Calcitriol solid lipidic dispersion and preparation method thereof

A technology of calcitriol and solid lipid, which is applied in the field of medicine, can solve the problems of poor thermal stability of calcitriol, drug content of toxic and side effects, and cannot reach the therapeutic level, etc., and achieves high drug stability and high affinity. Sex, storage and consumption benefits

Active Publication Date: 2014-07-09
SUN YAT SEN UNIV
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  • Summary
  • 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, four calcitriol solid lipid dispersion samples were prepared, and the ratio of raw materials is shown in Table 2.

[0053] Preparation of calcitriol solid lipid dispersion: according to the ratio of raw materials listed in Table 2, add calcitriol and BHT to the molten lipid carrier, and dissolve calcitriol by vortexing and ultrasonication for 5-20 minutes Dispersed in the lipid carrier to obtain the calcitriol lipid mixture; quickly add the calcitriol lipid mixture in the molten state to the solid carrier for adsorption and solidification.

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

[0055] Table 2 Raw material ratio (mass ratio) of calcitriol solid lipid dispersion

[0056]

[0057]

[0058] The stability test result comparison of calcitriol...

Embodiment 2

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

[0061] Table 3 Raw material ratio (mass ratio) of calcitriol solid lipid dispersion

[0062]

[0063] The stability test results of calcitriol in 5 calcitriol solid lipid dispersions prepared by the present embodiment are compared as figure 2 , Table 5. From figure 2 , Table 5 As can be seen, the stability of SLD5-SLD9 is improved by nearly 20% compared with the bulk drug; wherein SLD8-SLD9 is equivalent to SLD2 in Example 1, and after SLD5-SLD7 is added with the lipid carrier TPGS, the stability is higher than that of the implementation SLD2 in Example 1 is better.

Embodiment 3

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

[0066] Table 4 Raw material ratio (mass ratio) of calcitriol solid lipid dispersion

[0067]

[0068] The stability test results of calcitriol in 3 calcitriol solid lipid dispersions prepared by the present embodiment are compared as follows image 3 , Table 5. As can be seen from Table 5, the stability of SLD10-SLD12 is improved by nearly 20% compared with the bulk drug; wherein SLD12 is equivalent to SLD2 in Example 1, and after SLD10 and SLD11 are added with lipid carrier TPGS, the stability is better than that in Example 1 SLD2 is better.

[0069] Table 5 Stability of Calcitriol Solid Dispersion at 40°C Air...

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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 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 include vitamin D deficiency, calcium deficiency, endocrine system disorders, hyperthyroidism, certain drugs (adrenal corticosteroids, heparin, phenobarbital, phenytoin sodium, methotrexate, and methotrexate, etc.) Osteoporosis and many other reasons. Among them, the reduction of calcium absorption and the decrease of intestinal calcium absorption function due to the aging of the body are the most important reasons. In addition, patients with diabetes, kidney disease, gastrointestinal disease, bone tumors, and severe trauma are also prone t...

Claims

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Application Information

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Patent Type & Authority Patents(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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