Patent•
Butylphthalide self-emulsifying drug delivery system, its preparation method and application
26 Aug 2005-
TL;DR: In this paper, the authors proposed a self-emulsifying drug delivery system (SEDDS) for improving the absorbency of drugs by increasing the contact area between the mucous membranes of the gastrointestinal tract and butylphthalide.
Abstract: The present invention relates to novel drug delivery and release systems of butylphthalide, namely self-emulsifying drug delivery systems (SEDDS), their preparation, and their use in pharmaceutical formulations. The drug delivery system comprises 1 to 65% butylphthalide and 10 to 65% emulsifier as essential ingredients with various additives required according to the desired dosage form. The present invention improves the absorbency of drugs by significantly increasing the contact area between the mucous membranes of the gastrointestinal tract and butylphthalide.
Drug delivery, butylphthalide, emulsification
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TL;DR: The SEDDS offers the benefit of a protective effect against the hostile environment in the gut, and the unique fabrication techniques provide specific strategy to overcome the low bioavailability and poor solubility problems.
Abstract: Introduction: Oral administration of a drug is the most common, ideal and preferred route of administration. The main problem of oral drug formulations is their low bioavailability arises from poor aqueous solubility of drug. Aqueous solubility of lipophilic drugs can be improved by various techniques like salt formation, complexation, addition of co-solvent etc. but self-emulsifying drug-delivery system (SEDDS) is getting more attention for increasing the solubility of such drugs. The SEDDS is an isotropic mixture of drug, lipids, and emulsifiers, usually with one or more hydrophilic co-solvents/co-emulsifiers. This system is having ability to generate oil-in-water (o/w) emulsions or microemulsions upon gentle agitation followed by dilution with aqueous phase. The SEDDSs are relatively newer, lipid-based technological innovations possessing unparalleled potential in improving oral bioavailability of poorly water-soluble drugs.Areas covered: This review provides updated information regarding the types of SEDDS, their preparation techniques, drug delivery and related recent patents along with marketed formulations.Expert opinion: The SEDDS has been explored for improving bioavailability, rising intra-subject heterogeneity, and increasing solubility. SEDDS offers the benefit of a protective effect against the hostile environment in the gut. The unique fabrication techniques provide specific strategy to overcome the low bioavailability and poor solubility problems.
29 citations
TL;DR: In this paper, the authors provided a discussion on recent developments such as self-microemulsifying mouth dissolving film, supersaturable, herbal, and sponges carrying SMEDDS.
Abstract: Self-microemulsifying drug delivery system (SMEDDS) has emerged as a distinctive approach for the improvement of low bioavailability, high intra- and inter-subject changeability, and absence of dose proportionality difficulties associated with hydrophobic (water-repelling) drugs due to their incomparable potentials. SMEDDS is isotropic mixture of drug, surfactants, cosurfactants, and oil which have unique ability to form fine o/w microemulsion on slight shaking followed by dilution with fluid, such as gastrointestinal fluid. In vitro features such as concentration of surfactants, ratio of oil to surfactant, polarity of emulsion, zeta potential, and size of droplet play a vital role in drug absorption orally. It would be more accurate to say that it disperses out of oily droplets into gastrointestinal tract media, resulting in the development of equilibrium among outer dispersed media and the drugs dissolved in oily droplets in spite of saying that the drug is released from SMEDDS. This analysis is useful for the better understanding of SMEDDS for its recent advancements with an emphasis on absorption pathway of lipids, patents, and research work. The present article provides a discussion on recent developments such as self-microemulsifying mouth dissolving film, supersaturable, herbal, and sponges carrying SMEDDS.
9 citations
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TL;DR: The SEDDS offers the benefit of a protective effect against the hostile environment in the gut, and the unique fabrication techniques provide specific strategy to overcome the low bioavailability and poor solubility problems.
Abstract: Introduction: Oral administration of a drug is the most common, ideal and preferred route of administration. The main problem of oral drug formulations is their low bioavailability arises from poor aqueous solubility of drug. Aqueous solubility of lipophilic drugs can be improved by various techniques like salt formation, complexation, addition of co-solvent etc. but self-emulsifying drug-delivery system (SEDDS) is getting more attention for increasing the solubility of such drugs. The SEDDS is an isotropic mixture of drug, lipids, and emulsifiers, usually with one or more hydrophilic co-solvents/co-emulsifiers. This system is having ability to generate oil-in-water (o/w) emulsions or microemulsions upon gentle agitation followed by dilution with aqueous phase. The SEDDSs are relatively newer, lipid-based technological innovations possessing unparalleled potential in improving oral bioavailability of poorly water-soluble drugs.Areas covered: This review provides updated information regarding the types of SEDDS, their preparation techniques, drug delivery and related recent patents along with marketed formulations.Expert opinion: The SEDDS has been explored for improving bioavailability, rising intra-subject heterogeneity, and increasing solubility. SEDDS offers the benefit of a protective effect against the hostile environment in the gut. The unique fabrication techniques provide specific strategy to overcome the low bioavailability and poor solubility problems.
29 citations
TL;DR: In this paper, the authors provided a discussion on recent developments such as self-microemulsifying mouth dissolving film, supersaturable, herbal, and sponges carrying SMEDDS.
Abstract: Self-microemulsifying drug delivery system (SMEDDS) has emerged as a distinctive approach for the improvement of low bioavailability, high intra- and inter-subject changeability, and absence of dose proportionality difficulties associated with hydrophobic (water-repelling) drugs due to their incomparable potentials. SMEDDS is isotropic mixture of drug, surfactants, cosurfactants, and oil which have unique ability to form fine o/w microemulsion on slight shaking followed by dilution with fluid, such as gastrointestinal fluid. In vitro features such as concentration of surfactants, ratio of oil to surfactant, polarity of emulsion, zeta potential, and size of droplet play a vital role in drug absorption orally. It would be more accurate to say that it disperses out of oily droplets into gastrointestinal tract media, resulting in the development of equilibrium among outer dispersed media and the drugs dissolved in oily droplets in spite of saying that the drug is released from SMEDDS. This analysis is useful for the better understanding of SMEDDS for its recent advancements with an emphasis on absorption pathway of lipids, patents, and research work. The present article provides a discussion on recent developments such as self-microemulsifying mouth dissolving film, supersaturable, herbal, and sponges carrying SMEDDS.
9 citations