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Preparation method of tretinoin-cyclodextrin clathrate, and emulsifiable paste and gelata of the clathrate

A technology of cyclodextrin inclusion complex and retinoic acid, which is applied in the directions of active ingredients of hydroxy compounds, medical preparations of non-active ingredients, pharmaceutical formulations, etc. problems such as low rate, to achieve the effect of reducing photosensitivity, increasing solubility and dissolution rate

Inactive Publication Date: 2014-06-11
倪伟华
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The solubility and dissolution rate of retinoic acid in the retinoic acid inclusion compound obtained by the existing retinoic acid inclusion compound and its preparation method are relatively low, the applicable range is relatively narrow and the photosensitivity is poor

Method used

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Experimental program
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Embodiment Construction

[0011] The present invention will be further described in detail below in combination with specific embodiments.

[0012] Example 1 Example 2 Example 3 Vitamin A acid / mg 100 100 100 Tributylamine / mg 5 10 15 β-CD / g 5 5.5 6 Encapsulation rate % 92.4 93.4 92.8 Drug loading% 10.7 12.6 14.3 Inclusion ratio 1：1 1：1 1：1

[0013] The inclusion ratio of the inclusion compound determined by ultraviolet method is 1:1 (molar ratio);

[0014] Encapsulation efficiency = amount of drug contained in the inclusion compound / amount of drug injected;

[0015] Inclusion compound yield = inclusion compound amount / input amount (input drug amount+CD);

[0016] Take retinoic acid, β-CD, the mixture of retinoic acid and β-CD, and the inclusion complex of retinoic acid and β-CD, and press them into tablets with KBr. All compounds showed the characteristic peaks of β-CD, indicating that the inclusion process did not destroy the structu...

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Abstract

The invention relates to a preparation method of a tretinoin-cyclodextrin clathrate. The method comprises the following steps: (1) mixing 5-6 g of beta-CD with 50 mL of water, heating to 80-100 DEG C and dissolving; and (2) cooling to 40-50 DEG C, adding 100 mg of tretinoin and 5-10 mg of tributylamine, fully grinding to obtain a paste, refrigerating for 24 h, filtering after complete precipitation, washing the precipitate with anhydrous ethanol three times, and drying at low temperature of 40-50 DEG C to obtain the tretinoin-beta-CD clathrate. The preparation method of tretinoin-cyclodextrin clathrate provided by the technical scheme of the invention has the beneficial effects of increasing solubility and dissolution rate of tretinoin, reducing the photonasty of a traditional tretinoin preparation for external use, improving the scope of application of the tretinoin-beta-CD clathrate, and lowering the usage dosage.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a preparation method of retinoic acid external-use retinoic acid-cyclodextrin inclusion compound and cream and gel thereof. Background technique [0002] Retinoic acid is an intermediate product of vitamin A metabolism in the body. It mainly affects bone growth and promotes epithelial cell proliferation, differentiation, and keratolysis. It is clinically used to treat acne vulgaris, psoriasis, ichthyosis, lichen planus, and red hair. Pityriasis, keratosis pilaris, squamous cell carcinoma, melanoma and other diseases, the side effects are dry skin and mucous membranes, desquamation, nausea and vomiting, and loss of appetite. Sunlight can aggravate the stimulation of retinoic acid on the skin and lead to the decomposition of retinoic acid , Animal experiments suggest that retinoic acid can enhance the carcinogenic ability of ultraviolet rays, so it is most...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K9/00A61K9/06A61K31/203A61P17/00A61P17/06A61P17/10A61P31/20
Inventor 倪伟华
Owner 倪伟华
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