothed on the pro...

Embodiment 2

[0030] prescription composition

[0031] materials Amount added (g) percentage% Cinacalcet hydrochloride 10.0 5.56 Vitamin D 5.0 2.78 SIS 61.3 34.06 liquid paraffin 37.6 20.89 hydrogenated petroleum resin 63.0 35.00 Azone 0.4 0.21 Butylated hydroxytoluene 1.8 1.00 Titanium dioxide 0.9 0.50 batch 100 stickers

[0032] Preparation method: Heat and dissolve SIS, part of liquid paraffin, hydrogenated petroleum resin, and dibutyl hydroxytoluene in the prescribed amount, and mix well; add Azone to the above mixed liquid; mix the remaining liquid paraffin and titanium dioxide evenly, and then add to the above solution Middle; after the ointment cools down, add the prescribed amount of cinacalcet hydrochloride and vitamin D and stir evenly, apply the obtained medicated ointment evenly on the protective layer, and after laminating with the backing layer as the preparation, cut into a set size and shape, ...

Embodiment 3

[0034] Prescription composition:

[0035] materials Amount added (g) percentage% Cinacalcet hydrochloride 5.0 5.56 SIS 34.0 37.78 liquid paraffin 19.7 21.89 Polybutene 4.5 5.00 Terpene resin 10.8 12.00 Hydrogenated Rosin Glycerides 13.5 15.00 Menthol 0.3 0.33 Oleic acid 0.1 0.11 Avobenzone 1.8 2.00 Zinc stearate 0.3 0.33 batch 100 stickers

[0036] Preparation method: heat and dissolve SIS, part of liquid paraffin, polybutene, terpene resin, hydrogenated rosin glyceride, and avobenzone in the prescribed amount, and mix evenly; add menthol and oleic acid to the above mixed liquid; The remaining liquid paraffin and zinc stearate are mixed evenly and then added to the above solution; after the paste is cooled down, the prescribed amount of cinacalcet hydrochloride is added and stirred evenly, and the obtained medicated paste is evenly coated on the protective layer, After laminating w...

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Abstract

The invention discloses a skin external-use patch containing a calcium-sensing receptor stimulant. For the patch disclosed by the invention, a medicinal storage layer, a backing layer and a protection layer are adopted as the necessary ingredients of the patch, and meanwhile, other pharmaceutically acceptable excipients also can be added. The patch is administrated through the skin, so that the first-pass effect of the liver and the stimulation to the gastrointestinal tract are avoided, the untoward effects of the medicines are effectively reduced, the medication to patients is safe, meanwhile, compared with the tablets for oral administration, the patch provided by the invention has the permanent efficacies, and the bioavailability is obviously improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and mainly relates to an external skin patch containing a calcium sensitive receptor agonist and a preparation method thereof. Background technique [0002] Secondary hyperparathyroidism (SHPT) is a common complication of chronic kidney disease (CKD), and its prevalence increases with the progression of CKD. It mainly leads to abnormal mineral and bone metabolism in patients. In recent years, it has been recognized that its severity mainly leads to cardiovascular calcification, which is closely related to the survival and prognosis of dialysis patients. Active vitamin D drugs have been used in the clinical treatment of SHPT for nearly 30 years, because the treatment is often accompanied by hypercalcemia and hyperphosphatemia, which increases the risk of cardiovascular calcification and thus limits its clinical application. Most patients with SHPT who are ineffective in drug therapy can...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61K9/70A61K31/137A61K31/593A61P5/20
Inventor 赵焰平孙立欣杨娜卢迪周丽莹刘亚男
Owner BEIJING TIDE PHARMA
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