Oil-in-water type garlicin-garlic oil sub-microemulsion as well as method for preparing same

Abstract

The invention relates to an oil-in-water type garlicin-garlic oil sub-microemulsion distributed in an inner phase (oil phase) as well as a method for preparing the same. The formulation of the emulsion contains 0.5 to 3 weight portions of garlicin or garlic oil as a medicament, and the garlicin or the garlic oil is added with a pharmaceutic adjuvant and is prepared into a garlicin sub-microemulsion or a garlic oil sub-microemulsion, wherein the pharmaceutic adjuvant comprises 5 to 20 weight portions of injection oil, 0.2 to 5 weight portions of emulsifier, 0 to 5 weight portions of coemulsifier, 0.5 to 3 weight portions of isoosmotic adjusting agent, a proper amount of antioxidant, a proper amount of pH regulator and a proper amount of injection water. The invention discusses the medicament distribution in oil, an oil/water interfacial film and water when the garlicin or the garlic oil is in an oil-in-water type dispersion system macroscopically and microscopically; more than 98 percent of the medicaments are enwrapped in the oil phase and the medicament free in the water phase is less than 1 percent; and the problem of a garlicin or garlic oil intravenous injection preparation for a hydrophobic dug is solved, the stability of an emulsion thereof is improved, and the vascular stimulation in an intravenous injection is reduced, thus the adaptability of a patient is greatly improved. The oil-in-water type garlicin-garlic oil sub-microemulsion can be applied to the adjuvant therapy of bacteria resistance, cardiovascular and cerebrovascular diseases and tumors.

Description

Technical field: [0001] The invention relates to the technical field of medicine, specifically, it is an allicin and garlic oil-in-water type submicroemulsion distributed inwardly (oil phase) and a preparation method thereof. Background technique: [0002] Physicochemical properties and mechanism of action of garlic: Garlic (Allium sativum) is the underground bulb of the Allium genus in the Liliaceae family. It is pungent in taste and warm in nature. Garlic contains various components such as amino acids, peptides, proteins, enzymes, sugars, glycosides, vitamins, fats, inorganic salts and sulfur compounds [Chen Lifang. Clinical application of allicin. Tianjin Pharmacy, 2004, 16 (6) -58-61]. Enzymatic hydrolysis and chemical reactions in garlic produce a variety of active chemical components. Alliin is metabolized under the action of allinase to produce allicin and a series of antibiotic substances—sulfur-containing compounds [Song Weiguo, Li Baoju, Liu Kaikai. Research pro...

AI Technical Summary

Problems solved by technology

Chinese patent 200510055240.2 prepared a traditional Chinese medicine composition and its soft capsule, and combined β-carotene and allicin to make a soft capsule; Chinese patent 200610039610.8 prepared a kind of allicin enteric-coated dripping pill; Chinese patent 96116051.9 studied allicin Tablet and its production method; Chinese patent 200310115331.1 prepared a single-particle nanometer allicin microcapsule, which uses an organic solvent, which may cause organic solvent residues. Direct contact between allicin and the gastrointestinal tract will stimulate the peristalsis of the gastrointestinal tract. causing pain, diarrhea, and damage to the gastrointestinal mucosa

Because allicin is irritating to the stomach and easily destroyed by gastric juice, its oral bioavailability is low, and patients' compliance is poor

In order to improve the bioavailability of allicin, people began to study allicin intravenous injections. Chinese patents 88103251.4 and 200410014731.8 prepared garlic injections. Although the bioavailability was improved, ethanol and sulfurous acid were used as solubilizers to make it Increased vascular irritation and poor patient compliance; Tween-80 was added to the allicin injection developed by Chinese patent 200510051474, which also increased the irritation, and Tween-80 intravenous injection has certain toxicity; Chinese patent 03124592.7 and 03112233.7 developed a cyclodextrin inclusion compound injection, although it solved the problem of low solubility of allicin in water, but using a large amount of cyclodextrin compounds may not only cause adverse reactions such as hemolysis, but also increase cost of preparation

Allicin is a drug that is sensitive to light and heat, and has an irritating and specific garlic smell. The above-mentioned shortcomings of allicin cannot be well avoided by ordinary injections

In recent years, with the continuous deepening of research in the field of pharmacy, drug delivery systems play an important role in improving drug efficacy and facilitating patients' use. The research on the dosage forms of allicin reflects this trend. In order to solve this problem, Chinese patents have disclosed fat Research on injection administration of emulsions, liposomes, nanoparticles, self-(micro) emulsified oral preparations and other dosage forms of modern drug delivery systems, and Chinese patents 200410013573.4, 200510020730.9, 200510046401.1, 200610019770.6 and Chinese patent 200410060815.5 have disclosed garlic Allicin is made into fat emulsion to solve the problems of poor water solubility and great irritation of blood vessels injected in vivo

Chinese patents 200510047949.8 and 200510002446.9 have developed allicin solid lipid nanoparticles and liposome preparations, but these preparations have drug leakage and drug burst release behavior in vivo to varying degrees

The above published patents did not clarify the distribution characteristics and action mechanism of the drug in the oil phase, water phase and oil / water interface film phase in this dosage form. The inventors have mastered the microstructure characteristics of this dosage form through long-term in-depth research on this dosage form. And through experiments to clarify the characteristics of this dosage form macroscopically

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