Li "arrived in Riyadh to participate in the fourth meeting of the High-Level Sino-Saudi Joint Committee", the official Saudi Press Agency reported.
After Riyadh, Li will travel to the neighbouring United Arab Emirates, the ministry said, adding that his trip would conclude Friday.
Key US ally Saudi Arabia has in recent years sought to forge closer ties with both Beijing and Moscow.
China accounts for nearly a quarter of crude oil exports from Saudi Arabia, the world's largest crude exporter.
The Chinese premier's visit aims to "enhance cooperation and trade exchange" between China and Gulf states, analyst Mohamed bin Saleh al-Harbi told AFP.
Last year, China facilitated a historic rapprochement between Saudi Arabia and Iran.
China has also positioned itself as a more neutral actor on the Israeli-Palestinian conflict than its rival the United States, advocating a two-state solution while maintaining good ties with Israel.
Beijing has pointed to the Middle East as a key node in its Belt and Road infrastructure initiative, a central pillar of leader Xi Jinping's bid to expand China's clout overseas.
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