Calcitriol solid lipidic dispersion and preparation method thereof

A technology of calcitriol and solid lipid, applied in the field of medicine, can solve the problems of poor thermal stability of calcitriol, drug content of toxic and side effects, and failure to reach the therapeutic level, etc., and achieve high drug stability and high affinity Sexuality, the effect of being beneficial to storage and taking

Active Publication Date: 2013-03-20
SUN YAT SEN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Attention should be paid to the preparation of calcitriol into solid preparations: on the one hand, solid preparations are a heterogeneous dispersion system, and it is very difficult to uniformly disperse trace amounts of drugs into solid particles or powders; since calcitriol has a strong Physiological effects, a very small dose can produce obvious pharmacological effects. If the solid preparations are unevenly distributed during the production process, the local drug concentration will be too high, which will cause toxic side effects or the drug content will be too low to reach the therapeutic level. ; On the other hand, the heat stability of calcitriol is relatively poor, and oral solid preparation usually will go through the process of high-temperature drying in the production process, such as tablets, after wet granulation, must go through appropriate high temperature (such as 60~ 80°C) to dry before pressing into tablets or capsules

Method used

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  • Calcitriol solid lipidic dispersion and preparation method thereof
  • Calcitriol solid lipidic dispersion and preparation method thereof
  • Calcitriol solid lipidic dispersion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] In this example, 4 samples of calcitriol solid lipid dispersion were prepared, and the raw material ratios are shown in Table 2.

[0053] Preparation of calcitriol solid lipid dispersion: according to the raw material ratio listed in Table 2, add calcitriol and BHT into the molten lipid carrier, and dissolve calcitriol by vortexing and ultrasound for 5-20 minutes Disperse in a lipid carrier to obtain a calcitriol lipid mixture; quickly add the calcitriol lipid mixture in a molten state to a solid carrier to adsorb and solidify.

[0054] Stability test: The samples SLD1, SLD2, SLD3, and SLD4 were placed in an oven at 40°C and sealed from light, and samples were taken on the 10th day. The retention rate of calcitriol in the samples was determined by high performance liquid chromatography.

[0055] Table 2 The ratio of raw materials for calcitriol solid lipid dispersion (mass ratio)

[0056]

[0057]

[0058] The stability test results of calcitriol in the 4 calcitriol solid lipid...

Embodiment 2

[0060] In this example, five calcitriol solid lipid dispersions were prepared. The raw material formulations are shown in Table 3, and the preparation method is the same as that of Example 1. The difference lies in that the 5 calcitriol solid lipid dispersions in this example use 2 types of lipid carriers. The stability test method is the same as in Example 1.

[0061] Table 3 The ratio of raw materials of calcitriol solid lipid dispersion (mass ratio)

[0062]

[0063] The stability test results of calcitriol in the 5 calcitriol solid lipid dispersions prepared in this example are as follows: figure 2 , As shown in Table 5. From figure 2 Table 5 It can be seen that the stability of SLD5-SLD9 is nearly 20% higher than that of the bulk drug; among them, SLD8-SLD9 is equivalent to SLD2 in Example 1. After the lipid carrier TPGS is added to SLD5-SLD7, the stability is better. SLD2 in Example 1 is better.

Embodiment 3

[0065] In this example, three calcitriol solid lipid dispersions were prepared. The raw material formulations are shown in Table 4, and the preparation method is the same as in Example 1. The difference is that the 3 calcitriol solid lipid dispersions in this example use 3 lipid carriers. The stability test method is the same as in Example 1.

[0066] Table 4 The ratio of raw materials of calcitriol solid lipid dispersion (mass ratio)

[0067]

[0068] The stability test results of calcitriol in the three calcitriol solid lipid dispersions prepared in this example are as follows: image 3 , As shown in Table 5. It can be seen from Table 5 that the stability of SLD10-SLD12 is nearly 20% higher than that of the bulk drug; among them, SLD12 is equivalent to SLD2 in Example 1. After the lipid carrier TPGS is added to SLD10 and SLD11, the stability is better than that in Example 1. SLD2 is better.

[0069] Table 5: Stability of Calcitriol Solid Dispersion at 40℃ for 10 Days

[0070]

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Abstract

The invention discloses a calcitriol solid lipidic dispersion and a preparation method thereof. Raw materials of the calcitriol solid lipidic dispersion comprise calcitriol, one or more lipidic carriers and solid carriers, wherein a mass ratio of calcitriol to the one or more lipidic carriers is 1: (90-200000); a mass ratio of the one or more lipidic carriers to the solid carriers is (1-2): 1; and the one or more lipidic carriers are selected from caprylic triglyceride, capric triglyceride, caprylic / capric triglyceride, laurin, caprylic dilaurin, capric dilaurin, vitamin E, vitamin E succinate, vitamin E polyethylene glycol succinate and vitamin E acetate. The calcitriol solid lipidic dispersion has high drug stability and can keep a constant treatment level. The preparation method does not adopt an inorganic solvent, is suitable for industrial production and is conducive to storage and taking. An experiment proves that the calcitriol solid lipidic dispersion has good stability and dispersion uniformity satisfying requirements.

Description

Technical field [0001] The present invention relates to the technical field of medicine, in particular to a solid lipid dispersion of calcitriol and a preparation method thereof. Background technique [0002] Osteoporosis and other diseases related to the regulation of calcium metabolism have increasingly become serious diseases that endanger public health, and are common and easily overlooked bone metabolic diseases. The causes of osteoporosis are vitamin D deficiency, calcium deficiency, endocrine system disorders, hyperthyroidism, and certain drugs (adrenocortical hormones, heparin, phenobarbital, phenytoin, methotrexate, etc.) inducers There are many reasons such as osteoporosis. Among them, the decrease in calcium absorption and the decrease in intestinal calcium absorption caused by the aging of the body are the main reasons. In addition, patients with diabetes, kidney disease, gastrointestinal disease, bone tumors, severe trauma, etc. are also prone to complicated osteop...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/48A61K31/593A61K47/38A61K47/42A61K47/34A61K47/36A61P19/10A61P19/08A61P13/12A61P17/06A61P15/12A61P35/00A61P37/02
Inventor 吴传斌袁婷潘昕章正赞
Owner SUN YAT SEN UNIV
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